Reaction Details
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Gamma-aminobutyric acid receptor subunit alpha-1
Ligand
BDBM50242613
Substrate
n/a
Meas. Tech.
ChEMBL_507909 (CHEMBL952530)
EC50
250±n/a nM
Citation
Tan, KR; Gonthier, A; Baur, R; Ernst, M; Goeldner, M; Sigel, E Proximity-accelerated chemical coupling reaction in the benzodiazepine-binding site of gamma-aminobutyric acid type A receptors: superposition of different allosteric modulators. J Biol Chem 282:26316-25 (2007) [PubMed] Article More Info.:
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:
BDBM50242613
Synonyms:
8-Isothiocyanato-5-methyl-6-oxo-5,6-dihydro-4H-2,5,10b-triaza-benzo[e]azulene-3-carboxylic acid ethyl ester | CHEMBL485829
Type:
Small organic molecule
Emp. Form.:
C16H14N4O3S
Mol. Mass.:
342.372
SMILES:
CCOC(=O)c1ncn-2c1CN(C)C(=O)c1cc(ccc-21)N=C=S
Structure:
