Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T40474 | Target Info | |||
| Target Name | Proto-oncogene c-Met (MET) | ||||
| Synonyms | Tyrosine-protein kinase Met; Scatter factor receptor; SF receptor; Met proto-oncogene tyrosine kinase; Hepatocyte growth factor receptor; HGF/SF receptor; HGF-SF receptor; HGF receptor; C-met; C-Met receptor tyrosine kinase | ||||
| Target Type | Successful Target | ||||
| Gene Name | MET | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Adenosine triphosphate | Ligand Info | |||||
| Structure Description | Structure of MET receptor tyrosine kinase in complex with ATP | PDB:3DKC | ||||
| Method | X-ray diffraction | Resolution | 1.52 Å | Mutation | Yes | [1] |
| PDB Sequence |
VHIDLSALNP
1060 ELVQAVQHVV1070 IGPSSLIVHF1080 NEVIGRGHFG1090 CVYHGTLLDN1100 DGKKIHCAVK 1110 SLNRITDIGE1120 VSQFLTEGII1130 MKDFSHPNVL1140 SLLGICLRSE1150 GSPLVVLPYM 1160 KHGDLRNFIR1170 NETHNPTVKD1180 LIGFGLQVAK1190 GMKFLASKKF1200 VHRDLAARNC 1210 MLDEKFTVKV1220 ADFGLARDMY1230 DKEFDSVHNK1240 TGAKLPVKWM1250 ALESLQTQKF 1260 TTKSDVWSFG1270 VLLWELMTRG1280 APPYPDVNTF1290 DITVYLLQGR1300 RLLQPEYCPD 1310 PLYEVMLKCW1320 HPKAEMRPSF1330 SELVSRISAI1340 FSTFIGEHYV1350 HVNATYVNVK 1360 EG
|
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|
|
ILE1084
3.377
GLY1085
3.534
ARG1086
3.912
GLY1087
3.138
HIS1088
2.665
PHE1089
3.872
GLY1090
3.501
CYS1091
4.829
VAL1092
3.428
ALA1108
3.480
LYS1110
2.835
|
|||||
| Ligand Name: Crizotinib | Ligand Info | |||||
| Structure Description | X-ray Structure of PF-02341066 bound to the kinase domain of c-Met | PDB:2WGJ | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | No | [2] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLKKI1105 HCAVKSLNRI 1115 TDIGEVSQFL1125 TEGIIMKDFS1135 HPNVLSLLGI1145 CLRSEGSPLV1155 VLPYMKHGDL 1165 RNFIRNETHN1175 PTVKDLIGFG1185 LQVAKGMKYL1195 ASKKFVHRDL1205 AARNCMLDEK 1215 FTVKVADFGL1225 ARDMYDKEYY1235 SVHNKTGAKL1245 PVKWMALESL1255 QTQKFTTKSD 1265 VWSFGVLLWE1275 LMTRGAPPYP1285 DVNTFDITVY1295 LLQGRRLLQP1305 EYCPDPLYEV 1315 MLKCWHPKAE1325 MRPSFSELVS1335 RISAIFSTFI1345
|
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ILE1084
3.465
GLY1085
3.681
VAL1092
3.762
ALA1108
3.265
LYS1110
4.690
LEU1140
3.848
LEU1157
3.692
PRO1158
3.051
TYR1159
3.435
MET1160
2.910
LYS1161
3.865
|
|||||
| Ligand Name: Tepotinib | Ligand Info | |||||
| Structure Description | Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors | PDB:4R1V | ||||
| Method | X-ray diffraction | Resolution | 1.20 Å | Mutation | No | [3] |
| PDB Sequence |
LSALNPELVQ
1064 AVQHVVIGPS1074 SLIVHFNEVI1084 GRGHFGCVYH1094 GTLLDNDGKK1104 IHCAVKSLNR 1114 ITDIGEVSQF1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLRSSPLVV1156 LPYMKHGDLR 1166 NFIRNETHNP1176 TVKDLIGFGL1186 QVAKGMKYLA1196 SKKFVHRDLA1206 ARNCMLDEKF 1216 TVKVADFGLA1226 RDMYDKEYYS1236 VHNKTGAKLP1246 VKWMALESLQ1256 TQKFTTKSDV 1266 WSFGVLLWEL1276 MTRGAPPYPD1286 VNTFDITVYL1296 LQGRRLLQPE1306 YCPDPLYEVM 1316 LKCWHPKAEM1326 RPSFSELVSR1336 ISAIFSTFI
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .3E8 or .3E82 or .3E83 or :33E8;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230 or .A:1231; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.453
GLY1085
4.361
ARG1086
4.838
VAL1092
4.162
ALA1108
3.378
LEU1140
3.569
LEU1157
3.643
PRO1158
3.338
TYR1159
3.347
MET1160
3.042
LYS1161
3.393
HIS1162
4.036
|
|||||
| Ligand Name: Savolitinib | Ligand Info | |||||
| Structure Description | Crystal structure of wild-type cMET bound by savolitinib | PDB:6SDE | ||||
| Method | X-ray diffraction | Resolution | 2.49 Å | Mutation | No | [4] |
| PDB Sequence |
HVVIGPSSLI
1077 VHFNEVIGRG1087 HFGCVYHGTL1097 LKIHCAVKSL1112 NRIEVSQFLT1126 EGIIMKDFSH 1136 PNVLSLLGIC1146 LRSSPLVVLP1158 YMKHGDLRNF1168 IRNETHNPTV1178 KDLIGFGLQV 1188 AKGMKYLASK1198 KFVHRDLAAR1208 NCMLDEKFTV1218 KVADFGLARD1228 MYDKEYYSVH 1238 NKTGAKLPVK1248 WMALESLQTQ1258 KFTTKSDVWS1268 FGVLLWELMT1278 RGAPPYPDVN 1288 TFDITVYLLQ1298 GRRLLQPEYC1308 PDPLYEVMLK1318 CWHPKAEMRP1328 SFSELVSRIS 1338 AIFSTFIG
|
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .V0L or .V0L2 or .V0L3 or :3V0L;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230 or .A:1231; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.620
VAL1092
3.717
ALA1108
3.345
LYS1110
4.118
LEU1140
3.826
LEU1157
3.865
PRO1158
3.397
TYR1159
3.692
MET1160
2.840
ASP1164
3.570
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| Ligand Name: LY2801653 | Ligand Info | |||||
| Structure Description | Crystal structure of c-Met in complex with LY2801653 | PDB:4EEV | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | No | [5] |
| PDB Sequence |
PLLQNTVHID
1054 LSALNPELVQ1064 AVQHVVIGPS1074 SLIVHFNEVI1084 GRGHFGCVYH1094 GTLLDNDGKK 1104 IHCAVKSLNR1114 ITDIGEVSQF1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLRSEGSPL 1154 VVLPYMKHGD1164 LRNFIRNETH1174 NPTVKDLIGF1184 GLQVAKGMKY1194 LASKKFVHRD 1204 LAARNCMLDE1214 KFTVKVADFG1224 KLPVKWMALE1253 SLQTQKFTTK1263 SDVWSFGVLL 1273 WELMTRGAPP1283 YPDVNTFDIT1293 VYLLQGRRLL1303 QPEYCPDPLY1313 EVMLKCWHPK 1323 AEMRPSFSEL1333 VSRISAIFST1343 FIG
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .L1X or .L1X2 or .L1X3 or :3L1X;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1110 or .A:1127 or .A:1128 or .A:1130 or .A:1131 or .A:1134 or .A:1139 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1163 or .A:1195 or .A:1200 or .A:1202 or .A:1211 or .A:1220 or .A:1221 or .A:1222 or .A:1223; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.280
GLY1085
3.986
VAL1092
3.104
ALA1108
3.432
LYS1110
3.531
GLU1127
3.323
GLY1128
4.678
ILE1130
3.592
MET1131
3.449
PHE1134
3.708
VAL1139
3.825
LEU1140
3.765
LEU1157
3.477
|
|||||
| Ligand Name: SAR125844 | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF CMET IN COMPLEX WITH CMPD. | PDB:5HO6 | ||||
| Method | X-ray diffraction | Resolution | 1.97 Å | Mutation | Yes | [6] |
| PDB Sequence |
VQAVQHVVIG
1072 PCVYHGTLIH1106 CAVKSVSQFL1125 TEGIIMKDFS1135 HPNVLSLLGI1145 CGSPLVVLPY 1159 MKHGDLRNFI1169 RNETHNPTVK1179 DLIGFGLQVA1189 KGMKFLASKK1199 FVHRDLAARN 1209 CMLDEKFTVK1219 VADFGLARLP1246 VKWMALESLQ1256 TQKFTTKSDV1266 WSFGVLLWEL 1276 MTRGAPPYPD1286 VNTFDITVYL1296 LQGRRLLQPE1306 YCPDPLYEVM1316 LKCWHPKAEM 1326 RPSFSELVSR1336 ISAIFSTFIG1346 EHYVHVNATY1356
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .63K or .63K2 or .63K3 or :363K;style chemicals stick;color identity;select .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1211 or .A:1221 or .A:1222 or .A:1226; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: AMG 208 | Ligand Info | |||||
| Structure Description | X-ray Structure of c-Met with triazolopyridazine Inhibitor. | PDB:3CD8 | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | Yes | [7] |
| PDB Sequence |
DLSALNPELV
1063 QAVQHVVIGP1073 SSLIVHFNEV1083 IGRGHFGCVY1093 HGTLKIHCAV1109 KSLNRIGEVS 1122 QFLTEGIIMK1132 DFSHPNVLSL1142 LGICSPLVVL1157 PYMKHGDLRN1167 FIRNETHNPT 1177 VKDLIGFGLQ1187 VAKGMKYLAS1197 KKFVHRDLAA1207 RNCMLDEKFT1217 VKVADFGLAR 1227 DMYDKEYYSV1237 HKTGAKLPVK1248 WMALESLQTQ1258 KFTTKSDVWS1268 FGVLLWELMT 1278 RGAPPYPDVN1288 TFDITVYLLQ1298 GRRLLQPEYC1308 PDPLYEVMLK1318 CWHPKAEMRP 1328 SFSELVSRIS1338 AIFSTFIG
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .L5G or .L5G2 or .L5G3 or :3L5G;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.590
GLY1085
4.235
ARG1086
4.727
VAL1092
3.636
ALA1108
3.502
LEU1140
3.916
LEU1157
3.892
PRO1158
3.343
TYR1159
3.338
MET1160
3.174
LYS1161
3.893
|
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| Ligand Name: XL880 | Ligand Info | |||||
| Structure Description | Crystal structure of D1228V cMET bound by foretinib | PDB:6SDC | ||||
| Method | X-ray diffraction | Resolution | 1.67 Å | Mutation | Yes | [4] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLDGK1103 KIHCAVKSLN 1113 RITDIGEVSQ1123 FLTEGIIMKD1133 FSHPNVLSLL1143 GICLRSEGSP1153 LVVLPYMKHG 1163 DLRNFIRNHN1175 PTVKDLIGFG1185 LQVAKGMKYL1195 ASKKFVHRDL1205 AARNCMLDEK 1215 FTVKVADFGL1225 ARVMYDKEYY1235 SVAKLPVKWM1250 ALESLQTQKF1260 TTKSDVWSFG 1270 VLLWELMTRG1280 APPYPDVNTF1290 DITVYLLQGR1300 RLLQPEYCPD1310 PLYEVMLKCW 1320 HPKAEMRPSF1330 SELVSRISAI1340 FSTFIG
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .88Z or .88Z2 or .88Z3 or :388Z;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1110 or .A:1127 or .A:1128 or .A:1131 or .A:1134 or .A:1139 or .A:1140 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1171 or .A:1195 or .A:1200 or .A:1202 or .A:1211 or .A:1220 or .A:1221 or .A:1222 or .A:1223 or .A:1224 or .A:1226 or .A:1228 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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ILE1084
3.144
GLY1085
4.850
VAL1092
3.249
ALA1108
3.313
LYS1110
2.776
GLU1127
3.346
GLY1128
4.012
MET1131
3.338
PHE1134
3.602
VAL1139
3.869
LEU1140
3.758
VAL1155
4.658
LEU1157
3.656
PRO1158
3.296
TYR1159
3.335
MET1160
2.940
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: AMG 337 | Ligand Info | |||||
| Structure Description | Crystal structure of c-Met in complex with AMG 337 | PDB:5EYD | ||||
| Method | X-ray diffraction | Resolution | 1.85 Å | Mutation | No | [8] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLKIHC1107 AVKSLNRITD 1117 IGEVSQFLTE1127 GIIMKDFSHP1137 NVLSLLGICL1147 RSSPLVVLPY1159 MKHGDLRNFI 1169 RNETHNPTVK1179 DLIGFGLQVA1189 KGMKYLASKK1199 FVHRDLAARN1209 CMLDEKFTVK 1219 VADFGLARDM1229 YDKEYYSVHN1239 KTGAKLPVKW1249 MALESLQTQK1259 FTTKSDVWSF 1269 GVLLWELMTR1279 GAPPYPDVNT1289 FDITVYLLQG1299 RRLLQPEYCP1309 DPLYEVMLKC 1319 WHPKAEMRPS1329 FSELVSRISA1339 IFSTFIGEH
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .5T1 or .5T12 or .5T13 or :35T1;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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ILE1084
3.446
GLY1085
3.763
VAL1092
3.538
ALA1108
3.348
LYS1110
4.153
LEU1140
3.979
LEU1157
3.590
PRO1158
3.600
TYR1159
3.779
MET1160
2.979
LYS1161
3.960
HIS1162
4.445
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|||||
| Ligand Name: BMS-777607 | Ligand Info | |||||
| Structure Description | Crystal structure of D1228V cMET bound by BMS-777607 | PDB:6SDD | ||||
| Method | X-ray diffraction | Resolution | 1.93 Å | Mutation | Yes | [4] |
| PDB Sequence |
LVQAVQHVVI
1071 GPSSLIVHFN1081 EVIGHFGCVY1093 HGTLLDNDGK1103 KIHCAVKSLN1113 VSQFLTEGII 1130 MKDFSHPNVL1140 SLLGICLRSP1153 LVVLPYMKHG1163 DLRNFIRNET1173 HNPTVKDLIG 1183 FGLQVAKGMK1193 YLASKKFVHR1203 DLAARNCMLD1213 EKFTVKVADF1223 GLARVMYDKE 1233 YYSVHNKTGA1243 KLPVKWMALE1253 SLQTQKFTTK1263 SDVWSFGVLL1273 WELMTRGAPP 1283 YPDVNTFDIT1293 VYLLQGRRLL1303 QPEYCPDPLY1313 EVMLKCWHPK1323 AEMRPSFSEL 1333 VSRISAIFST1343 F
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .353 or .3532 or .3533 or :3353;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1110 or .A:1124 or .A:1127 or .A:1128 or .A:1131 or .A:1134 or .A:1139 or .A:1140 or .A:1142 or .A:1145 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1163 or .A:1195 or .A:1200 or .A:1202 or .A:1211 or .A:1220 or .A:1221 or .A:1222 or .A:1223; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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ILE1084
3.623
VAL1092
3.727
ALA1108
3.484
LYS1110
3.044
PHE1124
4.166
GLU1127
4.140
GLY1128
4.540
MET1131
3.488
PHE1134
3.884
VAL1139
3.983
LEU1140
3.642
LEU1142
4.768
ILE1145
4.285
VAL1155
3.828
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: SGX523 | Ligand Info | |||||
| Structure Description | Structure of MET receptor tyrosine kinase in complex with inhibitor SGX-523 | PDB:3DKF | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | Yes | [1] |
| PDB Sequence |
TVHIDLSALN
1059 PELVQAVQHV1069 VIGPSSLIVH1079 FNEVIGRGHF1089 GCVYHGTLKK1104 IHCAVKSLNR 1114 ITDIGEVSQF1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLRSEGSPL1154 VVLPYMKHGD 1164 LRNFIRNETH1174 NPTVKDLIGF1184 GLQVAKGMKF1194 LASKKFVHRD1204 LAARNCMLDE 1214 KFTVKVADFG1224 LARDMYKLPV1247 KWMALESLQT1257 QKFTTKSDVW1267 SFGVLLWELM 1277 TRGAPPYPDV1287 NTFDITVYLL1297 QGRRLLQPEY1307 CPDPLYEVML1317 KCWHPKAEMR 1327 PSFSELVSRI1337 SAIFSTFIGE1347 HYVHVNATYV1357 NVKE
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .SX8 or .SX82 or .SX83 or :3SX8;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.659
GLY1085
4.763
VAL1092
3.848
ALA1108
3.524
LEU1140
3.736
LEU1157
3.742
PRO1158
3.598
TYR1159
3.663
MET1160
2.927
ASP1164
3.127
|
|||||
| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: PF-4217903 | Ligand Info | |||||
| Structure Description | X-ray Structure of PF-04217903 bound to the kinase domain of c-Met | PDB:3ZXZ | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | No | [9] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLKKI1105 HCAVKSLNRI 1115 TDIGEVSQFL1125 TEGIIMKDFS1135 HPNVLSLLGI1145 CLRSEGSPLV1155 VLPYMKHGDL 1165 RNFIRNETHN1175 PTVKDLIGFG1185 LQVAKGMKYL1195 ASKKFVHRDL1205 AARNCMLDEK 1215 FTVKVADFGL1225 ARDMYDKEYY1235 SVHNKTGAKL1245 PVKWMALESL1255 QTQKFTTKSD 1265 VWSFGVLLWE1275 LMTRGAPPYP1285 DVNTFDITVY1295 LLQGRRLLQP1305 EYCPDPLYEV 1315 MLKCWHPKAE1325 MRPSFSELVS1335 RISAIFSTFI1345
|
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .KRW or .KRW2 or .KRW3 or :3KRW;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230 or .A:1231; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.410
GLY1085
4.488
VAL1092
3.763
ALA1108
3.389
LEU1140
3.898
LEU1157
3.900
PRO1158
3.520
TYR1159
3.661
MET1160
2.905
GLY1163
4.887
ASP1164
3.477
|
|||||
| Ligand Name: K252a | Ligand Info | |||||
| Structure Description | Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-Met in complex with the microbial alkaloid K-252a | PDB:1R0P | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | Yes | [10] |
| PDB Sequence |
TVHIDLSALN
1059 PELVQAVQHV1069 VIGPSSLIVH1079 FNEVIGRGHF1089 GCVYHGTLLD1099 KIHCAVKSLN 1113 RITDIGEVSQ1123 FLTEGIIMKD1133 FSHPNVLSLL1143 GICLRSEGSP1153 LVVLPYMKHG 1163 DLRNFIRNET1173 HNPTVKDLIG1183 FGLQVAKGMK1193 FLASKKFVHR1203 DLAARNCMLD 1213 EKFTVKVADF1223 GLARDMYDKE1233 FDSVHNKTGA1243 KLPVKWMALE1253 SLQTQKFTTK 1263 SDVWSFGVLL1273 WELMTRGAPP1283 YPITVYLLQG1299 RRLLQPEYCP1309 DPLYEVMLKC 1319 WHPKAEMRPS1329 FSELVSRISA1339 IFSTFIGEHY1349 VHVNATYVNV1359 K |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .KSA or .KSA2 or .KSA3 or :3KSA;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1163 or .A:1211 or .A:1226 or .A:1227 or .A:1228 or .A:1229 or .A:1230 or .A:1231; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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ILE1084
3.241
GLY1085
3.762
ARG1086
3.857
PHE1089
3.856
VAL1092
3.806
ALA1108
3.473
LYS1110
3.730
LEU1140
4.519
LEU1157
3.790
PRO1158
3.008
TYR1159
3.607
|
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| Ligand Name: AM7 | Ligand Info | |||||
| Structure Description | x-ray structure of c-Met with inhibitor. | PDB:2RFN | ||||
| Method | X-ray diffraction | Resolution | 2.50 Å | Mutation | No | [11] |
| PDB Sequence |
ALNPELVQAV
1066 QHVVIGPSSL1076 IVHFNEVIFG1090 CVYHGTLLDN1100 DGKKIHCAVK1110 SLNRITDIGE 1120 VSQFLTEGII1130 MKDFSHPNVL1140 SLLGICLRSE1150 GSPLVVLPYM1160 KHGDLRNFIR 1170 NETHNPTVKD1180 LIGFGLQVAK1190 GMKYLASKKF1200 VHRDLAARNC1210 MLDEKFTVKV 1220 ADPVKWMALE1253 SLQTQKFTTK1263 SDVWSFGVLL1273 WELMTRGAPP1283 YPDVNTFDIT 1293 VYLLQGRRLL1303 QPEYCPDPLY1313 EVMLKCWHPK1323 AEMRPSFSEL1333 VSRISAIFST 1343 FIGEHYVH
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .AM7 or .AM72 or .AM73 or :3AM7;style chemicals stick;color identity;select .A:1084 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1112 or .A:1124 or .A:1127 or .A:1128 or .A:1131 or .A:1140 or .A:1142 or .A:1145 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1211 or .A:1221 or .A:1222; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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ILE1084
3.246
PHE1089
3.487
VAL1092
3.372
ALA1108
3.377
LYS1110
3.445
LEU1112
4.323
PHE1124
3.500
GLU1127
3.265
GLY1128
3.586
MET1131
3.380
LEU1140
3.620
LEU1142
3.415
ILE1145
4.082
|
|||||
| Ligand Name: Phosphonotyrosine | Ligand Info | |||||
| Structure Description | Structure of dually-phosphorylated MET receptor kinase in complex with an MK-2461 analog with specificity for the activated receptor | PDB:3Q6W | ||||
| Method | X-ray diffraction | Resolution | 1.75 Å | Mutation | No | [12] |
| PDB Sequence |
TVHIDLSALN
1059 PELVQAVQHV1069 VIGPSSLIVH1079 FNEVIGRGHF1089 GCVYHGTLLD1099 NDGKKIHCAV 1109 KSLNRITDIG1119 EVSQFLTEGI1129 IMKDFSHPNV1139 LSLLGICLRS1149 EGSPLVVLPY 1159 MKHGDLRNFI1169 RNETHNPTVK1179 DLIGFGLQVA1189 KGMKYLASKK1199 FVHRDLAARN 1209 CMLDEKFTVK1219 VADFGLARDM1229 YDKESVHNKL1245 PVKWMALESL1255 QTQKFTTKSD 1265 VWSFGVLLWE1275 LMTRGAPPYP1285 DVNTFDITVY1295 LLQGRRLLQP1305 EYCPDPLYEV 1315 MLKCWHPKAE1325 MRPSFSELVS1335 RISAIFSTFI1345 GEHHHHH
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .PTR or .PTR2 or .PTR3 or :3PTR;style chemicals stick;color identity;select .A:1201 or .A:1203 or .A:1227 or .A:1228 or .A:1229 or .A:1232 or .A:1233 or .A:1236 or .A:1237 or .A:1238 or .A:1239 or .A:1258 or .A:1259 or .A:1260 or .A:1261; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: N-acetylmethionine | Ligand Info | |||||
| Structure Description | Structure of dually phosphorylated c-MET receptor kinase in complex with an MK-8033 analog | PDB:4IWD | ||||
| Method | X-ray diffraction | Resolution | 1.99 Å | Mutation | No | [13] |
| PDB Sequence |
QNTVHIDLSA
1057 LNPELVQAVQ1067 HVVIGPSSLI1077 VHFNEVIGRG1087 HFGCVYHGTL1097 LDNDGKKIHC 1107 AVKSLNRITD1117 IGEVSQFLTE1127 GIIMKDFSHP1137 NVLSLLGICL1147 RSEGSPLVVL 1157 PYMKHGDLRN1167 FIRNETHNPT1177 VKDLIGFGLQ1187 VAKGMKYLAS1197 KKFVHRDLAA 1207 RNCMLDEKFT1217 VKVADFGLAR1227 DMYDKESVHN1239 KLPVKWMALE1253 SLQTQKFTTK 1263 SDVWSFGVLL1273 WELMTRGAPP1283 YPDVNTFDIT1293 VYLLQGRRLL1303 QPEYCPDPLY 1313 EVMLKCWHPK1323 AEMRPSFSEL1333 VSRISAIFST1343 FIGEHHHHH
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .AME or .AME2 or .AME3 or :3AME;style chemicals stick;color identity;select .A:1048 or .A:1049 or .A:1050 or .A:1051; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: gamma-butyrolactone | Ligand Info | |||||
| Structure Description | Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors | PDB:4R1V | ||||
| Method | X-ray diffraction | Resolution | 1.20 Å | Mutation | No | [3] |
| PDB Sequence |
LSALNPELVQ
1064 AVQHVVIGPS1074 SLIVHFNEVI1084 GRGHFGCVYH1094 GTLLDNDGKK1104 IHCAVKSLNR 1114 ITDIGEVSQF1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLRSSPLVV1156 LPYMKHGDLR 1166 NFIRNETHNP1176 TVKDLIGFGL1186 QVAKGMKYLA1196 SKKFVHRDLA1206 ARNCMLDEKF 1216 TVKVADFGLA1226 RDMYDKEYYS1236 VHNKTGAKLP1246 VKWMALESLQ1256 TQKFTTKSDV 1266 WSFGVLLWEL1276 MTRGAPPYPD1286 VNTFDITVYL1296 LQGRRLLQPE1306 YCPDPLYEVM 1316 LKCWHPKAEM1326 RPSFSELVSR1336 ISAIFSTFI
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .GBL or .GBL2 or .GBL3 or :3GBL;style chemicals stick;color identity;select .A:1089 or .A:1131 or .A:1140 or .A:1141 or .A:1142 or .A:1155 or .A:1157 or .A:1162 or .A:1168 or .A:1171 or .A:1173 or .A:1174 or .A:1204 or .A:1216 or .A:1223 or .A:1224 or .A:1225 or .A:1226 or .A:1227 or .A:1228 or .A:1229 or .A:1235 or .A:1244; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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PHE1089
3.518
MET1131
3.261
LEU1140
3.298
SER1141
3.902
LEU1142
3.857
VAL1155
4.984
LEU1157
3.521
HIS1162
3.578
PHE1168
3.580
ASN1171
2.969
THR1173
4.453
HIS1174
3.543
|
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| Click to View More Binding Site Information of This Target and Ligand Pair | ||||||
| Ligand Name: N-{[4-({5-[(4-aminopiperidin-1-yl)methyl]pyrrolo[2,1-f][1,2,4]triazin-4-yl}oxy)-3-fluorophenyl]carbamoyl}-2-(4-fluorophenyl)acetamide | Ligand Info | |||||
| Structure Description | Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-MET in complex with a Pyrrolotriazine based inhibitor | PDB:3C1X | ||||
| Method | X-ray diffraction | Resolution | 2.17 Å | Mutation | Yes | [14] |
| PDB Sequence |
TVHIDLSALN
1059 PELVQAVQHV1069 VIGPSSLIVH1079 FNEVIGRGHF1089 GCVYHGTLLD1099 NDGKKIHCAV 1109 KSLNRITDIG1119 EVSQFLTEGI1129 IMKDFSHPNV1139 LSLLGICLRS1149 EGSPLVVLPY 1159 MKHGDLRNFI1169 RNETHNPTVK1179 DLIGFGLQVA1189 KGMKFLASKK1199 FVHRDLAARN 1209 CMLDEKFTVK1219 VADFLPVKWM1250 ALESLQTQKF1260 TTKSDVWSFG1270 VLLWELMTRG 1280 APPYPDVNTF1290 DITVYLLQGR1300 RLLQPEYCPD1310 PLYEVMLKCW1320 HPKAEMRPSF 1330 SELVSRISAI1340 FSTFIGEHYV1350 HVNATYVNVK1360
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .CKK or .CKK2 or .CKK3 or :3CKK;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1110 or .A:1127 or .A:1130 or .A:1131 or .A:1134 or .A:1139 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1163 or .A:1164 or .A:1195 or .A:1200 or .A:1202 or .A:1208 or .A:1211 or .A:1220 or .A:1221 or .A:1222 or .A:1223; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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ILE1084
4.411
GLY1085
4.951
VAL1092
3.206
ALA1108
3.286
LYS1110
3.356
GLU1127
2.632
ILE1130
4.852
MET1131
3.458
PHE1134
3.753
VAL1139
4.193
LEU1140
3.604
LEU1157
3.190
PRO1158
3.548
|
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| Ligand Name: N-(6-([1,2,4]triazolo[4,3-a]pyridin-3-ylthio)imidazo[1,2-b]pyridazin-2-yl)cyclopropanecarboxamide | Ligand Info | |||||
| Structure Description | MET Tyrosine Kinase Inhibition Enhances the Antitumor Efficacy of an HGF Antibody | PDB:5UAB | ||||
| Method | X-ray diffraction | Resolution | 1.90 Å | Mutation | No | [15] |
| PDB Sequence |
TDMSPINPEL
1062 VQAVQHVVIG1072 PSSLIVHFNE1082 VIGRGHFGCV1092 YHGTLHCAVK1110 SLNVSQFLTE 1127 GIIMKDFSHP1137 NVLSLLGICL1147 PLVVLPYMKH1162 GDLRNFIRNE1172 THNPTVKDLI 1182 GFGLQVAKGM1192 KYLASKKFVH1202 RDLAARNCML1212 DEKFTVKVAD1222 FGLARDMYDK 1232 EYYSVHNKTG1242 AKLPVKWMAL1252 ESLQTQKFTT1262 KSDVWSFGVL1272 LWELMTRGAP 1282 PYPDVNTFDI1292 TVYLLQGRRL1302 LQPEYCPDPL1312 YEVMLKCWHP1322 KAEMRPSFSE 1332 LVSRISAIFS1342 TFIGEHYVHV1352 NATYVNVK
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .84M or .84M2 or .84M3 or :384M;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.165
VAL1092
3.843
ALA1108
3.478
LEU1140
4.026
LEU1157
3.800
PRO1158
3.467
TYR1159
3.331
MET1160
2.769
LYS1161
3.599
HIS1162
4.168
|
|||||
| Ligand Name: N-(6-(Difluoro(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)methyl)imidazo[1,2-b]pyridazin-2-yl)cyclopropanecarboxamide | Ligand Info | |||||
| Structure Description | MET Tyrosine Kinase Inhibition Enhances the Antitumor Efficacy of an HGF Antibody | PDB:6UBW | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | No | [15] |
| PDB Sequence |
TDMSPINPEL
1062 VQAVQHVVIG1072 PSSLIVHFNE1082 VIGRGHFGCV1092 YHGTLLGKKI1105 HCAVKSLNIG 1119 EVSQFLTEGI1129 IMKDFSHPNV1139 LSLLGICLPL1154 VVLPYMKHGD1164 LRNFIRNETH 1174 NPTVKDLIGF1184 GLQVAKGMKY1194 LASKKFVHRD1204 LAARNCMLDE1214 KFTVKVADFG 1224 LARDMYDKEY1234 YSVHNKTGAK1244 LPVKWMALES1254 LQTQKFTTKS1264 DVWSFGVLLW 1274 ELMTRGAPPY1284 PDVNTFDITV1294 YLLQGRRLLQ1304 PEYCPDPLYE1314 VMLKCWHPKA 1324 EMRPSFSELV1334 SRISAIFSTF1344 IGEHYVHVNA1354 TYVNVK
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .84S or .84S2 or .84S3 or :384S;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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ILE1084
3.384
VAL1092
3.289
ALA1108
3.623
LYS1110
4.285
LEU1140
3.828
LEU1157
3.156
PRO1158
3.531
TYR1159
3.402
MET1160
2.868
LYS1161
3.638
HIS1162
4.118
|
|||||
| Ligand Name: N-(6-((6-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d][1,2,3]triazol-1-yl)methyl)imidazo[1,2-b]pyridazin-2-yl)cyclopropanecarboxamide | Ligand Info | |||||
| Structure Description | MET Tyrosine Kinase Inhibition Enhances the Antitumor Efficacy of an HGF Antibody | PDB:5UAD | ||||
| Method | X-ray diffraction | Resolution | 2.25 Å | Mutation | No | [15] |
| PDB Sequence |
TDMSPINPEL
1062 VQAVQHVVIG1072 PSSLIVHFNE1082 VIGRGHFGCV1092 YHGTLHCAVK1110 SLNIGEVSQF 1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLPLVVLPY1159 MKHGDLRNFI1169 RNETHNPTVK 1179 DLIGFGLQVA1189 KGMKYLASKK1199 FVHRDLAARN1209 CMLDEKFTVK1219 VADFGLARDM 1229 YDKEYYSVHN1239 KTGAKLPVKW1249 MALESLQTQK1259 FTTKSDVWSF1269 GVLLWELMTR 1279 GAPPYPDVNT1289 FDITVYLLQG1299 RRLLQPEYCP1309 DPLYEVMLKC1319 WHPKAEMRPS 1329 FSELVSRISA1339 IFSTFIGEHY1349 VHVNATYVNV1359 K
|
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .84P or .84P2 or .84P3 or :384P;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.049
VAL1092
3.846
ALA1108
3.626
LEU1140
3.861
LEU1157
3.773
PRO1158
3.415
TYR1159
3.433
MET1160
2.878
LYS1161
3.616
HIS1162
4.099
|
|||||
| Ligand Name: N-({4-[(6,7-Dimethoxyquinolin-4-Yl)oxy]phenyl}carbamothioyl)-2-Phenylacetamide | Ligand Info | |||||
| Structure Description | Crystal structure of human c-Met kinase domain with its inhibitor | PDB:3VW8 | ||||
| Method | X-ray diffraction | Resolution | 2.10 Å | Mutation | No | [16] |
| PDB Sequence |
VQYPLTDMSP
1034 ILTSGDDLSL1058 NPELVQAVQH1068 VVIGPSSLIV1078 HFNEVIGRGH1088 FGCVYHGTLL 1098 DNDGKKIHCA1108 VKSLNRITDI1118 GEVSQFLTEG1128 IIMKDFSHPN1138 VLSLLGICLR 1148 SEGSPLVVLP1158 YMKHGDLRNF1168 IRNETHNPTV1178 KDLIGFGLQV1188 AKGMKYLASK 1198 KFVHRDLAAR1208 NCMLDEKFTV1218 KVADFGLARD1228 MYDKEYYSAK1244 LPVKWMALES 1254 LQTQKFTTKS1264 DVWSFGVLLW1274 ELMTRGAPPY1284 PDITVYLLQG1299 RRLLQPEYCP 1309 DPLYEVMLKC1319 WHPKAEMRPS1329 FSELVSRISA1339 IFSTFIGEHY1349 VHV |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .DF6 or .DF62 or .DF63 or :3DF6;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1110 or .A:1127 or .A:1128 or .A:1130 or .A:1131 or .A:1134 or .A:1139 or .A:1140 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1195 or .A:1200 or .A:1202 or .A:1211 or .A:1220 or .A:1221 or .A:1222 or .A:1223; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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ILE1084
3.050
GLY1085
4.664
VAL1092
3.995
ALA1108
3.284
LYS1110
3.621
GLU1127
2.841
GLY1128
4.283
ILE1130
3.406
MET1131
3.516
PHE1134
4.340
VAL1139
3.940
LEU1140
3.421
VAL1155
3.912
LEU1157
3.374
|
|||||
| Ligand Name: N-(3-Fluoro-4-{[2-({3-[(Methylsulfonyl)methyl]phenyl}amino)pyrimidin-4-Yl]oxy}phenyl)-N'-(4-Fluorophenyl)cyclopropane-1,1-Dicarboxamide | Ligand Info | |||||
| Structure Description | Crystal structure of CMET in complex with novel inhibitor | PDB:4MXC | ||||
| Method | X-ray diffraction | Resolution | 1.63 Å | Mutation | No | [17] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLDND1101 GKKIHCAVKS 1111 LNRITDIGEV1121 SQFLTEGIIM1131 KDFSHPNVLS1141 LLGICLRSEG1151 SPLVVLPYMK 1161 HGDLRNFIRN1171 ETHNPTVKDL1181 IGFGLQVAKG1191 MKYLASKKFV1201 HRDLAARNCM 1211 LDEKFTVKVA1221 DFGLARDMYD1231 KEYYSVAKLP1246 VKWMALESLQ1256 TQKFTTKSDV 1266 WSFGVLLWEL1276 MTRGAPPYPD1286 VNTFDITVYL1296 LQGRRLLQPE1306 YCPDPLYEVM 1316 LKCWHPKAEM1326 RPSFSELVSR1336 ISAIFSTFIG1346
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .DWF or .DWF2 or .DWF3 or :3DWF;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1110 or .A:1127 or .A:1128 or .A:1131 or .A:1134 or .A:1139 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1167 or .A:1195 or .A:1200 or .A:1202 or .A:1211 or .A:1220 or .A:1221 or .A:1222 or .A:1223 or .A:1224 or .A:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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ILE1084
3.484
VAL1092
3.222
ALA1108
3.451
LYS1110
2.775
GLU1127
3.542
GLY1128
4.243
MET1131
3.493
PHE1134
3.710
VAL1139
3.780
LEU1140
3.714
LEU1157
3.866
PRO1158
3.218
TYR1159
3.502
MET1160
2.897
LYS1161
4.312
|
|||||
| Ligand Name: N-[3-Fluoro-4-({7-[2-(Morpholin-4-Yl)ethoxy]-1,6-Naphthyridin-4-Yl}oxy)phenyl]-N'-(4-Fluorophenyl)cyclopropane-1,1-Dicarboxamide | Ligand Info | |||||
| Structure Description | Crystal structure of c-Met kinase domain in complex with LXM108 | PDB:5HTI | ||||
| Method | X-ray diffraction | Resolution | 1.66 Å | Mutation | No | [18] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLDND1101 GKKIHCAVKS 1111 LNRITDIGEV1121 SQFLTEGIIM1131 KDFSHPNVLS1141 LLGICLRSEG1151 SPLVVLPYMK 1161 HGDLRNFIRN1171 ETHNPTVKDL1181 IGFGLQVAKG1191 MKYLASKKFV1201 HRDLAARNCM 1211 LDEKFTVKVA1221 DFGLARDMYD1231 KEYYSVAKLP1246 VKWMALESLQ1256 TQKFTTKSDV 1266 WSFGVLLWEL1276 MTRGAPPYPD1286 VNTFDITVYL1296 LQGRRLLQPE1306 YCPDPLYEVM 1316 LKCWHPKAEM1326 RPSFSELVSR1336 ISAIFSTFIG1346
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|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .66L or .66L2 or .66L3 or :366L;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1110 or .A:1127 or .A:1128 or .A:1131 or .A:1134 or .A:1139 or .A:1140 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1195 or .A:1200 or .A:1202 or .A:1211 or .A:1220 or .A:1221 or .A:1222 or .A:1223 or .A:1224; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.167
VAL1092
3.296
ALA1108
3.417
LYS1110
3.032
GLU1127
3.570
GLY1128
4.344
MET1131
3.317
PHE1134
3.591
VAL1139
3.960
LEU1140
3.662
VAL1155
4.950
LEU1157
3.692
PRO1158
3.243
TYR1159
3.217
|
|||||
| Ligand Name: 1-N'-[4-(2-anilinopyrimidin-4-yl)oxy-3-fluorophenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | Ligand Info | |||||
| Structure Description | Crystal structure of CMET in complex with a novel inhibitor | PDB:7V3R | ||||
| Method | X-ray diffraction | Resolution | 1.70 Å | Mutation | No | [19] |
| PDB Sequence |
IDLSALNPEL
1062 VQAVQHVVIG1072 PSSLIVHFNE1082 VIGRGHFGCV1092 YHGTLLDNDG1102 KKIHCAVKSL 1112 NRITDIGEVS1122 QFLTEGIIMK1132 DFSHPNVLSL1142 LGICLRSEGS1152 PLVVLPYMKH 1162 GDLRNFIRNE1172 THNPTVKDLI1182 GFGLQVAKGM1192 KYLASKKFVH1202 RDLAARNCML 1212 DEKFTVKVAD1222 FGLARDMYDK1232 EYYSLPVKWM1250 ALESLQTQKF1260 TTKSDVWSFG 1270 VLLWELMTRG1280 APPYPDVNTD1291 ITVYLLQGRR1301 LLQPEYCPDP1311 LYEVMLKCWH 1321 PKAEMRPSFS1331 ELVSRISAIF1341 STFIG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .5IE or .5IE2 or .5IE3 or :35IE;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1110 or .A:1127 or .A:1128 or .A:1131 or .A:1134 or .A:1139 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1195 or .A:1200 or .A:1202 or .A:1211 or .A:1220 or .A:1221 or .A:1222 or .A:1223; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.433
VAL1092
3.193
ALA1108
3.395
LYS1110
2.991
GLU1127
3.510
GLY1128
4.449
MET1131
3.581
PHE1134
3.586
VAL1139
3.640
LEU1140
3.657
LEU1157
3.718
PRO1158
3.240
TYR1159
3.444
|
|||||
| Ligand Name: 6-[Difluoro-[6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b][1,2,4]triazin-3-yl]methyl]quinoline | Ligand Info | |||||
| Structure Description | Crystal structure of CMET in complex with novel inhibitor | PDB:5EOB | ||||
| Method | X-ray diffraction | Resolution | 1.75 Å | Mutation | No | [20] |
| PDB Sequence |
LSALNPELVQ
1064 AVQHVVIGPS1074 SLIVHFNEVI1084 GRGHFGCVYH1094 GTLLDNDGKK1104 IHCAVKSLNR 1114 ITDIGEVSQF1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLRSEGSPL1154 VVLPYMKHGD 1164 LRNFIRNETH1174 NPTVKDLIGF1184 GLQVAKGMKY1194 LASKKFVHRD1204 LAARNCMLDE 1214 KFTVKVADFG1224 LARDMYDKEY1234 YSVTGAKLPV1247 KWMALESLQT1257 QKFTTKSDVW 1267 SFGVLLWELM1277 TRGAPPYPDV1287 NTFDITVYLL1297 QGRRLLQPEY1307 CPDPLYEVML 1317 KCWHPKAEMR1327 PSFSELVSRI1337 SAIFSTFI
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .5QQ or .5QQ2 or .5QQ3 or :35QQ;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.712
GLY1085
4.712
VAL1092
3.399
ALA1108
3.411
LYS1110
4.395
LEU1140
3.810
LEU1157
3.110
PRO1158
3.696
TYR1159
3.630
MET1160
2.946
|
|||||
| Ligand Name: 2-[3-(4-methoxybenzyl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-6-yl]-1H-indole | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF c-MET IN COMPLEX WITH NOVEL INHIBITOR | PDB:5YA5 | ||||
| Method | X-ray diffraction | Resolution | 1.89 Å | Mutation | No | [21] |
| PDB Sequence |
ALNPELVQAV
1066 QHVVIGPSSL1076 IVHFNEVIGR1086 GHFGCVYHGT1096 LLKKIHCAVK1110 SLNRSQFLTE 1127 GIIMKDFSHP1137 NVLSLLGICS1152 PLVVLPYMKH1162 GDLRNFIRNE1172 THNPTVKDLI 1182 GFGLQVAKGM1192 KYLASKKFVH1202 RDLAARNCML1212 DEKFTVKVAD1222 FGLARDMYDK 1232 EYYSVHNKTG1242 AKLPVKWMAL1252 ESLQTQKFTT1262 KSDVWSFGVL1272 LWELMTRGAP 1282 PYPDVNTFDI1292 TVYLLQGRRL1302 LQPEYCPDPL1312 YEVMLKCWHP1322 KAEMRPSFSE 1332 LVSRISAIFS1342 TFI
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .6TD or .6TD2 or .6TD3 or :36TD;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230 or .A:1231; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
4.176
VAL1092
3.917
ALA1108
3.592
LEU1140
3.743
LEU1157
3.939
PRO1158
3.841
TYR1159
3.516
MET1160
3.176
ASP1164
3.460
ASN1167
3.400
|
|||||
| Ligand Name: 1-N-(4-fluorophenyl)-1-N'-[3-fluoro-4-(10H-pyrido[3,2-b][1,4]benzoxazin-4-yloxy)phenyl]cyclopropane-1,1-dicarboxamide | Ligand Info | |||||
| Structure Description | Crystal structure of CMET in complex with a novel inhibitor | PDB:7V3S | ||||
| Method | X-ray diffraction | Resolution | 1.90 Å | Mutation | No | [19] |
| PDB Sequence |
IDLSALNPEL
1062 VQAVQHVVIG1072 PSSLIVHFNE1082 VIGRGHFGCV1092 YHGTLLDNDG1102 KKIHCAVKSL 1112 NRITDIGEVS1122 QFLTEGIIMK1132 DFSHPNVLSL1142 LGICLRSEGS1152 PLVVLPYMKH 1162 GDLRNFIRNE1172 THNPTVKDLI1182 GFGLQVAKGM1192 KYLASKKFVH1202 RDLAARNCML 1212 DEKFTVKVAD1222 FGLARDMEYY1240 AKLPVKWMAL1252 ESLQTQKFTT1262 KSDVWSFGVL 1272 LWELMTRGAP1282 PYPDVNTFDI1292 TVYLLQGRRL1302 LQPEYCPDPL1312 YEVMLKCWHP 1322 KAEMRPSFSE1332 LVSRISAIFS1342 TFIG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .5I9 or .5I92 or .5I93 or :35I9;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1110 or .A:1127 or .A:1128 or .A:1131 or .A:1134 or .A:1139 or .A:1140 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1195 or .A:1200 or .A:1202 or .A:1211 or .A:1220 or .A:1221 or .A:1222 or .A:1223 or .A:1224; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.456
VAL1092
3.288
ALA1108
3.487
LYS1110
2.818
GLU1127
3.523
GLY1128
4.298
MET1131
3.353
PHE1134
3.598
VAL1139
3.836
LEU1140
3.750
VAL1155
4.901
LEU1157
3.657
PRO1158
3.231
TYR1159
3.292
|
|||||
| Ligand Name: N-(3-Nitrobenzyl)-6-[1-(Piperidin-4-Yl)-1h-Pyrazol-4-Yl]-2-(Trifluoromethyl)pyrido[2,3-D]pyrimidin-4-Amine | Ligand Info | |||||
| Structure Description | Crystal structure of cMET in complex with novel inhibitor | PDB:4GG7 | ||||
| Method | X-ray diffraction | Resolution | 2.27 Å | Mutation | No | [22] |
| PDB Sequence |
QAVQHVVIGP
1073 SSLIVHFNEV1083 IGRGHFGCVY1093 HGTLLDNDGK1103 KIHCAVKSLN1113 RIGEVSQFLT 1126 EGIIMKDFSH1136 PNVLSLLGIC1146 LRSEGSPLVV1156 LPYMKHGDLR1166 NFIRNETHNP 1176 TVKDLIGFGL1186 QVAKGMKYLA1196 SKKFVHRDLA1206 ARNCMLDEKF1216 TVKVADFGLA 1226 RDMYDKEYYS1236 VHNKTGAKLP1246 VKWMALESLQ1256 TQKFTTKSDV1266 WSFGVLLWEL 1276 MTRGAPPYPD1286 VNTFDITVYL1296 LQGRRLLQPE1306 YCPDPLYEVM1316 LKCWHPKAEM 1326 RPSFSELVSR1336 ISAIFSTF
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .0J8 or .0J82 or .0J83 or :30J8;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.363
GLY1085
4.062
ARG1086
4.891
VAL1092
4.104
ALA1108
3.480
LEU1140
3.543
LEU1157
3.128
PRO1158
3.594
TYR1159
3.626
MET1160
2.945
LYS1161
3.401
|
|||||
| Ligand Name: 3-(4-Methylpiperazin-1-Yl)-N-(3-Nitrobenzyl)-7-(Trifluoromethyl)quinolin-5-Amine | Ligand Info | |||||
| Structure Description | Crystal structure of CMET in complex with novel inhibitor | PDB:4GG5 | ||||
| Method | X-ray diffraction | Resolution | 2.42 Å | Mutation | No | [22] |
| PDB Sequence |
QAVQHVVIGP
1073 SSLIVHFNEV1083 IGRGHFGCVY1093 HGTLLDNDGK1103 KIHCAVKSLN1113 RITDIQFLTE 1127 GIIMKDFSHP1137 NVLSLLGICL1147 RSPLVVLPYM1160 KHGDLRNFIR1170 NETHNPTVKD 1180 LIGFGLQVAK1190 GMKYLASKKF1200 VHRDLAARNC1210 MLDEKFTVKV1220 ADFGLARDMY 1230 DKEYYSVHNK1240 TGAKLPVKWM1250 ALESLQTQKF1260 TTKSDVWSFG1270 VLLWELMTRG 1280 APPYPDVNTF1290 DITVYLLQGR1300 RLLQPEYCPD1310 PLYEVMLKCW1320 HPKAEMRPSF 1330 SELVSRISAI1340 FSTF
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .0J3 or .0J32 or .0J33 or :30J3;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1163 or .A:1164 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.557
GLY1085
4.243
VAL1092
3.978
ALA1108
3.602
LEU1140
3.419
LEU1157
2.891
PRO1158
3.128
TYR1159
3.273
MET1160
2.910
LYS1161
3.990
|
|||||
| Ligand Name: (2e)-3-{6-[(1r)-1-(2,6-Dichloro-3-Fluorophenyl)ethoxy]quinolin-3-Yl}-N-Methylprop-2-Enamide | Ligand Info | |||||
| Structure Description | human c-MET kinase domain complexed with 6-benzyloxyquinoline inhibitor | PDB:3A4P | ||||
| Method | X-ray diffraction | Resolution | 2.54 Å | Mutation | Yes | [23] |
| PDB Sequence |
VQAVQHVVIG
1072 PSSLIVHFNE1082 VIGRGHFGCV1092 YHGTLLDKKI1105 HCAVKSLNRI1115 TDIGEVSQFL 1125 TEGIIMKDFS1135 HPNVLSLLGI1145 CLRSEGSPLV1155 VLPYMKHGDL1165 RNFIRNETHN 1175 PTVKDLIGFG1185 LQVAKGMKFL1195 ASKKFVHRDL1205 AARNCMLDEK1215 FTVKVADFGL 1225 ARDMYDKAKL1245 PVKWMALESL1255 QTQKFTTKSD1265 VWSFGVLLWE1275 LMTRGAPPYP 1285 DVNTFDITVY1295 LLQGRRLLQP1305 EYCPDPLYEV1315 MLKCWHPKAE1325 MRPSFSELVS 1335 RISAIFSTFI1345 GEHYVHVNAT1355 YVNVK
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .DFQ or .DFQ2 or .DFQ3 or :3DFQ;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.412
GLY1085
4.292
VAL1092
3.694
ALA1108
3.637
LYS1110
4.543
LEU1140
3.775
LEU1157
3.360
PRO1158
3.245
TYR1159
3.364
MET1160
2.804
LYS1161
2.869
|
|||||
| Ligand Name: 1-[(3r,4r)-4-(1h-Indol-3-Yl)-2,5-Dioxopyrrolidin-3-Yl]pyrrolo[3,2,1-Ij]quinolinium | Ligand Info | |||||
| Structure Description | Crystal structure of the catalytic domain of c-Met kinase in complex with ARQ 197 | PDB:3RHK | ||||
| Method | X-ray diffraction | Resolution | 1.94 Å | Mutation | No | [24] |
| PDB Sequence |
NTVHIDLSAL
1058 NPELVQAVQH1068 VVIGPSSLIV1078 HFNEVIGRGH1088 FGCVYHGTLL1098 DNDGKKIHCA 1108 VKSLNRITDI1118 GEVSQFLTEG1128 IIMKDFSHPN1138 VLSLLGICLR1148 SEGSPLVVLP 1158 YMKHGDLRNF1168 IRNETHNPTV1178 KDLIGFGLQV1188 AKGMKYLASK1198 KFVHRDLAAR 1208 NCMLDEKFTV1218 KVADFGLARD1228 MYDKEYYSVH1238 NKTGAKLPVK1248 WMALESLQTQ 1258 KFTTKSDVWS1268 FGVLLWELMT1278 RGAPPYPDVN1288 TFDITVYLLQ1298 GRRLLQPEYC 1308 PDPLYEVMLK1318 CWHPKAEMRP1328 SFSELVSRIS1338 AIFSTFIG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .M97 or .M972 or .M973 or :3M97;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1163 or .A:1211 or .A:1223 or .A:1226 or .A:1227; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: N-(2,5-Difluoro-4-{[2-(1-Methyl-1h-Pyrazol-4-Yl)pyridin-4-Yl]oxy}phenyl)-N'-(4-Fluorophenyl)cyclopropane-1,1-Dicarboxamide | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF THE HEPATOCYTE GROWTH FACTOR RECEPTOR C-MET IN COMPLEX WITH ALTIRATINIB ANALOG DP-4157 | PDB:5DG5 | ||||
| Method | X-ray diffraction | Resolution | 2.60 Å | Mutation | No | [25] |
| PDB Sequence |
TVHIDLSALN
1059 PELVQAVQHV1069 VIGPSSLIVH1079 FNEVIGRGHF1089 GCVYHGTLLD1099 NDGKKIHCAV 1109 KSLNRITDIG1119 EVSQFLTEGI1129 IMKDFSHPNV1139 LSLLGICLRS1149 EGSPLVVLPY 1159 MKHGDLRNFI1169 RNETHNPTVK1179 DLIGFGLQVA1189 KGMKYLASKK1199 FVHRDLAARN 1209 CMLDEKFTVK1219 VADFGLARDM1229 YDKEYYSVHN1239 KTGAKLPVKW1249 MALESLQTQK 1259 FTTKSDVWSF1269 GVLLWELMTR1279 GAPPYPDVNT1289 FDITVYLLQG1299 RRLLQPEYCP 1309 DPLYEVMLKC1319 WHPKAEMRPS1329 FSELVSRISA1339 IFSTFIG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .5B4 or .5B42 or .5B43 or :35B4;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1110 or .A:1127 or .A:1128 or .A:1130 or .A:1131 or .A:1134 or .A:1139 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1195 or .A:1200 or .A:1202 or .A:1211 or .A:1220 or .A:1221 or .A:1222 or .A:1223 or .A:1234; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.817
VAL1092
3.275
ALA1108
3.296
LYS1110
2.881
GLU1127
3.809
GLY1128
4.449
ILE1130
4.842
MET1131
3.250
PHE1134
3.829
VAL1139
3.491
LEU1140
3.089
LEU1157
3.176
PRO1158
3.162
TYR1159
2.924
|
|||||
| Ligand Name: 6-((6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl)methyl)quinoline | Ligand Info | |||||
| Structure Description | c-Met Kinase in Complex with NVP-BVU972 | PDB:3QTI | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | Yes | [26] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLDKI1105 HCAVKSLNRI 1115 TDIGEVSQFL1125 TEGIIMKDFS1135 HPNVLSLLGI1145 CLRSEGSPLV1155 VLPYMKHGDL 1165 RNFIRNETHN1175 PTVKDLIGFG1185 LQVAKGMKFL1195 ASKKFVHRDL1205 AARNCMLDEK 1215 FTVKVADFGL1225 ARDMYDKEFL1245 PVKWMALESL1255 QTQKFTTKSD1265 VWSFGVLLWE 1275 LMTRGAPPYP1285 DFDITVYLLQ1298 GRRLLQPEYC1308 PDPLYEVMLK1318 CWHPKAEMRP 1328 SFSELVSRIS1338 AIFSTFIGEH1348 YVHVNATYVN1358 VK
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .3QT or .3QT2 or .3QT3 or :33QT;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.481
GLY1085
4.735
VAL1092
3.944
ALA1108
3.437
LEU1140
3.593
LEU1157
4.006
PRO1158
3.618
TYR1159
3.704
MET1160
2.864
LYS1161
4.944
GLY1163
4.749
|
|||||
| Ligand Name: N-({4-[(2-aminopyridin-4-yl)oxy]-3-fluorophenyl}carbamoyl)-2-(4-fluorophenyl)acetamide | Ligand Info | |||||
| Structure Description | Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-met in complex with a aminopyridine based inhibitor | PDB:3CTH | ||||
| Method | X-ray diffraction | Resolution | 2.30 Å | Mutation | Yes | [27] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLDND1101 GKKIHCAVKS 1111 LNRITDIGEV1121 SQFLTEGIIM1131 KDFSHPNVLS1141 LLGICLRSEG1151 SPLVVLPYMK 1161 HGDLRNFIRN1171 ETHNPTVKDL1181 IGFGLQVAKG1191 MKFLASKKFV1201 HRDLAARNCM 1211 LDEKFTVKVA1221 DFGNKTGAKL1245 PVKWMALESL1255 QTQKFTTKSD1265 VWSFGVLLWE 1275 LMTRGAPPYP1285 DVNTFDITVY1295 LLQGRRLLQP1305 EYCPDPLYEV1315 MLKCWHPKAE 1325 MRPSFSELVS1335 RISAIFSTFI1345 GEHYVHVNAT1355 YVNVK
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .319 or .3192 or .3193 or :3319;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1110 or .A:1127 or .A:1130 or .A:1131 or .A:1134 or .A:1139 or .A:1140 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1163 or .A:1195 or .A:1200 or .A:1202 or .A:1211 or .A:1220 or .A:1221 or .A:1222 or .A:1223 or .A:1224; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
4.192
VAL1092
2.922
ALA1108
3.419
LYS1110
3.042
GLU1127
3.022
ILE1130
4.148
MET1131
3.158
PHE1134
3.602
VAL1139
4.001
LEU1140
3.751
VAL1155
4.424
LEU1157
3.016
PRO1158
3.190
|
|||||
| Ligand Name: 1-(4-fluorophenyl)-N-[3-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]-2-oxo-1,2-dihydropyridine-3-carboxamide | Ligand Info | |||||
| Structure Description | Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor C-MET in complex with a Pyrrolopyridinepyridone based inhibitor | PDB:3CE3 | ||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | Yes | [28] |
| PDB Sequence |
DLSALNPELV
1063 QAVQHVVIGP1073 SSLIVHFNEV1083 IGRGHFGCVY1093 HGTLLDNDGK1103 KIHCAVKSLN 1113 RITDIGEVSQ1123 FLTEGIIMKD1133 FSHPNVLSLL1143 GICLRSEGSP1153 LVVLPYMKHG 1163 DLRNFIRNET1173 HNPTVKDLIG1183 FGLQVAKGMK1193 FLASKKFVHR1203 DLAARNCMLD 1213 EKFTVKVADF1223 GNKTGAKLPV1247 KWMALESLQT1257 QKFTTKSDVW1267 SFGVLLWELM 1277 TRGAPPYPDV1287 NTFDITVYLL1297 QGRRLLQPEY1307 CPDPLYEVML1317 KCWHPKAEMR 1327 PSFSELVSRI1337 SAIFSTFIGE1347 HYVHVNATYV1357 NVK
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .1FN or .1FN2 or .1FN3 or :31FN;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1110 or .A:1127 or .A:1128 or .A:1130 or .A:1131 or .A:1134 or .A:1139 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1163 or .A:1195 or .A:1200 or .A:1202 or .A:1211 or .A:1220 or .A:1221 or .A:1222 or .A:1223 or .A:1224; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.751
VAL1092
3.436
ALA1108
3.333
LYS1110
3.076
GLU1127
3.252
GLY1128
4.610
ILE1130
4.973
MET1131
3.085
PHE1134
3.853
VAL1139
3.954
LEU1140
3.755
LEU1157
3.051
PRO1158
3.296
|
|||||
| Ligand Name: 2-({4-[(2-aminopyridin-4-yl)oxy]-3-fluorophenyl}amino)-N-(2,4-difluorophenyl)pyridine-3-carboxamide | Ligand Info | |||||
| Structure Description | Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor C-MET in complex with a biarylamine based inhibitor | PDB:3L8V | ||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | Yes | [29] |
| PDB Sequence |
DLSALNPELV
1063 QAVQHVVIGP1073 SSLIVHFNEV1083 IGRGHFGCVY1093 HGTLLDNDGK1103 KIHCAVKSLN 1113 RITDIGEVSQ1123 FLTEGIIMKD1133 FSHPNVLSLL1143 GICLRSEGSP1153 LVVLPYMKHG 1163 DLRNFIRNET1173 HNPTVKDLIG1183 FGLQVAKGMK1193 FLASKKFVHR1203 DLAARNCMLD 1213 EKFTVKVADF1223 GNKTGAKLPV1247 KWMALESLQT1257 QKFTTKSDVW1267 SFGVLLWELM 1277 TRGAPPYPDV1287 NTFDITVYLL1297 QGRRLLQPEY1307 CPDPLYEVML1317 KCWHPKAEMR 1327 PSFSELVSRI1337 SAIFSTFIGE1347 HYVHVNATYV1357 NVK
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .L8V or .L8V2 or .L8V3 or :3L8V;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1110 or .A:1127 or .A:1128 or .A:1131 or .A:1134 or .A:1139 or .A:1140 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1163 or .A:1195 or .A:1200 or .A:1202 or .A:1211 or .A:1220 or .A:1221 or .A:1222 or .A:1223; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.423
VAL1092
3.211
ALA1108
3.551
LYS1110
3.444
GLU1127
3.650
GLY1128
3.850
MET1131
3.349
PHE1134
3.640
VAL1139
3.837
LEU1140
3.980
VAL1155
3.682
LEU1157
3.007
|
|||||
| Ligand Name: 2-(4-fluorophenyl)-N-{[3-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]carbamoyl}acetamide | Ligand Info | |||||
| Structure Description | Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-met in complex with a aminopyridine based inhibitor | PDB:3CTJ | ||||
| Method | X-ray diffraction | Resolution | 2.50 Å | Mutation | Yes | [27] |
| PDB Sequence |
VHIDLSALNP
1060 ELVQAVQHVV1070 IGPSSLIVHF1080 NEVIGRGHFG1090 CVYHGTLLDN1100 DGKKIHCAVK 1110 SLNRITDIGE1120 VSQFLTEGII1130 MKDFSHPNVL1140 SLLGICLRSE1150 GSPLVVLPYM 1160 KHGDLRNFIR1170 NETHNPTVKD1180 LIGFGLQVAK1190 GMKFLASKKF1200 VHRDLAARNC 1210 MLDEKFTVKV1220 ADFLPVKWMA1251 LESLQTQKFT1261 TKSDVWSFGV1271 LLWELMTRGA 1281 PPYPDVNTFD1291 ITVYLLQGRR1301 LLQPEYCPDP1311 LYEVMLKCWH1321 PKAEMRPSFS 1331 ELVSRISAIF1341 STFIGEHYVH1351 VNATYVNVK
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .320 or .3202 or .3203 or :3320;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1110 or .A:1127 or .A:1130 or .A:1131 or .A:1134 or .A:1139 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1163 or .A:1195 or .A:1200 or .A:1202 or .A:1211 or .A:1220 or .A:1221 or .A:1222 or .A:1223; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
4.455
VAL1092
3.464
ALA1108
3.710
LYS1110
3.935
GLU1127
3.809
ILE1130
3.852
MET1131
3.559
PHE1134
3.962
VAL1139
4.208
LEU1140
3.779
LEU1157
3.364
PRO1158
3.464
|
|||||
| Ligand Name: methyl N-[6-[[6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulfanyl]-1H-benzimidazol-2-yl]carbamate | Ligand Info | |||||
| Structure Description | CRYSTAL STRUCTURE OF CMET WT with compound 3 | PDB:5HNI | ||||
| Method | X-ray diffraction | Resolution | 1.71 Å | Mutation | No | [6] |
| PDB Sequence |
VQAVQHVVIG
1072 PGCVYHGTLK1104 IHCAVKSVSQ1123 FLTEGIIMKD1133 FSHPNVLSLL1143 GICLRSEGSP 1153 LVVLPYMKHG1163 DLRNFIRNET1173 HNPTVKDLIG1183 FGLQVAKGMK1193 FLASKKFVHR 1203 DLAARNCMLD1213 EKFTVKVADF1223 GLARDMYWMA1251 LESLQTQKFT1261 TKSDVWSFGV 1271 LLWELMTRGA1281 PPYPDVNTFD1291 ITVYLLQGRR1301 LLQPEYCPDP1311 LYEVMLKCWH 1321 PKAEMRPSFS1331 ELVSRISAIF1341 STFIGEHYVH1351 VNATY
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .63B or .63B2 or .63B3 or :363B;style chemicals stick;color identity;select .X:1092 or .X:1094 or .X:1108 or .X:1140 or .X:1157 or .X:1158 or .X:1159 or .X:1160 or .X:1161 or .X:1162 or .X:1163 or .X:1164 or .X:1167 or .X:1208 or .X:1209 or .X:1211 or .X:1221 or .X:1222 or .X:1223 or .X:1226 or .X:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
VAL1092
3.798
HIS1094
4.960
ALA1108
3.592
LEU1140
3.822
LEU1157
3.948
PRO1158
3.472
TYR1159
3.458
MET1160
2.896
LYS1161
3.935
HIS1162
4.136
GLY1163
3.048
|
|||||
| Ligand Name: 4-[(6-Phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl]phenol | Ligand Info | |||||
| Structure Description | X-ray structure of c-Met with triazolopyridazine inhibitor. | PDB:3CCN | ||||
| Method | X-ray diffraction | Resolution | 1.90 Å | Mutation | Yes | [7] |
| PDB Sequence |
LSALNPELVQ
1064 AVQHVVIGPS1074 SLIVHFNEVI1084 GRGHFGCVYH1094 GTLKIHCAVK1110 SLNREVSQFL 1125 TEGIIMKDFS1135 HPNVLSLLGI1145 CLPLVVLPYM1160 KHGDLRNFIR1170 NETHNPTVKD 1180 LIGFGLQVAK1190 GMKYLASKKF1200 VHRDLAARNC1210 MLDEKFTVKV1220 ADFGLARDMY 1230 DKEYYSVHKT1241 GAKLPVKWMA1251 LESLQTQKFT1261 TKSDVWSFGV1271 LLWELMTRGA 1281 PPYPDVNTFD1291 ITVYLLQGRR1301 LLQPEYCPDP1311 LYEVMLKCWH1321 PKAEMRPSFS 1331 ELVSRISAIF1341 STFIG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .LKG or .LKG2 or .LKG3 or :3LKG;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.600
GLY1085
4.278
VAL1092
3.722
ALA1108
3.353
LEU1140
3.917
LEU1157
3.682
PRO1158
3.463
TYR1159
3.630
MET1160
2.989
ASP1164
3.539
|
|||||
| Ligand Name: 5-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-2-[(4-fluorophenyl)amino]-3-methylpyrimidin-4(3H)-one | Ligand Info | |||||
| Structure Description | Structure of c-Met with pyrimidone inhibitor 50 | PDB:3EFK | ||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | Yes | [30] |
| PDB Sequence |
DLSALNPELV
1063 QAVQHVVIGP1073 SSLIVHFNEV1083 IGRGHFGCVY1093 HGTLLDNDGK1103 KIHCAVKSLN 1113 RITDIGEVSQ1123 FLTEGIIMKD1133 FSHPNVLSLL1143 GICLRSEGSP1153 LVVLPYMKHG 1163 DLRNFIRNET1173 HNPTVKDLIG1183 FGLQVAKGMK1193 YLASKKFVHR1203 DLAARNCMLD 1213 EKFTVKVADF1223 PVKWMALESL1255 QTQKFTTKSD1265 VWSFGVLLWE1275 LMTRGAPPYP 1285 DVNTFDITVY1295 LLQGRRLLQP1305 EYCPDPLYEV1315 MLKCWHPKAE1325 MRPSFSELVS 1335 RISAIFSTFI1345 GEHYVH
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .MT4 or .MT42 or .MT43 or :3MT4;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1124 or .A:1125 or .A:1127 or .A:1128 or .A:1131 or .A:1140 or .A:1142 or .A:1145 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1211 or .A:1221 or .A:1222 or .A:1223; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.338
GLY1085
4.166
ARG1086
4.477
PHE1089
3.501
VAL1092
2.954
ALA1108
3.340
LYS1110
3.893
PHE1124
3.161
LEU1125
4.842
GLU1127
3.561
GLY1128
3.191
MET1131
3.515
LEU1140
3.342
LEU1142
3.789
|
|||||
| Ligand Name: N-(3-Chlorophenyl)-N-Methyl-2-Oxo-3-[(3,4,5-Trimethyl-1h-Pyrrol-2-Yl)methyl]-2h-Indole-5-Sulfonamide | Ligand Info | |||||
| Structure Description | X-ray structure of SU11274 bound to c-Met | PDB:2RFS | ||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | No | [11] |
| PDB Sequence |
QHVVIGPSSL
1076 IVHFNEVIGR1086 GHFGCVYHGT1096 LKIHCAVKSL1112 NIGEVSQFLT1126 EGIIMKDFSH 1136 PNVLSLLGIC1146 LSPLVVLPYM1160 KHGDLRNFIR1170 NETHNPTVKD1180 LIGFGLQVAK 1190 GMKYLASKKF1200 VHRDLAARNC1210 MLDEKFTVKV1220 ADFGLARDMY1230 DKEYYSVHTG 1242 AKLPVKWMAL1252 ESLQTQKFTT1262 KSDVWSFGVL1272 LWELMTRGAP1282 PYPDVNTFDI 1292 TVYLLQGRRL1302 LQPEYCPDPL1312 YEVMLKCWHP1322 KAEMRPSFSE1332 LVSRISAIFS 1342 TFIG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .AM8 or .AM82 or .AM83 or :3AM8;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1208 or .A:1209 or .A:1211 or .A:1221 or .A:1222 or .A:1223 or .A:1226 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.487
GLY1085
3.482
VAL1092
3.246
ALA1108
3.514
LEU1140
3.562
LEU1157
3.718
PRO1158
2.979
TYR1159
3.377
MET1160
2.974
LYS1161
3.302
HIS1162
4.885
|
|||||
| Ligand Name: 2-benzyl-5-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-3-methylpyrimidin-4(3H)-one | Ligand Info | |||||
| Structure Description | Structure of c-Met with pyrimidone inhibitor 7 | PDB:3EFJ | ||||
| Method | X-ray diffraction | Resolution | 2.60 Å | Mutation | Yes | [30] |
| PDB Sequence |
DLSALNPELV
1063 QAVQHVVIGP1073 SSLIVHFNEV1083 IGRGHFGCVY1093 HGTLLDNDGK1103 KIHCAVKSLN 1113 RITDIGEVSQ1123 FLTEGIIMKD1133 FSHPNVLSLL1143 GICLRSEGSP1153 LVVLPYMKHG 1163 DLRNFIRNET1173 HNPTVKDLIG1183 FGLQVAKGMK1193 YLASKKFVHR1203 DLAARNCMLD 1213 EKFTVKVADF1223 PVKWMALESL1255 QTQKFTTKSD1265 VWSFGVLLWE1275 LMTRGAPPYP 1285 DVNTFDITVY1295 LLQGRRLLQP1305 EYCPDPLYEV1315 MLKCWHPKAE1325 MRPSFSELVS 1335 RISAIFSTFI1345 GEHYVH
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .MT3 or .MT32 or .MT33 or :3MT3;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1112 or .A:1124 or .A:1127 or .A:1128 or .A:1131 or .A:1140 or .A:1142 or .A:1145 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1211 or .A:1221 or .A:1222 or .A:1223; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.380
GLY1085
4.157
PHE1089
3.612
VAL1092
3.156
ALA1108
3.405
LYS1110
2.996
LEU1112
4.384
PHE1124
3.497
GLU1127
3.564
GLY1128
3.615
MET1131
3.680
LEU1140
3.916
LEU1142
3.711
ILE1145
4.022
|
|||||
| Ligand Name: 6-{(1r)-1-Fluoro-1-[8-Fluoro-6-(3-Methyl-1,2-Oxazol-5-Yl)[1,2,4]triazolo[4,3-A]pyridin-3-Yl]ethyl}-3-Methoxyquinoline | Ligand Info | |||||
| Structure Description | Crystal structure of c-Met in complex with (R)-5-(8-fluoro-3-(1-fluoro-1-(3-methoxyquinolin-6-yl)ethyl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-3-methylisoxazole | PDB:4XMO | ||||
| Method | X-ray diffraction | Resolution | 1.75 Å | Mutation | No | [31] |
| PDB Sequence |
VHIDLSALNP
1060 ELVQAVQHVV1070 IGPSSLIVHF1080 NEVIGRGHFG1090 CVYHGTLKIH1106 CAVKSLNRIT 1116 DIGEVSQFLT1126 EGIIMKDFSH1136 PNVLSLLGIC1146 LRSEGSPLVV1156 LPYMKHGDLR 1166 NFIRNETHNP1176 TVKDLIGFGL1186 QVAKGMKYLA1196 SKKFVHRDLA1206 ARNCMLDEKF 1216 TVKVADFGLA1226 RDMYDKEYYS1236 VHNKTGAKLP1246 VKWMALESLQ1256 TQKFTTKSDV 1266 WSFGVLLWEL1276 MTRGAPPYPD1286 VNTFDITVYL1296 LQGRRLLQPE1306 YCPDPLYEVM 1316 LKCWHPKAEM1326 RPSFSELVSR1336 ISAIFSTFI
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .46G or .46G2 or .46G3 or :346G;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.206
GLY1085
4.836
ARG1086
4.523
VAL1092
3.667
ALA1108
3.405
LYS1110
3.997
LEU1140
3.826
LEU1157
3.635
PRO1158
3.729
TYR1159
3.665
MET1160
2.936
|
|||||
| Ligand Name: 6-[(1~{r})-1-[8-Fluoranyl-6-(3-Methyl-1,2-Oxazol-5-Yl)-[1,2,4]triazolo[4,3-A]pyridin-3-Yl]ethyl]-1,6-Naphthyridin-5-One | Ligand Info | |||||
| Structure Description | Crystal structure of c-Met in complex with naphthyridinone inhibitor 5 | PDB:5EYC | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | No | [8] |
| PDB Sequence |
IDLSALNPEL
1062 VQAVQHVVIG1072 PSSLIVHFNE1082 VIGRGHFGCV1092 YHGTLLKIHC1107 AVKSLNRITD 1117 IGEVSQFLTE1127 GIIMKDFSHP1137 NVLSLLGICL1147 RSEGSPLVVL1157 PYMKHGDLRN 1167 FIRNETHNPT1177 VKDLIGFGLQ1187 VAKGMKYLAS1197 KKFVHRDLAA1207 RNCMLDEKFT 1217 VKVADFGLAR1227 DMYDKEYYSV1237 HNKTGAKLPV1247 KWMALESLQT1257 QKFTTKSDVW 1267 SFGVLLWELM1277 TRGAPPYPDV1287 NTFDITVYLL1297 QGRRLLQPEY1307 CPDPLYEVML 1317 KCWHPKAEMR1327 PSFSELVSRI1337 SAIFSTFI
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .5SZ or .5SZ2 or .5SZ3 or :35SZ;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.482
GLY1085
3.788
ARG1086
4.919
VAL1092
3.473
ALA1108
3.405
LYS1110
4.113
LEU1140
3.906
LEU1157
3.547
PRO1158
3.621
TYR1159
3.648
MET1160
3.030
|
|||||
| Ligand Name: 6-{(1s)-1-[8-Fluoro-6-(3-Methyl-1,2-Oxazol-5-Yl)[1,2,4]triazolo[4,3-A]pyridin-3-Yl]ethyl}-3-(2-Methoxyethoxy)quinoline | Ligand Info | |||||
| Structure Description | Crystal structure of c-Met in complex with (S)-5-(8-fluoro-3-(1-(3-(2-methoxyethoxy)quinolin-6-yl)ethyl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl)-3-methylisoxazole | PDB:4XYF | ||||
| Method | X-ray diffraction | Resolution | 1.85 Å | Mutation | No | [31] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLKIH1106 CAVKSLNRIT 1116 DIGEVSQFLT1126 EGIIMKDFSH1136 PNVLSLLGIC1146 LRSEGSPLVV1156 LPYMKHGDLR 1166 NFIRNETHNP1176 TVKDLIGFGL1186 QVAKGMKYLA1196 SKKFVHRDLA1206 ARNCMLDEKF 1216 TVKVADFGLA1226 RDMYDKEYYS1236 VHNKTGAKLP1246 VKWMALESLQ1256 TQKFTTKSDV 1266 WSFGVLLWEL1276 MTRGAPPYPD1286 VNTFDITVYL1296 LQGRRLLQPE1306 YCPDPLYEVM 1316 LKCWHPKAEM1326 RPSFSELVSR1336 ISAIFSTFIG1346
|
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .44X or .44X2 or .44X3 or :344X;style chemicals stick;color identity;select .A:1084 or .A:1086 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.388
ARG1086
4.791
VAL1092
3.895
ALA1108
3.355
LYS1110
4.253
LEU1140
3.914
LEU1157
3.611
PRO1158
3.760
TYR1159
3.213
MET1160
2.961
LYS1161
3.688
HIS1162
4.101
|
|||||
| Ligand Name: 5-Phenyl-3-(Quinolin-6-Ylmethyl)-3,5,6,7-Tetrahydro-4h-[1,2,3]triazolo[4,5-C]pyridin-4-One | Ligand Info | |||||
| Structure Description | Crystal structure of c-Met in complex with triazolopyridinone inhibitor 3 | PDB:4DEH | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | No | [32] |
| PDB Sequence |
IDLSALNPEL
1062 VQAVQHVVIG1072 PSSLIVHFNE1082 VIGRGHFGCV1092 YHGTLKIHCA1108 VKSLNRITDI 1118 GEVSQFLTEG1128 IIMKDFSHPN1138 VLSLLGICLR1148 GSPLVVLPYM1160 KHGDLRNFIR 1170 NETHNPTVKD1180 LIGFGLQVAK1190 GMKYLASKKF1200 VHRDLAARNC1210 MLDEKFTVKV 1220 ADFGLARDMY1230 DKEYYSVHNK1240 TGAKLPVKWM1250 ALESLQTQKF1260 TTKSDVWSFG 1270 VLLWELMTRG1280 APPYPDVNTF1290 DITVYLLQGR1300 RLLQPEYCPD1310 PLYEVMLKCW 1320 HPKAEMRPSF1330 SELVSRISAI1340 FSTFIG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .0JK or .0JK2 or .0JK3 or :30JK;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.668
GLY1085
4.988
VAL1092
3.901
ALA1108
3.487
LEU1140
4.082
LEU1157
3.854
PRO1158
3.517
TYR1159
3.569
MET1160
3.060
ASP1164
3.481
|
|||||
| Ligand Name: 7-methoxy-N-((6-(3-methylisothiazol-5-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)-1,5-naphthyridin-4-amine | Ligand Info | |||||
| Structure Description | Crystal structure of c-Met in complex with triazolopyridazine inhibitor 2 | PDB:4DEG | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | No | [32] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLKIHC1107 AVKSLNRITD 1117 IGEVSQFLTE1127 GIIMKDFSHP1137 NVLSLLGICL1147 RSPLVVLPYM1160 KHGDLRNFIR 1170 NETHNPTVKD1180 LIGFGLQVAK1190 GMKYLASKKF1200 VHRDLAARNC1210 MLDEKFTVKV 1220 ADFGLARDMY1230 DKEYYSVHNK1240 TGAKLPVKWM1250 ALESLQTQKF1260 TTKSDVWSFG 1270 VLLWELMTRG1280 APPYPDVNTF1290 DITVYLLQGR1300 RLLQPEYCPD1310 PLYEVMLKCW 1320 HPKAEMRPSF1330 SELVSRISAI1340 FSTFIG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .0JJ or .0JJ2 or .0JJ3 or :30JJ;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.256
GLY1085
4.307
ARG1086
4.796
VAL1092
3.766
ALA1108
3.456
LYS1110
4.653
LEU1140
3.763
LEU1157
3.771
PRO1158
3.350
TYR1159
3.851
MET1160
3.084
LYS1161
3.728
|
|||||
| Ligand Name: 7-methoxy-N-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl]-1,5-naphthyridin-4-amine | Ligand Info | |||||
| Structure Description | Crystal structure of c-Met with triazolopyridazine inhibitor 13 | PDB:3I5N | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | Yes | [33] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLDND1101 GKKIHCAVKS 1111 LNREVSQFLT1126 EGIIMKDFSH1136 PNVLSLLGIC1146 LPLVVLPYMK1161 HGDLRNFIRN 1171 ETHNPTVKDL1181 IGFGLQVAKG1191 MKYLASKKFV1201 HRDLAARNCM1211 LDEKFTVKVA 1221 DFGLARDMYD1231 KEYYSVHKLP1246 VKWMALESLQ1256 TQKFTTKSDV1266 WSFGVLLWEL 1276 MTRGAPPYPD1286 VNTFDITVYL1296 LQGRRLLQPE1306 YCPDPLYEVM1316 LKCWHPKAEM 1326 RPSFSELVSR1336 ISAIFSTFIG1346
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .B2D or .B2D2 or .B2D3 or :3B2D;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.317
GLY1085
4.331
VAL1092
3.673
ALA1108
3.483
LYS1110
4.950
LEU1140
3.933
LEU1157
3.815
PRO1158
3.283
TYR1159
3.538
MET1160
3.097
LYS1161
4.006
|
|||||
| Ligand Name: N-[3-Fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl]-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide | Ligand Info | |||||
| Structure Description | Crystal structure of the c-Met kinase domain in complex with a pyrazolone inhibitor | PDB:5T3Q | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | No | [34] |
| PDB Sequence |
TVHIDLSALN
1059 PELVQAVQHV1069 VIGPSSLIVH1079 FNEVIGHFGC1091 VYHGTLLDND1101 GKKIHCAVKS 1111 LNRITDIGEV1121 SQFLTEGIIM1131 KDFSHPNVLS1141 LLGICLRSEG1151 SPLVVLPYMK 1161 HGDLRNFIRN1171 ETHNPTVKDL1181 IGFGLQVAKG1191 MKYLASKKFV1201 HRDLAARNCM 1211 LDEKFTVKVA1221 DLPVKWMALE1253 SLQTQKFTTK1263 SDVWSFGVLL1273 WELMTRGAPP 1283 YPDVNTFDIT1293 VYLLQGRRLL1303 QPEYCPDPLY1313 EVMLKCWHPK1323 AEMRPSFSEL 1333 VSRISAIFST1343 FIGEHYVH
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .75H or .75H2 or .75H3 or :375H;style chemicals stick;color identity;select .A:1084 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1112 or .A:1124 or .A:1127 or .A:1128 or .A:1131 or .A:1140 or .A:1142 or .A:1145 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1163 or .A:1200 or .A:1211 or .A:1221 or .A:1222; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.339
PHE1089
3.840
VAL1092
3.177
ALA1108
3.456
LYS1110
3.817
LEU1112
3.831
PHE1124
3.445
GLU1127
3.275
GLY1128
3.974
MET1131
3.377
LEU1140
3.591
LEU1142
4.603
|
|||||
| Ligand Name: N-{4-[(6,7-Dimethoxyquinolin-4-Yl)oxy]-3-Fluorophenyl}-1,5-Dimethyl-3-Oxo-2-Phenyl-2,3-Dihydro-1h-Pyrazole-4-Carboxamide | Ligand Info | |||||
| Structure Description | Crystal structure of c-Met in complex with pyrazolone inhibitor 26 | PDB:3U6H | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | No | [35] |
| PDB Sequence |
VHIDLSALNP
1060 ELVQAVQHVV1070 IGPSSLIVHF1080 NEVIGRGHFG1090 CVYHGTLLDN1100 DGKKIHCAVK 1110 SLNRITDIGE1120 VSQFLTEGII1130 MKDFSHPNVL1140 SLLGICLRSE1150 GSPLVVLPYM 1160 KHGDLRNFIR1170 NETHNPTVKD1180 LIGFGLQVAK1190 GMKYLASKKF1200 VHRDLAARNC 1210 MLDEKFTVKV1220 ADFGPVKWMA1251 LESLQTQKFT1261 TKSDVWSFGV1271 LLWELMTRGA 1281 PPYPDVNTFD1291 ITVYLLQGRR1301 LLQPEYCPDP1311 LYEVMLKCWH1321 PKAEMRPSFS 1331 ELVSRISAIF1341 STFIGEHYVH1351
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .03X or .03X2 or .03X3 or :303X;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1124 or .A:1127 or .A:1128 or .A:1131 or .A:1140 or .A:1142 or .A:1145 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1211 or .A:1221 or .A:1222 or .A:1223 or .A:1224; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.305
GLY1085
3.772
ARG1086
4.742
PHE1089
3.576
VAL1092
3.200
ALA1108
3.469
LYS1110
4.044
PHE1124
3.387
GLU1127
3.035
GLY1128
3.745
MET1131
3.370
LEU1140
3.565
LEU1142
4.423
ILE1145
4.201
|
|||||
| Ligand Name: 3-{(1s)-1-[3-(2-Methoxyethoxy)quinolin-6-Yl]ethyl}-5-(3-Methyl-1,2-Thiazol-5-Yl)-3,5-Dihydro-4h-[1,2,3]triazolo[4,5-C]pyridin-4-One | Ligand Info | |||||
| Structure Description | Crystal structure of c-Met in complex with triazolopyridinone inhibitor 24 | PDB:4DEI | ||||
| Method | X-ray diffraction | Resolution | 2.05 Å | Mutation | No | [32] |
| PDB Sequence |
IDLSALNPEL
1062 VQAVQHVVIG1072 PSSLIVHFNE1082 VIGRGHFGCV1092 YHGTLLDKIH1106 CAVKSLNRIG 1119 EVSQFLTEGI1129 IMKDFSHPNV1139 LSLLGICLRS1149 EGSPLVVLPY1159 MKHGDLRNFI 1169 RNETHNPTVK1179 DLIGFGLQVA1189 KGMKYLASKK1199 FVHRDLAARN1209 CMLDEKFTVK 1219 VADFGLARDM1229 YDKEYYSVHN1239 KTGAKLPVKW1249 MALESLQTQK1259 FTTKSDVWSF 1269 GVLLWELMTR1279 GAPPYPDVNT1289 FDITVYLLQG1299 RRLLQPEYCP1309 DPLYEVMLKC 1319 WHPKAEMRPS1329 FSELVSRISA1339 IFSTFIG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .0JL or .0JL2 or .0JL3 or :30JL;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230 or .A:1231; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.558
GLY1085
4.812
VAL1092
3.873
ALA1108
3.510
LYS1110
4.161
LEU1140
3.836
LEU1157
3.260
PRO1158
3.626
TYR1159
3.372
MET1160
2.937
LYS1161
3.699
GLY1163
4.091
|
|||||
| Ligand Name: N-{3-Fluoro-4-[(7-Methoxyquinolin-4-Yl)oxy]phenyl}-1-[(2r)-2-Hydroxypropyl]-5-Methyl-3-Oxo-2-Phenyl-2,3-Dihydro-1h-Pyrazole-4-Carboxamide | Ligand Info | |||||
| Structure Description | Crystal structure of c-Met in complex with pyrazolone inhibitor 58a | PDB:3U6I | ||||
| Method | X-ray diffraction | Resolution | 2.10 Å | Mutation | No | [35] |
| PDB Sequence |
VHIDLSALNP
1060 ELVQAVQHVV1070 IGPSSLIVHF1080 NEVIGRGHFG1090 CVYHGTLLDN1100 DGKKIHCAVK 1110 SLNRITDIGE1120 VSQFLTEGII1130 MKDFSHPNVL1140 SLLGICLRSE1150 GSPLVVLPYM 1160 KHGDLRNFIR1170 NETHNPTVKD1180 LIGFGLQVAK1190 GMKYLASKKF1200 VHRDLAARNC 1210 MLDEKFTVKV1220 ADFGLPVKWM1250 ALESLQTQKF1260 TTKSDVWSFG1270 VLLWELMTRG 1280 APPYPDVNTF1290 DITVYLLQGR1300 RLLQPEYCPD1310 PLYEVMLKCW1320 HPKAEMRPSF 1330 SELVSRISAI1340 FSTFIGEHYV1350 H
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .044 or .0442 or .0443 or :3044;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1112 or .A:1124 or .A:1127 or .A:1128 or .A:1130 or .A:1131 or .A:1140 or .A:1142 or .A:1145 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1163 or .A:1200 or .A:1211 or .A:1221 or .A:1222 or .A:1223 or .A:1224; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.599
GLY1085
4.536
PHE1089
3.484
VAL1092
3.271
ALA1108
3.472
LYS1110
3.810
LEU1112
4.381
PHE1124
3.383
GLU1127
3.119
GLY1128
3.599
ILE1130
4.841
MET1131
3.325
LEU1140
3.617
LEU1142
4.513
|
|||||
| Ligand Name: 3-{5-Oxo-3-[1-(Piperidin-4-Yl)-1h-Pyrazol-4-Yl]-5h-Benzo[4,5]cyclohepta[1,2-B]pyridin-7-Yl}-N-(Pyridin-2-Ylmethyl)propanamide | Ligand Info | |||||
| Structure Description | Structure of dually-phosphorylated MET receptor kinase in complex with an MK-2461 analog with specificity for the activated receptor | PDB:3Q6W | ||||
| Method | X-ray diffraction | Resolution | 1.75 Å | Mutation | No | [12] |
| PDB Sequence |
TVHIDLSALN
1059 PELVQAVQHV1069 VIGPSSLIVH1079 FNEVIGRGHF1089 GCVYHGTLLD1099 NDGKKIHCAV 1109 KSLNRITDIG1119 EVSQFLTEGI1129 IMKDFSHPNV1139 LSLLGICLRS1149 EGSPLVVLPY 1159 MKHGDLRNFI1169 RNETHNPTVK1179 DLIGFGLQVA1189 KGMKYLASKK1199 FVHRDLAARN 1209 CMLDEKFTVK1219 VADFGLARDM1229 YDKESVHNKL1245 PVKWMALESL1255 QTQKFTTKSD 1265 VWSFGVLLWE1275 LMTRGAPPYP1285 DVNTFDITVY1295 LLQGRRLLQP1305 EYCPDPLYEV 1315 MLKCWHPKAE1325 MRPSFSELVS1335 RISAIFSTFI1345 GEHHHHH
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .Q6W or .Q6W2 or .Q6W3 or :3Q6W;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1087 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1211 or .A:1221 or .A:1222; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.259
GLY1085
3.398
ARG1086
2.993
GLY1087
3.940
VAL1092
3.433
ALA1108
3.335
LYS1110
3.817
LEU1140
3.886
LEU1157
3.784
PRO1158
3.632
TYR1159
3.271
|
|||||
| Ligand Name: N-[(2r)-1,4-Dioxan-2-Ylmethyl]-N-Methyl-N'-{5-Oxo-3-[1-(Piperidin-4-Yl)-1h-Pyrazol-4-Yl]-5h-Benzo[4,5]cyclohepta[1,2-B]pyridin-7-Yl}sulfuric Diamide | Ligand Info | |||||
| Structure Description | Structure of dually phosphorylated c-MET receptor kinase in complex with an MK-2461 analog | PDB:3R7O | ||||
| Method | X-ray diffraction | Resolution | 2.30 Å | Mutation | No | [12] |
| PDB Sequence |
QNTVHIDLSA
1057 LNPELVQAVQ1067 HVVIGPSSLI1077 VHFNEVIGRG1087 HFGCVYHGTL1097 LDNDGKKIHC 1107 AVKSLNRITD1117 IGEVSQFLTE1127 GIIMKDFSHP1137 NVLSLLGICL1147 RSEGSPLVVL 1157 PYMKHGDLRN1167 FIRNETHNPT1177 VKDLIGFGLQ1187 VAKGMKYLAS1197 KKFVHRDLAA 1207 RNCMLDEKFT1217 VKVADFGLAR1227 DMYDKESVHN1239 KLPVKWMALE1253 SLQTQKFTTK 1263 SDVWSFGVLL1273 WELMTRGAPP1283 YPDVNTFDIT1293 VYLLQGRRLL1303 QPEYCPDPLY 1313 EVMLKCWHPK1323 AEMRPSFSEL1333 VSRISAIFST1343 FIGEHHHHH
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .M61 or .M612 or .M613 or :3M61;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1087 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1211 or .A:1221 or .A:1222; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.289
GLY1085
3.396
ARG1086
3.228
GLY1087
3.669
VAL1092
3.354
ALA1108
3.428
LYS1110
3.882
LEU1140
3.876
LEU1157
3.640
PRO1158
3.664
TYR1159
3.169
|
|||||
| Ligand Name: (S)-3-(1-(1h-Pyrrolo(2,3-B)pyridin-3-Yl)ethyl)-N-Isopropyl-(1,2,4)triazolo(4,3-B)pyridazin-6-Amine | Ligand Info | |||||
| Structure Description | X-ray Structure of c-Met kinase in complex with inhibitor (S)-3-(1-(1H-pyrrolo(2,3-b)pyridin-3-yl)ethyl)-N-isopropyl-(1,2,4)triazolo(4,3- b)pyridazin-6-amine | PDB:3ZCL | ||||
| Method | X-ray diffraction | Resolution | 1.40 Å | Mutation | No | [36] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLDKK1104 IHCAVKSLNR 1114 ITDIGEVSQF1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLRSEGSPL1154 VVLPYMKHGD 1164 LRNFIRNETH1174 NPTVKDLIGF1184 GLQVAKGMKY1194 LASKKFVHRD1204 LAARNCMLDE 1214 KFTVKVADFG1224 LARDMYDKEY1234 YSVHNKTGAK1244 LPVKWMALES1254 LQTQKFTTKS 1264 DVWSFGVLLW1274 ELMTRGAPPY1284 PDVNTFDITV1294 YLLQGRRLLQ1304 PEYCPDPLYE 1314 VMLKCWHPKA1324 EMRPSFSELV1334 SRISAIFSTF1344 I
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .5TF or .5TF2 or .5TF3 or :35TF;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1164 or .A:1208 or .A:1209 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.563
GLY1085
3.477
ARG1086
4.591
VAL1092
3.875
ALA1108
3.420
LYS1110
4.100
LEU1140
3.921
LEU1157
3.449
PRO1158
2.917
TYR1159
3.835
|
|||||
| Ligand Name: 4-[[6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-B][1,2,4]triazin-3-Yl]methyl]phenol | Ligand Info | |||||
| Structure Description | Crystal structure of C-MET kinase domain in complex with 4-((6-(4- fluorophenyl)-(1,2,4)triazolo(4,3-b)(1,2,4)triazin-3-yl)methyl)phenol | PDB:4AP7 | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | No | [9] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLKKI1105 HCAVKSLNRI 1115 TDIGEVSQFL1125 TEGIIMKDFS1135 HPNVLSLLGI1145 CLRSEGSPLV1155 VLPYMKHGDL 1165 RNFIRNETHN1175 PTVKDLIGFG1185 LQVAKGMKYL1195 ASKKFVHRDL1205 AARNCMLDEK 1215 FTVKVADFGL1225 ARDMYDKEYY1235 SVHNKTGAKL1245 PVKWMALESL1255 QTQKFTTKSD 1265 VWSFGVLLWE1275 LMTRGAPPYP1285 DVNTFDITVY1295 LLQGRRLLQP1305 EYCPDPLYEV 1315 MLKCWHPKAE1325 MRPSFSELVS1335 RISAIFSTFI1345
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .F47 or .F472 or .F473 or :3F47;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.740
GLY1085
4.115
VAL1092
3.679
ALA1108
3.322
LEU1140
3.869
LEU1157
3.876
PRO1158
3.562
TYR1159
3.673
MET1160
2.887
ASP1164
3.320
|
|||||
| Ligand Name: 4-[3-(1h-Pyrrolo[2,3-B]pyridin-3-Ylmethyl)-[1,2,4]triazolo[4,3-B][1,2,4]triazin-6-Yl]benzenecarbonitrile | Ligand Info | |||||
| Structure Description | Crystal structure of C-MET kinase domain in complex with 4-(3-((1H- pyrrolo(2,3-b)pyridin-3-yl)methyl)-(1,2,4)triazolo(4,3-b)(1,2,4) triazin-6-yl)benzonitrile | PDB:4AOI | ||||
| Method | X-ray diffraction | Resolution | 1.90 Å | Mutation | No | [9] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLKKI1105 HCAVKSLNRI 1115 TDIGEVSQFL1125 TEGIIMKDFS1135 HPNVLSLLGI1145 CLRSEGSPLV1155 VLPYMKHGDL 1165 RNFIRNETHN1175 PTVKDLIGFG1185 LQVAKGMKYL1195 ASKKFVHRDL1205 AARNCMLDEK 1215 FTVKVADFGL1225 ARDMYDKEYY1235 SVHNKTGAKL1245 PVKWMALESL1255 QTQKFTTKSD 1265 VWSFGVLLWE1275 LMTRGAPPYP1285 DVNTFDITVY1295 LLQGRRLLQP1305 EYCPDPLYEV 1315 MLKCWHPKAE1325 MRPSFSELVS1335 RISAIFSTF
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .4K0 or .4K02 or .4K03 or :34K0;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 1-{5-Oxo-3-[1-(Piperidin-4-Yl)-1h-Pyrazol-4-Yl]-5h-Benzo[4,5]cyclohepta[1,2-B]pyridin-7-Yl}-N-(Pyridin-2-Ylmethyl)methanesulfonamide | Ligand Info | |||||
| Structure Description | Structure of dually phosphorylated c-MET receptor kinase in complex with an MK-8033 analog | PDB:4IWD | ||||
| Method | X-ray diffraction | Resolution | 1.99 Å | Mutation | No | [13] |
| PDB Sequence |
QNTVHIDLSA
1057 LNPELVQAVQ1067 HVVIGPSSLI1077 VHFNEVIGRG1087 HFGCVYHGTL1097 LDNDGKKIHC 1107 AVKSLNRITD1117 IGEVSQFLTE1127 GIIMKDFSHP1137 NVLSLLGICL1147 RSEGSPLVVL 1157 PYMKHGDLRN1167 FIRNETHNPT1177 VKDLIGFGLQ1187 VAKGMKYLAS1197 KKFVHRDLAA 1207 RNCMLDEKFT1217 VKVADFGLAR1227 DMYDKESVHN1239 KLPVKWMALE1253 SLQTQKFTTK 1263 SDVWSFGVLL1273 WELMTRGAPP1283 YPDVNTFDIT1293 VYLLQGRRLL1303 QPEYCPDPLY 1313 EVMLKCWHPK1323 AEMRPSFSEL1333 VSRISAIFST1343 FIGEHHHHH
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .1JC or .1JC2 or .1JC3 or :31JC;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1087 or .A:1088 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1204 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.092
GLY1085
3.664
ARG1086
3.116
GLY1087
3.369
HIS1088
3.341
VAL1092
3.518
ALA1108
3.168
LYS1110
3.751
LEU1140
3.874
LEU1157
3.768
PRO1158
3.438
TYR1159
3.475
|
|||||
| Ligand Name: (3z)-5-[(2,6-Dichlorobenzyl)sulfonyl]-3-[(3,5-Dimethyl-4-{[(2s)-2-(Pyrrolidin-1-Ylmethyl)pyrrolidin-1-Yl]carbonyl}-1h-Pyrrol-2-Yl)methylidene]-1,3-Dihydro-2h-Indol-2-One | Ligand Info | |||||
| Structure Description | X-ray Structure of PHA-00665752 bound to the kinase domain of c-Met | PDB:2WKM | ||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | No | [2] |
| PDB Sequence |
NPELVQAVQH
1068 VVIGPSSLIV1078 HFNEVIGRGH1088 FGCVYHGTLL1098 DNDGKKIHCA1108 VKSLNRITDI 1118 GEVSQFLTEG1128 IIMKDFSHPN1138 VLSLLGICLR1148 SEGSPLVVLP1158 YMKHGDLRNF 1168 IRNETHNPTV1178 KDLIGFGLQV1188 AKGMKYLASK1198 KFVHRDLAAR1208 NCMLDEKFTV 1218 KVADFGLARD1228 MYDKEYYSVH1238 NKTGAKLPVK1248 WMALESLQTQ1258 KFTTKSDVWS 1268 FGVLLWELMT1278 RGAPPYPDVN1288 TFDITVYLLQ1298 GRRLLQPEYC1308 PDPLYEVMLK 1318 CWHPKAEMRP1328 SFSELVSRIS1338 AIFSTFI
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .PFY or .PFY2 or .PFY3 or :3PFY;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1208 or .A:1209 or .A:1211 or .A:1221 or .A:1222 or .A:1223 or .A:1226 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
4.273
GLY1085
4.337
VAL1092
3.357
ALA1108
3.413
LEU1140
3.490
LEU1157
3.970
PRO1158
2.780
TYR1159
3.133
MET1160
2.774
LYS1161
3.290
HIS1162
3.488
|
|||||
| Ligand Name: 6-[[6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-B][1,2,4]triazin-3-Yl]methyl]quinoline | Ligand Info | |||||
| Structure Description | X-ray Structure of c-Met kinase in complex with inhibitor 6-((6-(4- fluorophenyl)-(1,2,4)triazolo(4,3-b)(1,2,4)triazin-3-yl)methyl) quinoline. | PDB:3ZBX | ||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | No | [36] |
| PDB Sequence |
NPELVQAVQH
1068 VVIGPSSLIV1078 HFNEVIGRGH1088 FGCVYHGTLL1098 KKIHCAVKSL1112 NRITDIGEVS 1122 QFLTEGIIMK1132 DFSHPNVLSL1142 LGICLRSEGS1152 PLVVLPYMKH1162 GDLRNFIRNE 1172 THNPTVKDLI1182 GFGLQVAKGM1192 KYLASKKFVH1202 RDLAARNCML1212 DEKFTVKVAD 1222 FGLARDMYDK1232 EYYSVHNKTG1242 AKLPVKWMAL1252 ESLQTQKFTT1262 KSDVWSFGVL 1272 LWELMTRGAP1282 PYPDVNTFDI1292 TVYLLQGRRL1302 LQPEYCPDPL1312 YEVMLKCWHP 1322 KAEMRPSFSE1332 LVSRISAIFS1342 TFI
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .6XE or .6XE2 or .6XE3 or :36XE;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.274
GLY1085
4.310
VAL1092
3.804
ALA1108
3.430
LEU1140
3.953
LEU1157
3.926
PRO1158
3.483
TYR1159
3.799
MET1160
2.930
GLY1163
4.627
|
|||||
| Ligand Name: 6-{(1S)-1-[6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]ethyl}quinoline | Ligand Info | |||||
| Structure Description | X-ray Structure of c-Met kinase in complex with inhibitor (S)-6-(1-(6- (1-methyl-1H-pyrazol-4-yl)-(1,2,4)triazolo(4,3-b)pyridazin-3-yl)ethyl) quinoline. | PDB:3ZC5 | ||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | No | [36] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLKKI1105 HCAVKSLNRI 1115 TDIGEVSQFL1125 TEGIIMKDFS1135 HPNVLSLLGI1145 CLRSEGSPLV1155 VLPYMKHGDL 1165 RNFIRNETHN1175 PTVKDLIGFG1185 LQVAKGMKYL1195 ASKKFVHRDL1205 AARNCMLDEK 1215 FTVKVADFGL1225 ARDMYDKEYY1235 SVHNKTGAKL1245 PVKWMALESL1255 QTQKFTTKSD 1265 VWSFGVLLWE1275 LMTRGAPPYP1285 DVNTFDITVY1295 LLQGRRLLQP1305 EYCPDPLYEV 1315 MLKCWHPKAE1325 MRPSFSELVS1335 RISAIFSTFI1345
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .W9Z or .W9Z2 or .W9Z3 or :3W9Z;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230 or .A:1231; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.146
GLY1085
4.695
ARG1086
4.962
VAL1092
3.634
ALA1108
3.466
LYS1110
4.191
LEU1140
4.119
LEU1157
3.426
PRO1158
3.660
TYR1159
3.618
MET1160
2.988
|
|||||
| Ligand Name: 1-Benzyl-1H-pyrrolo[3,2-c]pyridin-4(5H)-one | Ligand Info | |||||
| Structure Description | Crystal structure of c-MET bound by compound 1 | PDB:7B3Q | ||||
| Method | X-ray diffraction | Resolution | 1.75 Å | Mutation | No | [37] |
| PDB Sequence |
LSALNPELVQ
1064 AVQHVVIGPS1074 SLIVHFNEVI1084 GRGHFGCVYH1094 GTLLDNDGKK1104 IHCAVKSLNR 1114 ITDIGEVSQF1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLRSEGSPL1154 VVLPYMKHGD 1164 LRNFIRNETH1174 NPTVKDLIGF1184 GLQVAKGMKY1194 LASKKFVHRD1204 LAARNCMLDE 1214 KFTVKVADFG1224 LARDMYDKEY1234 YSVHPVKWMA1251 LESLQTQKFT1261 TKSDVWSFGV 1271 LLWELMTRGA1281 PPYPDVNTFD1291 ITVYLLQGRR1301 LLQPEYCPDP1311 LYEVMLKCWH 1321 PKAEMRPSFS1331 ELVSRISAIF1341 STF
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .SV5 or .SV52 or .SV53 or :3SV5;style chemicals stick;color identity;select .A:1084 or .A:1089 or .A:1092 or .A:1108 or .A:1109 or .A:1110 or .A:1140 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1211 or .A:1225 or .A:1226 or .A:1227 or .A:1229; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 3-(phenylmethyl)-5-(1-piperidin-4-ylpyrazol-4-yl)-1~{H}-pyrrolo[2,3-b]pyridine | Ligand Info | |||||
| Structure Description | Crystal structure of c-MET bound by compound 6 | PDB:7B40 | ||||
| Method | X-ray diffraction | Resolution | 1.76 Å | Mutation | No | [37] |
| PDB Sequence |
LSALNPELVQ
1064 AVQHVVIGPS1074 SLIVHFNEVI1084 GRGHFGCVYH1094 GTLLDNDGKK1104 IHCAVKSLNR 1114 ITDIGEVSQF1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLGSPLVVL1157 PYMKHGDLRN 1167 FIRNETHNPT1177 VKDLIGFGLQ1187 VAKGMKYLAS1197 KKFVHRDLAA1207 RNCMLDEKFT 1217 VKVADFGLAR1227 DMYDKEYYPV1247 KWMALESLQT1257 QKFTTKSDVW1267 SFGVLLWELM 1277 TRGAPPYPDV1287 NTFDITVYLL1297 QGRRLLQPEY1307 CPDPLYEVML1317 KCWHPKAEMR 1327 PSFSELVSRI1337 SAIFSTFIG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .SWN or .SWN2 or .SWN3 or :3SWN;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1211 or .A:1226 or .A:1227 or .A:1229; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 5-Methoxy-1H-indazole | Ligand Info | |||||
| Structure Description | Crystal structure of c-MET bound by compound S1 | PDB:7B44 | ||||
| Method | X-ray diffraction | Resolution | 1.76 Å | Mutation | No | [37] |
| PDB Sequence |
LSALNPELVQ
1064 AVQHVVIGPS1074 SLIVHFNEVI1084 GRGHFGCVYH1094 GTLLDNDGKK1104 IHCAVKSLNR 1114 ITDIGEVSQF1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLGSPLVVL1157 PYMKHGDLRN 1167 FIRNETHNPT1177 VKDLIGFGLQ1187 VAKGMKYLAS1197 KKFVHRDLAA1207 RNCMLDEKFT 1217 VKVADFGLAR1227 DMYDKEYYSV1237 HPVKWMALES1254 LQTQKFTTKS1264 DVWSFGVLLW 1274 ELMTRGAPPY1284 PDVNTFDITV1294 YLLQGRRLLQ1304 PEYCPDPLYE1314 VMLKCWHPKA 1324 EMRPSFSELV1334 SRISAIFSTF1344 IG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .SVT or .SVT2 or .SVT3 or :3SVT;style chemicals stick;color identity;select .A:1084 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1211 or .A:1226 or .A:1229; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 3-(3-benzyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-4,5-dihydro-1H-pyrrolo[3,4-b]pyrrol-6-one | Ligand Info | |||||
| Structure Description | Crystal structure of c-MET bound by compound 5 | PDB:7B3Z | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | No | [37] |
| PDB Sequence |
LSALNPELVQ
1064 AVQHVVIGPS1074 SLIVHFNEVI1084 GRGHFGCVYH1094 GTLLDNDGKK1104 IHCAVKSLNR 1114 ITDIGEVSQF1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLGSPLVVL1157 PYMKHGDLRN 1167 FIRNETHNPT1177 VKDLIGFGLQ1187 VAKGMKYLAS1197 KKFVHRDLAA1207 RNCMLDEKFT 1217 VKVADFGLAR1227 DMYDKEYYPV1247 KWMALESLQT1257 QKFTTKSDVW1267 SFGVLLWELM 1277 TRGAPPYPDV1287 NTFDITVYLL1297 QGRRLLQPEY1307 CPDPLYEVML1317 KCWHPKAEMR 1327 PSFSELVSRI1337 SAIFSTF
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .SV8 or .SV82 or .SV83 or :3SV8;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1211 or .A:1225 or .A:1226 or .A:1227 or .A:1229; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.465
GLY1085
4.024
PHE1089
3.280
VAL1092
3.896
ALA1108
3.285
LYS1110
3.622
LEU1140
4.038
LEU1157
3.594
PRO1158
2.754
TYR1159
3.523
|
|||||
| Ligand Name: 3-[(3-fluorophenyl)methyl]-5-(1-piperidin-4-ylpyrazol-4-yl)-1~{H}-pyrrolo[2,3-b]pyridine | Ligand Info | |||||
| Structure Description | Crystal structure of c-MET bound by compound 8 | PDB:7B42 | ||||
| Method | X-ray diffraction | Resolution | 1.80 Å | Mutation | No | [37] |
| PDB Sequence |
LSALNPELVQ
1064 AVQHVVIGPS1074 SLIVHFNEVI1084 GRGHFGCVYH1094 GTLLDNDGKK1104 IHCAVKSLNR 1114 ITDIGEVSQF1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLGSPLVVL1157 PYMKHGDLRN 1167 FIRNETHNPT1177 VKDLIGFGLQ1187 VAKGMKYLAS1197 KKFVHRDLAA1207 RNCMLDEKFT 1217 VKVADFGLAR1227 DMYDKEYYSL1245 PVKWMALESL1255 QTQKFTTKSD1265 VWSFGVLLWE 1275 LMTRGAPPYP1285 DVNTFDITVY1295 LLQGRRLLQP1305 EYCPDPLYEV1315 MLKCWHPKAE 1325 MRPSFSELVS1335 RISAIFSTF
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .SW8 or .SW82 or .SW83 or :3SW8;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1227 or .A:1229; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.288
GLY1085
3.688
PHE1089
3.597
VAL1092
3.983
ALA1108
3.341
LYS1110
3.913
LEU1140
3.713
LEU1157
3.628
PRO1158
3.030
TYR1159
3.586
|
|||||
| Ligand Name: 3-[(4-fluorophenyl)methyl]-5-(1-piperidin-4-ylpyrazol-4-yl)-1~{H}-pyrrolo[2,3-b]pyridine | Ligand Info | |||||
| Structure Description | Crystal structure of c-MET bound by compound 9 | PDB:7B43 | ||||
| Method | X-ray diffraction | Resolution | 1.87 Å | Mutation | No | [37] |
| PDB Sequence |
LSALNPELVQ
1064 AVQHVVIGPS1074 SLIVHFNEVI1084 GRGHFGCVYH1094 GTLLDNDGKK1104 IHCAVKSLNR 1114 ITDIGEVSQF1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLGSPLVVL1157 PYMKHGDLRN 1167 FIRNETHNPT1177 VKDLIGFGLQ1187 VAKGMKYLAS1197 KKFVHRDLAA1207 RNCMLDEKFT 1217 VKVADFGLAR1227 DMYDKEYYPV1247 KWMALESLQT1257 QKFTTKSDVW1267 SFGVLLWELM 1277 TRGAPPYPDV1287 NTFDITVYLL1297 QGRRLLQPEY1307 CPDPLYEVML1317 KCWHPKAEMR 1327 PSFSELVSRI1337 SAIFSTF
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .SW5 or .SW52 or .SW53 or :3SW5;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1211 or .A:1225 or .A:1226 or .A:1227 or .A:1229; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.298
GLY1085
3.699
ARG1086
4.021
PHE1089
3.459
VAL1092
3.617
ALA1108
3.296
LYS1110
3.093
LEU1140
4.587
LEU1157
3.579
PRO1158
3.030
|
|||||
| Ligand Name: 3-(3-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-4,5-dihydro-1H-pyrrolo[3,4-b]pyrrol-6-one | Ligand Info | |||||
| Structure Description | Crystal structure of c-MET bound by compound 3 | PDB:7B3V | ||||
| Method | X-ray diffraction | Resolution | 1.93 Å | Mutation | No | [37] |
| PDB Sequence |
ALNPELVQAV
1066 QHVVIGPSSL1076 IVHFNEVIGR1086 GHFGCVYHGT1096 LLDNDGKKIH1106 CAVKSLNRIT 1116 DIGEVSQFLT1126 EGIIMKDFSH1136 PNVLSLLGIC1146 LRSEGSPLVV1156 LPYMKHGDLR 1166 NFIRNETHNP1176 TVKDLIGFGL1186 QVAKGMKYLA1196 SKKFVHRDLA1206 ARNCMLDEKF 1216 TVKVADFGLA1226 RDMYLPVKWM1250 ALESLQTQKF1260 TTKSDVWSFG1270 VLLWELMTRG 1280 APPYPDVNTF1290 DITVYLLQGR1300 RLLQPEYCPD1310 PLYEVMLKCW1320 HPKAEMRPSF 1330 SELVSRISAI1340 FSTF
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .SWB or .SWB2 or .SWB3 or :3SWB;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1089 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1163 or .A:1164 or .A:1211 or .A:1229; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 1-[2-(1-Ethylpiperidin-4-yl)ethyl]-3-[6-[(6-thiophen-2-yl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)sulfanyl]-1,3-benzothiazol-2-yl]urea | Ligand Info | |||||
| Structure Description | Crystal structure of c-Met mutant Y1230H in complex with compound 14 | PDB:5HLW | ||||
| Method | X-ray diffraction | Resolution | 1.97 Å | Mutation | Yes | [6] |
| PDB Sequence |
ALNPELVQAV
1066 QHVVIGSSLI1077 VHFNEVIGRH1088 FGCVYHGTLL1098 DGKKIHCAVK1110 SLNRIDIGEV 1121 SQFLTEGIIM1131 KDFSHPNVLS1141 LLGICSPLVV1156 LPYMKHGDLR1166 NFIRNETHNP 1176 TVKDLIGFGL1186 QVAKGMKYLA1196 SKKFVHRDLA1206 ARNCMLDEKF1216 TVKVADFGLA 1226 RDMHDKEYYS1236 VAKLPVKWMA1251 LESLQTQKFT1261 TKSDVWSFGV1271 LLWELMTRGA 1281 PPYPDVNTFD1291 ITVYLLQGRR1301 LLQPEYCPDP1311 LYEVMLKCWH1321 PKAEMRPSFS 1331 ELVSRISAIF1341 STFIGEHYVH1351 VNAT
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .62E or .62E2 or .62E3 or :362E;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1171 or .A:1208 or .A:1209 or .A:1211 or .A:1221 or .A:1222 or .A:1223 or .A:1226 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.568
GLY1085
4.053
VAL1092
4.010
ALA1108
3.646
LEU1140
3.807
LEU1157
3.643
PRO1158
3.381
TYR1159
3.039
MET1160
2.655
LYS1161
3.309
HIS1162
3.747
|
|||||
| Ligand Name: 3-[(2-fluorophenyl)methyl]-5-(1-piperidin-4-ylpyrazol-4-yl)-1~{H}-pyrrolo[2,3-b]pyridine | Ligand Info | |||||
| Structure Description | Crystal structure of c-MET bound by compound 7 | PDB:7B41 | ||||
| Method | X-ray diffraction | Resolution | 1.97 Å | Mutation | No | [37] |
| PDB Sequence |
LSALNPELVQ
1064 AVQHVVIGPS1074 SLIVHFNEVI1084 GRGHFGCVYH1094 GTLLDNDGKK1104 IHCAVKSLNR 1114 ITDIGEVSQF1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLGSPLVVL1157 PYMKHGDLRN 1167 FIRNETHNPT1177 VKDLIGFGLQ1187 VAKGMKYLAS1197 KKFVHRDLAA1207 RNCMLDEKFT 1217 VKVADFGLAR1227 DMYDKEYYSL1245 PVKWMALESL1255 QTQKFTTKSD1265 VWSFGVLLWE 1275 LMTRGAPPYP1285 DVNTFDITVY1295 LLQGRRLLQP1305 EYCPDPLYEV1315 MLKCWHPKAE 1325 MRPSFSELVS1335 RISAIFSTFI1345 G
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .SWK or .SWK2 or .SWK3 or :3SWK;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1211 or .A:1225 or .A:1226 or .A:1227 or .A:1229; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.308
GLY1085
3.504
PHE1089
3.581
VAL1092
3.529
ALA1108
3.214
LYS1110
3.898
LEU1140
4.204
LEU1157
3.565
PRO1158
2.994
TYR1159
3.549
|
|||||
| Ligand Name: 3-(6-fluoro-1H-indazol-4-yl)-4,5-dihydro-1H-pyrrolo[3,4-b]pyrrol-6-one | Ligand Info | |||||
| Structure Description | Crystal structure of c-MET bound by compound 4 | PDB:7B3W | ||||
| Method | X-ray diffraction | Resolution | 2.02 Å | Mutation | No | [37] |
| PDB Sequence |
QHVVIGPSSL
1076 IVHFNEVIGR1086 GHFGCVYHGT1096 LLDGKKIHCA1108 VKSLNRIIMK1132 DFSHPNVLSL 1142 LGICLRSPLV1155 VLPYMKHGDL1165 RNFIRNETHN1175 PTVKDLIGFG1185 LQVAKGMKYL 1195 ASKKFVHRDL1205 AARNCMLDEK1215 FTVKVADFGL1225 ARDMYDKEYY1235 SVHNKTGAKL 1245 PVKWMALESL1255 QTQKFTTKSD1265 VWSFGVLLWE1275 LMTRGAPPYP1285 DVNTFDITVY 1295 LLQGRRLLQP1305 EYCPDPLYEV1315 MLKCWHPKAE1325 MRPSFSELVS1335 RISAIFSTF |
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .SVH or .SVH2 or .SVH3 or :3SVH;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1163 or .A:1164 or .A:1211 or .A:1226 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 1H-Pyrrolo[2,3-B]pyridine, 3-(phenylmethyl)- | Ligand Info | |||||
| Structure Description | Crystal structure of c-MET bound by compound 2 | PDB:7B3T | ||||
| Method | X-ray diffraction | Resolution | 2.23 Å | Mutation | No | [37] |
| PDB Sequence |
LVQAVQHVVI
1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLDND1101 GKKIHCAVKS1111 LQFLTEGIIM 1131 KDFSHPNVLS1141 LLGICLSPLV1155 VLPYMKHGDL1165 RNFIRNETHN1175 PTVKDLIGFG 1185 LQVAKGMKYL1195 ASKKFVHRDL1205 AARNCMLDEK1215 FTVKVADFGL1225 ARDMYDKEYY 1235 SLPVKWMALE1253 SLQTQKFTTK1263 SDVWSFGVLL1273 WELMTRGAPP1283 YPDVNTFDIT 1293 VYLLQGRRLL1303 QPEYCPDPLY1313 EVMLKCWHPK1323 AEMRPSFSEL1333 VSRISAIFST 1343 F
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .SVK or .SVK2 or .SVK3 or :3SVK;style chemicals stick;color identity;select .A:1084 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1163 or .A:1211 or .A:1226 or .A:1227 or .A:1229; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 3-[3-(4-Methylpiperazin-1-yl)-7-(trifluoromethyl)quinoxalin-5-yl]phenol | Ligand Info | |||||
| Structure Description | Human c-Met Kinase in complex with quinoxaline inhibitor | PDB:3F66 | ||||
| Method | X-ray diffraction | Resolution | 1.40 Å | Mutation | No | [38] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLKIH1106 CAVKSLNRIT 1116 DIGEVSQFLT1126 EGIIMKDFSH1136 PNVLSLLGIC1146 LRSEGSPLVV1156 LPYMKHGDLR 1166 NFIRNETHNP1176 TVKDLIGFGL1186 QVAKGMKYLA1196 SKKFVHRDLA1206 ARNCMLDEKF 1216 TVKVADFGLA1226 RDMYDKEYYS1236 VAKLPVKWMA1251 LESLQTQKFT1261 TKSDVWSFGV 1271 LLWELMTRGA1281 PPYPDVNTFD1291 ITVYLLQGRR1301 LLQPEYCPDP1311 LYEVMLKCWH 1321 PKAEMRPSFS1331 ELVSRISAIF1341 STFIGEHY
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .IHX or .IHX2 or .IHX3 or :3IHX;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1163 or .A:1164 or .A:1211 or .A:1226 or .A:1230; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 3-[bis(fluoranyl)methyl]-~{N}-methyl-~{N}-[(1~{R})-8-methyl-5-(3-methyl-1~{H}-indazol-6-yl)-1,2,3,4-tetrahydronaphthalen-1-yl]pyridine-2-carboxamide | Ligand Info | |||||
| Structure Description | Crystal structure of D1228V c-MET bound by compound 1. | PDB:8ANS | ||||
| Method | X-ray diffraction | Resolution | 2.01 Å | Mutation | Yes | [39] |
| PDB Sequence |
HIDLSALNPE
1061 LVQAVQHVVI1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLDKK1104 IHCAVKSLNR 1114 ITDIGEVSQF1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLRSEGSPL1154 VVLPYMKHGD 1164 LRNFIRNETH1174 NPTVKDLIGF1184 GLQVAKGMKY1194 LASKKFVHRD1204 LAARNCMLDE 1214 KFTVKVADFG1224 LARVMLPVKW1249 MALESLQTQK1259 FTTKSDVWSF1269 GVLLWELMTR 1279 GAPPYPDVNT1289 FDITVYLLQG1299 RRLLQPEYCP1309 DPLYEVMLKC1319 WHPKAEMRPS 1329 FSELVSRISA1339 IFSTFIG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .MDI or .MDI2 or .MDI3 or :3MDI;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1089 or .A:1092 or .A:1108 or .A:1109 or .A:1110 or .A:1112 or .A:1120 or .A:1121 or .A:1122 or .A:1125 or .A:1140 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1163 or .A:1211 or .A:1221 or .A:1222 or .A:1223 or .A:1224; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.700
GLY1085
4.345
PHE1089
3.479
VAL1092
3.665
ALA1108
3.392
VAL1109
4.937
LYS1110
3.613
LEU1112
4.931
GLU1120
3.314
VAL1121
3.540
SER1122
2.966
LEU1125
3.532
|
|||||
| Ligand Name: 3-[bis(fluoranyl)methyl]-~{N}-methyl-~{N}-[(1~{R})-8-methyl-5-(3-methyl-1~{H}-indazol-6-yl)-1,2,3,4-tetrahydronaphthalen-1-yl]pyridine-2-carboxamide | Ligand Info | |||||
| Structure Description | Crystal structure of wild-type c-MET bound by compound 7. | PDB:8AN8 | ||||
| Method | X-ray diffraction | Resolution | 2.39 Å | Mutation | No | [40] |
| PDB Sequence |
PSSLIVHFNE
1082 VIGRGHFGCV1092 YHGTLLKIHC1107 AVKSGEVSQF1124 LTEGIIMFSH1136 PNVLSLLGIC 1146 LPLVVLPYMK1161 HGDLRNFIRN1171 ETHNPTVKDL1181 IGFGLQVAKG1191 MKYLASKKFV 1201 HRDLAARNCM1211 LDEKFTVKVA1221 DFGLARDMYD1231 KEYYPVKWMA1251 LESLQTQKFT 1261 TKSDVWSFGV1271 LLWELMTRGA1281 PPYPDVNTFD1291 ITVYLLQGRR1301 LLQPEYCPDP 1311 LYEVMLKCWH1321 PKAEMRPSFS1331 ELVSRISAIF1341 STFI
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .N0U or .N0U2 or .N0U3 or :3N0U;style chemicals stick;color identity;select .A:1084 or .A:1089 or .A:1092 or .A:1108 or .A:1110 or .A:1120 or .A:1121 or .A:1122 or .A:1125 or .A:1140 or .A:1155 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1163 or .A:1211 or .A:1222 or .A:1223 or .A:1224; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.728
PHE1089
3.789
VAL1092
3.964
ALA1108
3.369
LYS1110
3.776
GLU1120
3.227
VAL1121
3.184
SER1122
2.908
LEU1125
3.431
LEU1140
4.454
|
|||||
| Ligand Name: 1-[(2-Nitrophenyl)sulfonyl]-1H-pyrrolo[3,2-B]pyridine-6-carboxamide | Ligand Info | |||||
| Structure Description | Human c-Met Kinase in complex with azaindole inhibitor | PDB:2WD1 | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | No | [41] |
| PDB Sequence |
LSALNPELVQ
1064 AVQHVVIGPS1074 SLIVHFNEVI1084 GRGHFGCVYH1094 GTLLDNDGKK1104 IHCAVKSLNR 1114 ITDIGEVSQF1124 LTEGIIMKDF1134 SHPNVLSLLG1144 ICLRSPLVVL1157 PYMKHGDLRN 1167 FIRNETHNPT1177 VKDLIGFGLQ1187 VAKGMKYLAS1197 KKFVHRDLAA1207 RNCMLDEKFT 1217 VKVADFGLAR1227 DMYDKEYYSV1237 HNKTGAKLPV1247 KWMALESLQT1257 QKFTTKSDVW 1267 SFGVLLWELM1277 TRGAPPYPDV1287 NTFDITVYLL1297 QGRRLLQPEY1307 CPDPLYEVML 1317 KCWHPKAEMR1327 PSFSELVSRI1337 SAIFSTFIG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ZZY or .ZZY2 or .ZZY3 or :3ZZY;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1164 or .A:1208 or .A:1209 or .A:1211 or .A:1221 or .A:1222 or .A:1223 or .A:1226 or .A:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.230
GLY1085
4.128
VAL1092
3.450
ALA1108
3.321
LYS1110
4.869
LEU1140
3.146
LEU1157
3.588
PRO1158
3.288
TYR1159
3.559
MET1160
2.899
|
|||||
| Ligand Name: 3-(Diethylamino)propyl (3-{[5-(3,4-Dimethoxyphenyl)-2-Oxo-2h-1,3,4-Thiadiazin-3(6h)-Yl]methyl}phenyl)carbamate | Ligand Info | |||||
| Structure Description | Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitor | PDB:4R1Y | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | No | [3] |
| PDB Sequence |
LVQAVQHVVI
1071 GPSSLIVHFN1081 EVIGRGHFGC1091 VYHGTLLIHC1107 AVKSLNSQFL1125 TEGIIMKDFS 1135 HPNVLSLLGI1145 CLSPLVVLPY1159 MKHGDLRNFI1169 RNETHNPTVK1179 DLIGFGLQVA 1189 KGMKYLASKK1199 FVHRDLAARN1209 CMLDEKFTVK1219 VADFGLARDM1229 YDKEYYSVHT 1241 GAKLPVKWMA1251 LESLQTQKFT1261 TKSDVWSFGV1271 LLWELMTRGA1281 PPYPDVNTFD 1291 ITVYLLQGRR1301 LLQPEYCPDP1311 LYEVMLKCWH1321 PKAEMRPSFS1331 ELVSRISAIF 1341 STFIG
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .3EH or .3EH2 or .3EH3 or :33EH;style chemicals stick;color identity;select .A:1084 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230 or .A:1231; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.229
VAL1092
4.252
ALA1108
3.594
LEU1140
3.850
LEU1157
3.728
PRO1158
3.565
TYR1159
3.442
MET1160
2.826
LYS1161
3.631
HIS1162
4.178
GLY1163
3.827
|
|||||
| Ligand Name: 7-[(1r)-1-(2,6-Dichloro-3-Fluorophenyl)ethoxy]-3-[1-(Piperidin-4-Yl)-1h-Pyrazol-4-Yl]furo[3,2-C]pyridin-6-Amine | Ligand Info | |||||
| Structure Description | C-Met in complex with OSI ligand | PDB:4KNB | ||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | No | [42] |
| PDB Sequence |
QAVQHVVIGP
1073 SSLIVHFNEV1083 IGRGHFGCVY1093 HGTLLKIHCA1108 VKSLTDIGEV1121 SQFLTEGIIM 1131 KDFSHPNVLS1141 LLGICLRSEG1151 SPLVVLPYMK1161 HGDLRNFIRN1171 ETHNPTVKDL 1181 IGFGLQVAKG1191 MKYLASKKFV1201 HRDLAARNCM1211 LDEKFTVKVA1221 DFGLARDMYD 1231 KEYYSVHNKT1241 GAKLPVKWMA1251 LESLQTQKFT1261 TKSDVWSFGV1271 LLWELMTRGA 1281 PPYPDVNTFD1291 ITVYLLQGRR1301 LLQPEYCPDP1311 LYEVMLKCWH1321 PKAEMRPSFS 1331 ELVSRISAIF1341 STF
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .1RU or .1RU2 or .1RU3 or :31RU;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1092 or .A:1108 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1161 or .A:1162 or .A:1163 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.821
GLY1085
3.735
ARG1086
4.725
VAL1092
3.952
ALA1108
3.698
LEU1140
3.595
LEU1157
3.941
PRO1158
3.161
TYR1159
3.420
MET1160
2.997
LYS1161
3.619
|
|||||
| Ligand Name: (2S)-N'-[(3R)-4-chloro-7-methyl-2-oxo-2,3-dihydro-1H-indol-3-yl]-2-(4-hydroxyphenyl)propanehydrazide | Ligand Info | |||||
| Structure Description | Crystal structure of C-MET kinase domain in complex with N'-((3Z)-4- chloro-7-methyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2-(4- hydroxyphenyl)propanohydrazide | PDB:3ZZE | ||||
| Method | X-ray diffraction | Resolution | 1.87 Å | Mutation | No | [9] |
| PDB Sequence |
NPELVQAVQH
1068 VVIGPSSLIV1078 HFNEVIGRGH1088 FGCVYHGTLL1098 DNDGKKIHCA1108 VKSLNRITDI 1118 GEVSQFLTEG1128 IIMKDFSHPN1138 VLSLLGICLR1148 SEGSPLVVLP1158 YMKHGDLRNF 1168 IRNETHNPTV1178 KDLIGFGLQV1188 AKGMKYLASK1198 KFVHRDLAAR1208 NCMLDEKFTV 1218 KVADFGLARD1228 MYDKEYYSVH1238 NKTGAKLPVK1248 WMALESLQTQ1258 KFTTKSDVWS 1268 FGVLLWELMT1278 RGAPPYPDVN1288 TFDITVYLLQ1298 GRRLLQPEYC1308 PDPLYEVMLK 1318 CWHPKAEMRP1328 SFSELVSRIS1338 AIFSTFI
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .6XP or .6XP2 or .6XP3 or :36XP;style chemicals stick;color identity;select .A:1084 or .A:1085 or .A:1086 or .A:1092 or .A:1108 or .A:1110 or .A:1140 or .A:1157 or .A:1158 or .A:1159 or .A:1160 or .A:1164 or .A:1167 or .A:1208 or .A:1209 or .A:1210 or .A:1211 or .A:1221 or .A:1222 or .A:1226 or .A:1230 or .A:1231; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
ILE1084
3.969
GLY1085
3.537
ARG1086
4.615
VAL1092
3.736
ALA1108
3.479
LYS1110
4.498
LEU1140
3.483
LEU1157
3.241
PRO1158
3.437
TYR1159
3.703
MET1160
2.817
|
|||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol Cancer Ther. 2009 Dec;8(12):3181-90. | ||||
| REF 2 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). J Med Chem. 2011 Sep 22;54(18):6342-63. | ||||
| REF 3 | Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1597-602. | ||||
| REF 4 | Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors. ACS Med Chem Lett. 2019 Aug 2;10(9):1322-1327. | ||||
| REF 5 | LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models. Invest New Drugs. 2013 Aug;31(4):833-44. | ||||
| REF 6 | Discovery and Pharmacokinetic and Pharmacological Properties of the Potent and Selective MET Kinase Inhibitor 1-{6-[6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanyl]benzothiazol-2-yl}-3-(2-morpholin-4-ylethyl)urea (SAR125844). J Med Chem. 2016 Aug 11;59(15):7066-74. | ||||
| REF 7 | Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase. J Med Chem. 2008 May 22;51(10):2879-82. | ||||
| REF 8 | Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity. J Med Chem. 2016 Mar 24;59(6):2328-42. | ||||
| REF 9 | Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of cancer. J Med Chem. 2012 Sep 27;55(18):8091-109. | ||||
| REF 10 | Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-Met and its complex with the microbial alkaloid K-252a. Proc Natl Acad Sci U S A. 2003 Oct 28;100(22):12654-9. | ||||
| REF 11 | c-Met inhibitors with novel binding mode show activity against several hereditary papillary renal cell carcinoma-related mutations. J Biol Chem. 2008 Feb 1;283(5):2675-83. | ||||
| REF 12 | Structural basis for selective small molecule kinase inhibition of activated c-Met. J Biol Chem. 2011 Apr 1;286(13):11218-25. | ||||
| REF 13 | Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met. J Med Chem. 2013 Mar 28;56(6):2294-310. | ||||
| REF 14 | Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1945-51. | ||||
| REF 15 | MET Tyrosine Kinase Inhibition Enhances the Antitumor Efficacy of an HGF Antibody. Mol Cancer Ther. 2017 Jul;16(7):1269-1278. | ||||
| REF 16 | Structure-based design, synthesis, and evaluation of imidazo[1,2-b]pyridazine and imidazo[1,2-a]pyridine derivatives as novel dual c-Met and VEGFR2 kinase inhibitors. Bioorg Med Chem. 2013 Dec 15;21(24):7686-98. | ||||
| REF 17 | Discovery of Anilinopyrimidines as Dual Inhibitors of c-Met and VEGFR-2: Synthesis, SAR, and Cellular Activity. ACS Med Chem Lett. 2014 Mar 26;5(6):673-8. | ||||
| REF 18 | Crystal structure of c-Met kinase domain in complex with LXM108 | ||||
| REF 19 | Discovery of 10H-Benzo[b]pyrido[2,3-e][1,4]oxazine AXL Inhibitors via Structure-Based Drug Design Targeting c-Met Kinase. doi:10.1021/acs.jmedchem.2c00962. | ||||
| REF 20 | Discovery of 6-(difluoro(6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b][1,2,4]triazin-3-yl)methyl)quinoline as a highly potent and selective c-Met inhibitor. Eur J Med Chem. 2016 Jun 30;116:239-251. | ||||
| REF 21 | Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors. Eur J Med Chem. 2018 Jan 1;143:491-502. | ||||
| REF 22 | Multisubstituted quinoxalines and pyrido[2,3-d]pyrimidines: synthesis and SAR study as tyrosine kinase c-Met inhibitors. Bioorg Med Chem Lett. 2012 Oct 15;22(20):6368-72. | ||||
| REF 23 | Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1405-9. | ||||
| REF 24 | Discovery of a novel mode of protein kinase inhibition characterized by the mechanism of inhibition of human mesenchymal-epithelial transition factor (c-Met) protein autophosphorylation by ARQ 197. J Biol Chem. 2011 Jun 10;286(23):20666-76. | ||||
| REF 25 | Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated Drug Resistance via Balanced Inhibition of MET, TIE2, and VEGFR2. Mol Cancer Ther. 2015 Sep;14(9):2023-34. | ||||
| REF 26 | A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients. Cancer Res. 2011 Aug 1;71(15):5255-64. | ||||
| REF 27 | Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3224-9. | ||||
| REF 28 | Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities. J Med Chem. 2008 Sep 11;51(17):5330-41. | ||||
| REF 29 | Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors. Bioorg Med Chem Lett. 2010 May 1;20(9):2998-3002. | ||||
| REF 30 | Design, synthesis, and biological evaluation of potent c-Met inhibitors. J Med Chem. 2008 Sep 25;51(18):5766-79. | ||||
| REF 31 | Discovery of potent and selective 8-fluorotriazolopyridine c-Met inhibitors. J Med Chem. 2015 Mar 12;58(5):2417-30. | ||||
| REF 32 | Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors. Bioorg Med Chem Lett. 2012 Jun 15;22(12):4089-93. | ||||
| REF 33 | Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6307-12. | ||||
| REF 34 | Discovery of AMG337: Using structure guided scaffold hydridization to optimize physicochemical properties and target coverage of a MET kinase inhibitor | ||||
| REF 35 | Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives. J Med Chem. 2012 Mar 8;55(5):1858-67. | ||||
| REF 36 | Lessons from (S)-6-(1-(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)ethyl)quinoline (PF-04254644), an inhibitor of receptor tyrosine kinase c-Met with high protein kinase selectivity but broad phosphodiesterase family inhibition leading to myocardial degeneration in rats. J Med Chem. 2013 Sep 12;56(17):6651-65. | ||||
| REF 37 | Structural Basis for Targeting the Folded P-Loop Conformation of c-MET. ACS Med Chem Lett. 2020 Dec 8;12(1):162-167. | ||||
| REF 38 | Discovery of a novel series of quinoxalines as inhibitors of c-Met kinase. Bioorg Med Chem Lett. 2009 Jan 15;19(2):397-400. | ||||
| REF 39 | Discovery of a selective c-MET inhibitor with a novel binding mode. Bioorg Med Chem Lett. 2022 Nov 1;75:128948. | ||||
| REF 40 | Discovery of a selective c-MET inhibitor with a novel binding mode. doi:10.1016/j.bmcl.2022.128948. | ||||
| REF 41 | Discovery of 4-azaindoles as novel inhibitors of c-Met kinase. Bioorg Med Chem Lett. 2009 May 15;19(10):2780-4. | ||||
| REF 42 | Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4381-7. | ||||
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