Structure of PDB 5csx Chain A

Receptor sequence
>5csxA (length=261) Species: 9606 (Homo sapiens) [Search protein sequence]
DDWEIPDGQITVGQRIGSGSFGTVYKGKWHGDVAVKMLNVTAPTPQQLQA
FKNEVGVLRKTRHVNILLFMGYSTKPQLAIVTQWCEGSSLYHHLHASETK
FEMKKLIDIARQTARGMDYLHAKSIIHRDLKSNNIFLHEDNTVKIGDFGL
ATVKSRSGSILWMAPEVIRMQDPYSFQSDVYAFGIVLYELMTGQLPYSNI
NNRDQIIEMVGRGSLSPDLSKVRSNCPKRMKRLMAECLKKKRDERPSFPR
ILAEIEELARE
3D structure
PDB5csx 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
Resolution2.51 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 S159
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 54J A I463 V471 A481 K483 L505 L514 F516 I527 T529 W531 C532 G593 D594 F595 K601 I16 V24 A34 K36 L58 L67 F69 I80 T82 W84 C85 G146 D147 F148 K154 PDBbind-CN: -logKd/Ki=8.22,Kd=6nM
BindingDB: IC50=0.400000nM,Kd=0.330000nM
BS02 GLC A E501 H574 G593 D594 K601 R603 E54 H127 G146 D147 K154 R156
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:5csx, PDBe:5csx, PDBj:5csx
PDBsum5csx
PubMed26916115
UniProtP15056|BRAF_HUMAN Serine/threonine-protein kinase B-raf (Gene Name=BRAF)

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