Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T26368 | ||||
Target Name | Gamma-aminobutyric-acid receptor alpha-5 subunit | ||||
Target Type | Clinical Trial |
||||
Drug Potency against Target | Beta-Carboline-3-carboxylic acid t-butyl ester | Drug Info | Ki = 110.8 nM | [531188] | |
(2E,4S)-4-ammoniopent-2-enoate | Drug Info | IC50 = 2600 nM | [533514] | ||
L-655708 | Drug Info | Ki = 0.4 nM | [527005] | ||
MRK016 | Drug Info | Ki = 0.2 nM | [527950] | ||
Ro-4938581 | Drug Info | Ki = 2 nM | [530391] | ||
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole | Drug Info | Ki = 10000 nM | [531188] | ||
CI-218872 | Drug Info | Ki = 561 nM | [531188] | ||
(4R)-4-ammoniopentanoate | Drug Info | IC50 = 2500 nM | [533514] | ||
3-ethoxy-9H-pyrido[3,4-b]indole | Drug Info | Ki = 826 nM | [531188] | ||
3-(isopentyloxy)-9H-pyrido[3,4-b]indole | Drug Info | Ki = 3000 nM | [531188] | ||
(4S)-4-ammoniopentanoate | Drug Info | IC50 = 2900 nM | [533514] | ||
Ro-154513 | Drug Info | Ki = 0.26 nM | [534122] | ||
Ro-4938581 | Drug Info | Ki = 4.6 nM | [530391] | ||
3-(benzyloxy)-9H-pyrido[3,4-b]indole | Drug Info | Ki = 10000 nM | [531188] | ||
3-isobutoxy-9H-pyrido[3,4-b]indole | Drug Info | Ki = 1000 nM | [531188] | ||
3-propoxy-9H-pyrido[3,4-b]indole | Drug Info | Ki = 591 nM | [531188] | ||
Ro-151310 | Drug Info | Ki = 54.6 nM | [531044] | ||
GAMMA-AMINO-BUTANOIC ACID | Drug Info | Ki = 200 nM | [533580] | ||
Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate | Drug Info | Ki = 286 nM | [531188] | ||
Ethyl 9H-pyrido[3,4-b]indole-3-carboxylate | Drug Info | Ki = 26.8 nM | [531188] | ||
AMENTOFLAVONE | Drug Info | Ki = 6 nM | [526653] | ||
5-[(1R)-1-ammonioethyl]isoxazol-3-olate | Drug Info | IC50 = 9500 nM | [533514] | ||
Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate | Drug Info | Ki = 216 nM | [531188] | ||
3-butoxy-9H-pyrido[3,4-b]indole | Drug Info | Ki = 1000 nM | [531188] | ||
5-[(1S)-1-ammonioethyl]isoxazol-3-olate | Drug Info | IC50 = 5800 nM | [533514] | ||
References | |||||
Ref 531188 | Bioorg 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 533514 | J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. | ||||
Ref 527005 | J 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 527950 | J Med Chem. 2006 Jan 12;49(1):35-8.Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders. | ||||
Ref 530391 | Bioorg 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. | ||||
Ref 531188 | Bioorg 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 531188 | Bioorg 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 533514 | J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. | ||||
Ref 531188 | Bioorg 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 531188 | Bioorg 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 533514 | J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. | ||||
Ref 534122 | J 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 530391 | Bioorg 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. | ||||
Ref 531188 | Bioorg 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 531188 | Bioorg 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 531188 | Bioorg 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 531044 | Bioorg Med Chem. 2010 Nov 15;18(22):7731-8. Epub 2010 Jun 1.The GABA(A) receptor as a target for photochromic molecules. | ||||
Ref 533580 | J Med Chem. 1980 Jun;23(6):702-4.New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide. | ||||
Ref 531188 | Bioorg 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 531188 | Bioorg 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 526653 | Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. | ||||
Ref 533514 | J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. | ||||
Ref 531188 | Bioorg 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 531188 | Bioorg 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 533514 | J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. |
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