Reaction Details Report a problem with these data
Target
Gamma-aminobutyric acid receptor subunit alpha-1
Ligand
BDBM50144861
Substrate
n/a
Meas. Tech.
ChEMBL_2280326
Ki
0.400000±n/a nM
Citation
 Károlyi, BI; Potor, A; Kapus, GL; Fodor, L; Bobok, A; Krámos, B; Magdó, I; Bata, I; Szabó, G Novel imidazo[1,5-a]quinoxaline derivatives: SAR, selectivity and modeling challenges en route to the identification of an ?5-GABAA receptor NAM. Bioorg Med Chem Lett 80:0 (2023) [PubMed] 
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:
BDBM50144861
Synonyms:
3-(5-Methyl-isoxazol-3-yl)-6-(pyridin-2-ylmethoxy)-[1,2,4]triazolo[3,4-a]phthalazine | 5-methyl-3-(6-(pyridin-2-ylmethoxy)-[1,2,4]triazolo[3,4-a]phthalazin-3-yl)isoxazole | CHEMBL68684
Type:
Small organic molecule
Emp. Form.:
C19H14N6O2
Mol. Mass.:
358.3535
SMILES:
Cc1cc(no1)-c1nnc2c3ccccc3c(OCc3ccccn3)nn12
Structure:
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