Reaction Details |
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Target | Gamma-aminobutyric acid receptor subunit alpha-1 |
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Ligand | BDBM50337268 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_726365 (CHEMBL1687497) |
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IC50 | 67±n/a nM |
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Citation | Hintermann, S; Hurth, K; Nozulak, J; Tintelnot-Blomley, M; Aichholz, R; Blanz, J; Kaupmann, K; Mosbacher, J Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor. Bioorg Med Chem Lett21:1523-6 (2011) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Gamma-aminobutyric acid receptor subunit alpha-1 |
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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: | MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG
LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC
PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM
TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP
LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID
RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
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BDBM50337268 |
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n/a |
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Name | BDBM50337268 |
Synonyms: | 3-(2-chlorobenzyloxy)-2-(4-chlorophenyl)-8,8-dimethyl-6,7,8,9-tetrahydro-2H-pyrazolo[4,3-c]quinoline | CHEMBL1681892 |
Type | Small organic molecule |
Emp. Form. | C25H23Cl2N3O |
Mol. Mass. | 452.376 |
SMILES | CC1(C)CCc2ncc3c(OCc4ccccc4Cl)n(nc3c2C1)-c1ccc(Cl)cc1 |
Structure |
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