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Bile acid receptor FXR Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
GuggulsteroneIC5012000.0 [1], 44900.0 [2], 89360.0 [3], 89400.0 [4], 100000.0 [5]
GuggulsteroneKi5000.0 [1]
E-GuggulsteroneIC504100.0 [1], 41000.0 [2], 44000.0 [3], 100000.0 [4]
E-GuggulsteroneKi5000.0 [1]
(E)-3-(2-Chloro-4-((3-(2,6-dichlorophenyl)-5-isopropylisoxazol-4-yl)methoxy)styryl)benzoic acidIC5019.8 [1], 64.0 [2], 112.0 [3]
N-(4-Methyl-3-morpholin-4-ylsulfonylphenyl)-3-(4-methylphenyl)-1-phenylpyrazole-4-carboxamideIC5047.0 [1], 2620.0 [2]
(2S)-2-[6-Chloro-2-(4-chlorophenyl)-5-fluorobenzimidazol-1-yl]-N,2-dicyclohexylacetamideIC5013.0 [1]
2-(Ethylamino)-6-[3-[4-(trifluoromethoxy)phenyl]propanoyl]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidine-4-carboxamideIC5010000.0 [1]
1-[(3-Methoxyphenyl)methyl]-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)-3-(4-methylphenyl)pyrazole-4-carboxamideIC507.5 [1], 468.5 [2]
3-[(1S)-1-(1-Methylbenzimidazol-2-yl)-2-[1-(2-methylpropanoyl)piperidin-4-yl]ethyl]-1-(4-phenoxyphenyl)imidazolidine-2,4-dioneIC500.0 [1], 38.0 [2]
3-[(1S)-1-(1,6-Dimethylbenzimidazol-2-yl)-2-[1-(2-methylpropyl)piperidin-4-yl]ethyl]-1-(4-phenoxyphenyl)imidazolidine-2,4-dioneIC5016400.0 [1], 17400.0 [2]
3-[(1S)-1-(1,6-Dimethylbenzimidazol-2-yl)-2-[1-(2-methylpropanoyl)piperidin-4-yl]ethyl]-1-(4-phenoxyphenyl)imidazolidine-2,4-dioneIC500.0 [1], 35.0 [2]
3-[(1S)-1-(6-Chloro-1-methylbenzimidazol-2-yl)-2-[1-(2-methylpropanoyl)piperidin-4-yl]ethyl]-1-(4-phenoxyphenyl)imidazolidine-2,4-dioneIC500.05 [1], 130.0 [2]
3-[(1S)-2-(1-Acetylpiperidin-4-yl)-1-(1-methylbenzimidazol-2-yl)ethyl]-1-(4-phenoxyphenyl)imidazolidine-2,4-dioneIC500.0 [1], 740.0 [2]
3-[(1S)-2-(1-Acetylpiperidin-4-yl)-1-(6-chloro-1-methylbenzimidazol-2-yl)ethyl]-1-(4-phenoxyphenyl)imidazolidine-2,4-dioneIC500.8 [1], 3500.0 [2]
3-[(1S)-1-(5-Fluoro-1-methylbenzimidazol-2-yl)-2-[1-(2-methylpropanoyl)piperidin-4-yl]ethyl]-1-(4-phenoxyphenyl)imidazolidine-2,4-dioneIC500.06 [1], 340.0 [2]
3-[(1S)-2-(1-Acetylpiperidin-4-yl)-1-(1,6-dimethylbenzimidazol-2-yl)ethyl]-1-(4-phenoxyphenyl)imidazolidine-2,4-dioneIC500.2 [1], 1300.0 [2]
3-[(1S)-1-(1,6-Dimethylbenzimidazol-2-yl)-2-piperidin-4-ylethyl]-1-(4-phenoxyphenyl)imidazolidine-2,4-dioneIC504510.0 [1], 64000.0 [2]
3-[(1S)-2-[1-(Cyclopentanecarbonyl)piperidin-4-yl]-1-(1,6-dimethylbenzimidazol-2-yl)ethyl]-1-(4-phenoxyphenyl)imidazolidine-2,4-dioneIC500.01 [1], 30.0 [2]
3-[(1S)-2-(1-Acetylpiperidin-4-yl)-1-(5-fluoro-1-methylbenzimidazol-2-yl)ethyl]-1-(4-phenoxyphenyl)imidazolidine-2,4-dioneIC501.0 [1], 8300.0 [2]
2-[4-[(4-Tert-butyl-2-methoxybenzoyl)amino]phenyl]acetic acidIC501.3 [1], 9.2 [2]
3,5-Dimethyl-N-[4-methyl-3-(morpholine-4-sulfonyl)phenyl]-1-phenyl-1H-pyrazole-4-carboxamideIC503300.0 [1], 11800.0 [2]
N-(4-Methyl-3-morpholin-4-ylsulfonylphenyl)-1-phenyl-5-(trifluoromethyl)pyrazole-4-carboxamideIC50996.0 [1], 11800.0 [2]
N-(4-Fluoro-3-morpholin-4-ylsulfonylphenyl)-1-phenylpyrazole-4-carboxamideIC508300.0 [1], 9400.0 [2]
N-(3-Morpholin-4-ylsulfonylphenyl)-1-phenyl-3-pyridin-3-ylpyrazole-4-carboxamideIC501300.0 [1], 10800.0 [2]
2-[3-[(4-Tert-butylbenzoyl)amino]phenyl]acetic acidIC50350.0 [1], 400.0 [2]
5-Methyl-1-(3-methylphenyl)-N-(3-morpholin-4-ylsulfonylphenyl)pyrazole-4-carboxamideIC506600.0 [1], 29300.0 [2]
N-(4-Methyl-3-morpholin-4-ylsulfonylphenyl)-3-(4-methylphenyl)-1-[[3-(trifluoromethyl)phenyl]methyl]pyrazole-4-carboxamideIC5018.4 [1], 515.0 [2]
1-(4-Hydroxybutyl)-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)-3-(4-methylphenyl)pyrazole-4-carboxamideIC50130.3 [1], 2610.0 [2]
1-[(3-Methoxyphenyl)methyl]-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)-3-propan-2-ylpyrazole-4-carboxamideIC50199.4 [1], 3110.0 [2]
3-(3-Methoxyphenyl)-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)-1-propan-2-ylpyrazole-4-carboxamideIC50159.7 [1], 3490.0 [2]
3-(3-Methoxyphenyl)-1-[(3-methoxyphenyl)methyl]-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)pyrazole-4-carboxamideIC5042.8 [1], 1240.0 [2]
N-(4-Methyl-3-morpholin-4-ylsulfonylphenyl)-1-propan-2-yl-3-[4-(trifluoromethyl)phenyl]pyrazole-4-carboxamideIC5077.5 [1], 1950.0 [2]
1-[(3-Methoxyphenyl)methyl]-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)-3-[4-(trifluoromethyl)phenyl]pyrazole-4-carboxamideIC5030.9 [1], 592.7 [2]
3-(2-Methoxyethyl)-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)-1-propan-2-ylpyrazole-4-carboxamideIC503420.0 [1], 29580.0 [2]
3-(2-Methoxyethyl)-1-[(3-methoxyphenyl)methyl]-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)pyrazole-4-carboxamideIC50389.5 [1], 11100.0 [2]
N-Methyl-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)-3-(4-methylphenyl)-1-propan-2-ylpyrazole-4-carboxamideIC50489.4 [1], 16160.0 [2]
N-[[1-[(3-Methoxyphenyl)methyl]-3-propan-2-ylpyrazol-4-yl]methyl]-4-methyl-3-morpholin-4-ylsulfonylanilineIC502310.0 [1], 27830.0 [2]
1-(4-Fluorophenyl)-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)-3-(4-methylphenyl)pyrazole-4-carboxamideIC5024.3 [1], 2490.0 [2]
1-(3-Chlorophenyl)-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)-3-(4-methylphenyl)pyrazole-4-carboxamideIC5010.4 [1], 5910.0 [2]
1-(2,4-Dichlorophenyl)-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)-3-(4-methylphenyl)pyrazole-4-carboxamideIC5014.1 [1], 1240.0 [2]
N-(4-Methyl-3-morpholin-4-ylsulfonylphenyl)-3-(4-methylphenyl)-1-[3-(trifluoromethyl)phenyl]pyrazole-4-carboxamideIC5023.9 [1], 22290.0 [2]
1-(1,3-Benzothiazol-2-yl)-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)-3-(4-methylphenyl)pyrazole-4-carboxamideIC5017.7 [1], 7910.0 [2]
N-(4-Methyl-3-morpholin-4-ylsulfonylphenyl)-3-(4-methylphenyl)-1-propan-2-ylpyrazole-4-carboxamideIC5049.1 [1], 1690.0 [2]
1-Butyl-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)-3-(4-methylphenyl)pyrazole-4-carboxamideIC5052.5 [1], 11510.0 [2]
N-(4-Methyl-3-morpholin-4-ylsulfonylphenyl)-3-(4-methylphenyl)-1-(naphthalen-2-ylmethyl)pyrazole-4-carboxamideIC5010.2 [1], 844.1 [2]
1-(Cyclopropylmethyl)-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)-3-(4-methylphenyl)pyrazole-4-carboxamideIC5076.9 [1], 848.8 [2]
LevothyroxineIC507860.0 [1]
RaloxifeneIC5011560.0 [1]
ClotrimazoleIC503240.0 [1]
FulvestrantIC50790.0 [1]
NimodipineIC508960.0 [1]
LoratadineIC503070.0 [1]
Lithocholic acidIC5018.3 [1]
FelodipineIC504960.0 [1]
6-Bromoindirubin-3'-oximeIC503400.0 [1]
GW7647IC504910.0 [1]
2,5-DihydroxytyrosineIC507920.0 [1]
(2-Methyl-1-propyl-1H-indol-3-yl)-1-naphthalenylmethanoneIC503220.0 [1]
SulconazoleIC506880.0 [1]
Nbi 27914IC502770.0 [1]
1-[5-Ethyl-2-hydroxy-4-[[6-methyl-6-(1H-tetrazol-5-YL)heptyl]oxy]phenyl]ethanoneIC5035200.0 [1]
IvermectineIC50260.0 [1]
FlutrimazoleIC5013800.0 [1]
(R,R)-cis-Diethyl tetrahydro-2,8-chrysenediolIC501310.0 [1]
Palmitoyl-DL-carnitine chlorideIC509750.0 [1]
12-Deacetyl-12-epi-19-deoxyscalarinIC5031600.0 [1]
12-Epi-scalarinIC5060400.0 [1]
{4-[(2-Naphthylacetyl)amino]phenyl}acetic acidIC5027000.0 [1]
3-Tert-butyl-4-hydroxyphenyl phenylacetateIC50100000.0 [1]
12-O-Deacetyl-12-epi-scalarinIC5075000.0 [1]
3-(4-{[(4-Tert-butylphenyl)carbonyl]amino}phenyl)propanoic acidIC50630.0 [1]
Ethyl 3-(3,4-difluorobenzoyl)-1,1-dimethyl-1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylateIC5021.0 [1]
3-[[2-[(4-Tert-butylbenzoyl)amino]-5-chlorobenzoyl]amino]benzoic acidIC5012300.0 [1]
2-[4-[[3-(3,5-Dichlorophenyl)benzoyl]amino]phenyl]acetic acidIC509100.0 [1]
7-(4-Acetyl-2-ethyl-5-hydroxyphenoxy)-2,2-dimethylheptanoic acidIC50100000.0 [1]
12-O-Deacetyl-12-epi-19-deoxy-21-hydroxyscalarinIC502400.0 [1]
3-[(E)-2-[2-Chloro-4-[[3-(3,5-dichloropyridin-4-yl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]ethenyl]benzoic acidIC50690.0 [1]
Tuberatolide AIC503900.0 [1]
(E)-3-(3,4-Dimethoxyphenyl)-1-(3-hydroxyphenyl)prop-2-en-1-oneIC5020000.0 [1]
2,4-Diethyl-5-[6-methyl-6-(2H-tetrazol-5-yl)heptoxy]phenolIC503100.0 [1]
3-[[2-[(4-Tert-butylbenzoyl)amino]-5-methoxybenzoyl]amino]benzoic acidIC5015100.0 [1]
2-[2-[(4-Tert-butylbenzoyl)amino]phenyl]acetic acidIC50102.0 [1]
(3-Tert-butyl-4-hydroxyphenyl) (E)-3-phenylprop-2-enoateIC50100000.0 [1]
(3-Tert-butyl-4-hydroxyphenyl) 2-methoxybenzoateIC50100000.0 [1]
(3-Tert-butyl-4-hydroxyphenyl) 4-nitrobenzoateIC5012700.0 [1]
(3-Tert-butyl-4-hydroxyphenyl) 2-chloro-4-nitrobenzoateIC508800.0 [1]
(3-Tert-butyl-4-hydroxyphenyl) 2,6-dichloro-4-nitrobenzoateIC505900.0 [1]
(3-Tert-butyl-4-hydroxyphenyl) 4-aminobenzoateIC5034200.0 [1]
(3-Tert-butyl-4-hydroxyphenyl) 4-amino-2-chlorobenzoateIC507200.0 [1]
(3-Tert-butyl-4-hydroxyphenyl) 4-amino-2,6-dichlorobenzoateIC50600.0 [1]
N-(3-Tert-butyl-4-hydroxyphenyl)-2,4-dichlorobenzamideIC5013600.0 [1]
2,4-Dichloro-N-(3,5-ditert-butyl-4-hydroxyphenyl)benzamideIC50100000.0 [1]
2,4-Dichloro-N-(4-hydroxy-3-propan-2-ylphenyl)benzamideIC50100000.0 [1]
2,4-Dichloro-N-(3-ethyl-4-hydroxyphenyl)benzamideIC50100000.0 [1]
N-(3-Tert-butyl-4-methoxyphenyl)-2,4-dichlorobenzamideIC50100000.0 [1]
N-(3-Tert-butyl-4-prop-2-enoxyphenyl)-2,4-dichlorobenzamideIC50100000.0 [1]
[2-Tert-butyl-4-[(2,4-dichlorobenzoyl)amino]phenyl] acetateIC5015500.0 [1]
4-Amino-N-(3-tert-butyl-4-hydroxyphenyl)-2,6-dichlorobenzamideIC505200.0 [1]
N-(3-Tert-butyl-4-hydroxyphenyl)-2,6-dichloro-4-(pyridin-3-ylmethylamino)benzamideIC503600.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Bile acid receptor FXR Inhibitors (IC50, Ki)." AAT Bioquest, Inc.10 May2024https://www.aatbio.com/data-sets/bile-acid-receptor-fxr-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 10). Quest Database™ Bile acid receptor FXR Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/bile-acid-receptor-fxr-inhibitors-ic50-ki.
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