Target Binding Site Detail
| 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 | |||||
| Ligand General Information | Top | ||||
|---|---|---|---|---|---|
| Ligand Name | Phosphonotyrosine | Ligand Info | |||
| Canonical SMILES | C1=CC(=CC=C1CC(C(=O)O)N)OP(=O)(O)O | ||||
| InChI | 1S/C9H12NO6P/c10-8(9(11)12)5-6-1-3-7(4-2-6)16-17(13,14)15/h1-4,8H,5,10H2,(H,11,12)(H2,13,14,15)/t8-/m0/s1 | ||||
| InChIKey | DCWXELXMIBXGTH-QMMMGPOBSA-N | ||||
| PubChem Compound ID | 30819 | ||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| PDB ID: 3Q6W Structure of dually-phosphorylated MET receptor kinase in complex with an MK-2461 analog with specificity for the activated receptor | ||||||
| Method | X-ray diffraction | Resolution | 1.75 Å | Mutation | No | [1] |
| 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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| PDB ID: 3R7O Structure of dually phosphorylated c-MET receptor kinase in complex with an MK-2461 analog | ||||||
| Method | X-ray diffraction | Resolution | 2.30 Å | Mutation | No | [1] |
| 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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| PDB ID: 4IWD Structure of dually phosphorylated c-MET receptor kinase in complex with an MK-8033 analog | ||||||
| Method | X-ray diffraction | Resolution | 1.99 Å | Mutation | No | [2] |
| 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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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structural basis for selective small molecule kinase inhibition of activated c-Met. J Biol Chem. 2011 Apr 1;286(13):11218-25. | ||||
| REF 2 | 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. | ||||
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