Target Validation Information
Target ID T62292
Target Name Gamma-aminobutyric-acid receptor alpha-3 subunit
Target Type
Clinical Trial
Drug Potency against Target Ro-154513 Drug Info Ki = 2.5 nM [1]
3-(isopentyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 3000 nM [2]
6-bromo-3-ethoxycarbonyl-4-quinolone Drug Info Ki = 26 nM [3]
6-ethyl-3-(3-methylbutoxycarbonyl)-4-quinolone Drug Info Ki = 89 nM [3]
6-benzyl-3-ethoxycarbonyl-4-quinolone Drug Info Ki = 7.2 nM [3]
GAMMA-AMINO-BUTANOIC ACID Drug Info Ki = 200 nM [4]
5-[(1R)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 9500 nM [5]
Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 116 nM [2]
(4R)-4-ammoniopentanoate Drug Info IC50 = 2500 nM [5]
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 859 nM [2]
Ethyl 9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 5.7 nM [2]
3-(benzyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 3000 nM [2]
Beta-Carboline-3-carboxylic acid t-butyl ester Drug Info Ki = 18.9 nM [2]
AMENTOFLAVONE Drug Info Ki = 6 nM [6]
L-655708 Drug Info Ki = 11 nM [7]
(2E,4S)-4-ammoniopent-2-enoate Drug Info IC50 = 2600 nM [5]
Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 34 nM [2]
CI-218872 Drug Info Ki = 1161 nM [2]
RY-066 Drug Info Ki = 48 nM [8]
Ro-151310 Drug Info Ki = 9.2 nM [9]
MRK016 Drug Info Ki = 0.2 nM [10]
5-[(1S)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 5800 nM [5]
Ro-4938581 Drug Info Ki = 14 nM [11]
3-ethoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 28.2 nM [2]
(4S)-4-ammoniopentanoate Drug Info IC50 = 2900 nM [5]
3-butoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 245 nM [2]
3-isobutoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 139.2 nM [2]
Ro-4938581 Drug Info Ki = 80 nM [11]
3-propoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 68.8 nM [2]
References
REF 1J Med Chem. 1996 Apr 26;39(9):1928-34.Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABAA receptors.
REF 2Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
REF 3J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
REF 4J Med Chem. 1980 Jun;23(6):702-4.New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide.
REF 5J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects.
REF 6Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors.
REF 7J Med Chem. 2004 Mar 25;47(7):1807-22.3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
REF 8J Med Chem. 1998 Oct 8;41(21):4130-42.Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparative molecular field analysis.
REF 9Bioorg Med Chem. 2010 Nov 15;18(22):7731-8. Epub 2010 Jun 1.The GABA(A) receptor as a target for photochromic molecules.
REF 10J Med Chem. 2005 Nov 17;48(23):7089-92.7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.
REF 11Bioorg Med Chem Lett. 2009 Oct 15;19(20):5940-4. Epub 2009 Aug 15.The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction.

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