Target
Gamma-aminobutyric acid receptor subunit alpha-1
Ligand
BDBM513088
Substrate
n/a
Meas. Tech.
Electrophysiology
Ki
5.40±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:
BDBM513088
Synonyms:
N-(1,1-dioxothian-4-yl)-6-((5-methyl-3-(6-methylpyridin-3-yl)-1,2-oxazol-4-yl)methoxy)pyridine-3-carboxamide | US11091471, Example 21
Type:
Small organic molecule
Emp. Form.:
C22H24N4O5S
Mol. Mass.:
456.515
SMILES:
Cc1onc(c1COc1ccc(cn1)C(=O)NC1CCS(=O)(=O)CC1)-c1ccc(C)nc1
Structure:
Search PDB for entries with ligand similarity: