Structure of PDB 4zsa Chain B

Receptor sequence
>4zsaB (length=282) Species: 9606 (Homo sapiens) [Search protein sequence]
EYELPEDPRWELPRDRLVLGKPLGEGAFGQVVLAEAIGLDKDKPNRVTKV
AVKMLKSDATEKDLSDLISEMEMMKMIGKHKNIINLLGACTQDGPLYVIV
EYASKGNLREYLQARRPPEEQLSSKDLVSCAYQVARGMEYLASKKCIHRD
LAARNVLVTEDNVMKIADFGLIDYYKKTTNGRLPVKWMAPEALFDRIYTH
QSDVWSFGVLLWEIFTLGGSPYPGVPVEELFKLLKEGHRMDKPSNCTNEL
YMMMRDCWHAVPSQRPTFKQLVEDLDRIVALT
3D structure
PDB4zsa Design, synthesis and biological evaluation of novel FGFR inhibitors bearing an indazole scaffold.
ChainB
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) D623 A625 R627 N628 D641
Catalytic site (residue number reindexed from 1) D150 A152 R154 N155 D168
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 4UT B F489 A512 E531 V561 Y563 A564 S565 G567 L630 F28 A51 E70 V100 Y102 A103 S104 G106 L157 MOAD: ic50=15nM
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

View graph for
Biological Process
External links
PDB RCSB:4zsa, PDBe:4zsa, PDBj:4zsa
PDBsum4zsa
PubMed26080733
UniProtP11362|FGFR1_HUMAN Fibroblast growth factor receptor 1 (Gene Name=FGFR1)

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