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Target
Gamma-aminobutyric acid receptor subunit alpha-5
Ligand
BDBM85683
Substrate
n/a
Ki
210±n/a nM
Comments
PDSP_555
Citation
 Vanover, KE; Rosenzweig-Lipson, S; Hawkinson, JE; Lan, NC; Belluzzi, JD; Stein, L; Barrett, JE; Wood, PL; Carter, RB Characterization of the anxiolytic properties of a novel neuroactive steroid, Co 2-6749 (GMA-839; WAY-141839; 3alpha, 21-dihydroxy-3beta-trifluoromethyl-19-nor-5beta-pregnan-20-one), a selective modulator of gamma-aminobutyric acid(A) receptors. J Pharmacol Exp Ther 295:337-45 (2000) [PubMed]
Target
Name:
Gamma-aminobutyric acid receptor subunit alpha-5
Synonyms:
GABA A Alpha5Beta2Gamma2 | GABA A Alpha5Beta3Gamma2 | GABA A Alpha5m10Beta2Gamma2 | GABA A Alpha5m8Beta2Gamma2 | GABA A Alpha5m9Beta2Gamma2 | GABA A alpha5 | GABA A receptor alpha-5/beta-3/gamma-2 | GABA receptor alpha-5 subunit | GBRA5_RAT | Gabra-5 | Gabra5 | Gamma-aminobutyric acid receptor subunit alpha-5
Type:
Enzyme Catalytic Domain
Mol. Mass.:
52350.79
Organism:
RAT
Description:
GABA A alpha5 0 RAT::P19969
Residue:
464
Sequence:
MDNGMLSRFIMTKTLLVFCISMTLSSHFGFSQMPTSSVQDETNDNITIFTRILDGLLDGYDNRLRPGLGERITQVRTDIYVTSFGPVSDTEMEYTIDVFFRQSWKDERLRFKGPMQRLPLNNLLASKIWTPDTFFHNGKKSIAHNMTTPNKLLRLEDDGTLLYTMRLTISAECPMQLEDFPMDAHACPLKFGSYAYPNSEVVYVWTNGSTKSVVVAEDGSRLNQYHLMGQTVGTENISTSTGEYTIMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKKALEAAKIKKKERELILNKSTNAFTTGKLTHPPNIPKEQLPGGTGNAVGTASIRASEEKTSESKKTYNSISKIDKMSRIVFPILFGTFNLVYWATYLNREPVIKGATSPK
  
Inhibitor
Name:
BDBM85683
Synonyms:
Co 2-6749 | Co-2-6749 | GMA-839 | WAY-141839
Type:
Small organic molecule
Emp. Form.:
C21H31F3O3
Mol. Mass.:
388.4642
SMILES:
C[C@]12CC[C@H]3[C@@H](CC[C@@H]4C[C@](O)(CC[C@H]34)C(F)(F)F)[C@@H]1CC[C@@H]2C(=O)CO
Structure:
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