Structure of PDB 6gqk Chain B

Receptor sequence
>6gqkB (length=293) Species: 9606 (Homo sapiens) [Search protein sequence]
DPTQLPYDHKWEFPRNRLSFGKTLGAGAFGKVVEATAQGLIKSDAAMTVA
VKMLKPSAHSTEREALMSELKVLSYLGNHENIVNLLGACTHGGPTLVITE
YCCYGDLLNFLRRKRDEFVPYKVDFLTLEHLLSFSYQVAKGMAFLASKNC
IHRDLAARNILLTHGNITKICDFGLARDIKNDSNYVDKGNARLPVKWMAP
ESIFNSVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFR
MSSPEYAPAEMYDIMKTCWDADPDKRPTFKQIVQDIEKQISES
3D structure
PDB6gqk Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.
ChainB
Resolution2.31 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D792 R796 N797 D810
Catalytic site (residue number reindexed from 1) D154 R158 N159 D172
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 F88 B L595 V603 A621 K623 Y672 C673 L799 C809 D810 F811 L24 V32 A50 K52 Y101 C102 L161 C171 D172 F173
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase activity
GO:0004714 transmembrane receptor protein tyrosine kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation
GO:0007169 cell surface receptor protein tyrosine kinase signaling pathway

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Molecular Function
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Biological Process
External links
PDB RCSB:6gqk, PDBe:6gqk, PDBj:6gqk
PDBsum6gqk
PubMed30204441
UniProtP10721|KIT_HUMAN Mast/stem cell growth factor receptor Kit (Gene Name=KIT)

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