Reaction Details Report a problem with these data
Target
Gamma-aminobutyric acid receptor subunit alpha-1
Ligand
BDBM50337263
Substrate
n/a
Meas. Tech.
ChEMBL_726365 (CHEMBL1687497)
IC50
1±n/a nM
Citation
 Hintermann, S; Hurth, K; Nozulak, J; Tintelnot-Blomley, M; Aichholz, R; Blanz, J; Kaupmann, K; Mosbacher, J Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor. Bioorg Med Chem Lett 21:1523-6 (2011) [PubMed]  Article 
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:
BDBM50337263
Synonyms:
3-(2-chlorobenzyloxy)-2-(2-fluorophenyl)-2H-pyrazolo[4,3-c]quinoline | CHEMBL1681887
Type:
Small organic molecule
Emp. Form.:
C23H15ClFN3O
Mol. Mass.:
403.836
SMILES:
Fc1ccccc1-n1nc2c(cnc3ccccc23)c1OCc1ccccc1Cl
Structure:
Search PDB for entries with ligand similarity: