Target Validation Information
TTD ID	T26368
Target Name	GABA(A) receptor alpha-5 (GABRA5)
Type of Target	Successful
Drug Potency against Target	(2E,4S)-4-ammoniopent-2-enoate	Drug Info	IC50 = 2600 nM	[7]
	(4R)-4-ammoniopentanoate	Drug Info	IC50 = 2500 nM	[7]
	(4S)-4-ammoniopentanoate	Drug Info	IC50 = 2900 nM	[7]
	3-(3-Methyl-butoxy)-9H-beta-carboline	Drug Info	Ki = 3000 nM	[6]
	3-(benzyloxy)-9H-pyrido[3,4-b]indole	Drug Info	Ki = 10000 nM	[6]
	3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole	Drug Info	Ki = 10000 nM	[6]
	3-Butoxy-9H-beta-carboline	Drug Info	Ki = 1000 nM	[6]
	3-Ethoxy-9H-beta-carboline	Drug Info	Ki = 826 nM	[6]
	3-Isobutoxy-9H-beta-carboline	Drug Info	Ki = 1000 nM	[6]
	3-Propoxy-9H-beta-carboline	Drug Info	Ki = 591 nM	[6]
	5-[(1R)-1-ammonioethyl]isoxazol-3-olate	Drug Info	IC50 = 9500 nM	[7]
	5-[(1S)-1-ammonioethyl]isoxazol-3-olate	Drug Info	IC50 = 5800 nM	[7]
	9H-beta-Carboline-3-carboxylic acid ethyl ester	Drug Info	Ki = 26.8 nM	[6]
	AMENTOFLAVONE	Drug Info	Ki = 6 nM	[1]
	Beta-Carboline-3-carboxylic acid t-butyl ester	Drug Info	Ki = 110.8 nM	[6]
	CI-218872	Drug Info	Ki = 561 nM	[6]
	Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate	Drug Info	Ki = 286 nM	[6]
	GSK683699	Drug Info	Ki = 200 nM	[8]
	L-655708	Drug Info	Ki = 0.4 nM	[2]
	MRK016	Drug Info	Ki = 0.2 nM	[3]
	Ro-15-3505	Drug Info	Ki = 54.6 nM	[5]
	Ro-4938581	Drug Info	Ki = 2 nM	[4]
	Ro-4938581	Drug Info	Ki = 4.6 nM	[4]
	Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate	Drug Info	Ki = 216 nM	[6]
	[3H]Ro154513	Drug Info	Ki = 0.26 nM	[9]
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	Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety... J Med Chem. 2006 Jan 12;49(1):35-8.
REF 4	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 5	The GABA(A) receptor as a target for photochromic molecules. Bioorg Med Chem. 2010 Nov 15;18(22):7731-8.
REF 6	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 7	gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. J Med Chem. 1981 Dec;24(12):1377-83.
REF 8	New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide. J Med Chem. 1980 Jun;23(6):702-4.
REF 9	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.

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