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GABA-A receptor; alpha-6/beta-3/gamma-2 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
Ethyl 8-ethynyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi28.8 [1]
Ethyl (7S)-15-methoxy-12-oxo-2,4,11-triazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(17),3,5,13,15-pentaene-5-carboxylateKi83.0 [1], 83.2 [2]
Tert-butyl 8-ethynyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi5.1 [1]
ZolpidemKi10000.0 [1]
Ethyl-8-azido-5,6-dihydro-5-methyl-6-oxo-4H-imidazo-1,4-benzodiazepine-3-carboxylateKi3.8 [1]
Ethyl beta-carboline-3-carboxylateKi1000.0 [1], 2700.0 [2]
3-Methyl-6-[3-(trifluoromethyl)phenyl]-[1,2,4]triazolo[4,3-b]pyridazineKi10000.0 [1]
Tert-Butyl beta-carboline-3-carboxylateKi5000.0 [1]
3-Propoxy-9H-pyrido[3,4-b]indoleKi1000.0 [1]
3-Ethoxy-beta-carbolineKi1000.0 [1]
CID 9971547Ki300.0 [1], 9000.0 [2]
3-Butoxy-9H-beta-carbolineKi1000.0 [1]
3-Isobutoxy-9H-beta-carbolineKi10000.0 [1]
3-Benzyloxy-9H-beta-carbolineKi10000.0 [1]
3-(Isopentyloxy)-9H-pyrido[3,4-b]indoleKi10000.0 [1]
Tert-butyl 5-methyl-6-oxo-8-(2-trimethylsilylethynyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi58.6 [1]
Ethyl 5-methyl-6-oxo-8-(2-trimethylsilylethynyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi113.7 [1], 114.0 [2]
CID 5255267Ki2000.0 [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-carboxylateKi125.0 [1], 126.0 [2]
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-carboxylateKi340.0 [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-carboxylateKi46.0 [1]
FlumazenilKi148.0 [1]
FlunitrazepamKi2000.0 [1]
Methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylateKi134.0 [1]
AbecarnilKi1000.0 [1], 10000.0 [2]
Ethyl 8-chloro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylateKi54.6 [1]
6-Benzyloxy-4-methoxymethyl-beta-carboline-3-carboxylic acid ethyl esterKi1000.0 [1]
3-Isopropoxy-9H-beta-carbolineKi10000.0 [1]
Tert-Butyl 8-chloro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylateKi4.0 [1]
6-Methoxy-4-methoxymethyl-9H-beta-carboline-3-carboxylic acid ethyl esterKi479.0 [1], 10000.0 [2]
6-Propoxy-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl esterKi1340.0 [1], 1343.0 [2]
Cyclopropylmethyl 8-chloro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi168.0 [1]
5-Methyl-8-chloro-3-acetyl-4H-imidazo[1,5-a][1,4]benzodiazepine-6(5H)-oneKi29500.0 [1]
8-Chloro-2-(4-methoxy-phenyl)-2,5-dihydro-pyrazolo[4,3-c]quinolin-3-oneKi1.9 [1]
Tert-butyl 8-bromo-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi9.4 [1]
3-Ethyl-5-methyl-8-chloro-4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-oneKi3648.0 [1], 3650.0 [2]
3-Pentanoyl-5-methyl-8-chloro-4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-oneKi2930.0 [1]
Tert-butyl 5-methyl-8-nitro-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi22.5 [1]
Ethyl 8-ethyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi176.0 [1]
Tert-butyl 8-iodo-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi4.6 [1]
3-Pentyl-5-methyl-8-chloro-4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-oneKi960.0 [1]
Tert-butyl 8-azido-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi5.25 [1]
5-Methyl-8-chloro-3-[(diethylamino)methyl]-4H-imidazo[1,5-a][1,4]benzodiazepine-6(5H)-oneKi30160.0 [1], 30200.0 [2]
5-Methyl-8-chloro-3-[(diisopropylamino)methyl]-4H-imidazo[1,5-a][1,4]benzodiazepine-6(5H)-oneKi8600.0 [1]
3-Chloromethyl-5-methyl-8-chloro-4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-oneKi300.0 [1]
Ethyl 8-ethoxy-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi51.5 [1]
CID 10519948Ki44.3 [1]
Tert-butyl 8-ethyl-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi22.9 [1]
Ethyl 5-methyl-6-oxo-8-(3-trimethylsilylprop-1-ynyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi300.0 [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-carboxylateKi180.0 [1]
Ethyl 5-methyl-6-oxo-8-prop-1-ynyl-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi100.0 [1]
4-Methoxymethyl-9H-beta-carboline-3-carboxylic acid ethyl esterKi1150.0 [1]
4-Ethyl-6,7-dimethoxy-9H-beta-carboline-3-carboxylic acid ethyl esterKi74.9 [1]
6-Benzyloxy-4-ethyl-9H-beta-carboline-3-carboxylic acid ethyl esterKi10000.0 [1]
3-Hydroxymethyl-5-methyl-8-chloro-4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-oneKi300.0 [1]
3-Ethoxymethyl-5-methyl-8-chloro-4,5-dihydro-6H-imidazo[1,5-a][1,4]benzodiazepin-6-oneKi300.0 [1]
Tert-butyl 8-isothiocyanato-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi30.7 [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-oneKi301.0 [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-carboxylateKi31.0 [1]
Tert-butyl 5-methyl-6-oxo-8-pyrrolidin-1-yl-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi325.0 [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-carboxylateKi1000.0 [1]
4-Methoxymethyl-6-propoxy-9H-beta-carbolin-3-ylamineKi3000.0 [1]
Tert-butyl 5-methyl-6-oxo-8-(3-trimethylsilylprop-1-ynyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi301.0 [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-oneKi266.0 [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-carboxylateKi61.0 [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-oneKi1000.0 [1]
Ethyl 8-cyano-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi1000.0 [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-oneKi361.0 [1]
4-Methoxymethyl-6-octyloxy-9H-beta-carboline-3-carboxylic acid ethyl esterKi3000.0 [1]
4-Methoxymethyl-3,6-dipropoxy-9H-beta-carbolineKi1000.0 [1], 10000.0 [2]
4-Ethyl-6-octyloxy-9H-beta-carboline-3-carboxylic acid ethyl esterKi30000.0 [1]
Ethyl 8-bromo-5-methyl-6-oxo-5,6-dihydro-4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxylateKi22.0 [1]
4-Methoxymethyl-9-methyl-6-octyloxy-9H-beta-carboline-3-carboxylic acid ethyl esterKi3000.0 [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-carboxylateKi1000.0 [1]
Tert-butyl 8-hydroxy-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi6.89 [1]
Tert-butyl 8-methoxy-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi8.28 [1]
Tert-butyl 8-(dimethylamino)-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi118.0 [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-oneKi333.0 [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-oneKi150.0 [1]
Tert-butyl 5-methyl-6-oxo-8-piperidin-1-yl-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylateKi247.0 [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-carboxylateKi42.0 [1]
(7S)-14-Ethynyl-5-(3-propan-2-yl-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-oneKi267.0 [1]
3-Ethoxy-4-ethyl-6,7-dimethoxy-9H-beta-carbolineKi300.0 [1]
4-Ethyl-3,6,7-trimethoxy-9H-beta-carbolineKi300.0 [1]
4-Ethyl-9-methyl-9H-beta-carboline-3-carboxylic acid ethyl esterKi10000.0 [1]
DiazepamKi3000.0 [1]
LindaneIC504.9 [1]
TriazolamKi10000.0 [1]
FipronilIC5017.0 [1]
BretazenilKi12.7 [1]
2-Phenyl-3aH-pyrazolo[4,3-c]quinolin-3-oneKi17.0 [1]
4H-Imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylic acid, 5,6-dihydro-5-methyl-6-oxo-, ethyl esterKi300.0 [1]
3-[3-Tert-butyl-2-[(2-methyl-1,2,4-triazol-3-yl)methoxy]pyrazolo[1,5-d][1,2,4]triazin-7-yl]-5-methyl-1,2-oxazoleKi4000.0 [1]
1,3-Dihydro-5-phenyl-2H-1,4-benzodiazepin-2-oneKi3000.0 [1]
7-Chloro-5-methyl-3-(5-propan-2-yl-1,2,4-oxadiazol-3-yl)-4H-imidazo[1,5-a][1,4]benzodiazepin-6-oneKi227.0 [1]
7,12-Dihydro-5,7,12-triaza-indeno[1,2-a]fluoreneKi1000.0 [1]
1-Methyl-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-oneKi3000.0 [1]
3-Chloro-9H-beta-carbolineKi10000.0 [1]
1H-1,4-Benzodiazepine-7-carbonitrile, 2,3-dihydro-1-methyl-2-oxo-5-phenyl-Ki3000.0 [1]
1-(9H-beta-Carbolin-3-yl)-butan-1-oneKi3000.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ GABA-A receptor; alpha-6/beta-3/gamma-2 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Dec2024https://www.aatbio.com/data-sets/gaba-a-receptor-alpha-6-beta-3-gamma-2-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 21). Quest Database™ GABA-A receptor; alpha-6/beta-3/gamma-2 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/gaba-a-receptor-alpha-6-beta-3-gamma-2-inhibitors-ic50-ki.
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