Structure of PDB 4r1v Chain A

Receptor sequence
>4r1vA (length=289) Species: 9606 (Homo sapiens) [Search protein sequence]
LSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLLDNDGKK
IHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSSPLVV
LPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKFVHRDLA
ARNCMLDEKFTVKVADFGLARDMYDKEYYSVHNKTGAKLPVKWMALESLQ
TQKFTTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPE
YCPDPLYEVMLKCWHPKAEMRPSFSELVSRISAIFSTFI
3D structure
PDB4r1v Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.
ChainA
Resolution1.2 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D1204 A1206 R1208 N1209 D1222 A1243
Catalytic site (residue number reindexed from 1) D148 A150 R152 N153 D166 A187
Enzyme Commision number 2.7.10.1: receptor protein-tyrosine kinase.
Interaction with ligand
Site
#		 Ligand Ligand
chain		 Binding residues on receptor
(original residue number in PDB)		 Binding residues on receptor
(residue number reindexed from 1)		 Binding affinity
BS01 3E8 A I1084 A1108 L1140 P1158 Y1159 M1160 K1161 G1163 D1164 R1208 M1211 A1221 D1222 Y1230 I30 A54 L86 P102 Y103 M104 K105 G107 D108 R152 M155 A165 D166 Y174 MOAD: ic50<1nM
PDBbind-CN: -logKd/Ki=9.00,IC50<1nM
BindingDB: IC50=<100nM
BS02 GBL A M1131 L1157 F1223 G1224 L1225 M77 L101 F167 G168 L169
BS03 GBL A H1162 F1168 N1171 F1216 H106 F112 N115 F160
BS04 GBL A R1227 D1228 M1229 K1244 R171 D172 M173 K188
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation

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Molecular Function
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Biological Process
External links
PDB RCSB:4r1v, PDBe:4r1v, PDBj:4r1v
PDBsum4r1v
PubMed25736998
UniProtP08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)

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