Structure of PDB 4h1m Chain A

Receptor sequence
>4h1mA (length=256) Species: 9606 (Homo sapiens) [Search protein sequence]
IAREDVVLNRILGEGFFGEVYEGVYTNHKGEKINVAVKTCKKDCTLDNKE
KFMSEAVIMKNLDHPHIVKLIGIIEEEPTWIIMELYPYGELGHYLERNKN
SLKVLTLVLYSLQICKAMAYLESINCVHRDIAVRNILVASPECVKLGDFG
LSLPIKWMSPESINFRRFTTASDVWMFAVCMWEILSFGKQPFFWLENKDV
IGVLEKGDRLPKPDLCPPVLYTLMTRCWDYDPSDRPRFTELVCSLSDVYQ
MEKDIA
3D structure
PDB4h1m Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors.
ChainA
Resolution1.99 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D549 A551 R553 N554 D567 L587
Catalytic site (residue number reindexed from 1) D130 A132 R134 N135 D148 L153
Enzyme Commision number 2.7.10.2: non-specific 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 0YJ A G432 V439 K457 E474 M478 V487 M502 G566 D567 F568 G13 V20 K38 E55 M59 V68 M83 G147 D148 F149 MOAD: ic50=78nM
PDBbind-CN: -logKd/Ki=7.11,IC50=78nM
BindingDB: IC50=78nM
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:4h1m, PDBe:4h1m, PDBj:4h1m
PDBsum4h1m
PubMed23153798
UniProtQ14289|FAK2_HUMAN Protein-tyrosine kinase 2-beta (Gene Name=PTK2B)

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