Target
Gamma-aminobutyric acid receptor subunit alpha-1
Ligand
BDBM50049736
Substrate
n/a
Meas. Tech.
ChEMBL_491127 (CHEMBL991895)
EC50
74400±n/a nM
Citation
 Harris, DClayton, TCook, JSahbaie, PHalliwell, RFFurtmüller, RHuck, SSieghart, WDeLorey, TM Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit. J Med Chem 51:3788-803 (2008) [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:
BDBM50049736
Synonyms:
8-Ethynyl-5-methyl-6-oxo-5,6-dihydro-4H-2,5,10b-triaza-benzo[e]azulene-3-carboxylic acid tert-butyl ester | 8-Ethynyl-5-methyl-6-oxo-5,6-dihydro-4H-2,5,10b-triaza-benzo[e]azulene-3-carboxylic acid tert-butyl ester(RY 24) | CHEMBL58757
Type:
Small organic molecule
Emp. Form.:
C19H19N3O3
Mol. Mass.:
337.3725
SMILES:
CN1Cc2c(ncn2-c2ccc(cc2C1=O)C#C)C(=O)OC(C)(C)C
Structure:
Search PDB for entries with ligand similarity: