Target Validation Information
TTD ID T51452
Target Name GABA(A) receptor alpha-2 (GABRA2)
Type of Target
Successful
Drug Potency against Target (2E,4S)-4-ammoniopent-2-enoate Drug Info IC50 = 2600 nM [8]
(4R)-4-ammoniopentanoate Drug Info IC50 = 2500 nM [8]
(4S)-4-ammoniopentanoate Drug Info IC50 = 2900 nM [8]
3-(3-Methyl-butoxy)-9H-beta-carboline Drug Info Ki = 3000 nM [7]
3-(benzyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 3000 nM [7]
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 818 nM [7]
3-Butoxy-9H-beta-carboline Drug Info Ki = 194 nM [7]
3-Ethoxy-9H-beta-carboline Drug Info Ki = 25.1 nM [7]
3-Ethoxy-9H-beta-carboline Drug Info Ki = 25.1 nM [11]
3-Isobutoxy-9H-beta-carboline Drug Info Ki = 123.6 nM [7]
3-Propoxy-9H-beta-carboline Drug Info Ki = 52.3 nM [7]
5-[(1R)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 9500 nM [8]
5-[(1S)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 5800 nM [8]
9H-beta-Carboline-3-carboxylic acid ethyl ester Drug Info Ki = 4.9 nM [7]
AMENTOFLAVONE Drug Info Ki = 6 nM [1]
Beta-Carboline-3-carboxylic acid t-butyl ester Drug Info Ki = 15 nM [7]
CGS-17867A Drug Info Ki = 0.77 nM [3]
CI-218872 Drug Info Ki = 1964 nM [7]
Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 31 nM [7]
GSK683699 Drug Info Ki = 200 nM [9]
L-655708 Drug Info Ki = 22 nM [2]
MRK016 Drug Info Ki = 0.31 nM [4]
Ro-15-3505 Drug Info Ki = 16.3 nM [6]
Ro-4938581 Drug Info Ki = 185 nM [5]
Ro-4938581 Drug Info Ki = 24 nM [5]
RY-066 Drug Info Ki = 60 nM [12]
Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 60 nM [7]
[3H]Ro154513 Drug Info Ki = 2.6 nM [10]
References
REF 1 Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.
REF 2 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor li... J Med Chem. 2004 Mar 25;47(7):1807-22.
REF 3 2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3441-4.
REF 4 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-a... J Med Chem. 2005 Nov 17;48(23):7089-92.
REF 5 The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment... Bioorg Med Chem Lett. 2009 Oct 15;19(20):5940-4.
REF 6 The GABA(A) receptor as a target for photochromic molecules. Bioorg Med Chem. 2010 Nov 15;18(22):7731-8.
REF 7 Design, synthesis, and subtype selectivity of 3,6-disubstituted -carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents f... Bioorg Med Chem. 2010 Nov 1;18(21):7548-64.
REF 8 gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. J Med Chem. 1981 Dec;24(12):1377-83.
REF 9 New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide. J Med Chem. 1980 Jun;23(6):702-4.
REF 10 Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABA... J Med Chem. 1996 Apr 26;39(9):1928-34.
REF 11 Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) a... J Med Chem. 1998 Jul 2;41(14):2537-52.
REF 12 Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines a... J Med Chem. 1998 Oct 8;41(21):4130-42.

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