GABA-A receptor; anion channel Inhibitors (IC50, Ki)

Structure ▲ ▼	Compound Name ▲ ▼	Standard Type ▲ ▼	Standard Values (in nM) ▲ ▼
	Diazepam	IC50	12.0 [1]
	Diazepam	Ki	10.0 [1]
	4-Butyl-3-[(3-chlorophenyl)methyl]-1H-1,2,4-triazole-5-thione	IC50	370.0 [1], 467.0 [2], 567.0 [3]
	4-Butyl-3-[(3-chlorophenyl)methyl]-1H-1,2,4-triazole-5-thione	Ki	88.0 [1], 93.3 [2], 113.0 [3]
	3-[(3-Chlorophenyl)methyl]-4-hexyl-1H-1,2,4-triazole-5-thione	IC50	361.0 [1], 535.0 [2], 626.0 [3]
	3-[(3-Chlorophenyl)methyl]-4-hexyl-1H-1,2,4-triazole-5-thione	Ki	116.7 [1], 126.0 [2], 149.0 [3]
	Muscimol	IC50	2.0 [1], 16.0 [2], 135.0 [3]
	Muscimol	Ki	6.0 [1], 11.0 [2]
	(4S)-4-Amino-2-pentenoic acid	IC50	2500.0 [1], 2600.0 [2], 3500.0 [3], 4100.0 [4], 21000.0 [5]
	(E,4R)-4-Aminopent-2-enoic acid	IC50	84000.0 [1], 88000.0 [2], 145000.0 [3], 148000.0 [4], 670000.0 [5]
	5-[(R)-1-Aminoethyl]isoxazol-3-ol	IC50	8200.0 [1], 8900.0 [2], 9500.0 [3], 19000.0 [4], 83000.0 [5]
	5-[(S)-1-Aminoethyl]isoxazol-3-ol	IC50	510.0 [1], 640.0 [2], 740.0 [3], 1600.0 [4], 5800.0 [5]
	(R)-4-Aminopentanoic acid	IC50	2500.0 [1], 4300.0 [2], 5000.0 [3], 6100.0 [4], 21000.0 [5]
	(S)-4-Aminovaleric acid	IC50	2500.0 [1], 2900.0 [2], 4700.0 [3], 5200.0 [4], 24000.0 [5]
	gamma-Aminobutyric acid	IC50	25.0 [1], 1450.0 [2]
	gamma-Aminobutyric acid	Ki	33.0 [1], 200.0 [2]
	Bicuculline	IC50	6200.0 [1], 15000.0 [2], 44000.0 [3]
	Olanzapine	Ki	10000.0 [1]
	Flumazenil	Ki	0.9 [1]
	Clonazepam	IC50	555904257.3 [1]
	Clonazepam	Ki	0.85 [1]
	Flavone	Ki	17.0 [1], 1000.0 [2]
	Gabazine	IC50	8.0 [1], 140.0 [2]
	Amentoflavone	Ki	6.0 [1]
	Delorazepam	IC50	2.8 [1], 555904257.3 [2]
	N-Desmethylolanzapine	Ki	10000.0 [1]
	7-Chloro-5-(2,6-dichlorophenyl)-1-methyl-1H-benzo[e][1,4]diazepin-2(3H)-one	IC50	7.0 [1], 181970085.9 [2]
	7-Chloro-5-(2,6-dichlorophenyl)-1,3-dihydro-1,4-benzodiazepin-2-one	IC50	5.5 [1], 142889395.9 [2]
	2-Hydroxymethyl Olanzapine	Ki	1000.0 [1], 10000.0 [2]
	5-[[3-(1,3-Benzodioxol-5-yl)-6-iminopyridazin-1-yl]methyl]-1,2-thiazol-3-one;hydrobromide	IC50	0.76 [1], 17.0 [2]
	(5Ar,7R,9aS,11aS)-2-amino-7-hydroxy-9a,11a-dimethyl-3,3a,3b,4,5,5a,6,7,8,9,9b,11-dodecahydronaphtho[2,1-e]indol-10-one	IC50	3.0 [1], 43.0 [2]
	5-[(6-Imino-3-methyl-5-phenylpyridazin-1-yl)methyl]-1,2-thiazol-3-one;hydrobromide	IC50	1000.0 [1], 6600.0 [2]
	5-[[6-(4-Chlorophenyl)-3-iminopyridazin-2(3H)-yl]methyl]isoxazol-3-ol	IC50	80.0 [1], 1200.0 [2]
	5-[[4-Phenyl-1-iminophthalazin-2(1H)-yl]methyl]isoxazol-3-ol	IC50	120.0 [1], 190.0 [2]
	5-[[6-(4-Chlorophenyl)-3-iminopyridazin-2(3H)-yl]methyl]isothiazol-3-ol	IC50	29.0 [1], 150.0 [2]
	5-[[4-Phenyl-1-iminophthalazin-2(1H)-yl]methyl]isothiazol-3-ol	IC50	25.0 [1], 160.0 [2]
	[2-(5-Imidazo[4,5-b]pyridin-3-yl-1H-indol-3-yl)-ethyl]-dimethyl-amine	IC50	89.0 [1]
	Olanzapine N-Oxide	Ki	10000.0 [1]
	4-Amino-2,9-dimethyl-9H-pyrido[2,3-b]indole-3-carboxylic acid methyl ester	IC50	2000.0 [1], 14600.0 [2]
	Propyl 4-amino-2,9-dimethylpyrido[2,3-b]indole-3-carboxylate	IC50	2000.0 [1], 2200.0 [2]
	4-Amino-2,9-dimethyl-9H-pyrido[2,3-b]indole-3-carboxylic acid, ethyl ester	IC50	2000.0 [1], 4600.0 [2]
	1-[3-[[(2R)-1-Methylpyrrolidin-2-yl]methyl]-1H-indol-5-yl]benzimidazole-5-carbonitrile	IC50	2.8 [1], 3.3 [2]
	5-[[6-(1,3-Benzodioxol-5-yl)-3-iminopyridazin-2(3H)-yl]methyl]isoxazol-3-ol	IC50	6.0 [1], 75.0 [2]
	Cocaine	IC50	127000.0 [1]
	Liothyronine	IC50	23000.0 [1]
	Phenytoin	Ki	100000.0 [1]
	Sodium valproate	Ki	100000.0 [1]
	Tubocurarine chloride	IC50	58000.0 [1]
	Apigenin	Ki	3019.95 [1]
	Flunitrazepam	IC50	263026799.2 [1]
	Baicalein	Ki	5623.41 [1]
	Allopregnanolone	IC50	22.0 [1]
	Baicalin	Ki	77624.71 [1]
	Fipronil	IC50	2.3 [1]
	Chrysin	Ki	3019.95 [1]
	Nitrazepam	IC50	100000000.0 [1]
	Temazepam	IC50	62517269.28 [1]
	Zafirlukast	IC50	10000.0 [1]
	Wogonin	Ki	2041.74 [1]
	9H-Pyrido[3,4-B]indole	IC50	1621.81 [1]
	Harman	IC50	12302.69 [1]
	Nordazepam	IC50	106414301.8 [1]
	Isoguvacine	Ki	55.0 [1]
	Ethyl beta-carboline-3-carboxylate	IC50	5.01 [1]
	Progabide	Ki	40000.0 [1]
	Scutellarein	Ki	12022.64 [1]
	beta-Carboline-3-carboxylic acid methyl ester	IC50	5.01 [1]
	Hispidulin	Ki	1000.0 [1]
	Ganaxolone	IC50	42.0 [1]
	(3-Aminopropyl)(n-butyl)phosphinic acid	IC50	508000.0 [1]
	Bis(7)-Tacrine	IC50	6000.0 [1]
	Tert-Butyl beta-carboline-3-carboxylate	IC50	10.0 [1]
	Halazepam	IC50	10864256.24 [1]
	Isonipecotic acid	Ki	510.0 [1]
	7-Aminoflunitrazepam	IC50	15381546.4 [1]
	Meclonazepam	IC50	833681184.6 [1]
	2,5-Dihydro-2-(4-methoxyphenyl)-3H-pyrazolo(4,3-c)quinolin-3-one	IC50	0.1 [1]
	Norfludiazepam	IC50	500034535.0 [1]
	7-Aminoclonazepam	IC50	13335214.32 [1]
	Ctep	Ki	3160.0 [1]
	Sodium N-(alpha-(4-chlorophenyl)-5-fluoro-2-hydroxy-benzylidene)-4-aminobutyrate	Ki	680.0 [1]
	Basimglurant	Ki	3160.0 [1]
	3-Propoxy-9H-pyrido[3,4-b]indole	IC50	10.96 [1]
	2-Phenyl-3aH-pyrazolo[4,3-c]quinolin-3-one	IC50	0.4 [1]
	2-Aminonicotinic acid	Ki	100000.0 [1]
	2-(4-Chlorophenyl)-3aH-pyrazolo[4,3-c]quinolin-3-one	IC50	0.6 [1]
	6-Bromoflavone	Ki	70.79 [1]
	Naluzotan	Ki	2000.0 [1]
	Norflunitrazepam	IC50	666806769.2 [1]
	1-Ethyl-9H-pyrido[3,4-b]indole	IC50	251188.64 [1]
	(3R)-5-(2-Fluorophenyl)-3-(1H-indol-3-ylmethyl)-1-methyl-3H-1,4-benzodiazepin-2-one	IC50	100000.0 [1]
	1,3-Dihydro-5-phenyl-2H-1,4-benzodiazepin-2-one	IC50	2857590.54 [1]
	7-Aminonitrazepam	IC50	2588212.92 [1]
	5-(2-Chlorophenyl)-1,3-dihydro-1-methyl-7-nitro-2H-1,4-benzodiazepin-2-one	IC50	454988060.2 [1]
	3-Ethoxy-beta-carboline	IC50	23.99 [1]
	Pitrazepin	IC50	240.0 [1]
	6-Aminonicotinic acid	Ki	4400.0 [1]
	4'-Fluoroflavone	Ki	3630.78 [1]
	N-Benzyl-2-(1H-indol-3-yl)-2-oxoacetamide	Ki	120.23 [1]
	3-(N-Methylpyrrolidin-2-ylmethyl)-5-(3-nitropyrid-2-ylamino)-1H-indole	IC50	9600.0 [1]

Entire TableStructureCompound NameStandard TypeStandard Values (in nM)

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References

This online tool may be cited as follows

MLA	"Quest Database™ GABA-A receptor; anion channel Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 31 Mar. 2025, https://www.aatbio.com/data-sets/gaba-a-receptor-anion-channel-inhibitors-ic50-ki.
APA	AAT Bioquest, Inc. (2025, March 31). Quest Database™ GABA-A receptor; anion channel Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/gaba-a-receptor-anion-channel-inhibitors-ic50-ki.
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