Target
Gamma-aminobutyric acid receptor subunit alpha-3
Ligand
BDBM50179998
Substrate
n/a
Meas. Tech.
ChEMBL_938812 (CHEMBL2327956)
Ki
0.70±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:
BDBM50179998
Synonyms:
7-tert-butyl-3-(2,5-difluorophenyl)-6-((2-methyl-2H-1,2,4-triazol-3-yl)methoxy)-[1,2,4]triazolo[4,3-b]pyridazine | CHEMBL373250
Type:
Small organic molecule
Emp. Form.:
C19H19F2N7O
Mol. Mass.:
399.3973
SMILES:
Cn1ncnc1COc1nn2c(nnc2cc1C(C)(C)C)-c1cc(F)ccc1F
Structure:
Search PDB for entries with ligand similarity: