Therapeutic Targets Database
BIDD Pharmainformatics Databases


Target Validation Information
Target NameGamma-aminobutyric-acid receptor alpha-2 subunit    
Type of TargetResearch target    
Drug Potency against Target(4R)-4-ammoniopentanoateIC50 = 2500 nM[1]
(2E,4S)-4-ammoniopent-2-enoateIC50 = 2600 nM[1]
(4S)-4-ammoniopentanoateIC50 = 2900 nM[1]
5-[(1S)-1-ammonioethyl]isoxazol-3-olateIC50 = 5800 nM[1]
5-[(1R)-1-ammonioethyl]isoxazol-3-olateIC50 = 9500 nM[1]
TPA-023Ki = 0.31 nM[2]
CGS-17867AKi = 0.77 nM[3]
3-isobutoxy-9H-pyrido[3,4-b]indoleKi = 123.6 nM[4]
beta-Carboline-3-carboxylic acid t-butyl esterKi = 15 nM[4]
Ro-151310Ki = 16.3 nM[5]
Ro-4938581Ki = 185 nM[6]
3-butoxy-9H-pyrido[3,4-b]indoleKi = 194 nM[4]
CI-218872Ki = 1964 nM[4]
Ro-154513Ki = 2.6 nM[7]
L-655708;NCGC00025115-02Ki = 22 nM[9]
Ro-4882224Ki = 24 nM[6]
3-Ethoxy-9H-beta-carbolineKi = 25.1 nM[10]
3-ethoxy-9H-pyrido[3,4-b]indoleKi = 25.1 nM[4]
3-(benzyloxy)-9H-pyrido[3,4-b]indoleKi = 3000 nM[4]
3-(isopentyloxy)-9H-pyrido[3,4-b]indoleKi = 3000 nM[4]
ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylateKi = 31 nM[4]
Ethyl 9H-pyrido[3,4-b]indole-3-carboxylateKi = 4.9 nM[4]
3-propoxy-9H-pyrido[3,4-b]indoleKi = 52.3 nM[4]
RY-066Ki = 60 nM[12]
sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylateKi = 60 nM[4]
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indoleKi = 818 nM[4]
Ref 1J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. To Reference
Ref 2J 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. To Reference
Ref 3Bioorg Med Chem Lett. 2004 Jul 5;14(13):3441-4.2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor. To Reference
Ref 4Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted -carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse. To Reference
Ref 5Bioorg Med Chem. 2010 Nov 15;18(22):7731-8. Epub 2010 Jun 1.The GABA(A) receptor as a target for photochromic molecules. To Reference
Ref 6Bioorg 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. To Reference
Ref 7J 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. To Reference
Ref 8J Med Chem. 1980 Jun;23(6):702-4.New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide. To Reference
Ref 9J 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. To Reference
Ref 10J Med Chem. 1998 Jul 2;41(14):2537-52.Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) at wild type and recombinant GABAA receptors. To Reference
Ref 11Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. To Reference
Ref 12J 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. To Reference


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