Structure of PDB 4xv9 Chain A

Receptor sequence
>4xv9A (length=261) Species: 9606 (Homo sapiens) [Search protein sequence]
DDWEIPDGQITVGQRIGSGSFGTVYKGKWHGDVAVKMLNVTAPTPQQLQA
FKNEVGVLRKTRHVNILLFMGYSTKPQLAIVTQWCEGSSLYHHLHASETK
FEMKKLIDIARQTARGMDYLHAKSIIHRDLKSNNIFLHEDNTVKIGDFGL
ALSGSILWMAPEVIRMQDSNPYSFQSDVYAFGIVLYELMTGQLPYSNINN
RDQIIEMVGRGSLSPDLSKVRSNCPKRMKRLMAECLKKKRDERPSFPRIL
AEIEELARELS
3D structure
PDB4xv9 RAF inhibitors that evade paradoxical MAPK pathway activation.
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) D576 K578 N580 N581 D594 S616
Catalytic site (residue number reindexed from 1) D129 K131 N133 N134 D147 S155
Enzyme Commision number 2.7.11.1: non-specific serine/threonine protein 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 1OO A V471 A481 K483 L505 L514 T529 W531 C532 H574 F583 I592 G593 D594 F595 V24 A34 K36 L58 L67 T82 W84 C85 H127 F136 I145 G146 D147 F148 MOAD: ic50=0.19uM
PDBbind-CN: -logKd/Ki=6.72,IC50=0.19uM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation

View graph for
Molecular Function

View graph for
Biological Process
External links
PDB RCSB:4xv9, PDBe:4xv9, PDBj:4xv9
PDBsum4xv9
PubMed26466569
UniProtP15056|BRAF_HUMAN Serine/threonine-protein kinase B-raf (Gene Name=BRAF)

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