Structure of PDB 5v8o Chain A

Receptor sequence
>5v8oA (length=351) Species: 9606 (Homo sapiens) [Search protein sequence]
GASKLRAVLEKLKLSRDDISTAAGMVKGVVDHLLLRLKCDSAFRGVGLLN
TGSHVKISAPNEFDVMFKLEVPRIQLEEYSNTRAYYFVKFKRNPKENPLS
QFLEGEILSASKMLSKFRKIIKEEINDIKDTDVIMKRKRAVTLLISEKIS
VDITLALESKSSWPASTQEGLRIQNWLSAKVRKQLRLKPFYLVPKHAKFQ
EETWRLSFSHIEKEILNNHGKSKTCCENKEEKCCRKDCLKLMKYLLEQLK
ERFKDKKHLDKFSSYHVKTAFFHVCTQNPQDSQWDRKDLGLCFDNCVTYF
LQCLRTEKLENYFIPEFNLFSSNLIDKRSKEFLTKQIEYERNNEFPVFDE
F
3D structure
PDB5v8o Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay.
ChainA
Resolution3.1 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 2.7.7.86: cyclic GMP-AMP synthase.
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 ZN A H390 C397 C404 H219 C226 C233
BS02 8ZM A R376 Y436 N482 F488 L490 R205 Y265 N311 F317 L319 PDBbind-CN: -logKd/Ki=3.77,Kd=171uM
BindingDB: Kd=170000nM,IC50=78000nM
External links
PDB RCSB:5v8o, PDBe:5v8o, PDBj:5v8o
PDBsum5v8o
PubMed28934246
UniProtQ8N884|CGAS_HUMAN Cyclic GMP-AMP synthase (Gene Name=CGAS)

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