GABA-A receptor; alpha-1/beta-2/gamma-2 Inhibitors (IC50, Ki)

Structure ▲ ▼	Compound Name ▲ ▼	Standard Type ▲ ▼	Standard Values (in nM) ▲ ▼
	Diazepam	Ki	12.0 [1], 13.0 [2]
	Gabazine	IC50	240.0 [1], 349.0 [2]
	Ethyl-8-azido-5,6-dihydro-5-methyl-6-oxo-4H-imidazo-1,4-benzodiazepine-3-carboxylate	Ki	3.3 [1], 15.0 [2]
	Flunitrazepam	Ki	3.9 [1]
	Zolpidem	IC50	10000.0 [1]
	Etomidate	IC50	577000.0 [1]
	3-[(1S)-1-Phenylethyl]-4-imidazolecarboxylic acid ethyl ester	IC50	295000.0 [1]
	Amentoflavone	IC50	281838293.1 [1]
	(3-Aminopropyl)(n-butyl)phosphinic acid	IC50	508000.0 [1]
	Ethyl 8-chloro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylate	Ki	6.8 [1]
	5-(4-Piperidyl)isoxazol-3-ol	IC50	501187.23 [1]
	Panadiplon	Ki	3.5 [1]
	Ethyl 8-ethynyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	28.4 [1]
	2-(3-Methyldiazirin-3-yl)ethyl 3-[(1R)-1-phenylethyl]imidazole-4-carboxylate	IC50	104000.0 [1]
	Tert-butyl 8-ethynyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	26.9 [1]
	4-(2-Naphthylmethyl)-5-(4-piperidinyl)isoxazole-3-ol	IC50	1819.7 [1]
	1-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-(1H-indol-3-yl)ethane-1,2-dione	Ki	380.0 [1]
	Tert-butyl 5-methyl-6-oxo-8-(2-trimethylsilylethynyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	197.0 [1]
	Ethyl 5-methyl-6-oxo-8-(2-trimethylsilylethynyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	121.1 [1]
	Tert-butyl 8-bromo-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	11.4 [1]
	6-Ethyl-4-hydroxyquinoline-3-carboxylic acid ethyl ester	Ki	5.9 [1]
	Ethyl 8-ethyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	20.4 [1]
	3-(5-Cyclopropyl-1,2,4-oxadiazol-3-yl)-N,N-dimethyl-4H-imidazo[1,5-a]quinoxaline-5-carboxamide	Ki	1.7 [1]
	CID 10519948	Ki	3.8 [1]
	Tert-butyl 8-ethyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	14.8 [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 5-methyl-6-oxo-8-prop-1-ynyl-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate	Ki	10.1 [1]
	6-Benzyl-3-ethoxycarbonyl-4-quinolone	Ki	0.27 [1]
	4,5-Dihydro-3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-acetylimidazo[1,5-a]quinoxaline	Ki	2.7 [1]
	1-(1H-Indole-3-yl)-2-(isoindoline-2-yl)glyoxal	Ki	200.0 [1]
	4-(1-Hydroxypyrazol-4-yl)piperidine	IC50	500000.0 [1]
	4,5-Dihydro-3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-benzoylimidazo[1,5-a]quinoxaline	Ki	0.3 [1]
	(3R)-N-Benzyl-1-[2-(1H-indol-3-yl)-2-oxoacetyl]-N-methylpiperidine-3-carboxamide	Ki	7.3 [1]
	[3-(5-Cyclopropyl-1,2,4-oxadiazol-3-yl)-6-methyl-4H-imidazo[1,5-a]quinoxalin-5-yl]-morpholin-4-ylmethanone	Ki	4.7 [1]
	[7-Chloro-3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-4H-imidazo[1,5-a]quinoxalin-5-yl]-morpholin-4-ylmethanone	Ki	0.22 [1]
	N-Ethyl-3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)imidazo[1,5-a]quinoxaline-5(4H)-carboxamide	Ki	4.5 [1]
	[3-(5-Cyclopropyl-1,2,4-oxadiazol-3-yl)-6-fluoro-4H-imidazo[1,5-a]quinoxalin-5-yl]-morpholin-4-ylmethanone	Ki	0.17 [1]
	[3-(5-Cyclopropyl-1,2,4-oxadiazol-3-yl)-7-fluoro-4H-imidazo[1,5-a]quinoxalin-5-yl]-morpholin-4-ylmethanone	Ki	0.3 [1]
	2-(3-Methyldiazirin-3-yl)ethyl 3-[(1S)-1-phenylethyl]imidazole-4-carboxylate	IC50	66260.0 [1]
	6-Benzyl-3-pyridin-2-yl-1H-pyrazolo[1,5-a]pyrimidin-7-one	Ki	183.0 [1]
	4-[1-Hydroxy-5-(2-phenyl-1H-imidazol-5-yl)pyrazol-4-yl]piperidine	IC50	690.0 [1]
	4-[1-Hydroxy-3-(1H-imidazol-5-yl)pyrazol-4-yl]piperidine	IC50	30000.0 [1]
	4-[1-Hydroxy-3-(2-phenyl-1H-imidazol-5-yl)pyrazol-4-yl]piperidine	IC50	9700.0 [1]
	1-[2-(1H-Indol-3-yl)-2-oxo-acetyl]-piperidine-3-carboxylic acid benzyl ester	Ki	77.0 [1]
	N-Benzyl-1-[2-(1H-indol-3-yl)-2-oxoacetyl]piperidine-3-carboxamide	Ki	300.0 [1]
	N-Benzyl-1-[2-(1H-indol-3-yl)-2-oxoacetyl]-N-methylpiperidine-3-carboxamide	Ki	14.0 [1]
	(3S)-N-Benzyl-1-[2-(1H-indol-3-yl)-2-oxoacetyl]-N-methylpiperidine-3-carboxamide	Ki	140.0 [1]
	4-(Biphenyl-3-yl)-5-(piperidin-4-yl)isoxazol-3-ol	IC50	77.62 [1]
	Ethyl 1-(2-(1H-indol-3-yl)-2-oxoacetyl)piperidine-3-carboxylate	Ki	880.0 [1]
	6-Benzyl-3-(2-cyclopentylacetyl)-1H-quinolin-4-one	Ki	0.51 [1]
	3-(2-Cyclopentylacetyl)-6-(pyridin-3-ylmethyl)-1H-quinolin-4-one	Ki	0.88 [1]
	1-[1,2-Dioxo-2-(1H-indole-3-yl)ethyl]pyrrolidine-2-acetic acid ethyl ester	Ki	890.0 [1]
	1-[1,2-Dioxo-2-(7-methoxy-1H-indole-3-yl)ethyl]pyrrolidine-2-acetic acid ethyl ester	Ki	460.0 [1]
	1-[1,2-Dioxo-2-(7-methyl-1H-indole-3-yl)ethyl]pyrrolidine-2-acetic acid ethyl ester	Ki	510.0 [1]
	1-(2-Benzyl-pyrrolidin-1-yl)-2-(1H-indol-3-yl)-ethane-1,2-dione	Ki	440.0 [1]
	Diethyl (3S,5R)-1-[2-(1H-indol-3-yl)-2-oxoacetyl]piperidine-3,5-dicarboxylate	Ki	14.0 [1]
	Diethyl (3R,5R)-1-[2-(1H-indol-3-yl)-2-oxoacetyl]piperidine-3,5-dicarboxylate	Ki	400.0 [1]
	3-Pentanoyl-1H-quinolin-4-one	Ki	0.97 [1]
	6-Benzyl-3-pentanoyl-1H-quinolin-4-one	Ki	0.12 [1]
	6-Benzyl-3-butanoyl-1H-quinolin-4-one	Ki	0.12 [1]
	3-Pentanoyl-6-(2-phenylethyl)-1H-quinolin-4-one	Ki	0.53 [1]
	3-Pentanoyl-6-(3-phenylpropyl)-1H-quinolin-4-one	Ki	3.2 [1]
	6-(Naphthalen-2-ylmethyl)-3-pentanoyl-1H-quinolin-4-one	Ki	2.7 [1]
	3-Pentanoyl-6-(pyridin-4-ylmethyl)-1H-quinolin-4-one	Ki	0.39 [1]
	3-Pentanoyl-6-(pyridin-3-ylmethyl)-1H-quinolin-4-one	Ki	0.12 [1]
	3-Pentanoyl-6-(pyridin-2-ylmethyl)-1H-quinolin-4-one	Ki	0.14 [1]
	2-Pentanoyl-5,6,7,8-tetrahydro-1H-quinolin-4-one	Ki	11.0 [1]
	6-Ethyl-3-pentanoyl-1H-quinolin-4-one	Ki	0.38 [1]
	3-(2-Cyclopentylacetyl)-6-ethyl-1H-quinolin-4-one	Ki	5.1 [1]
	3-(1,1'-Biphenyl-3-yl)-4-(4-piperidinyl)-1H-pyrazole-1-ol	IC50	210.0 [1]
	15-Methoxy-12-oxa-9-aza-3-azoniatetracyclo[9.7.0.03,8.013,18]octadeca-1(11),3,5,7,13(18),14,16-heptaen-10-one;chloride	Ki	746.5 [1]
	4-(1-Hydroxy-5-phenylpyrazol-4-yl)piperidine;hydrobromide	IC50	154.88 [1]
	4-(1-Hydroxy-3-methylpyrazol-4-yl)piperidine;hydrobromide	IC50	66069.34 [1]
	4-(1-Hydroxy-3-phenylpyrazol-4-yl)piperidine;hydrobromide	IC50	1862.09 [1]
	4-[1-Hydroxy-3-(4-methylphenyl)pyrazol-4-yl]piperidine;hydrobromide	IC50	1412.54 [1]
	4-[1-Hydroxy-3-(4-phenylphenyl)pyrazol-4-yl]piperidine;hydrobromide	IC50	1412.54 [1]
	4-[1-Hydroxy-3-(naphthalen-2-ylmethyl)pyrazol-4-yl]piperidine;hydrobromide	IC50	165.96 [1]
	4-(1-Hydroxypyrazol-4-yl)piperidine;hydrochloride	IC50	501187.23 [1]
	4-[1-Hydroxy-5-(naphthalen-2-ylmethyl)pyrazol-4-yl]piperidine;hydrochloride	IC50	794.33 [1]
	4-[5-[(1-Bromonaphthalen-2-yl)methyl]-1-hydroxypyrazol-4-yl]piperidine;hydrochloride	IC50	478.63 [1]
	4-[1-Hydroxy-5-(3-phenylphenyl)pyrazol-4-yl]piperidine;hydrochloride	IC50	23.99 [1]
	4-[1-Hydroxy-3-(2-methylphenyl)pyrazol-4-yl]piperidine;hydrochloride	IC50	2630.27 [1]
	4-[1-Hydroxy-3-(3-methylphenyl)pyrazol-4-yl]piperidine;hydrochloride	IC50	1905.46 [1]
	4-[1-Hydroxy-3-(3-phenylphenyl)pyrazol-4-yl]piperidine;hydrochloride	IC50	213.8 [1]
	4-(3-Benzyl-1-hydroxypyrazol-4-yl)piperidine;hydrochloride	IC50	8317.64 [1]
	4-[1-Hydroxy-5-(naphthalen-2-ylmethyl)-3-phenylpyrazol-4-yl]piperidine;hydrochloride	IC50	3162.28 [1]
	(2Z)-2-[(3R,5S,8S,9S,10S,13S,14S)-3-Hydroxy-10,13-dimethyl-11-oxo-2,3,4,5,6,7,8,9,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-17-ylidene]acetonitrile	IC50	25.0 [1]
	(3R,5S,8S,9S,10S,13S,14S)-3-Hydroxy-10,13-dimethyl-11-oxo-1,2,3,4,5,6,7,8,9,12,14,15-dodecahydrocyclopenta[a]phenanthrene-17-carbaldehyde	IC50	997.0 [1]
	(3R,5S,8S,9S,10S,13S,14S,17S)-3-Hydroxy-10,13-dimethyl-11-oxo-1,2,3,4,5,6,7,8,9,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-17-carbaldehyde	IC50	770.0 [1]
	2-[(3R,5S,8S,9S,10S,13R,14S,17R)-3-Hydroxy-10,13-dimethyl-11-oxo-1,2,3,4,5,6,7,8,9,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]acetonitrile	IC50	1020.0 [1]
	(2E)-2-[(3R,5S,8S,9S,10S,13S,14S)-3-Hydroxy-10,13-dimethyl-11-oxo-2,3,4,5,6,7,8,9,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-17-ylidene]acetonitrile	IC50	501.0 [1]
	(2Z)-2-[(3R,5S,8S,9S,10S,13S,14S)-3-Hydroxy-10,13-dimethyl-11-oxo-2,3,4,5,6,7,8,9,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-17-ylidene]propanenitrile	IC50	629.0 [1]
	(2E)-2-[(3R,5S,8S,9S,10S,13S,14S)-3-Hydroxy-10,13-dimethyl-11-oxo-2,3,4,5,6,7,8,9,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-17-ylidene]propanenitrile	IC50	1840.0 [1]
	3-Iodo-5-oxido-N-(pyridin-3-ylmethyl)pyrazolo[5,1-c][1,2,4]benzotriazin-5-ium-8-amine	Ki	0.45 [1]
	3-Methyl-5-oxido-8-(pyridin-4-ylmethoxy)pyrazolo[5,1-c][1,2,4]benzotriazin-5-ium	Ki	22.7 [1]
	3-(1-Benzyl-2-phenyl-1H-imidazole-4-yl)-4-(4-piperidinyl)-1H-pyrazole-1-ol	IC50	210.0 [1]
	4-[5-(1-Benzyl-2-phenylimidazol-4-yl)-1-hydroxypyrazol-4-yl]piperidine	IC50	780.0 [1]
	(2E)-2-[(3R,5R,8S,9S,10S,13S,14S)-3-Hydroxy-10,13-dimethyl-11-oxo-2,3,4,5,6,7,8,9,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-17-ylidene]acetonitrile	IC50	1200.0 [1]
	(2Z)-2-[(2S,3S,5S,8S,9S,10S,13S,14S)-3-Hydroxy-2-methoxy-10,13-dimethyl-11-oxo-2,3,4,5,6,7,8,9,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-17-ylidene]acetonitrile	IC50	28.0 [1]
	(2E)-2-[(2S,3S,5S,8S,9S,10S,13S,14S)-3-Hydroxy-2-methoxy-10,13-dimethyl-11-oxo-2,3,4,5,6,7,8,9,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-17-ylidene]acetonitrile	IC50	544.0 [1]

Entire TableStructureCompound NameStandard TypeStandard Values (in nM)

Items per page: 510All1 - 10 of 100 ⟨⟩

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References

This online tool may be cited as follows

MLA	"Quest Database™ GABA-A receptor; alpha-1/beta-2/gamma-2 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 8 May. 2024, https://www.aatbio.com/data-sets/gaba-a-receptor-alpha-1-beta-2-gamma-2-inhibitors-ic50-ki.
APA	AAT Bioquest, Inc. (2024, May 8). Quest Database™ GABA-A receptor; alpha-1/beta-2/gamma-2 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/gaba-a-receptor-alpha-1-beta-2-gamma-2-inhibitors-ic50-ki.
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