Structure of PDB 4xv1 Chain A

Receptor sequence
>4xv1A (length=239) Species: 9606 (Homo sapiens) [Search protein sequence]
DWEIPDGQITVGQRIGSGTVYKGKWHGDVAVKMLNVAPTPQQLQAFKNEV
GVLRKTRHVNILLFMGYSTKPQLAIVTQWCEGSSLYHHLHASKFEMKKLI
DIARQTARGMDYLHAKSIIHRDLKSNNIFLHEDNTVKIGDFGSGSILWMA
PEVIRNPYSFQSDVYAFGIVLYELMTGQLPYSNINNRDQIIEMVGRGSLS
PDLSKVNCPKRMKRLMAECLKKKRDERPSFPRILAEIEE
3D structure
PDB4xv1 RAF inhibitors that evade paradoxical MAPK pathway activation.
ChainA
Resolution2.47 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) D122 K124 N126 N127 D140 S145
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 904 A I463 A481 L505 L514 T529 Q530 W531 C532 D594 I15 A30 L53 L62 T77 Q78 W79 C80 D140 MOAD: ic50=0.0042uM
PDBbind-CN: -logKd/Ki=8.38,IC50=0.0042uM
BindingDB: IC50=16nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase 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:4xv1, PDBe:4xv1, PDBj:4xv1
PDBsum4xv1
PubMed26466569
UniProtP15056|BRAF_HUMAN Serine/threonine-protein kinase B-raf (Gene Name=BRAF)

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