Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T48069 | Target Info | |||
| Target Name | Insulin-like growth factor I receptor (IGF1R) | ||||
| Synonyms | Type 1 insulin-like growth factor receptor; Insulin-like growth factor 1 receptor; IGF-IR; IGF-I receptor; IGF-1R; IGF-1 receptor; CD221 antigen; CD221 | ||||
| Target Type | Successful Target | ||||
| Gene Name | IGF1R | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: BMS-754807 | Ligand Info | |||||
| Structure Description | Crystal structure of insulin-like growth factor 1 receptor (IGF-1R-WT) complex with BMS-754807 [1-(4-((5-cyclopropyl-1H-pyrazol-3-yl)amino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)-N-(6-fluoro-3-pyridinyl)-2-methyl-L-prolinamide] | PDB:3I81 | ||||
| Method | X-ray diffraction | Resolution | 2.08 Å | Mutation | No | [1] |
| PDB Sequence |
DVYVPDEWEV
964 AREKITMSRE974 LGQGSFGMVY984 EGVAKGVVKD994 EPETRVAIKT1004 VNEAASMRER 1014 IEFLNEASVM1024 KEFNCHHVVR1034 LLGVVSQGQP1044 TLVIMELMTR1054 GDLKSYLRSL 1064 RPEENNPVLA1075 PPSLSKMIQM1085 AGEIADGMAY1095 LNANKFVHRD1105 LAARNCMVAE 1115 DFTVKIGDFG1125 MTRDIYETDY1135 YRLLPVRWMS1150 PESLKDGVFT1160 TYSDVWSFGV 1170 VLWEIATLAE1180 QPYQGLSNEQ1190 VLRFVMEGGL1200 LDKPDNCPDM1210 LFELMRMCWQ 1220 YNPKMRPSFL1230 EIISSIKEEM1240 EPGFREVSFY1250 YSEENK
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LEU975
3.488
GLY976
3.813
GLN977
3.471
GLY978
4.828
VAL983
3.531
ALA1001
3.444
LYS1003
4.050
VAL1033
4.472
MET1049
3.552
GLU1050
2.880
LEU1051
3.929
MET1052
2.995
THR1053
3.305
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| Ligand Name: AEW-541 | Ligand Info | |||||
| Structure Description | Structure of NVP-AEW541 in complex with IGF-1R kinase | PDB:5HZN | ||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | Yes | [2] |
| PDB Sequence |
AADVYVPDEW
989 EVAREKITMS999 RELGQGSFGM1009 VYEGVAKGVV1019 KDEPETRVAI1029 KTVNEAASMR 1039 ERIEFLNEAS1049 VMKEFNCHHV1059 VRLLGVVSQG1069 QPTLVIMELM1079 TRGDLKSYLR 1089 SLRPAPPSLS1107 KMIQMAGEIA1117 DGMAYLNANK1127 FVHRDLAARN1137 CMVAEDFTVK 1147 IGDFGMTRDI1157 YETDYYRKGG1167 KGLLPVRWMS1177 PESLKDGVFT1187 TYSDVWSFGV 1197 VLWEIATLAE1207 QPYQGLSNEQ1217 VLRFVMEGGL1227 LDKPDNCPDM1237 LFELMRMCWQ 1247 YNPKMRPSFL1257 EIISSIKEEM1267 EPGFREVSFY1277 YSEENK
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LEU1002
3.785
GLY1003
3.123
GLN1004
3.449
GLY1005
3.529
SER1006
4.196
PHE1007
3.667
VAL1010
3.868
ALA1028
3.484
LYS1030
2.596
PHE1044
3.829
GLU1047
3.511
ALA1048
4.207
MET1051
3.979
VAL1060
3.590
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| Ligand Name: AMP-PNP | Ligand Info | |||||
| Structure Description | IGF-1 receptor kinase domain | PDB:1JQH | ||||
| Method | X-ray diffraction | Resolution | 2.10 Å | Mutation | Yes | [3] |
| PDB Sequence |
ADVYVPDEWE
993 VAREKITMSR1003 ELGQGSFGMV1013 YEGVAKGVVK1023 DEPETRVAIK1033 TVNEAASMRE 1043 RIEFLNEASV1053 MKEFNCHHVV1063 RLLGVVSQGQ1073 PTLVIMELMT1083 RGDLKSYLRS 1093 LRPEVLAPPS1108 LSKMIQMAGE1118 IADGMAYLNA1128 NKFVHRDLAA1138 RNCMVAEDFT 1148 VKIGDFGMTY1165 YRKGGKGLLP1175 VRWMSPESLK1185 DGVFTTYSDV1195 WSFGVVLWEI 1205 ATLAEQPYQG1215 LSNEQVLRFV1225 MEGGLLDKPD1235 NCPDMLFELM1245 RMCWQYNPKM 1255 RPSFLEIISS1265 IKEEMEPGFR1275 EVSFYYSEEN1285 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 .ANP or .ANP2 or .ANP3 or :3ANP;style chemicals stick;color identity;select .A:1005 or .A:1006 or .A:1007 or .A:1008 or .A:1009 or .A:1010 or .A:1011 or .A:1013 or .A:1031 or .A:1033 or .A:1063 or .A:1079 or .A:1080 or .A:1081 or .A:1082 or .A:1083 or .A:1085 or .A:1086 or .A:1142 or .A:1153 or .A:1171; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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LEU1005
3.344
GLY1006
3.414
GLN1007
3.066
GLY1008
2.837
SER1009
2.744
PHE1010
4.418
GLY1011
4.924
VAL1013
3.433
ALA1031
3.683
LYS1033
2.997
VAL1063
4.045
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| Ligand Name: L-betagamma-meATP | Ligand Info | |||||
| Structure Description | Structure of the Insulin-like Growth Factor 1 Receptor Kinase | PDB:1K3A | ||||
| Method | X-ray diffraction | Resolution | 2.10 Å | Mutation | Yes | [4] |
| PDB Sequence |
VPDEWEVARE
967 KITMSRELGQ977 GSFGMVYEGV987 AKGVVKDEPE997 TRVAIKTVNE1007 AASMRERIEF 1017 LNEASVMKEF1027 NCHHVVRLLG1037 VVSQGQPTLV1047 IMELMTRGDL1057 KSYLRSLRPE 1067 MPSLSKMIQM1085 AGEIADGMAY1095 LNANKFVHRD1105 LAARNCMVAE1115 DFTVKIGDFG 1125 MTRDIETDRK1138 GGKGLLPVRW1148 MSPESLKDGV1158 FTTYSDVWSF1168 GVVLWEIATL 1178 AEQPYQGLSN1188 EQVLRFVMEG1198 GLLDKPDNCP1208 DMLLELMRMC1218 WQYNPKMRPS 1228 FLEIISSIKE1238 EMEPGFREVS1248 FYYSEENK
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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 .ACP or .ACP2 or .ACP3 or :3ACP;style chemicals stick;color identity;select .A:975 or .A:976 or .A:977 or .A:978 or .A:979 or .A:983 or .A:1001 or .A:1003 or .A:1033 or .A:1049 or .A:1050 or .A:1051 or .A:1052 or .A:1053 or .A:1055 or .A:1056 or .A:1110 or .A:1112 or .A:1123; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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LEU975
3.401
GLY976
4.111
GLN977
3.389
GLY978
3.131
SER979
2.609
VAL983
3.442
ALA1001
3.442
LYS1003
3.796
VAL1033
4.085
MET1049
4.450
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| Ligand Name: Phosphonotyrosine | Ligand Info | |||||
| Structure Description | Structure of the Insulin-like Growth Factor 1 Receptor Kinase | PDB:1K3A | ||||
| Method | X-ray diffraction | Resolution | 2.10 Å | Mutation | Yes | [4] |
| PDB Sequence |
VPDEWEVARE
967 KITMSRELGQ977 GSFGMVYEGV987 AKGVVKDEPE997 TRVAIKTVNE1007 AASMRERIEF 1017 LNEASVMKEF1027 NCHHVVRLLG1037 VVSQGQPTLV1047 IMELMTRGDL1057 KSYLRSLRPE 1067 MPSLSKMIQM1085 AGEIADGMAY1095 LNANKFVHRD1105 LAARNCMVAE1115 DFTVKIGDFG 1125 MTRDIETDRK1138 GGKGLLPVRW1148 MSPESLKDGV1158 FTTYSDVWSF1168 GVVLWEIATL 1178 AEQPYQGLSN1188 EQVLRFVMEG1198 GLLDKPDNCP1208 DMLLELMRMC1218 WQYNPKMRPS 1228 FLEIISSIKE1238 EMEPGFREVS1248 FYYSEENK
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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:1100 or .A:1102 or .A:1104 or .A:1128 or .A:1129 or .A:1130 or .A:1132 or .A:1133 or .A:1134 or .A:1137 or .A:1138 or .A:1157 or .A:1158 or .A:1159 or .A:1160; 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: D-malate | Ligand Info | |||||
| Structure Description | Structure of the ectodomain of the human Type 1 insulin-like growth factor receptor | PDB:5U8R | ||||
| Method | X-ray diffraction | Resolution | 3.00 Å | Mutation | No | [5] |
| PDB Sequence |
EICGPGIDIR
10 NDYQQLKRLE20 NCTVIEGYLH30 ILLISKARSY43 RFPKLTVITE53 YLLLFRVAGL 63 ESLGDLFPNL73 TVIRGWKLFY83 NYALVIFEMT93 NLKDIGLYNL103 RNITRGAIRI 113 EKNADLCYLS123 TVDWSLILDA133 VSNNYIVGNK143 PPKECGDLCP153 GCEKTTINNE 170 YNYRCWTTNR180 CQKMCPSTCG190 KRACTENNEC200 CHPECLGSCS210 APDNDTACVA 220 CRHYYYAGVC230 VPACPPNTYR240 FEGWRCVDRD250 FCANILSAES260 SDSEGFVIHD 270 GECMQECPSG280 FIRNGSQSMY290 CIPCEGPCPK300 VCEEEKKTKT310 IDSVTSAQML 320 QGCTIFKGNL330 LINIRRGNNI340 ASELENFMGL350 IEVVTGYVKI360 RHSHALVSLS 370 FLKNLRLILG380 EEQLEGNYSF390 YVLDNQNLQQ400 LWDWDHRNLT410 IKAGKMYFAF 420 NPKLCVSEIY430 RMEEVTGTKG440 RQSKGDINTR450 NNGERASCES460 DVLHFTSTTT 470 SKNRIIITWH480 RYRPPDYRDL490 ISFTVYYKEA500 PFKNVTEYNS518 WNMVDVDLPP 528 NKDVEPGILL538 HGLKPWTQYA548 VYVKAVTLTM558 VENDHIRGAK568 SEILYIRTNA 578 SVPSIPLDVL588 SASNSSSQLI598 VKWNPPSLPN608 GNLSYYIVRW618 QRQPQDGYLY 628 RHNYCSKDKI638 PIRKEKEEAE687 YRKVFENFLH697 NSIFVPREYP746 FFESRVDNKE 756 RTVISNLRPF766 TLYRIDIHSC776 NHEAEKLGCS786 ASNFVFARTM796 PAEGADDIPG 806 PVTWEPRPEN816 SIFLKWPEPE826 NPNGLILMYE836 IKYGSQVEDQ846 RECVSRQEYR 856 KYGGAKLNRL866 NPGNYTARIQ876 ATSLSGNGSW886 TDPVFFYVQA896 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 .MLT or .MLT2 or .MLT3 or :3MLT;style chemicals stick;color identity;select .A:28 or .A:30 or .A:54 or .A:82 or .A:226 or .A:245 or .A:246 or .A:247 or .A:248 or .A:251; 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: 3-(4-Chloro-1H-pyrrolo[2,3-b]pyridin-2-yl)-5,6-dimethoxy-1-methyl-1H-pyrrolo[3,2-b]pyridine | Ligand Info | |||||
| Structure Description | Crystal structure of bisphosphorylated IGF1-R Kinase domain (2P) in complex with a bis-azaindole inhibitor | PDB:3LVP | ||||
| Method | X-ray diffraction | Resolution | 3.00 Å | Mutation | No | [6] |
| PDB Sequence |
PDEWEVAREK
998 ITMSRELGQG1008 SFGMVYEGVA1018 KGVVKDEPET1028 RVAIKTVNEA1038 ASMRERIEFL 1048 NEASVMKEFN1058 CHHVVRLLGV1068 VSQGQPTLVI1078 MELMTRGDLK1088 SYLRSLRPEM 1098 EPVLAPPSLS1110 KMIQMAGEIA1120 DGMAYLNANK1130 FVHRDLAARN1140 CMVAEDFTVK 1150 IGDFGMTRDI1160 YGGKGLLPVR1177 WMSPESLKDG1187 VFTTYSDVWS1197 FGVVLWEIAT 1207 LAEQPYQGLS1217 NEQVLRFVME1227 GGLLDKPDNC1237 PDMLFELMRM1247 CWQYNPKMRP 1257 SFLEIISSIK1267 EEMEPGFREV1277 SFYYSEENK
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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 .PDR or .PDR2 or .PDR3 or :3PDR;style chemicals stick;color identity;select .A:1005 or .A:1006 or .A:1007 or .A:1008 or .A:1013 or .A:1031 or .A:1033 or .A:1063 or .A:1079 or .A:1080 or .A:1081 or .A:1082 or .A:1083 or .A:1084 or .A:1085 or .A:1142; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: 5-Chloranyl-4-Imidazo[1,2-A]pyridin-3-Yl-N-(5-Methyl-1-Piperidin-4-Yl-Pyrazol-4-Yl)pyrimidin-2-Amine | Ligand Info | |||||
| Structure Description | IGFR-1R complex with a pyrimidine inhibitor. | PDB:5FXQ | ||||
| Method | X-ray diffraction | Resolution | 2.30 Å | Mutation | No | [7] |
| PDB Sequence |
SYFSAADVYV
988 PDEWEVAREK998 ITMSRELGQG1008 SFGMVYEGVA1018 KGVVKDEPET1028 RVAIKTVEAA 1039 SMRERIEFLN1049 EASVMKEFNC1059 HHVVRLLGVV1069 SQGQPTLVIM1079 ELMTRGDLKS 1089 YLRSLRPEMN1101 PVLAPPSLSK1111 MIQMAGEIAD1121 GMAYLNANKF1131 VHRDLAARNC 1141 MVAEDFTVKI1151 GDFGMTRDIY1161 ETDYYRKGLL1174 PVRWMSPESL1184 KDGVFTTYSD 1194 VWSFGVVLWE1204 IATLAEQPYQ1214 GLSNEQVLRF1224 VMEGGLLDKP1234 DNCPDMLFEL 1244 MRMCWQYNPK1254 MRPSFLEIIS1264 SIKEEMEPGF1274 REVSFYYSEE1284 NK |
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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 .GD5 or .GD52 or .GD53 or :3GD5;style chemicals stick;color identity;select .A:1005 or .A:1006 or .A:1007 or .A:1008 or .A:1013 or .A:1031 or .A:1033 or .A:1063 or .A:1079 or .A:1080 or .A:1081 or .A:1082 or .A:1083 or .A:1084 or .A:1085 or .A:1086 or .A:1142 or .A:1153 or .A:1156 or .A:1160; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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LEU1005
3.259
GLY1006
3.995
GLN1007
3.796
GLY1008
4.233
VAL1013
3.867
ALA1031
3.443
LYS1033
3.938
VAL1063
4.905
MET1079
3.552
GLU1080
3.273
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| Ligand Name: 5-Chloranyl-4-Imidazo[1,2-A]pyridin-3-Yl-N-(3-Methyl-1-Piperidin-4-Yl-Pyrazol-4-Yl)pyrimidin-2-Amine | Ligand Info | |||||
| Structure Description | IGFR-1R complex with a pyrimidine inhibitor. | PDB:5FXR | ||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | No | [7] |
| PDB Sequence |
GYFSADVYVP
989 DEWEVAREKI999 TMSRELGQGS1009 FGMVYEGVAK1019 GVVKDEPETR1029 VAIKTVEAAS 1040 MRERIEFLNE1050 ASVMKEFNCH1060 HVVRLLGVVS1070 QGQPTLVIME1080 LMTRGDLKSY 1090 LRSLRPEMEN1100 NPVLAPPSLS1110 KMIQMAGEIA1120 DGMAYLNANK1130 FVHRDLAARN 1140 CMVAEDFTVK1150 IGDFGMTRDI1160 YETDYYRKGL1173 LPVRWMSPES1183 LKDGVFTTYS 1193 DVWSFGVVLW1203 EIATLAEQPY1213 QGLSNEQVLR1223 FVMEGGLLDK1233 PDNCPDMLFE 1243 LMRMCWQYNP1253 KMRPSFLEII1263 SSIKEEMEPG1273 FREVSFYYSE1283 |
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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 .8LN or .8LN2 or .8LN3 or :38LN;style chemicals stick;color identity;select .A:1005 or .A:1006 or .A:1007 or .A:1008 or .A:1013 or .A:1031 or .A:1033 or .A:1063 or .A:1079 or .A:1080 or .A:1081 or .A:1082 or .A:1083 or .A:1084 or .A:1085 or .A:1086 or .A:1142 or .A:1153 or .A:1156 or .A:1160; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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LEU1005
3.243
GLY1006
4.039
GLN1007
3.954
GLY1008
4.225
VAL1013
3.640
ALA1031
3.487
LYS1033
3.875
VAL1063
4.921
MET1079
3.778
GLU1080
3.323
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| Ligand Name: (4Z)-6-bromo-4-({[4-(pyrrolidin-1-ylmethyl)phenyl]amino}methylidene)isoquinoline-1,3(2H,4H)-dione | Ligand Info | |||||
| Structure Description | Complex Structure of Insulin-like Growth Factor Receptor and Isoquinolinedione Inhibitor | PDB:2ZM3 | ||||
| Method | X-ray diffraction | Resolution | 2.50 Å | Mutation | No | [8] |
| PDB Sequence |
SFSAADVYVP
989 DEWEVAREKI999 TMSRELGQGS1009 FGMVYEGVAK1019 GVVKDEPETR1029 VAIKTVNEAA 1039 SMRERIEFLN1049 EASVMKEFNC1059 HHVVRLLGVV1069 SQGQPTLVIM1079 ELMTRGDLKS 1089 YLRSLRPENP1102 VLAPPSLSKM1112 IQMAGEIADG1122 MAYLNANKFV1132 HRDLAARNCM 1142 VAEDFTVKIG1152 DFGMTRDIET1163 DRKGGKGLLP1175 VRWMSPESLK1185 DGVFTTYSDV 1195 WSFGVVLWEI1205 ATLAEQPYQG1215 LSNEQVLRFV1225 MEGGLLDKPD1235 NCPDMLFELM 1245 RMCWQYNPKM1255 RPSFLEIISS1265 IKEEMEPGFR1275 EVSFYYSEEN1285 |
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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 .575 or .5752 or .5753 or :3575;style chemicals stick;color identity;select .A:1003 or .A:1005 or .A:1006 or .A:1007 or .A:1008 or .A:1013 or .A:1031 or .A:1033 or .A:1063 or .A:1079 or .A:1080 or .A:1081 or .A:1082 or .A:1083 or .A:1084 or .A:1085 or .A:1142 or .A:1152; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: 4-[[3-Chloro-4-(1-Methylimidazol-2-Yl)sulfanyl-Phenyl]amino]-7-[3-(2-Hydroxyethyl-Methyl-Amino)propoxy]-6-Methoxy-Quinoline-3-Carbonitrile | Ligand Info | |||||
| Structure Description | Complex Structure of Insulin-like Growth Factor Receptor and 3-Cyanoquinoline Inhibitor | PDB:3F5P | ||||
| Method | X-ray diffraction | Resolution | 2.90 Å | Mutation | No | [9] |
| PDB Sequence |
SFSAADVYVP
989 DEWEVAREKI999 TMSRELGQGS1009 FGMVYEGVAK1019 GVVKDEPETR1029 VAIKTVNEAA 1039 SMRERIEFLN1049 EASVMKEFNC1059 HHVVRLLGVV1069 SQGQPTLVIM1079 ELMTRGDLKS 1089 YLRSLRPEML1104 APPSLSKMIQ1114 MAGEIADGMA1124 YLNANKFVHR1134 DLAARNCMVA 1144 EDFTVKIGDF1154 GMTRDIETDR1167 KGGKGLLPVR1177 WMSPESLKDG1187 VFTTYSDVWS 1197 FGVVLWEIAT1207 LAEQPYQGLS1217 NEQVLRFVME1227 GGLLDKPDNC1237 PDMLFELMRM 1247 CWQYNPKMRP1257 SFLEIISSIK1267 EEMEPGFREV1277 SFYYSEENK
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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 .741 or .7412 or .7413 or :3741;style chemicals stick;color identity;select .A:1003 or .A:1005 or .A:1006 or .A:1009 or .A:1010 or .A:1013 or .A:1031 or .A:1032 or .A:1033 or .A:1047 or .A:1050 or .A:1051 or .A:1054 or .A:1063 or .A:1065 or .A:1077 or .A:1078 or .A:1079 or .A:1080 or .A:1081 or .A:1082 or .A:1083 or .A:1084 or .A:1085 or .A:1142; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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ARG1003
4.677
LEU1005
3.435
GLY1006
4.717
SER1009
3.597
PHE1010
4.239
VAL1013
3.787
ALA1031
3.641
ILE1032
4.060
LYS1033
3.223
PHE1047
3.323
GLU1050
3.432
ALA1051
4.568
MET1054
3.841
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| Ligand Name: 3-[5-(1h-Imidazol-1-Yl)-7-Methyl-1h-Benzimidazol-2-Yl]-4-[(Pyridin-2-Ylmethyl)amino]pyridin-2(1h)-One | Ligand Info | |||||
| Structure Description | Structure of IGF-1R kinase domain complexed with a benzimidazole inhibitor | PDB:2OJ9 | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | No | [10] |
| PDB Sequence |
ADVYVPDEWE
963 VAREKITMSR973 ELGQGSFGMV983 YEGVAKGVVK993 DEPETRVAIK1003 TVNEAASMRE 1013 RIEFLNEASV1023 MKEFNCHHVV1033 RLLGVVSQGQ1043 PTLVIMELMT1053 RGDLKSYLRS 1063 LRPEPPSLSK1081 MIQMAGEIAD1091 GMAYLNANKF1101 VHRDLAARNC1111 MVAEDFTVKI 1121 GDFGMTRDIY1131 ETDYYRKGGK1141 GLLPVRWMSP1151 ESLKDGVFTT1161 YSDVWSFGVV 1171 LWEIATLAEQ1181 PYQGLSNEQV1191 LRFVMEGGLL1201 DKPDNCPDML1211 FELMRMCWQY 1221 NPKMRPSFLE1231 IISSIKEEME1241 PGFREVSFYY1251 SEENK
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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 .BMI or .BMI2 or .BMI3 or :3BMI;style chemicals stick;color identity;select .A:975 or .A:976 or .A:977 or .A:978 or .A:979 or .A:983 or .A:1001 or .A:1003 or .A:1033 or .A:1049 or .A:1050 or .A:1051 or .A:1052 or .A:1053 or .A:1054 or .A:1055 or .A:1056 or .A:1112 or .A:1126 or .A:1127 or .A:1130; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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LEU975
3.118
GLY976
3.761
GLN977
3.702
GLY978
4.005
SER979
4.806
VAL983
3.711
ALA1001
3.356
LYS1003
4.070
VAL1033
4.141
MET1049
3.594
GLU1050
2.846
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| Ligand Name: N-({4-[(3-cyclopropyl-1H-pyrazol-5-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl}methyl)-6-fluoropyridine-3-carboxamide | Ligand Info | |||||
| Structure Description | Crystal structure of insulin-like growth factor 1 receptor (IGF-1R-WT) complex with a carbon-linked proline isostere inhibitor (34) | PDB:3NW7 | ||||
| Method | X-ray diffraction | Resolution | 2.11 Å | Mutation | No | [11] |
| PDB Sequence |
YVPDEWEVAR
966 EKITMSRELG976 QGSFGMVYEG986 VAKGVVKDEP996 ETRVAIKTVN1006 EAASMRERIE 1016 FLNEASVMKE1026 FNCHHVVRLL1036 GVVSQGQPTL1046 VIMELMTRGD1056 LKSYLRSLRP 1066 EMENNPVLAP1076 PSLSKMIQMA1086 GEIADGMAYL1096 NANKFVHRDL1106 AARNCMVAED 1116 FTVKIGDFGM1126 TRDIYETDYY1136 RKGLLPVRWM1149 SPESLKDGVF1159 TTYSDVWSFG 1169 VVLWEIATLA1179 EQPYQGLSNE1189 QVLRFVMEGG1199 LLDKPDNCPD1209 MLFELMRMCW 1219 QYNPKMRPSF1229 LEIISSIKEE1239 MEPGFREVSF1249 YYSEENK
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .LGV or .LGV2 or .LGV3 or :3LGV;style chemicals stick;color identity;select .A:975 or .A:976 or .A:977 or .A:978 or .A:983 or .A:1001 or .A:1003 or .A:1033 or .A:1049 or .A:1050 or .A:1051 or .A:1052 or .A:1053 or .A:1054 or .A:1055 or .A:1056 or .A:1109 or .A:1110 or .A:1111 or .A:1112 or .A:1122 or .A:1123 or .A:1126 or .A:1127; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU975
3.186
GLY976
3.550
GLN977
3.373
GLY978
4.714
VAL983
3.708
ALA1001
3.279
LYS1003
3.371
VAL1033
4.379
MET1049
3.478
GLU1050
2.859
LEU1051
3.857
MET1052
2.907
|
|||||
| Ligand Name: N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-{(2R)-1-[(6-fluoropyridin-3-yl)carbonyl]pyrrolidin-2-yl}pyrrolo[2,1-f][1,2,4]triazin-4-amine | Ligand Info | |||||
| Structure Description | Crystal structure of insulin-like growth factor 1 receptor (IGF-1R-WT) complex with a carbon-linked proline isostere inhibitor (11B) | PDB:3NW5 | ||||
| Method | X-ray diffraction | Resolution | 2.14 Å | Mutation | No | [11] |
| PDB Sequence |
DVYVPDEWEV
964 AREKITMSRE974 LGQGSFGMVY984 EGVAKGVVKD994 EPETRVAIKT1004 VNEAASMRER 1014 IEFLNEASVM1024 KEFNCHHVVR1034 LLGVVSQGQP1044 TLVIMELMTR1054 GDLKSYLRSL 1064 RPEMENNPVL1074 APPSLSKMIQ1084 MAGEIADGMA1094 YLNANKFVHR1104 DLAARNCMVA 1114 EDFTVKIGDF1124 GMTRDIYETD1134 YYRKGGKGLL1144 PVRWMSPESL1154 KDGVFTTYSD 1164 VWSFGVVLWE1174 IATLAEQPYQ1184 GLSNEQVLRF1194 VMEGGLLDKP1204 DNCPDMLFEL 1214 MRMCWQYNPK1224 MRPSFLEIIS1234 SIKEEMEPGF1244 REVSFYYSEE1254 NK |
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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 .LGX or .LGX2 or .LGX3 or :3LGX;style chemicals stick;color identity;select .A:975 or .A:976 or .A:977 or .A:978 or .A:983 or .A:1001 or .A:1003 or .A:1033 or .A:1049 or .A:1050 or .A:1051 or .A:1052 or .A:1053 or .A:1054 or .A:1055 or .A:1056 or .A:1059 or .A:1112 or .A:1123 or .A:1130 or .A:1131; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU975
3.663
GLY976
3.375
GLN977
3.185
GLY978
4.029
VAL983
3.618
ALA1001
3.296
LYS1003
3.732
VAL1033
4.343
MET1049
3.526
GLU1050
2.735
LEU1051
3.899
|
|||||
| Ligand Name: N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-{(2S)-1-[(6-fluoropyridin-3-yl)carbonyl]pyrrolidin-2-yl}pyrrolo[2,1-f][1,2,4]triazin-4-amine | Ligand Info | |||||
| Structure Description | Crystal structure of insulin-like growth factor 1 receptor (IGF-1R-WT) complex with a carbon-linked proline isostere inhibitor (11A) | PDB:3NW6 | ||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | No | [11] |
| PDB Sequence |
VYVPDEWEVA
965 REKITMSREL975 GQGSFGMVYE985 GVAKGVVKDE995 PETRVAIKTV1005 NEAASMRERI 1015 EFLNEASVMK1025 EFNCHHVVRL1035 LGVVSQGQPT1045 LVIMELMTRG1055 DLKSYLRSLR 1065 PEMENNPVLA1075 PPSLSKMIQM1085 AGEIADGMAY1095 LNANKFVHRD1105 LAARNCMVAE 1115 DFTVKIGDFG1125 MTRDIYETDY1135 YRKGGKGLLP1145 VRWMSPESLK1155 DGVFTTYSDV 1165 WSFGVVLWEI1175 ATLAEQPYQG1185 LSNEQVLRFV1195 MEGGLLDKPD1205 NCPDMLFELM 1215 RMCWQYNPKM1225 RPSFLEIISS1235 IKEEMEPGFR1245 EVSFYYSEEN1255 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 .LGW or .LGW2 or .LGW3 or :3LGW;style chemicals stick;color identity;select .A:975 or .A:976 or .A:977 or .A:978 or .A:983 or .A:1001 or .A:1003 or .A:1033 or .A:1049 or .A:1050 or .A:1051 or .A:1052 or .A:1053 or .A:1054 or .A:1055 or .A:1056 or .A:1109 or .A:1110 or .A:1112 or .A:1122 or .A:1123 or .A:1126 or .A:1128; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU975
3.579
GLY976
3.264
GLN977
3.666
GLY978
4.474
VAL983
3.421
ALA1001
3.283
LYS1003
3.744
VAL1033
4.464
MET1049
3.643
GLU1050
2.814
LEU1051
3.861
MET1052
2.969
|
|||||
| Ligand Name: (5s)-5-Methyl-1-(Quinolin-4-Ylmethyl)-3-{4-[(Trifluoromethyl)sulfonyl]phenyl}imidazolidine-2,4-Dione | Ligand Info | |||||
| Structure Description | Human unphosphorylated IGF1-R Kinase domain in complex with an hydantoin inhibitor | PDB:3O23 | ||||
| Method | X-ray diffraction | Resolution | 2.10 Å | Mutation | Yes | [12] |
| PDB Sequence |
EWEVAREKIT
1000 MSRELGQGSF1010 GMVYEGVAKG1020 VVKDEPETRV1030 AIKTVNEAAS1040 MRERIEFLNE 1050 ASVMKEFNCH1060 HVVRLLGVVS1070 QGQPTLVIME1080 LMTRGDLKSY1090 LRSLRPEMEN 1100 NPVLAPPSLS1110 KMIQMAGEIA1120 DGMAYLNANK1130 FVHRDLAARN1140 CMVAEDFTVK 1150 IGDFGMTRDI1160 YETDYYRKGG1170 KGLLPVRWMS1180 PESLKDGVFT1190 TYSDVWSFGV 1200 VLWEIATLAE1210 QPYQGLSNEQ1220 VLRFVMEGGL1230 LDKPDNCPDM1240 LFELMRMCWQ 1250 YNPKMRPSFL1260 EIISSIKEEM1270 EPGFREVSFY1280 YSE
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .MQY or .MQY2 or .MQY3 or :3MQY;style chemicals stick;color identity;select .A:1005 or .A:1013 or .A:1031 or .A:1033 or .A:1054 or .A:1057 or .A:1062 or .A:1063 or .A:1079 or .A:1080 or .A:1081 or .A:1082 or .A:1085 or .A:1086 or .A:1126 or .A:1131 or .A:1133 or .A:1142 or .A:1151 or .A:1152 or .A:1153 or .A:1154 or .A:1155 or .A:1156; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU1005
4.333
VAL1013
4.681
ALA1031
3.737
LYS1033
3.114
MET1054
3.608
PHE1057
3.495
VAL1062
3.617
VAL1063
3.725
MET1079
3.008
GLU1080
3.380
LEU1081
3.399
MET1082
3.045
|
|||||
| Ligand Name: 3-cyano-N-{1-[4-(5-cyano-1H-indol-3-yl)butyl]piperidin-4-yl}-1H-indole-7-carboxamide | Ligand Info | |||||
| Structure Description | IGF-1RK in complex with ligand MSC1609119A-1 | PDB:3LW0 | ||||
| Method | X-ray diffraction | Resolution | 1.79 Å | Mutation | Yes | [13] |
| PDB Sequence |
AADVYVPDEW
992 EVAREKITMS1002 RELGQGSFGM1012 VYEGVAKGVV1022 KDEPETRVAI1032 KTVNEAASMR 1042 ERIEFLNEAS1052 VMKEFNCHHV1062 VRLLGVVSQG1072 QPTLVIMELM1082 TRGDLKSYLR 1092 SLRPPPSLSK1111 MIQMAGEIAD1121 GMAYLNANKF1131 VHRDLAARNC1141 MVAEDFTVKI 1151 GDFGMTRDIY1161 ETDYYRKGLL1174 PVRWMSPESL1184 KDGVFTTYSD1194 VWSFGVVLWE 1204 IATLAEQPYQ1214 GLSNEQVLRF1224 VMEGGLLDKP1234 DNCPDMLFEL1244 MRMCWQYNPK 1254 MRPSFLEIIS1264 SIKEEMEPGF1274 REVSFYYSEE1284 NK
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .CCX or .CCX2 or .CCX3 or :3CCX;style chemicals stick;color identity;select .A:1033 or .A:1047 or .A:1050 or .A:1051 or .A:1054 or .A:1062 or .A:1063 or .A:1064 or .A:1065 or .A:1077 or .A:1079 or .A:1090 or .A:1091 or .A:1094 or .A:1107 or .A:1111 or .A:1114 or .A:1115 or .A:1118 or .A:1131 or .A:1133 or .A:1134 or .A:1135 or .A:1146 or .A:1147 or .A:1148 or .A:1151 or .A:1152 or .A:1153 or .A:1173 or .A:1174 or .A:1189 or .A:1271 or .A:1272 or .A:1273; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LYS1033
3.760
PHE1047
4.887
GLU1050
3.893
ALA1051
3.528
MET1054
3.593
VAL1062
3.843
VAL1063
2.820
ARG1064
4.197
LEU1065
3.978
VAL1077
3.732
MET1079
3.799
TYR1090
3.478
LEU1091
3.880
LEU1094
3.922
PRO1107
4.150
LYS1111
3.796
GLN1114
3.668
MET1115
3.504
|
|||||
| Ligand Name: N-{2-Methoxy-4-[(1-Methylpiperidin-4-Yl)oxy]phenyl}-4-(1h-Pyrrolo[2,3-C]pyridin-3-Yl)pyrimidin-2-Amine | Ligand Info | |||||
| Structure Description | Human IGF in complex with a Dyrk1B inhibitor | PDB:4D2R | ||||
| Method | X-ray diffraction | Resolution | 2.10 Å | Mutation | No | [14] |
| PDB Sequence |
DVYVPDEWEV
994 AREKITMSRE1004 LGQGSFGMVY1014 EGVAKGVVKD1024 EPETRVAIKT1034 VNEAASMRER 1044 IEFLNEASVM1054 KEFNCHHVVR1064 LLGVVSQGQP1074 TLVIMELMTR1084 GDLKSYLRSL 1094 RPEMENNPVL1104 APPSLSKMIQ1114 MAGEIADGMA1124 YLNANKFVHR1134 DLAARNCMVA 1144 EDFTVKIGDF1154 GMTRDIYETD1164 YYRKKGLLPV1176 RWMSPESLKD1186 GVFTTYSDVW 1196 SFGVVLWEIA1206 TLAEQPYQGL1216 SNEQVLRFVM1226 EGGLLDKPDN1236 CPDMLFELMR 1246 MCWQYNPKMR1256 PSFLEIISSI1266 KEEMEPGFRE1276 VSFYYSEENK1286 |
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .DYK or .DYK2 or .DYK3 or :3DYK;style chemicals stick;color identity;select .A:1005 or .A:1006 or .A:1007 or .A:1008 or .A:1013 or .A:1015 or .A:1029 or .A:1031 or .A:1080 or .A:1081 or .A:1082 or .A:1083 or .A:1084 or .A:1085 or .A:1142 or .A:1156; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: 3-[cis-3-(4-Methylpiperazin-1-yl)cyclobutyl]-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-8-amine | Ligand Info | |||||
| Structure Description | Crystal structure of the insulin-like growth factor-1 receptor kinase in complex with PQIP | PDB:3D94 | ||||
| Method | X-ray diffraction | Resolution | 2.30 Å | Mutation | Yes | [15] |
| PDB Sequence |
VYVPDEWEVA
965 REKITMSREL975 GQGSFGMVYE985 GVAKGVVKDE995 PETRVAIKTV1005 NEAASMRERI 1015 EFLNEASVMK1025 EFNCHHVVRL1035 LGVVSQGQPT1045 LVIMELMTRG1055 DLKSYLRSLR 1065 PSLSKMIQMA1086 GEIADGMAYL1096 NANKFVHRDL1106 AARNCVAEDF1117 TVKIGDFGMT 1127 RDIYETDYYR1137 KGGKGLLPVR1147 WMSPESLKDG1157 VFTTYSDVWS1167 FGVVLWEIAT 1177 LAEQPYQGLS1187 NEQVLRFVME1197 GGLLDKPDNC1207 PDMLLELMRM1217 CWQYNPKMRP 1227 SFLEIISSIK1237 EEMEPGFREV1247 SFYYSEEN
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .D94 or .D942 or .D943 or :3D94;style chemicals stick;color identity;select .A:975 or .A:976 or .A:977 or .A:978 or .A:979 or .A:980 or .A:983 or .A:1001 or .A:1003 or .A:1017 or .A:1020 or .A:1021 or .A:1024 or .A:1033 or .A:1047 or .A:1049 or .A:1050 or .A:1051 or .A:1052 or .A:1056 or .A:1109 or .A:1121 or .A:1122 or .A:1123 or .A:1124 or .A:1125; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU975
3.420
GLY976
3.683
GLN977
3.130
GLY978
4.033
SER979
4.219
PHE980
3.564
VAL983
3.829
ALA1001
3.276
LYS1003
2.799
PHE1017
3.551
GLU1020
3.980
ALA1021
3.875
MET1024
3.589
|
|||||
| Ligand Name: L-Methionine (S)-S-oxide | Ligand Info | |||||
| Structure Description | Crystal structure of the insulin-like growth factor-1 receptor kinase in complex with PQIP | PDB:3D94 | ||||
| Method | X-ray diffraction | Resolution | 2.30 Å | Mutation | Yes | [15] |
| PDB Sequence |
VYVPDEWEVA
965 REKITMSREL975 GQGSFGMVYE985 GVAKGVVKDE995 PETRVAIKTV1005 NEAASMRERI 1015 EFLNEASVMK1025 EFNCHHVVRL1035 LGVVSQGQPT1045 LVIMELMTRG1055 DLKSYLRSLR 1065 PSLSKMIQMA1086 GEIADGMAYL1096 NANKFVHRDL1106 AARNCVAEDF1117 TVKIGDFGMT 1127 RDIYETDYYR1137 KGGKGLLPVR1147 WMSPESLKDG1157 VFTTYSDVWS1167 FGVVLWEIAT 1177 LAEQPYQGLS1187 NEQVLRFVME1197 GGLLDKPDNC1207 PDMLLELMRM1217 CWQYNPKMRP 1227 SFLEIISSIK1237 EEMEPGFREV1247 SFYYSEEN
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .MHO or .MHO2 or .MHO3 or :3MHO;style chemicals stick;color identity;select .A:1033 or .A:1052 or .A:1055 or .A:1056 or .A:1057 or .A:1109 or .A:1110 or .A:1111 or .A:1113 or .A:1114 or .A:1118 or .A:1119 or .A:1120 or .A:1122; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
||||||
| Ligand Name: N(2)-[3-methoxy-4-(morpholin-4-yl)phenyl]-N(4)-(quinolin-3-yl)pyrimidine-2,4-diamine | Ligand Info | |||||
| Structure Description | Cocrystal structure of unphosphorylated igf with pyrimidine 8 | PDB:3QQU | ||||
| Method | X-ray diffraction | Resolution | 2.90 Å | Mutation | No | [16] |
| PDB Sequence |
EWEVAREKIT
997 MSRELGQGSF1007 GMVYEGVAKG1017 VVKDEPETRV1027 AIKTVNEAAS1037 MRERIEFLNE 1047 ASVMKEFNCH1057 HVVRLLGVVS1067 QGQPTLVIME1077 LMTRGDLKSY1087 LRSLRPPSLS 1107 KMIQMAGEIA1117 DGMAYLNANK1127 FVHRDLAARN1137 CMVAEDFTVK1147 IGDFGMTRDI 1157 YETDYYRKGG1167 KGLLPVRWMS1177 PESLKDGVFT1187 TYSDVWSFGV1197 VLWEIATLAE 1207 QPYQGLSNEQ1217 VLRFVMEGGL1227 LDKPDNCPDM1237 LFELMRMCWQ1247 YNPKMRPSFL 1257 EIISSIKEEM1267 EPGFREVSFY1277 YSEEN
|
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .01P or .01P2 or .01P3 or :301P;style chemicals stick;color identity;select .A:1002 or .A:1003 or .A:1004 or .A:1005 or .A:1010 or .A:1028 or .A:1030 or .A:1060 or .A:1076 or .A:1077 or .A:1078 or .A:1079 or .A:1080 or .A:1082 or .A:1083 or .A:1139 or .A:1150 or .A:1153 or .A:1156; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU1002
3.951
GLY1003
3.604
GLN1004
3.310
GLY1005
3.870
VAL1010
3.700
ALA1028
3.633
LYS1030
4.187
VAL1060
3.830
MET1076
4.692
GLU1077
2.817
|
|||||
| Ligand Name: 2-[4-[4-[[(6Z)-5-chloranyl-6-pyrazolo[1,5-a]pyridin-3-ylidene-1H-pyrimidin-2-yl]amino]-3,5-dimethyl-pyrazol-1-yl]piperidin-1-yl]-N,N-dimethyl-ethanamide | Ligand Info | |||||
| Structure Description | IGFR-1R complex with a pyrimidine inhibitor. | PDB:5FXS | ||||
| Method | X-ray diffraction | Resolution | 1.90 Å | Mutation | No | [7] |
| PDB Sequence |
SYFSAADVYV
988 PDEWEVAREK998 ITMSRELGQG1008 SFGMVYEGVA1018 KGVVKDEPET1028 RVAIKTVNEA 1038 ASMRERIEFL1048 NEASVMKEFN1058 CHHVVRLLGV1068 VSQGQPTLVI1078 MELMTRGDLK 1088 SYLRSLRPEM1098 ENNPVLAPPS1108 LSKMIQMAGE1118 IADGMAYLNA1128 NKFVHRDLAA 1138 RNCMVAEDFT1148 VKIGDFGMTR1158 AIYETDYYRK1168 GGKGLLPVRW1178 MSPESLKDGV 1188 FTTYSDVWSF1198 GVVLWEIATL1208 AEEPYQGLSN1218 EQVLRFVMEG1228 GLLDKPDNCP 1238 DMLFELMRMC1248 WQYNPKMRPS1258 FLEIISSIKE1268 EMEPGFREVS1278 FYYSEENK |
|||||
|
Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .OZN or .OZN2 or .OZN3 or :3OZN;style chemicals stick;color identity;select .A:1005 or .A:1006 or .A:1007 or .A:1008 or .A:1010 or .A:1013 or .A:1031 or .A:1033 or .A:1063 or .A:1079 or .A:1080 or .A:1081 or .A:1082 or .A:1083 or .A:1084 or .A:1085 or .A:1086 or .A:1142 or .A:1153 or .A:1156 or .A:1160; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
|
LEU1005
3.511
GLY1006
4.107
GLN1007
4.283
GLY1008
4.481
PHE1010
4.529
VAL1013
3.600
ALA1031
3.502
LYS1033
4.168
VAL1063
4.904
MET1079
3.612
GLU1080
3.382
|
|||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in cli... J Med Chem. 2009 Dec 10;52(23):7360-3. | ||||
| REF 2 | Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors. Bioorg Med Chem Lett. 2016 Apr 15;26(8):2065-7. | ||||
| REF 3 | Crystal structure of bisphosphorylated IGF-1 receptor kinase: insight into domain movements upon kinase activation. Structure. 2001 Oct;9(10):955-65. | ||||
| REF 4 | Structure and autoregulation of the insulin-like growth factor 1 receptor kinase. Nat Struct Biol. 2001 Dec;8(12):1058-63. | ||||
| REF 5 | How ligand binds to the type 1 insulin-like growth factor receptor. Nat Commun. 2018 Feb 26;9(1):821. | ||||
| REF 6 | Design of potent IGF1-R inhibitors related to bis-azaindoles. Chem Biol Drug Des. 2010 Aug;76(2):100-6. | ||||
| REF 7 | Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R). J Med Chem. 2016 May 26;59(10):4859-66. | ||||
| REF 8 | Lead identification to generate isoquinolinedione inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment. Bioorg Med Chem Lett. 2008 Jun 15;18(12):3641-5. | ||||
| REF 9 | Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment. Bioorg Med Chem Lett. 2009 Jan 1;19(1):62-6. | ||||
| REF 10 | Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R). Bioorg Med Chem Lett. 2007 Apr 15;17(8):2317-21. | ||||
| REF 11 | Proline isosteres in a series of 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitors of IGF-1R kinase and IR kinase. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5027-30. | ||||
| REF 12 | Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: advantages in comparison with competitive inhibitors. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2224-8. | ||||
| REF 13 | Allosteric IGF-1R Inhibitors. ACS Med Chem Lett. 2010 May 18;1(5):199-203. | ||||
| REF 14 | Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis. J Med Chem. 2015 Mar 26;58(6):2834-44. | ||||
| REF 15 | Small-molecule inhibition and activation-loop trans-phosphorylation of the IGF1 receptor. EMBO J. 2008 Jul 23;27(14):1985-94. | ||||
| REF 16 | Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2394-9. | ||||
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