GABA-A receptor; alpha-2/beta-3/gamma-2 Inhibitors (IC50, Ki)

Structure ▲ ▼	Compound Name ▲ ▼	Standard Type ▲ ▼	Standard Values (in nM) ▲ ▼
	Diazepam	Ki	6.6 [1]
	Methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate	Ki	13.0 [1]
	Zolpidem	Ki	103.0 [1]
	3-Methyl-6-[3-(trifluoromethyl)phenyl]-[1,2,4]triazolo[4,3-b]pyridazine	Ki	720.0 [1], 1960.0 [2], 1964.0 [3], 2000.0 [4]
	Ethyl 8-ethynyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	21.4 [1]
	Chlordiazepoxide	Ki	392.0 [1], 460.0 [2]
	CID 9971547	Ki	300.0 [1]
	Tert-butyl 8-ethynyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	26.3 [1]
	Flunitrazepam	Ki	1.1 [1], 2.5 [2]
	Ethyl-8-azido-5,6-dihydro-5-methyl-6-oxo-4H-imidazo-1,4-benzodiazepine-3-carboxylate	Ki	2.6 [1]
	Ethyl beta-carboline-3-carboxylate	Ki	4.9 [1]
	Tert-Butyl beta-carboline-3-carboxylate	Ki	15.0 [1]
	3-Propoxy-9H-pyrido[3,4-b]indole	Ki	52.3 [1]
	3-Ethoxy-beta-carboline	Ki	25.1 [1]
	3-Butoxy-9H-beta-carboline	Ki	194.0 [1]
	3-(2-Hydroxyethylsulfanyl)-6,6-dimethyl-1-(1,3-thiazol-2-yl)-5,7-dihydro-2-benzothiophen-4-one	Ki	16.0 [1]
	3-Isobutoxy-9H-beta-carboline	Ki	123.6 [1], 124.0 [2]
	3-Benzyloxy-9H-beta-carboline	Ki	3000.0 [1]
	3-(Isopentyloxy)-9H-pyrido[3,4-b]indole	Ki	3000.0 [1]
	alpha,alpha-Dimethyl-3-[3-(3-pyridyl)-4-fluorophenyl]imidazo[1,2-a]pyrimidine-7-methanol	Ki	3.7 [1], 4.0 [2]
	Tert-butyl 5-methyl-6-oxo-8-(2-trimethylsilylethynyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	143.0 [1]
	5-Methyl-8-chloro-3-acetyl-4H-imidazo[1,5-a][1,4]benzodiazepine-6(5H)-one	Ki	33800.0 [1], 33834.0 [2]
	Ethyl 5-methyl-6-oxo-8-(2-trimethylsilylethynyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	141.9 [1], 142.0 [2]
	6-Phenyl-9-(pyridin-2-ylmethoxy)-4,5,7,8-tetrazatetracyclo[9.2.2.02,10.03,7]pentadeca-2(10),3,5,8-tetraene	Ki	21.7 [1], 26.0 [2]
	5-Methyl-3-(6-(pyridin-2-ylmethoxy)-[1,2,4]triazolo[3,4-a]phthalazin-3-yl)isoxazole	Ki	1.5 [1], 2.7 [2]
	9-[(6-Methylpyridin-2-yl)methoxy]-6-phenyl-4,5,7,8-tetrazatetracyclo[9.2.2.02,10.03,7]pentadeca-2(10),3,5,8-tetraene	Ki	36.0 [1], 44.5 [2], 46.0 [3]
	CID 5255267	Ki	1000.0 [1]
	Ethyl (7S)-15-ethynyl-12-oxo-2,4,11-triazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(17),3,5,13,15-pentaene-5-carboxylate	Ki	44.0 [1]
	Ethyl (7S)-12-oxo-15-(2-trimethylsilylethynyl)-2,4,11-triazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(17),3,5,13,15-pentaene-5-carboxylate	Ki	124.0 [1]
	Ethyl (7S)-15-bromo-12-oxo-2,4,11-triazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(17),3,5,13,15-pentaene-5-carboxylate	Ki	29.0 [1]
	Flumazenil	Ki	0.9 [1]
	Abecarnil	Ki	15.3 [1]
	7-Tert-butyl-6-[(2-ethyl-1,2,4-triazol-3-yl)methoxy]-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine	Ki	0.3 [1], 0.31 [2]
	Ethyl 8-chloro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylate	Ki	16.3 [1]
	6-Benzyloxy-4-methoxymethyl-beta-carboline-3-carboxylic acid ethyl ester	Ki	4.2 [1]
	alpha5IA	Ki	0.58 [1]
	3-Isopropoxy-9H-beta-carboline	Ki	3000.0 [1]
	Tert-Butyl 8-chloro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylate	Ki	21.6 [1]
	6-Methoxy-4-methoxymethyl-9H-beta-carboline-3-carboxylic acid ethyl ester	Ki	1.19 [1]
	6-Propoxy-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester	Ki	1.21 [1]
	(E)-1-(1-(3-(Pyridin-3-yl)phenyl)-1H-benzo(d)imidazol-5-yl)ethanone O-ethyl oxime	Ki	13.1 [1], 14.0 [2]
	Cyclopropylmethyl 8-chloro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	48.2 [1]
	Tert-butyl 8-bromo-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	10.7 [1]
	3-Ethyl-5-methyl-8-chloro-4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-one	Ki	1527.0 [1], 1530.0 [2]
	3-Pentanoyl-5-methyl-8-chloro-4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-one	Ki	2865.0 [1], 2870.0 [2]
	Tert-butyl 5-methyl-8-nitro-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	49.8 [1]
	Ethyl 8-ethyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	27.0 [1]
	Tert-butyl 8-iodo-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	11.2 [1]
	3-Pentyl-5-methyl-8-chloro-4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-one	Ki	2900.0 [1]
	5-Methyl-8-chloro-3-[(diethylamino)methyl]-4H-imidazo[1,5-a][1,4]benzodiazepine-6(5H)-one	Ki	30000.0 [1]
	5-Methyl-8-chloro-3-[(diisopropylamino)methyl]-4H-imidazo[1,5-a][1,4]benzodiazepine-6(5H)-one	Ki	12590.0 [1], 12600.0 [2]
	3-Chloromethyl-5-methyl-8-chloro-4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-one	Ki	300.0 [1]
	Ethyl 8-ethoxy-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	36.0 [1]
	CID 10519948	Ki	7.2 [1]
	Tert-butyl 8-ethyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	56.0 [1]
	Ethyl 5-methyl-6-oxo-8-(3-trimethylsilylprop-1-ynyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	300.0 [1]
	Ethyl (7S)-11-oxo-14-(2-trimethylsilylethynyl)-2,4,10-triazatetracyclo[10.4.0.02,6.07,10]hexadeca-1(16),3,5,12,14-pentaene-5-carboxylate	Ki	60.0 [1]
	Ethyl 5-methyl-6-oxo-8-prop-1-ynyl-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	22.2 [1]
	3-(2-Hydroxyethylthio)-6,6-dimethyl-1-(1H-pyrazole-3-yl)-6,7-dihydrobenzo[c]thiophene-4(5H)-one	Ki	21.0 [1]
	3-(Isopropylthio)-6,6-dimethyl-1-(1H-pyrazole-3-yl)-6,7-dihydrobenzo[c]thiophene-4(5H)-one	Ki	12.0 [1]
	3-(Ethylthio)-6,6-dimethyl-1-(1H-pyrazole-3-yl)-6,7-dihydrobenzo[c]thiophene-4(5H)-one	Ki	16.0 [1]
	4-Methoxymethyl-9H-beta-carboline-3-carboxylic acid ethyl ester	Ki	2.79 [1], 2.8 [2]
	4-Ethyl-6,7-dimethoxy-9H-beta-carboline-3-carboxylic acid ethyl ester	Ki	18.7 [1]
	6-Benzyloxy-4-ethyl-9H-beta-carboline-3-carboxylic acid ethyl ester	Ki	78.3 [1]
	6,6-Dimethyl-3-(methylthio)-1-(1H-pyrazol-3-yl)-6,7-dihydrobenzo[c]thiophen-4(5H)-one	Ki	56.0 [1]
	3-Hydroxymethyl-5-methyl-8-chloro-4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-one	Ki	300.0 [1]
	3-Ethoxymethyl-5-methyl-8-chloro-4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-one	Ki	300.0 [1]
	Tert-butyl 8-isothiocyanato-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	33.7 [1]
	(7S)-15-Ethynyl-5-(3-methyl-1,2,4-oxadiazol-5-yl)-2,4,11-triazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(17),3,5,13,15-pentaen-12-one	Ki	70.0 [1]
	Ethyl (7S)-14-bromo-11-oxo-2,4,10-triazatetracyclo[10.4.0.02,6.07,10]hexadeca-1(16),3,5,12,14-pentaene-5-carboxylate	Ki	13.0 [1]
	Ethyl (7R)-15-bromo-12-oxo-2,4,11-triazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(17),3,5,13,15-pentaene-5-carboxylate	Ki	1000.0 [1]
	4-Methoxymethyl-6-propoxy-9H-beta-carbolin-3-ylamine	Ki	540.0 [1]
	Tert-butyl 5-methyl-6-oxo-8-(3-trimethylsilylprop-1-ynyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	387.0 [1]
	Ethyl 8-ethenyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	10.2 [1]
	(7S)-14-Ethynyl-5-(3-methyl-1,2,4-oxadiazol-5-yl)-2,4,10-triazatetracyclo[10.4.0.02,6.07,10]hexadeca-1(16),3,5,12,14-pentaen-11-one	Ki	56.0 [1]
	Ethyl (7R)-15-ethynyl-12-oxo-2,4,11-triazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(17),3,5,13,15-pentaene-5-carboxylate	Ki	318.0 [1]
	(7R)-15-Ethynyl-5-(3-methyl-1,2,4-oxadiazol-5-yl)-2,4,11-triazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(17),3,5,13,15-pentaen-12-one	Ki	1000.0 [1]
	Ethyl 8-cyano-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	45.0 [1]
	(7S)-5-(3-Ethyl-1,2,4-oxadiazol-5-yl)-14-ethynyl-2,4,10-triazatetracyclo[10.4.0.02,6.07,10]hexadeca-1(16),3,5,12,14-pentaen-11-one	Ki	150.0 [1]
	4-Methoxymethyl-6-octyloxy-9H-beta-carboline-3-carboxylic acid ethyl ester	Ki	3000.0 [1]
	4-Methoxymethyl-3,6-dipropoxy-9H-beta-carboline	Ki	214.0 [1]
	4-Ethyl-6-octyloxy-9H-beta-carboline-3-carboxylic acid ethyl ester	Ki	29700.0 [1]
	Ethyl 8-bromo-5-methyl-6-oxo-5,6-dihydro-4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxylate	Ki	27.0 [1]
	4-Methoxymethyl-9-methyl-6-octyloxy-9H-beta-carboline-3-carboxylic acid ethyl ester	Ki	3000.0 [1]
	Ethyl (7R)-12-oxo-15-(2-trimethylsilylethynyl)-2,4,11-triazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(17),3,5,13,15-pentaene-5-carboxylate	Ki	1000.0 [1]
	(7S)-15-Ethynyl-5-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)-2,4,11-triazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(17),3,5,13,15-pentaen-12-one	Ki	85.0 [1]
	(7S)-5-(3-Ethyl-1,2,4-oxadiazol-5-yl)-15-ethynyl-2,4,11-triazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(17),3,5,13,15-pentaen-12-one	Ki	40.0 [1]
	Ethyl (7S)-14-ethynyl-11-oxo-2,4,10-triazatetracyclo[10.4.0.02,6.07,10]hexadeca-1(16),3,5,12,14-pentaene-5-carboxylate	Ki	12.0 [1]
	1-(2-Pyridyl)-3-(2-hydroxyethylthio)-6,6-dimethyl-6,7-dihydrobenzo[c]thiophene-4(5H)-one	Ki	5.2 [1]
	1-(4-Pyridyl)-3-(methylthio)-6,6-dimethyl-6,7-dihydrobenzo[c]thiophene-4(5H)-one	Ki	43.0 [1]
	1-(2-Pyridyl)-3-(methylthio)-6,6-dimethyl-6,7-dihydrobenzo[c]thiophene-4(5H)-one	Ki	26.0 [1]
	1-(3-Pyridyl)-3-(methylthio)-6,6-dimethyl-6,7-dihydrobenzo[c]thiophene-4(5H)-one	Ki	31.0 [1]
	5-Methyl-3-[9-[(6-methylpyridin-2-yl)methoxy]-4,5,7,8-tetrazatetracyclo[9.2.2.02,10.03,7]pentadeca-2(10),3,5,8-tetraen-6-yl]-1,2-oxazole	Ki	86.0 [1]
	1-(2-Thiazolyl)-3-(methylthio)-6,6-dimethyl-6,7-dihydrobenzo[c]thiophene-4(5H)-one	Ki	44.0 [1]
	9-[(1-Methyl-1,2,4-triazol-3-yl)methoxy]-6-phenyl-4,5,7,8-tetrazatetracyclo[9.2.2.02,10.03,7]pentadeca-2(10),3,5,8-tetraene	Ki	16.0 [1], 16.3 [2]
	5-Methyl-3-[6-[(6-methylpyridin-2-yl)methoxy]-[1,2,4]triazolo[3,4-a]phthalazin-3-yl]-1,2-oxazole	Ki	1.6 [1]
	9-[(6-Methylpyridin-2-yl)methoxy]-6-thiophen-3-yl-4,5,7,8-tetrazatetracyclo[9.2.2.02,10.03,7]pentadeca-2(10),3,5,8-tetraene	Ki	110.0 [1]
	6-(Furan-3-yl)-9-[(6-methylpyridin-2-yl)methoxy]-4,5,7,8-tetrazatetracyclo[9.2.2.02,10.03,7]pentadeca-2(10),3,5,8-tetraene	Ki	63.0 [1]
	6-(6-Methylpyridin-2-yl)methyloxy-3-phenyl-1,2,4-triazolo[3,4-a]phthalazine	Ki	1.0 [1], 8.0 [2]

Entire TableStructureCompound NameStandard TypeStandard Values (in nM)

Items per page: 510All1 - 10 of 99 ⟨⟩

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References

This online tool may be cited as follows

MLA	"Quest Database™ GABA-A receptor; alpha-2/beta-3/gamma-2 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 20 Feb. 2025, https://www.aatbio.com/data-sets/gaba-a-receptor-alpha-2-beta-3-gamma-2-inhibitors-ic50-ki.
APA	AAT Bioquest, Inc. (2025, February 20). Quest Database™ GABA-A receptor; alpha-2/beta-3/gamma-2 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/gaba-a-receptor-alpha-2-beta-3-gamma-2-inhibitors-ic50-ki.
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