Reaction Details
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Gamma-aminobutyric acid receptor subunit alpha-1
Ligand
BDBM50459891
Substrate
n/a
Meas. Tech.
ChEMBL_1767464 (CHEMBL4219576)
EC50
15000±n/a nM
Citation
Sparling, BA; DiMauro, EF Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors. Bioorg Med Chem Lett 27:3207-3218 (2017) [PubMed] Article More Info.:
Target
Name:
Gamma-aminobutyric acid receptor subunit alpha-1
Synonyms:
Benzodiazepine central | Benzodiazepine receptors | GABA A Benzodiazepine | GABA A Benzodiazepine Type I | GABA A Benzodiazepine Type II | GABA A Benzodiazepine Type IIL | GABA A Benzodiazepine Type IIM | GABA A Benzodiazepine omega1 | GABA A Benzodiazepine omega2 | GABA A Benzodiazepine omega5 | GABA A alpha1 | GABA A anti-Alpha1 | GABA receptor alpha-1 subunit | GABA, Chloride, TBOB | GABA-PICROTOXIN | GBRA1_RAT | Gabra-1 | Gabra1 | TBPS
Type:
Enzyme
Mol. Mass.:
51770.21
Organism:
Rattus norvegicus (Rat)
Description:
P62813
Residue:
455
Sequence:
MKKSRGLSDYLWAWTLILSTLSGRSYGQPSQDELKDNTTVFTRILDRLLDGYDNRLRPGLGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASKIWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHACPLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDPLIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKIDRLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
Inhibitor
Name:
BDBM50459891
Synonyms:
CHEMBL4229086
Type:
Small organic molecule
Emp. Form.:
C17H17F2NO2
Mol. Mass.:
305.3192
SMILES:
CCCCNC(=O)c1cc(ccc1O)-c1ccc(F)cc1F
Structure:
