Target
Cyclic GMP-AMP synthase
Ligand
BDBM50250110
Substrate
n/a
Meas. Tech.
ChEMBL_1680902 (CHEMBL4031179)
Kd
171000±n/a nM
Citation
 Hall, JBrault, AVincent, FWeng, SWang, HDumlao, DAulabaugh, AAivazian, DCastro, DChen, MCulp, JDower, KGardner, JHawrylik, SGolenbock, DHepworth, DHorn, MJones, LJones, PLatz, ELi, JLin, LLLin, WLin, DLovering, FNiljanskul, NNistler, RPierce, BPlotnikova, OSchmitt, DShanker, SSmith, JSnyder, WSubashi, TTrujillo, JTyminski, EWang, GWong, JLefker, BDakin, LLeach, K Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay. PLoS ONE 12:1-16 (2017) [PubMed]  Article 
Target
Name:
Cyclic GMP-AMP synthase
Synonyms:
2.7.7.86 | C6orf150 | CGAS | CGAS_HUMAN | Cyclic GMP-AMP synthase | MB21D1 | Mab-21 domain-containing protein 1 | Synonyms=C6orf150 | cGAMP synthase | h-cGAS
Type:
PROTEIN
Mol. Mass.:
58845.55
Organism:
Homo sapiens
Description:
ChEMBL_117333
Residue:
522
Sequence:
MQPWHGKAMQRASEAGATAPKASARNARGAPMDPTESPAAPEAALPKAGKFGPARKSGSRQKKSAPDTQERPPVRATGARAKKAPQRAQDTQPSDATSAPGAEGLEPPAAREPALSRAGSCRQRGARCSTKPRPPPGPWDVPSPGLPVSAPILVRRDAAPGASKLRAVLEKLKLSRDDISTAAGMVKGVVDHLLLRLKCDSAFRGVGLLNTGSYYEHVKISAPNEFDVMFKLEVPRIQLEEYSNTRAYYFVKFKRNPKENPLSQFLEGEILSASKMLSKFRKIIKEEINDIKDTDVIMKRKRGGSPAVTLLISEKISVDITLALESKSSWPASTQEGLRIQNWLSAKVRKQLRLKPFYLVPKHAKEGNGFQEETWRLSFSHIEKEILNNHGKSKTCCENKEEKCCRKDCLKLMKYLLEQLKERFKDKKHLDKFSSYHVKTAFFHVCTQNPQDSQWDRKDLGLCFDNCVTYFLQCLRTEKLENYFIPEFNLFSSNLIDKRSKEFLTKQIEYERNNEFPVFDEF
  
Inhibitor
Name:
BDBM50250110
Synonyms:
CHEMBL4065757
Type:
Small organic molecule
Emp. Form.:
C10H7N5O
Mol. Mass.:
213.1955
SMILES:
Oc1cc(nc2nnnn12)-c1ccccc1
Structure:
Search PDB for entries with ligand similarity: