Target
Gamma-aminobutyric acid receptor subunit alpha-1
Ligand
BDBM50001728
Substrate
n/a
Meas. Tech.
ChEMBL_219118 (CHEMBL823141)
EC50
37±n/a nM
Citation
 Albaugh, PAMarshall, LGregory, JWhite, GHutchison, ARoss, PCGallagher, DWTallman, JFCrago, MCassella, JV Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor. J Med Chem 45:5043-51 (2002) [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:
BDBM50001728
Synonyms:
8-Chloro-1-methyl-6-phenyl-4H-s-triazolo(4,3-a)(1,4)benzodiazepine | 8-chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine | ALPRAZOLAM | CHEMBL661 | Xanax
Type:
Small organic molecule
Emp. Form.:
C17H13ClN4
Mol. Mass.:
308.765
SMILES:
Cc1nnc2CN=C(c3ccccc3)c3cc(Cl)ccc3-n12 |t:6|
Structure:
Search PDB for entries with ligand similarity: