Structure of PDB 6itj Chain B

Receptor sequence
>6itjB (length=293) Species: 9606 (Homo sapiens) [Search protein sequence]
GVSEYELPEDPRWELPRDRLVLGKPLGEGAFGQVVLAEAIGLDKDKPNRV
TKVAVKMLKSDATEKDLSDLISEMEMMKMIGKHKNIINLLGACTQDGPLY
VIVEYASKGNLREYLQARRPPGLEYSYPEEQLSSKDLVSCAYQVARGMEY
LASKKCIHRDLAARNVLVTEDNVMKIADFGLAIDYYKKTTNGRLPVKWMA
PEALFDRIYTHQSDVWSFGVLLWEIFTLGGSPYPGVPVEELFKLLKEGHR
MDKPSNCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRIVALT
3D structure
PDB6itj Discovery and Development of a Series of Pyrazolo[3,4-d]pyridazinone Compounds as the Novel Covalent Fibroblast Growth Factor Receptor Inhibitors by the Rational Drug Design.
ChainB
Resolution1.994 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D623 A625 R627 N628 D641
Catalytic site (residue number reindexed from 1) D160 A162 R164 N165 D178
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 AXU B F489 V492 A512 K514 V561 Y563 A564 L630 F31 V34 A54 K56 V103 Y105 A106 L167 MOAD: ic50=10.8nM
BindingDB: IC50=11nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase activity
GO:0005007 fibroblast growth factor receptor 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:6itj, PDBe:6itj, PDBj:6itj
PDBsum6itj
PubMed31335138
UniProtP11362|FGFR1_HUMAN Fibroblast growth factor receptor 1 (Gene Name=FGFR1)

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