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Retinoid X receptor alpha Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
(2E,4E,6Z)-7-[3,5-Ditert-butyl-2-(2,2-difluoroethoxy)phenyl]-3-methylocta-2,4,6-trienoic acidIC500.0 [1], 8.0 [2]
(2E,4E,6Z)-7-[3,5-Ditert-butyl-2-(2,2-difluoroethoxy)phenyl]-3-methylocta-2,4,6-trienoic acidKi1.5 [1], 2.7 [2], 3.0 [3], 18.0 [4]
BexaroteneKi14.0 [1], 16.0 [2], 21.0 [3], 36.0 [4]
AlitretinoinIC5029.0 [1], 32.0 [2]
AlitretinoinKi8.0 [1], 8.4 [2], 12.0 [3]
TretinoinIC501000.0 [1]
TretinoinKi0.4 [1], 330.0 [2], 350.0 [3]
6-(1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopropyl)nicotinic acidIC508.0 [1]
6-(1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopropyl)nicotinic acidKi3.0 [1], 12.9 [2], 18.0 [3]
CID 11755040IC50290.0 [1], 900.0 [2], 1200.0 [3]
(2E,4E,6E)-7-[3,5-Ditert-butyl-2-(2,2-difluoroethoxy)phenyl]-6-fluoro-3-methylocta-2,4,6-trienoic acidIC506.8 [1]
(2E,4E,6E)-7-[3,5-Ditert-butyl-2-(2,2-difluoroethoxy)phenyl]-6-fluoro-3-methylocta-2,4,6-trienoic acidKi7.8 [1]
7-(2-Butoxy-3,5-diisopropyl-phenyl)-3-methyl-octa-2,4,6-trienoic acidIC504.0 [1]
7-(2-Butoxy-3,5-diisopropyl-phenyl)-3-methyl-octa-2,4,6-trienoic acidKi4.0 [1]
7-(3,5-Di-tert-butyl-2-ethoxy-phenyl)-3-methyl-octa-2,4,6-trienoic acidIC508.0 [1]
7-(3,5-Di-tert-butyl-2-ethoxy-phenyl)-3-methyl-octa-2,4,6-trienoic acidKi11.0 [1], 11.4 [2]
7-(2-Ethoxy-3,5-diisopropyl-phenyl)-3-methyl-octa-2,4,6-trienoic acidKi2.0 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-5-(2-fluorophenyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acidIC503.1 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-5-(2-fluorophenyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acidKi2.3 [1]
(E)-3-[4-[3,5-Ditert-butyl-2-(3-fluoropropoxy)phenyl]-1-benzothiophen-2-yl]but-2-enoic acidIC508.0 [1]
(E)-3-[4-[3,5-Ditert-butyl-2-(3-fluoropropoxy)phenyl]-1-benzothiophen-2-yl]but-2-enoic acidKi3.0 [1]
(E)-3-[4-(3,5-Diisopropyl-2-propoxy-phenyl)-benzo[b]thiophen-2-yl]-but-2-enoic acidIC5016.0 [1]
(E)-3-[4-(3,5-Diisopropyl-2-propoxy-phenyl)-benzo[b]thiophen-2-yl]-but-2-enoic acidKi14.0 [1]
(E)-3-[7-(3,5-Diisopropyl-2-propoxy-phenyl)-benzofuran-2-yl]-but-2-enoic acidIC50128.0 [1]
(E)-3-[7-(3,5-Diisopropyl-2-propoxy-phenyl)-benzofuran-2-yl]-but-2-enoic acidKi44.0 [1]
(Z)-3-[7-[2-(2,2-Difluoroethoxy)-3,5-di(propan-2-yl)phenyl]-1-benzofuran-2-yl]-2-fluorobut-2-enoic acidIC5022.0 [1]
(Z)-3-[7-[2-(2,2-Difluoroethoxy)-3,5-di(propan-2-yl)phenyl]-1-benzofuran-2-yl]-2-fluorobut-2-enoic acidKi101.0 [1]
(E)-3-[4-[3,5-Ditert-butyl-2-(2,2-difluoroethoxy)phenyl]-1-benzothiophen-2-yl]but-2-enoic acidIC5024.0 [1]
(E)-3-[4-[3,5-Ditert-butyl-2-(2,2-difluoroethoxy)phenyl]-1-benzothiophen-2-yl]but-2-enoic acidKi12.0 [1]
(E)-3-[4-[3,5-Ditert-butyl-2-(3,3-difluoropropoxy)phenyl]-1-benzothiophen-2-yl]but-2-enoic acidIC5016.0 [1]
(E)-3-[4-[3,5-Ditert-butyl-2-(3,3-difluoropropoxy)phenyl]-1-benzothiophen-2-yl]but-2-enoic acidKi7.0 [1]
(E)-3-[4-[3,5-Ditert-butyl-2-(2,2,2-trifluoroethoxy)phenyl]-1-benzothiophen-2-yl]but-2-enoic acidIC5014.0 [1]
(E)-3-[4-[3,5-Ditert-butyl-2-(2,2,2-trifluoroethoxy)phenyl]-1-benzothiophen-2-yl]but-2-enoic acidKi3.0 [1]
(E)-3-{7-[2-(3-Fluoro-propoxy)-3,5-diisopropyl-phenyl]-benzofuran-2-yl}-but-2-enoic acidIC50194.0 [1]
(E)-3-{7-[2-(3-Fluoro-propoxy)-3,5-diisopropyl-phenyl]-benzofuran-2-yl}-but-2-enoic acidKi47.0 [1]
(E)-3-[7-[3,5-Di(propan-2-yl)-2-(2,2,2-trifluoroethoxy)phenyl]-1-benzofuran-2-yl]but-2-enoic acidIC50347.0 [1]
(E)-3-[7-[3,5-Di(propan-2-yl)-2-(2,2,2-trifluoroethoxy)phenyl]-1-benzofuran-2-yl]but-2-enoic acidKi198.0 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-3,5-di(propan-2-yl)phenyl]-3-methylocta-2,4,6-trienoic acidIC501.0 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-3,5-di(propan-2-yl)phenyl]-3-methylocta-2,4,6-trienoic acidKi2.0 [1]
(E)-3-[7-[2-(2,2-Difluoroethoxy)-3,5-di(propan-2-yl)phenyl]-1-benzofuran-2-yl]but-2-enoic acidIC50300.0 [1]
(E)-3-[7-[2-(2,2-Difluoroethoxy)-3,5-di(propan-2-yl)phenyl]-1-benzofuran-2-yl]but-2-enoic acidKi161.0 [1]
(2E,4E,6Z)-7-[2-Ethoxy-3,5-bis(2-methylbutan-2-yl)phenyl]-3-methylocta-2,4,6-trienoic acidIC5017.0 [1]
(2E,4E,6Z)-7-[2-Ethoxy-3,5-bis(2-methylbutan-2-yl)phenyl]-3-methylocta-2,4,6-trienoic acidKi2.0 [1]
(2E,4E,6Z)-7-[2-(2-Fluoroethoxy)-3,5-di(propan-2-yl)phenyl]-3-methylocta-2,4,6-trienoic acidIC504.0 [1]
(2E,4E,6Z)-7-[2-(2-Fluoroethoxy)-3,5-di(propan-2-yl)phenyl]-3-methylocta-2,4,6-trienoic acidKi1.0 [1]
(2E,4E,6Z)-7-[3,5-Bis(2-methylbutan-2-yl)-2-propoxyphenyl]-3-methylocta-2,4,6-trienoic acidIC5013.0 [1]
(2E,4E,6Z)-7-[3,5-Bis(2-methylbutan-2-yl)-2-propoxyphenyl]-3-methylocta-2,4,6-trienoic acidKi23.0 [1]
7-(3,5-Diisopropyl-2-propoxy-phenyl)-3-methyl-octa-2,4,6-trienoic acidIC504.0 [1]
7-(3,5-Diisopropyl-2-propoxy-phenyl)-3-methyl-octa-2,4,6-trienoic acidKi3.0 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-3,5-bis(2-methylbutan-2-yl)phenyl]-3-methylocta-2,4,6-trienoic acidIC5016.0 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-3,5-bis(2-methylbutan-2-yl)phenyl]-3-methylocta-2,4,6-trienoic acidKi29.0 [1]
4-(2-Cyano-5-ethyl-7,7,10,10-tetramethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl)-2-fluorobenzoic acidIC50500.0 [1], 770.0 [2]
4-[5-Ethyl-7,7,10,10-tetramethyl-2-[[3-(trifluoromethyl)phenyl]sulfonylamino]-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acidIC5095.0 [1], 160.0 [2]
4-[7,7,10,10-Tetramethyl-5-propyl-2-[[3-(trifluoromethyl)phenyl]sulfonylamino]-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acidIC5076.0 [1], 190.0 [2]
(E)-3-[4-(3,5-Ditert-butyl-2-heptoxyphenyl)-1-benzothiophen-2-yl]but-2-enoic acidIC5083.0 [1]
(E)-3-[4-(3,5-Ditert-butyl-2-heptoxyphenyl)-1-benzothiophen-2-yl]but-2-enoic acidKi5.0 [1]
(Z)-3-[7-[2-Butoxy-3,5-di(propan-2-yl)phenyl]-1-benzofuran-2-yl]-2-fluorobut-2-enoic acidIC5011.0 [1]
(Z)-3-[7-[2-Butoxy-3,5-di(propan-2-yl)phenyl]-1-benzofuran-2-yl]-2-fluorobut-2-enoic acidKi16.0 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-5-(furan-2-yl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acidIC503.6 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-5-(furan-2-yl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acidKi3.0 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-3-propan-2-yl-5-thiophen-2-ylphenyl]-3-methylocta-2,4,6-trienoic acidIC501.9 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-3-propan-2-yl-5-thiophen-2-ylphenyl]-3-methylocta-2,4,6-trienoic acidKi0.8 [1]
(2E,4E,6E)-7-[2-Butoxy-3,5-di(propan-2-yl)phenyl]-6-fluoro-3-methylocta-2,4,6-trienoic acidIC504.7 [1]
(2E,4E,6E)-7-[2-Butoxy-3,5-di(propan-2-yl)phenyl]-6-fluoro-3-methylocta-2,4,6-trienoic acidKi4.4 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-5-(3-fluorophenyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acidIC503.9 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-5-(3-fluorophenyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acidKi1.0 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-5-(3,5-difluorophenyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acidIC504.6 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-5-(3,5-difluorophenyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acidKi2.6 [1]
(2E,4E,6Z)-3-Methyl-7-[3-(1,1,2,2,2-pentafluoroethyl)-5-propan-2-yl-2-propoxyphenyl]octa-2,4,6-trienoic acidIC5010.7 [1]
(2E,4E,6Z)-3-Methyl-7-[3-(1,1,2,2,2-pentafluoroethyl)-5-propan-2-yl-2-propoxyphenyl]octa-2,4,6-trienoic acidKi85.8 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-3-phenyl-5-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acidIC5057.9 [1]
(2E,4E,6Z)-7-[2-(2,2-Difluoroethoxy)-3-phenyl-5-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acidKi6.1 [1]
(2E,4E,6Z)-3-Methyl-7-[5-(1,1,2,2,2-pentafluoroethyl)-3-propan-2-yl-2-propoxyphenyl]octa-2,4,6-trienoic acidIC505.1 [1]
(2E,4E,6Z)-3-Methyl-7-[5-(1,1,2,2,2-pentafluoroethyl)-3-propan-2-yl-2-propoxyphenyl]octa-2,4,6-trienoic acidKi25.6 [1]
(2E,4E,6Z)-7-[2-Ethoxy-5-(1,1,2,2,2-pentafluoroethyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acidIC505.3 [1]
(2E,4E,6Z)-7-[2-Ethoxy-5-(1,1,2,2,2-pentafluoroethyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acidKi6.3 [1]
4-(5,7,7,10,10-Pentamethyl-2-methylsulfanyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl)benzoic acidIC502000.0 [1], 3000.0 [2]
4-[2-(4-Methoxyphenyl)sulfanyl-5,7,7,10,10-pentamethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acidIC50720.0 [1], 1600.0 [2]
4-[5,7,7,10,10-Pentamethyl-2-[4-(trifluoromethoxy)phenyl]sulfanyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acidIC50390.0 [1], 1000.0 [2]
4-[2-[(4-Chlorophenyl)methylsulfanyl]-5,7,7,10,10-pentamethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acidIC50670.0 [1], 1600.0 [2]
4-[2-[(4-Methoxyphenyl)methylsulfanyl]-5,7,7,10,10-pentamethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acidIC504900.0 [1], 5500.0 [2]
4-(5,7,7,10,10-Pentamethyl-2-methylsulfonyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl)benzoic acidIC501400.0 [1], 1700.0 [2]
4-(5,7,7,10,10-Pentamethyl-2-propylsulfonyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl)benzoic acidIC50450.0 [1], 920.0 [2]
4-[2-(4-Methoxyphenyl)sulfonyl-5,7,7,10,10-pentamethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acidIC50170.0 [1], 360.0 [2]
4-[5,7,7,10,10-Pentamethyl-2-[4-(trifluoromethoxy)phenyl]sulfonyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acidIC50130.0 [1], 240.0 [2]
4-[2-[(4-Chlorophenyl)methylsulfonyl]-5,7,7,10,10-pentamethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acidIC50420.0 [1], 950.0 [2]
4-[2-[(4-Methoxyphenyl)methylsulfonyl]-5,7,7,10,10-pentamethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acidIC50780.0 [1], 1400.0 [2]
4-[5,7,7,10,10-Pentamethyl-2-(methylsulfamoyl)-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acidIC501300.0 [1]
4-[2-(Dimethylsulfamoyl)-5,7,7,10,10-pentamethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acidIC502000.0 [1], 2200.0 [2]
4-[2-(Butylsulfamoyl)-5,7,7,10,10-pentamethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acidIC50190.0 [1], 410.0 [2]
4-[5,7,7,10,10-Pentamethyl-2-[[4-(trifluoromethoxy)phenyl]sulfamoyl]-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acidIC50460.0 [1], 960.0 [2]
4-(5,7,7,10,10-Pentamethyl-2-pyrrolidin-1-ylsulfonyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl)benzoic acidIC50450.0 [1], 1000.0 [2]
4-(5,7,7,10,10-Pentamethyl-2-morpholin-4-ylsulfonyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl)benzoic acidIC50450.0 [1], 1000.0 [2]
4-[5,7,7,10,10-Pentamethyl-2-(4-methylpiperazin-1-yl)sulfonyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl]benzoic acidIC501000.0 [1], 1900.0 [2]
4-(5,7,7,10,10-Pentamethyl-2-morpholin-4-yl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl)benzoic acidIC503900.0 [1], 7000.0 [2]
4-(2-Acetyl-5,7,7,10,10-pentamethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl)benzoic acidIC50890.0 [1], 1100.0 [2]
4-(2-Acetyl-5-ethyl-7,7,10,10-tetramethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl)benzoic acidIC50790.0 [1], 970.0 [2]
4-(2-Acetyl-5,7,7,10,10-pentamethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl)-2-fluorobenzoic acidIC501100.0 [1], 1700.0 [2]
4-(2-Acetyl-5-ethyl-7,7,10,10-tetramethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl)-3-fluorobenzoic acidIC503000.0 [1], 3300.0 [2]
4-(2-Cyano-5-ethyl-7,7,10,10-tetramethyl-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl)benzoic acidIC50320.0 [1], 480.0 [2]



References

This online tool may be cited as follows

MLA

"Quest Database™ Retinoid X receptor alpha Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Nov2024https://www.aatbio.com/data-sets/retinoid-x-receptor-alpha-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024November 21). Quest Database™ Retinoid X receptor alpha Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/retinoid-x-receptor-alpha-inhibitors-ic50-ki.
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