Structure of PDB 3h3c Chain A

Receptor sequence
>3h3cA (length=263) Species: 9606 (Homo sapiens) [Search protein sequence]
PQYGIAREDVVLNRILGEGFFGEVYEGVYTNHKGEKINVAVKTCKKDCTL
DNKEKFMSEAVIMKNLDHPHIVKLIGIIEEEPTWIIMELYPYGELGHYLE
RNKNSLKVLTLVLYSLQICKAMAYLESINCVHRDIAVRNILVASPECVKL
GDFGLTRLPIKWMSPESINFRRFTTASDVWMFAVCMWEILSFGKQPFFWL
ENKDVIGVLEKGDRLPKPDLCPPVLYTLMTRCWDYDPSDRPRFTELVCSL
SDVYQMEKDIAME
3D structure
PDB3h3c Sulfoximine-substituted trifluoromethylpyrimidine analogs as inhibitors of proline-rich tyrosine kinase 2 (PYK2) show reduced hERG activity.
ChainA
Resolution2.0 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) D134 A136 R138 N139 D152 L158
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 P1E A L431 L504 Y505 G508 E509 L556 L16 L89 Y90 G93 E94 L141 MOAD: ic50=140nM
PDBbind-CN: -logKd/Ki=6.85,IC50=140nM
BindingDB: IC50=88nM
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:3h3c, PDBe:3h3c, PDBj:3h3c
PDBsum3h3c
PubMed19428251
UniProtQ14289|FAK2_HUMAN Protein-tyrosine kinase 2-beta (Gene Name=PTK2B)

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