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Cytochrome P450 3A5 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
KetoconazoleIC50120.0 [1]
CYP3cideIC5017000.0 [1], 71000.0 [2]
TacrolimusKi2690.0 [1]
CID 78209992IC5050.0 [1]
E-NorendoxifenKi829.0 [1]
Mgl-3196IC5050000.0 [1]
1-[4-(4-Cyanophenyl)phenyl]-3-[4-(1H-imidazo[4,5-b]pyridin-7-yl)phenyl]ureaIC5033000.0 [1]
RelacorilantIC504900.0 [1]
2-((4'-Chlorobiphenyl-2-yl)methylsulfinyl)acetamideIC50159000.0 [1]
N-Propan-2-yl-3-[(4-pyridin-4-ylphenyl)carbamoylamino]benzamideIC50980.0 [1]
N-Propan-2-yl-3-[[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]carbamoylamino]benzamideIC5034000.0 [1]
3-[[4-(5-Methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]carbamoylamino]-N-propan-2-ylbenzamideIC5060000.0 [1]
2-[[2-(3,4-Dichlorophenoxy)phenyl]methylsulfinyl]acetamideIC5032000.0 [1]
[5-Ethylsulfonyl-2-[(2S)-1,1,1-trifluoropropan-2-yl]oxyphenyl]-[2-(2-fluorophenyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]methanoneIC5010000.0 [1]
[2-(4,4-Difluoropiperidin-1-yl)-5-methylsulfonylphenyl]-[2-(2-methylpyridin-4-yl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]methanoneIC5010000.0 [1]
[2-(2-Fluorophenyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]-[5-methylsulfonyl-2-[(2S)-1,1,1-trifluoropropan-2-yl]oxyphenyl]methanoneIC5010000.0 [1]
3-[2-(5-Fluoropyridin-3-yl)-4,6-dihydropyrrolo[3,4-c]pyrazole-5-carbonyl]-4-propan-2-yloxybenzonitrileIC5010000.0 [1]
[2-(5-Fluoropyridin-3-yl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]-[5-methylsulfonyl-2-[(2S)-1,1,1-trifluoropropan-2-yl]oxyphenyl]methanoneIC5010000.0 [1]
[5-Methylsulfonyl-2-[(2S)-1,1,1-trifluoropropan-2-yl]oxyphenyl]-(2-phenyl-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl)methanoneIC5010000.0 [1]
[2-(2-Fluorophenyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]-(5-methylsulfonyl-2-propan-2-yloxyphenyl)methanoneIC5010000.0 [1]
[2-(4,4-Difluoropiperidin-1-yl)-5-methylsulfonylphenyl]-[2-(5-fluoropyridin-3-yl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]methanoneIC5010000.0 [1]
[2-(3-Fluorophenyl)-5-methylsulfonylphenyl]-[2-(5-fluoropyridin-3-yl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]methanoneIC5010000.0 [1]
[2-(3-Methylphenyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]-[5-methylsulfonyl-2-[(2S)-1,1,1-trifluoropropan-2-yl]oxyphenyl]methanoneIC5010000.0 [1]
(2-Phenyl-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl)-[5-propan-2-ylsulfonyl-2-[(2S)-1,1,1-trifluoropropan-2-yl]oxyphenyl]methanoneIC5010000.0 [1]
[5-Ethylsulfonyl-2-[(2S)-1,1,1-trifluoropropan-2-yl]oxyphenyl]-[2-(2-methylpyridin-4-yl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]methanoneIC5010000.0 [1]
3-(2-Phenyl-4,6-dihydropyrrolo[3,4-c]pyrazole-5-carbonyl)-4-propan-2-yloxybenzonitrileIC5010000.0 [1]
4-(3-Fluorophenyl)-3-[2-(2-methylpyridin-4-yl)-4,6-dihydropyrrolo[3,4-c]pyrazole-5-carbonyl]benzonitrileIC5010000.0 [1]
4-(Cyclopropylmethoxy)-3-[2-(2-methylpyridin-4-yl)-4,6-dihydropyrrolo[3,4-c]pyrazole-5-carbonyl]benzonitrileIC5010000.0 [1]
[2-(3-Fluorophenyl)-5-methylsulfonylphenyl]-[2-(2-methylpyridin-4-yl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]methanoneIC5010000.0 [1]
[5-Ethylsulfonyl-2-[(2S)-1,1,1-trifluoropropan-2-yl]oxyphenyl]-[2-(5-fluoropyridin-3-yl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]methanoneIC5010000.0 [1]
[2-(Cyclopropylmethoxy)-5-methylsulfonylphenyl]-[2-(2-fluorophenyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]methanoneIC5010000.0 [1]
[2-(4,4-Difluoropiperidin-1-yl)-5-methylsulfonylphenyl]-[2-(2-fluorophenyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]methanoneIC5010000.0 [1]
GlyT1 Inhibitor 1IC5010000.0 [1]
3-[2-(2-Methylpyridin-4-yl)-4,6-dihydropyrrolo[3,4-c]pyrazole-5-carbonyl]-4-[(2S)-1,1,1-trifluoropropan-2-yl]oxybenzonitrileIC5010000.0 [1]
3-[2-(5-Fluoropyridin-3-yl)-4,6-dihydropyrrolo[3,4-c]pyrazole-5-carbonyl]-4-[(2S)-1,1,1-trifluoropropan-2-yl]oxybenzonitrileIC5010000.0 [1]
3-[2-(2-Fluorophenyl)-4,6-dihydropyrrolo[3,4-c]pyrazole-5-carbonyl]-4-[(2S)-1,1,1-trifluoropropan-2-yl]oxybenzonitrileIC5010000.0 [1]
(2-Cyclopentyl-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl)-[5-methylsulfonyl-2-[(2S)-1,1,1-trifluoropropan-2-yl]oxyphenyl]methanoneIC5010000.0 [1]
[2-(2-Methylpyridin-4-yl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]-[5-methylsulfonyl-2-[(2S)-1,1,1-trifluoropropan-2-yl]oxyphenyl]methanoneIC5010000.0 [1]
3-(2-Cyclopentyl-4,6-dihydropyrrolo[3,4-c]pyrazole-5-carbonyl)-4-[(2S)-1,1,1-trifluoropropan-2-yl]oxybenzonitrileIC5010000.0 [1]
4-(4,4-Difluoropiperidin-1-yl)-3-[2-(2-methylpyridin-4-yl)-4,6-dihydropyrrolo[3,4-c]pyrazole-5-carbonyl]benzonitrileIC5010000.0 [1]
[2-(2-Fluorophenyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]-[2-(3-fluorophenyl)-5-methylsulfonylphenyl]methanoneIC5010000.0 [1]
4-(3-Fluorophenyl)-3-[2-(5-fluoropyridin-3-yl)-4,6-dihydropyrrolo[3,4-c]pyrazole-5-carbonyl]benzonitrileIC5010000.0 [1]
[2-(2-Fluorophenyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]-[2-[(2-methylpropan-2-yl)oxy]-5-methylsulfonylphenyl]methanoneIC5010000.0 [1]
6-Cyano-N-[(1R)-1-[1-ethyl-6-(trifluoromethyl)imidazo[4,5-c]pyridin-2-yl]ethyl]pyridine-3-sulfonamideIC5020000.0 [1]
6-Cyano-N-[(1R)-1-(6-cyclopropyl-1-ethylimidazo[4,5-c]pyridin-2-yl)ethyl]pyridine-3-sulfonamideIC5020000.0 [1]
1-(3-Fluorophenyl)-3-[4-(1H-imidazo[4,5-b]pyridin-7-yl)phenyl]ureaIC5011400.0 [1]
1-(4-(3H-Imidazo[4,5-b]pyridin-7-yl)phenyl)-3-(3-chlorophenyl)ureaIC5052000.0 [1]
1-[4-(1H-Imidazo[4,5-b]pyridin-7-yl)phenyl]-3-phenylureaIC5044000.0 [1]
1-[4-(1H-Imidazo[4,5-b]pyridin-7-yl)phenyl]-3-[3-(morpholine-4-carbonyl)phenyl]ureaIC5060000.0 [1]
1-[4-(4-Hydroxyphenyl)phenyl]-3-[4-(1H-imidazo[4,5-b]pyridin-7-yl)phenyl]ureaIC5021000.0 [1]
1-[4-(1H-Imidazo[4,5-b]pyridin-7-yl)phenyl]-3-(3-nitrophenyl)ureaIC5031500.0 [1]
3-[[4-(5-Ethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]carbamoylamino]-N-propan-2-ylbenzamideIC508100.0 [1]
1-[4-(1H-Imidazo[4,5-b]pyridin-7-yl)phenyl]-3-(4-naphthalen-1-ylphenyl)ureaIC5013000.0 [1]
N,N-Diethyl-3-[[4-(1H-imidazo[4,5-b]pyridin-7-yl)phenyl]carbamoylamino]benzamideIC508600.0 [1]
1-[4-(1H-Imidazo[4,5-b]pyridin-7-yl)phenyl]-3-[3-(piperidine-1-carbonyl)phenyl]ureaIC505500.0 [1]
3-[[4-(5-Chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]carbamoylamino]-N-propan-2-ylbenzamideIC5044000.0 [1]
N-Cyclopentyl-3-[[4-(1H-imidazo[4,5-b]pyridin-7-yl)phenyl]carbamoylamino]benzamideIC506900.0 [1]
3-[[4-(1H-Imidazo[4,5-b]pyridin-7-yl)phenyl]carbamoylamino]-N,N-dimethylbenzamideIC5060000.0 [1]
3-[[4-(1H-Imidazo[4,5-b]pyridin-7-yl)phenyl]carbamoylamino]-N,N-di(propan-2-yl)benzamideIC501600.0 [1]
1-[4-(1H-Imidazo[4,5-b]pyridin-7-yl)phenyl]-3-[4-(3-methoxyphenyl)phenyl]ureaIC506800.0 [1]
1-(4-Bromophenyl)-3-[4-(1H-imidazo[4,5-b]pyridin-7-yl)phenyl]ureaIC5060000.0 [1]
1-(2-Chlorophenyl)-3-[4-(1H-imidazo[4,5-b]pyridin-7-yl)phenyl]ureaIC506100.0 [1]
1-(3-Bromophenyl)-3-[4-(1H-imidazo[4,5-b]pyridin-7-yl)phenyl]ureaIC5011400.0 [1]
N-Ethyl-3-[[4-(1H-imidazo[4,5-b]pyridin-7-yl)phenyl]carbamoylamino]benzamideIC5020300.0 [1]
N-[(1R)-1-[1-Ethyl-6-(trifluoromethyl)benzimidazol-2-yl]ethyl]pyridine-3-sulfonamideIC50830.0 [1]
2-[[7-Oxo-5-(2-phenylethyl)-3H-[1,2,4]triazolo[1,5-a]pyridine-8-carbonyl]amino]acetic acid;hydrochlorideIC50100000.0 [1]
4-[(E)-1-[4-(2-Aminoethoxy)phenyl]-1-(4-hydroxyphenyl)but-1-en-2-yl]phenolKi855.0 [1]
2-[[4-[[6-Amino-2-(2-methoxyethoxy)-8-oxo-7H-purin-9-yl]methyl]benzoyl]amino]ethoxy-[3,4-di(dodecanoyloxy)butyl]phosphinic acidIC5010500.0 [1]
[3-[2-[[4-[[6-Amino-2-(2-methoxyethoxy)-8-oxo-7H-purin-9-yl]methyl]benzoyl]amino]ethoxy-hydroxyphosphoryl]oxy-2-dodecanoyloxypropyl] dodecanoateIC5010500.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Cytochrome P450 3A5 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.22 Dec2024https://www.aatbio.com/data-sets/cytochrome-p450-3a5-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 22). Quest Database™ Cytochrome P450 3A5 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/cytochrome-p450-3a5-inhibitors-ic50-ki.
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