Target
Gamma-aminobutyric acid receptor subunit alpha-3
Ligand
BDBM50142570
Substrate
n/a
Meas. Tech.
ChEMBL_938812 (CHEMBL2327956)
Ki
0.50±n/a nM
Citation
 Bagal, SKBrown, ADCox, PJOmoto, KOwen, RMPryde, DCSidders, BSkerratt, SEStevens, EBStorer, RISwain, NA Ion channels as therapeutic targets: a drug discovery perspective. J Med Chem 56:593-624 (2013) [PubMed]  Article 
Target
Name:
Gamma-aminobutyric acid receptor subunit alpha-3
Synonyms:
GABA A Alpha3Beta3Gamma2 | GABA A receptor alpha-3/beta-2/gamma-2 | GABA C | GABA receptor alpha-3 subunit | GABA-A receptor | GABRA3 | GBRA3_HUMAN | Gamma-aminobutyric acid receptor subunit alpha-3 | agonist GABA site
Type:
Enzyme Catalytic Domain
Mol. Mass.:
55175.47
Organism:
Homo sapiens (Human)
Description:
GABA A Alpha3Beta1Gamma2 0 HUMAN::P34903
Residue:
492
Sequence:
MIITQTSHCYMTSLGILFLINILPGTTGQGESRRQEPGDFVKQDIGGLSPKHAPDIPDDSTDNITIFTRILDRLLDGYDNRLRPGLGDAVTEVKTDIYVTSFGPVSDTDMEYTIDVFFRQTWHDERLKFDGPMKILPLNNLLASKIWTPDTFFHNGKKSVAHNMTTPNKLLRLVDNGTLLYTMRLTIHAECPMHLEDFPMDVHACPLKFGSYAYTTAEVVYSWTLGKNKSVEVAQDGSRLNQYDLLGHVVGTEIIRSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRSWAWEGKKVPEALEMKKKTPAAPAKKTSTTFNIVGTTYPINLAKDTEFSTISKGAAPSASSTPTIIASPKATYVQDSPTETKTYNSVSKVDKISRIIFPVLFAIFNLVYWATYVNRESAIKGMIRKQ
  
Inhibitor
Name:
BDBM50142570
Synonyms:
9-(4-Methyl-thiazol-2-yl)-11-pyridin-4-yl-6,7-dihydro-5H-2,7a-diaza-dibenzo[a,c]cyclohepten-8-one | CHEMBL45198
Type:
Small organic molecule
Emp. Form.:
C22H18N4OS
Mol. Mass.:
386.47
SMILES:
Cc1csc(n1)-c1cc(-c2ccncc2)c2-c3cnccc3CCCn2c1=O
Structure:
Search PDB for entries with ligand similarity: