Target
Gamma-aminobutyric acid receptor subunit alpha-1
Ligand
BDBM50120773
Substrate
n/a
Meas. Tech.
ChEMBL_219118 (CHEMBL823141)
EC50
93±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:
BDBM50120773
Synonyms:
8-(2-Fluoro-benzoyl)-2-(2-fluoro-phenyl)-6,7,8,9-tetrahydro-5H-1,3a,5,8-tetraaza-cyclopenta[a]naphthalen-4-one | CHEMBL146302
Type:
Small organic molecule
Emp. Form.:
C22H16F2N4O2
Mol. Mass.:
406.3848
SMILES:
Fc1ccccc1C(=O)N1CCc2[nH]c(=O)n3cc(nc3c2C1)-c1ccccc1F
Structure:
Search PDB for entries with ligand similarity: