Target
Gamma-aminobutyric acid receptor subunit alpha-1
Ligand
BDBM50017309
Substrate
n/a
Ki
2.3±n/a nM
Comments
PDSP_821
Citation
 Hadingham, KLWingrove, PLe Bourdelles, BPalmer, KJRagan, CIWhiting, PJ Cloning of cDNA sequences encoding human alpha 2 and alpha 3 gamma-aminobutyric acidA receptor subunits and characterization of the benzodiazepine pharmacology of recombinant alpha 1-, alpha 2-, alpha 3-, and alpha 5-containing human gamma-aminobutyric acidA receptors. Mol Pharmacol 43:970-5 (1993) [PubMed] 
Target
Name:
Gamma-aminobutyric acid receptor subunit alpha-1
Synonyms:
Benzodiazepine central | GABA A Benzodiazepine brain | GABA A Benzodiazepine liver | GABA receptor alpha-1 subunit | GABA(A) receptor subunit alpha-1 | GABA-A | GABA-A receptor | GABRA1 | GBRA1_HUMAN | Gamma-aminobutyric acid receptor subunit alpha (GABAA) | TBPS | agonist GABA site
Type:
Protein
Mol. Mass.:
51817.35
Organism:
Homo sapiens (Human)
Description:
P14867
Residue:
456
Sequence:
MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPGLGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASKIWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHACPLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDPLIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKIDRLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
  
Inhibitor
Name:
BDBM50017309
Synonyms:
7-Chloro-3-(5-isopropyl-[1,2,4]oxadiazol-3-yl)-5-methyl-4,5-dihydro-2,5,10b-triaza-benzo[e]azulen-6-one | CHEMBL307202 | FG 8205
Type:
Small organic molecule
Emp. Form.:
C17H16ClN5O2
Mol. Mass.:
357.794
SMILES:
CC(C)c1nc(no1)-c1ncn-2c1CN(C)C(=O)c1c(Cl)cccc-21
Structure:
Search PDB for entries with ligand similarity: