Structure of PDB 5csw Chain A

Receptor sequence
>5cswA (length=254) Species: 9606 (Homo sapiens) [Search protein sequence]
DWEIPDGQITVGQRIGSGSFGTVYKGKWHGDVAVKMLNVTAPTPQQLQAF
KNEVGVLRKTRHVNILLFMGYSTKPQLAIVTQWCEGSSLYHHLHASETKF
EMKKLIDIARQTARGMDYLHAKSIIHRDLKSNNIFLHEDNTVKIGDFGSI
LWMAPEVIRMQDSNPYSFQSDVYAFGIVLYELMTGQLPYSNINNRDQIIE
MVGRGSLSPDLSKVRSNCPKRMKRLMAECLKKKRDERPSFPRILAEIEEL
AREL
3D structure
PDB5csw A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation.
ChainA
Resolution2.66 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) D128 K130 N132 N133 D146 S149
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 P06 A S465 V471 K483 L505 L514 F516 T529 W531 C532 F583 D594 S17 V23 K35 L57 L66 F68 T81 W83 C84 F135 D146 PDBbind-CN: -logKd/Ki=8.40,Kd=4nM
BindingDB: IC50=1.000000nM,EC50=529nM
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:5csw, PDBe:5csw, PDBj:5csw
PDBsum5csw
PubMed26916115
UniProtP15056|BRAF_HUMAN Serine/threonine-protein kinase B-raf (Gene Name=BRAF)

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