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

Structure
▲
▼
Compound Name
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▼
Standard Type
▲
▼
Standard Values (in nM)
▲
▼
DiazepamKi12.0 [1], 13.0 [2]
GabazineIC50240.0 [1], 349.0 [2]
Ethyl-8-azido-5,6-dihydro-5-methyl-6-oxo-4H-imidazo-1,4-benzodiazepine-3-carboxylateKi3.3 [1], 15.0 [2]
FlunitrazepamKi3.9 [1]
ZolpidemIC5010000.0 [1]
EtomidateIC50577000.0 [1]
3-[(1S)-1-Phenylethyl]-4-imidazolecarboxylic acid ethyl esterIC50295000.0 [1]
AmentoflavoneIC50281838293.1 [1]
(3-Aminopropyl)(n-butyl)phosphinic acidIC50508000.0 [1]
Ethyl 8-chloro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylateKi6.8 [1]
5-(4-Piperidyl)isoxazol-3-olIC50501187.23 [1]
PanadiplonKi3.5 [1]
Ethyl 8-ethynyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi28.4 [1]
2-(3-Methyldiazirin-3-yl)ethyl 3-[(1R)-1-phenylethyl]imidazole-4-carboxylateIC50104000.0 [1]
Tert-butyl 8-ethynyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi26.9 [1]
4-(2-Naphthylmethyl)-5-(4-piperidinyl)isoxazole-3-olIC501819.7 [1]
1-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-(1H-indol-3-yl)ethane-1,2-dioneKi380.0 [1]
Tert-butyl 5-methyl-6-oxo-8-(2-trimethylsilylethynyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi197.0 [1]
Ethyl 5-methyl-6-oxo-8-(2-trimethylsilylethynyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi121.1 [1]
Tert-butyl 8-bromo-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi11.4 [1]
6-Ethyl-4-hydroxyquinoline-3-carboxylic acid ethyl esterKi5.9 [1]
Ethyl 8-ethyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi20.4 [1]
3-(5-Cyclopropyl-1,2,4-oxadiazol-3-yl)-N,N-dimethyl-4H-imidazo[1,5-a]quinoxaline-5-carboxamideKi1.7 [1]
CID 10519948Ki3.8 [1]
Tert-butyl 8-ethyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi14.8 [1]
Ethyl 5-methyl-6-oxo-8-(3-trimethylsilylprop-1-ynyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi300.0 [1]
Ethyl 5-methyl-6-oxo-8-prop-1-ynyl-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi10.1 [1]
6-Benzyl-3-ethoxycarbonyl-4-quinoloneKi0.27 [1]
4,5-Dihydro-3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-acetylimidazo[1,5-a]quinoxalineKi2.7 [1]
1-(1H-Indole-3-yl)-2-(isoindoline-2-yl)glyoxalKi200.0 [1]
4-(1-Hydroxypyrazol-4-yl)piperidineIC50500000.0 [1]
4,5-Dihydro-3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-benzoylimidazo[1,5-a]quinoxalineKi0.3 [1]
(3R)-N-Benzyl-1-[2-(1H-indol-3-yl)-2-oxoacetyl]-N-methylpiperidine-3-carboxamideKi7.3 [1]
[3-(5-Cyclopropyl-1,2,4-oxadiazol-3-yl)-6-methyl-4H-imidazo[1,5-a]quinoxalin-5-yl]-morpholin-4-ylmethanoneKi4.7 [1]
[7-Chloro-3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-4H-imidazo[1,5-a]quinoxalin-5-yl]-morpholin-4-ylmethanoneKi0.22 [1]
N-Ethyl-3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)imidazo[1,5-a]quinoxaline-5(4H)-carboxamideKi4.5 [1]
[3-(5-Cyclopropyl-1,2,4-oxadiazol-3-yl)-6-fluoro-4H-imidazo[1,5-a]quinoxalin-5-yl]-morpholin-4-ylmethanoneKi0.17 [1]
[3-(5-Cyclopropyl-1,2,4-oxadiazol-3-yl)-7-fluoro-4H-imidazo[1,5-a]quinoxalin-5-yl]-morpholin-4-ylmethanoneKi0.3 [1]
2-(3-Methyldiazirin-3-yl)ethyl 3-[(1S)-1-phenylethyl]imidazole-4-carboxylateIC5066260.0 [1]
6-Benzyl-3-pyridin-2-yl-1H-pyrazolo[1,5-a]pyrimidin-7-oneKi183.0 [1]
4-[1-Hydroxy-5-(2-phenyl-1H-imidazol-5-yl)pyrazol-4-yl]piperidineIC50690.0 [1]
4-[1-Hydroxy-3-(1H-imidazol-5-yl)pyrazol-4-yl]piperidineIC5030000.0 [1]
4-[1-Hydroxy-3-(2-phenyl-1H-imidazol-5-yl)pyrazol-4-yl]piperidineIC509700.0 [1]
1-[2-(1H-Indol-3-yl)-2-oxo-acetyl]-piperidine-3-carboxylic acid benzyl esterKi77.0 [1]
N-Benzyl-1-[2-(1H-indol-3-yl)-2-oxoacetyl]piperidine-3-carboxamideKi300.0 [1]
N-Benzyl-1-[2-(1H-indol-3-yl)-2-oxoacetyl]-N-methylpiperidine-3-carboxamideKi14.0 [1]
(3S)-N-Benzyl-1-[2-(1H-indol-3-yl)-2-oxoacetyl]-N-methylpiperidine-3-carboxamideKi140.0 [1]
4-(Biphenyl-3-yl)-5-(piperidin-4-yl)isoxazol-3-olIC5077.62 [1]
Ethyl 1-(2-(1H-indol-3-yl)-2-oxoacetyl)piperidine-3-carboxylateKi880.0 [1]
6-Benzyl-3-(2-cyclopentylacetyl)-1H-quinolin-4-oneKi0.51 [1]
3-(2-Cyclopentylacetyl)-6-(pyridin-3-ylmethyl)-1H-quinolin-4-oneKi0.88 [1]
1-[1,2-Dioxo-2-(1H-indole-3-yl)ethyl]pyrrolidine-2-acetic acid ethyl esterKi890.0 [1]
1-[1,2-Dioxo-2-(7-methoxy-1H-indole-3-yl)ethyl]pyrrolidine-2-acetic acid ethyl esterKi460.0 [1]
1-[1,2-Dioxo-2-(7-methyl-1H-indole-3-yl)ethyl]pyrrolidine-2-acetic acid ethyl esterKi510.0 [1]
1-(2-Benzyl-pyrrolidin-1-yl)-2-(1H-indol-3-yl)-ethane-1,2-dioneKi440.0 [1]
Diethyl (3S,5R)-1-[2-(1H-indol-3-yl)-2-oxoacetyl]piperidine-3,5-dicarboxylateKi14.0 [1]
Diethyl (3R,5R)-1-[2-(1H-indol-3-yl)-2-oxoacetyl]piperidine-3,5-dicarboxylateKi400.0 [1]
3-Pentanoyl-1H-quinolin-4-oneKi0.97 [1]
6-Benzyl-3-pentanoyl-1H-quinolin-4-oneKi0.12 [1]
6-Benzyl-3-butanoyl-1H-quinolin-4-oneKi0.12 [1]
3-Pentanoyl-6-(2-phenylethyl)-1H-quinolin-4-oneKi0.53 [1]
3-Pentanoyl-6-(3-phenylpropyl)-1H-quinolin-4-oneKi3.2 [1]
6-(Naphthalen-2-ylmethyl)-3-pentanoyl-1H-quinolin-4-oneKi2.7 [1]
3-Pentanoyl-6-(pyridin-4-ylmethyl)-1H-quinolin-4-oneKi0.39 [1]
3-Pentanoyl-6-(pyridin-3-ylmethyl)-1H-quinolin-4-oneKi0.12 [1]
3-Pentanoyl-6-(pyridin-2-ylmethyl)-1H-quinolin-4-oneKi0.14 [1]
2-Pentanoyl-5,6,7,8-tetrahydro-1H-quinolin-4-oneKi11.0 [1]
6-Ethyl-3-pentanoyl-1H-quinolin-4-oneKi0.38 [1]
3-(2-Cyclopentylacetyl)-6-ethyl-1H-quinolin-4-oneKi5.1 [1]
3-(1,1'-Biphenyl-3-yl)-4-(4-piperidinyl)-1H-pyrazole-1-olIC50210.0 [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;chlorideKi746.5 [1]
4-(1-Hydroxy-5-phenylpyrazol-4-yl)piperidine;hydrobromideIC50154.88 [1]
4-(1-Hydroxy-3-methylpyrazol-4-yl)piperidine;hydrobromideIC5066069.34 [1]
4-(1-Hydroxy-3-phenylpyrazol-4-yl)piperidine;hydrobromideIC501862.09 [1]
4-[1-Hydroxy-3-(4-methylphenyl)pyrazol-4-yl]piperidine;hydrobromideIC501412.54 [1]
4-[1-Hydroxy-3-(4-phenylphenyl)pyrazol-4-yl]piperidine;hydrobromideIC501412.54 [1]
4-[1-Hydroxy-3-(naphthalen-2-ylmethyl)pyrazol-4-yl]piperidine;hydrobromideIC50165.96 [1]
4-(1-Hydroxypyrazol-4-yl)piperidine;hydrochlorideIC50501187.23 [1]
4-[1-Hydroxy-5-(naphthalen-2-ylmethyl)pyrazol-4-yl]piperidine;hydrochlorideIC50794.33 [1]
4-[5-[(1-Bromonaphthalen-2-yl)methyl]-1-hydroxypyrazol-4-yl]piperidine;hydrochlorideIC50478.63 [1]
4-[1-Hydroxy-5-(3-phenylphenyl)pyrazol-4-yl]piperidine;hydrochlorideIC5023.99 [1]
4-[1-Hydroxy-3-(2-methylphenyl)pyrazol-4-yl]piperidine;hydrochlorideIC502630.27 [1]
4-[1-Hydroxy-3-(3-methylphenyl)pyrazol-4-yl]piperidine;hydrochlorideIC501905.46 [1]
4-[1-Hydroxy-3-(3-phenylphenyl)pyrazol-4-yl]piperidine;hydrochlorideIC50213.8 [1]
4-(3-Benzyl-1-hydroxypyrazol-4-yl)piperidine;hydrochlorideIC508317.64 [1]
4-[1-Hydroxy-5-(naphthalen-2-ylmethyl)-3-phenylpyrazol-4-yl]piperidine;hydrochlorideIC503162.28 [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]acetonitrileIC5025.0 [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-carbaldehydeIC50997.0 [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-carbaldehydeIC50770.0 [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]acetonitrileIC501020.0 [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]acetonitrileIC50501.0 [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]propanenitrileIC50629.0 [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]propanenitrileIC501840.0 [1]
3-Iodo-5-oxido-N-(pyridin-3-ylmethyl)pyrazolo[5,1-c][1,2,4]benzotriazin-5-ium-8-amineKi0.45 [1]
3-Methyl-5-oxido-8-(pyridin-4-ylmethoxy)pyrazolo[5,1-c][1,2,4]benzotriazin-5-iumKi22.7 [1]
3-(1-Benzyl-2-phenyl-1H-imidazole-4-yl)-4-(4-piperidinyl)-1H-pyrazole-1-olIC50210.0 [1]
4-[5-(1-Benzyl-2-phenylimidazol-4-yl)-1-hydroxypyrazol-4-yl]piperidineIC50780.0 [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]acetonitrileIC501200.0 [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]acetonitrileIC5028.0 [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]acetonitrileIC50544.0 [1]
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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., 20 Feb. 2025, https://www.aatbio.com/data-sets/gaba-a-receptor-alpha-1-beta-2-gamma-2-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 20). 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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