Target
Gamma-aminobutyric acid receptor subunit alpha-1
Ligand
BDBM513298
Substrate
n/a
Meas. Tech.
Electrophysiology
Ki
7.60±n/a nM
Citation
 Buettelmann, BCecere, GFasching, BGroebke Zbinden, KHernandez, MKnust, HKoblet, APinard, EThomas, A Isoxazolyl ether derivatives as GABAA α5 PAM US Patent  US11091471 Publication Date 8/17/2021 
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:
BDBM513298
Synonyms:
US11091471, Example 166 | trans-N-((1RS,3RS)-3-methoxycyclopentyl)-6-((5-methyl-3-(6-methylpyridin-3-yl)isoxazol-4-yl)methoxy)pyridazine-3-carboxamide
Type:
Small organic molecule
Emp. Form.:
C22H25N5O4
Mol. Mass.:
423.465
SMILES:
CO[C@@H]1CC[C@H](C1)NC(=O)c1ccc(OCc2c(C)onc2-c2ccc(C)nc2)nn1 |r|
Structure:
Search PDB for entries with ligand similarity: