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Urotensin II receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
3,4-Dichloro-N-[(3S)-1-[[4-[3-(dimethylamino)propoxy]phenyl]methyl]pyrrolidin-3-yl]benzamideIC50158.49 [1], 170.0 [2]
3,4-Dichloro-N-[(3S)-1-[[4-[3-(dimethylamino)propoxy]phenyl]methyl]pyrrolidin-3-yl]benzamideKi199.53 [1], 200.0 [2], 250.0 [3]
CID 21023902IC506.0 [1], 8.0 [2], 14.0 [3]
CID 21023902Ki5.4 [1], 8.0 [2]
Human Urotensin IIIC5013.0 [1]
Human Urotensin IIKi0.79 [1]
PalosuranIC505.0 [1], 39.0 [2], 320.0 [3]
PalosuranKi41.0 [1]
(2S)-2-[[(4R,7S,10S,13S,16S,19S)-10-(4-Aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acidKi0.25 [1]
(2S)-2-[[(4R,7S,10S,13S,16S,19S)-10-(4-Aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-20,20-dimethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acidKi0.2 [1]
UrantideKi5.01 [1]
N-[(2S)-1-[[(3S)-1-[[4-[3-(Dimethylamino)propoxy]phenyl]methyl]pyrrolidin-3-yl]amino]-4-methyl-1-oxopentan-2-yl]-1-benzothiophene-2-carboxamideIC50630.96 [1]
N-[(2S)-1-[[(3S)-1-[[4-[3-(Dimethylamino)propoxy]phenyl]methyl]pyrrolidin-3-yl]amino]-4-methyl-1-oxopentan-2-yl]-1-benzothiophene-2-carboxamideKi110.0 [1], 125.89 [2]
(4R,10Br)-4-(3,4-dimethoxyphenyl)-10-(4-ethylpiperazin-1-yl)-2,3,4,10b-tetrahydro-1H-pyrido[1,2-b]isoindol-6-oneKi64.0 [1], 390.0 [2]
2-Bromo-N-[4-chloro-3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]phenyl]-4,5-dimethoxybenzenesulfonamideIC5023.0 [1], 43.0 [2]
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-Aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acidKi0.25 [1], 1.23 [2]
(2S)-2-[[(4R,7S,10S,13S,16S,19R)-10-(4-Aminobutyl)-19-[[(2S)-2-aminopropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acidIC5012.0 [1], 19.5 [2]
Benzamide,N-[(3S)-1-[[3-bromo-4-(4-piperidinyloxy)phenyl]methyl]-3-pyrrolidinyl]-3,4-dichloro-IC504.0 [1]
Benzamide,N-[(3S)-1-[[3-bromo-4-(4-piperidinyloxy)phenyl]methyl]-3-pyrrolidinyl]-3,4-dichloro-Ki4.0 [1]
2-(3,4-Dichloro-N-methylanilino)-1-[(2R,3R)-3-phenyl-2-(pyrrolidin-1-ylmethyl)piperidin-1-yl]ethanoneKi6.0 [1], 6.31 [2]
CID 25126427IC508.0 [1]
CID 25126427Ki4.0 [1]
4-Bromo-N-{(S)-1-[4-(3-dimethylamino-propoxy)-benzyl]-pyrrolidin-3-yl}-benzamideKi316.23 [1], 320.0 [2]
2-(3,4-Dichloro-N-methylanilino)-1-[(2S,3S)-3-phenyl-2-(pyrrolidin-1-ylmethyl)piperidin-1-yl]ethanoneKi1584.89 [1], 1600.0 [2]
2-(3,4-Dichloro-N-methylanilino)-1-[2-(pyrrolidin-1-ylmethyl)piperidin-1-yl]ethanoneIC50630.96 [1]
2-(3,4-Dichloro-N-methylanilino)-1-[2-(pyrrolidin-1-ylmethyl)piperidin-1-yl]ethanoneKi398.11 [1]
2-(3,4-Dichloro-N-methylanilino)-1-[3-phenyl-2-(pyrrolidin-1-ylmethyl)piperidin-1-yl]ethanoneKi16.0 [1]
(2S)-2-[[(4S,7S,10S,13S,16S,19S)-10-(4-Aminobutyl)-19-[[(2S)-2-amino-3-carboxypropanoyl]amino]-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-3,3,20,20-tetramethyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acidKi1.26 [1]
2-Bromo-N-[3-[2-(dimethylamino)ethoxy]-4-(trifluoromethyl)phenyl]-4,5-dimethoxybenzenesulfonamideIC50100.0 [1], 134.0 [2]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-(4-propan-2-ylpiperazin-1-yl)isoindol-2-yl]butyl]thiophene-2-sulfonamideIC50150.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-(4-propan-2-ylpiperazin-1-yl)isoindol-2-yl]butyl]thiophene-2-sulfonamideKi45.0 [1]
N-[4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]thiophene-2-sulfonamideIC50250.0 [1]
N-[4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]thiophene-2-sulfonamideKi76.0 [1]
2-[(3,4-Dimethoxyphenyl)methyl]-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindole-1,3-dioneIC501900.0 [1]
2-[(3,4-Dimethoxyphenyl)methyl]-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindole-1,3-dioneKi570.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]-3,5-dimethyl-1H-pyrazole-4-sulfonamideIC5047.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]-3,5-dimethyl-1H-pyrazole-4-sulfonamideKi13.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]thiophene-2-sulfonamideIC50240.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]thiophene-2-sulfonamideKi49.0 [1]
N-Butyl-5H-pyrido[4,3-b]indol-1-amineIC50501.19 [1]
N-Butyl-5H-pyrido[4,3-b]indol-1-amineKi3.98 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[7-(4-ethylpiperazin-1-yl)-3-oxo-1H-isoindol-2-yl]butyl]-3,5-dimethyl-1H-pyrazole-4-carboxamideIC50130.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[7-(4-ethylpiperazin-1-yl)-3-oxo-1H-isoindol-2-yl]butyl]-3,5-dimethyl-1H-pyrazole-4-carboxamideKi11.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[7-(4-ethylpiperazin-1-yl)-3-oxo-1H-isoindol-2-yl]butyl]-N-methylthiophene-2-sulfonamideIC5088.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[7-(4-ethylpiperazin-1-yl)-3-oxo-1H-isoindol-2-yl]butyl]-N-methylthiophene-2-sulfonamideKi5.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[3-oxo-7-(4-propan-2-ylpiperazin-1-yl)-1H-isoindol-2-yl]butyl]thiophene-2-sulfonamideIC5053.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[3-oxo-7-(4-propan-2-ylpiperazin-1-yl)-1H-isoindol-2-yl]butyl]thiophene-2-sulfonamideKi4.0 [1]
2-[(1R)-1-(3,4-Dimethoxyphenyl)-4-(thiophen-2-ylmethylamino)butyl]-4-(4-ethylpiperazin-1-yl)-3H-isoindol-1-oneIC5059.0 [1]
2-[(1R)-1-(3,4-Dimethoxyphenyl)-4-(thiophen-2-ylmethylamino)butyl]-4-(4-ethylpiperazin-1-yl)-3H-isoindol-1-oneKi18.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[7-(4-ethylpiperazin-1-yl)-3-oxo-1H-isoindol-2-yl]butyl]thiophene-2-carboxamideIC50140.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[7-(4-ethylpiperazin-1-yl)-3-oxo-1H-isoindol-2-yl]butyl]thiophene-2-carboxamideKi18.0 [1]
N-[(4R)-4-[7-(4-Cyclopropylpiperazin-1-yl)-3-oxo-1H-isoindol-2-yl]-4-(3,4-dimethoxyphenyl)butyl]-N-methylthiophene-2-sulfonamideIC501200.0 [1]
N-[(4R)-4-[7-(4-Cyclopropylpiperazin-1-yl)-3-oxo-1H-isoindol-2-yl]-4-(3,4-dimethoxyphenyl)butyl]-N-methylthiophene-2-sulfonamideKi59.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[3-oxo-7-(4-propan-2-ylpiperazin-1-yl)-1H-isoindol-2-yl]butyl]-N-methylthiophene-2-sulfonamideIC50500.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[3-oxo-7-(4-propan-2-ylpiperazin-1-yl)-1H-isoindol-2-yl]butyl]-N-methylthiophene-2-sulfonamideKi11.0 [1]
N-[(4R)-4-[7-(4-Cyclobutylpiperazin-1-yl)-3-oxo-1H-isoindol-2-yl]-4-(3,4-dimethoxyphenyl)butyl]-N-methylthiophene-2-sulfonamideIC50510.0 [1]
N-[(4R)-4-[7-(4-Cyclobutylpiperazin-1-yl)-3-oxo-1H-isoindol-2-yl]-4-(3,4-dimethoxyphenyl)butyl]-N-methylthiophene-2-sulfonamideKi44.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[7-(4-methylpiperazin-1-yl)-3-oxo-1H-isoindol-2-yl]butyl]-N-methylthiophene-2-sulfonamideIC50340.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[7-(4-methylpiperazin-1-yl)-3-oxo-1H-isoindol-2-yl]butyl]-N-methylthiophene-2-sulfonamideKi6.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-(1,3-dioxo-4-piperazin-1-ylisoindol-2-yl)butyl]thiophene-2-sulfonamideIC50500.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-(1,3-dioxo-4-piperazin-1-ylisoindol-2-yl)butyl]thiophene-2-sulfonamideKi150.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[4-(4-methylpiperazin-1-yl)-1,3-dioxoisoindol-2-yl]butyl]thiophene-2-sulfonamideIC50220.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[4-(4-methylpiperazin-1-yl)-1,3-dioxoisoindol-2-yl]butyl]thiophene-2-sulfonamideKi59.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[4-(4-ethylpiperazin-1-yl)-1,3-dioxoisoindol-2-yl]butyl]thiophene-2-sulfonamideIC50150.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[4-(4-ethylpiperazin-1-yl)-1,3-dioxoisoindol-2-yl]butyl]thiophene-2-sulfonamideKi35.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]-5-methyl-1,2-oxazole-4-sulfonamideIC50130.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]-5-methyl-1,2-oxazole-4-sulfonamideKi32.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]-5-methyl-1,2-oxazole-4-carboxamideIC50760.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]-5-methyl-1,2-oxazole-4-carboxamideKi130.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]-3,5-dimethyl-1H-pyrazole-4-carboxamideIC5037.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]-3,5-dimethyl-1H-pyrazole-4-carboxamideKi87.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]-1,2-dimethylimidazole-4-sulfonamideIC50220.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]-1,2-dimethylimidazole-4-sulfonamideKi16.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[4-(4-ethylpiperazin-1-yl)-1,3-dioxoisoindol-2-yl]butyl]-1,2-dimethylimidazole-4-sulfonamideIC50810.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[4-(4-ethylpiperazin-1-yl)-1,3-dioxoisoindol-2-yl]butyl]-1,2-dimethylimidazole-4-sulfonamideKi97.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-(3-oxo-7-piperazin-1-yl-1H-isoindol-2-yl)butyl]-N-methylthiophene-2-sulfonamideIC50410.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-(3-oxo-7-piperazin-1-yl-1H-isoindol-2-yl)butyl]-N-methylthiophene-2-sulfonamideKi49.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[3-oxo-7-[4-[(1R)-1-phenylethyl]piperazin-1-yl]-1H-isoindol-2-yl]butyl]-5-methyl-1,2-oxazole-4-carboxamideIC50320.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[3-oxo-7-[4-[(1R)-1-phenylethyl]piperazin-1-yl]-1H-isoindol-2-yl]butyl]-5-methyl-1,2-oxazole-4-carboxamideKi15.0 [1]
N-[(4S)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]thiophene-2-sulfonamideIC50260.0 [1]
N-[(4S)-4-(3,4-Dimethoxyphenyl)-4-[1,3-dioxo-4-[4-[(1R)-1-phenylethyl]piperazin-1-yl]isoindol-2-yl]butyl]thiophene-2-sulfonamideKi120.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[7-(4-ethylpiperazin-1-yl)-3-oxo-1H-isoindol-2-yl]butyl]-1H-imidazole-5-sulfonamideIC5051.0 [1]
N-[(4R)-4-(3,4-Dimethoxyphenyl)-4-[7-(4-ethylpiperazin-1-yl)-3-oxo-1H-isoindol-2-yl]butyl]-1H-imidazole-5-sulfonamideKi25.0 [1]
2-[(1R)-4-[(6-Chloropyrazin-2-yl)amino]-1-(3,4-dimethoxyphenyl)butyl]-4-(4-ethylpiperazin-1-yl)-3H-isoindol-1-oneIC50500.0 [1]
2-[(1R)-4-[(6-Chloropyrazin-2-yl)amino]-1-(3,4-dimethoxyphenyl)butyl]-4-(4-ethylpiperazin-1-yl)-3H-isoindol-1-oneKi62.0 [1]
2-[(1R)-1-(3,4-Dimethoxyphenyl)-4-[(6-methoxypyrazin-2-yl)amino]butyl]-4-(4-ethylpiperazin-1-yl)-3H-isoindol-1-oneIC5062.0 [1]
2-[(1R)-1-(3,4-Dimethoxyphenyl)-4-[(6-methoxypyrazin-2-yl)amino]butyl]-4-(4-ethylpiperazin-1-yl)-3H-isoindol-1-oneKi8.0 [1]
(3R)-3-[5-[(2-Bromo-4,5-dimethoxyphenyl)sulfonylmethyl]-2-chlorophenoxy]-1-methylpyrrolidineIC5034.0 [1], 60.0 [2]
(3S)-3-[5-[(2-Bromo-4,5-dimethoxyphenyl)sulfonylmethyl]-2-chlorophenoxy]-1-methylpyrrolidineIC50742.0 [1], 1280.0 [2]
N-[(2-Bromo-4,5-dimethoxyphenyl)methyl]-4-chloro-3-[(3R)-1-methylpyrrolidin-3-yl]oxyanilineIC50237.0 [1], 1328.0 [2]
N-[(2-Bromo-4,5-dimethoxyphenyl)methyl]-4-chloro-3-[(3S)-1-methylpyrrolidin-3-yl]oxyanilineIC501350.0 [1], 1450.0 [2]
N-[(2-Bromo-4,5-dimethoxyphenyl)methyl]-4-chloro-3-[2-(dimethylamino)ethoxy]anilineIC501200.0 [1], 1300.0 [2]
N-[(2-Bromophenyl)methyl]-4-chloro-3-[2-(dimethylamino)ethoxy]anilineIC503500.0 [1], 6000.0 [2]
4-Chloro-3-[2-(dimethylamino)ethoxy]-N-[[2-(trifluoromethyl)phenyl]methyl]anilineIC50520.0 [1], 765.0 [2]
2-Bromo-4,5-dimethoxy-N-[3-[(3S)-1-methylpiperidin-3-yl]oxy-4-(trifluoromethyl)phenyl]benzenesulfonamideIC505000.0 [1], 5500.0 [2]
2-Bromo-4,5-dimethoxy-N-[3-[(3R)-1-methylpiperidin-3-yl]oxy-4-(trifluoromethyl)phenyl]benzenesulfonamideIC50120.0 [1], 160.0 [2]
2-Bromo-4,5-dimethoxy-N-[3-[[(2R)-1-methylpyrrolidin-2-yl]methoxy]-4-(trifluoromethyl)phenyl]benzenesulfonamideIC50350.0 [1], 800.0 [2]
N-[(5-Bromo-1,3-benzodioxol-4-yl)methyl]-3-[(3S)-1-methylpyrrolidin-3-yl]oxy-4-(trifluoromethyl)anilineIC50620.0 [1], 1400.0 [2]
N-[(2-Bromophenyl)methyl]-3-[(3S)-1-methylpyrrolidin-3-yl]oxy-4-(trifluoromethyl)anilineIC50821.0 [1], 1870.0 [2]
N-[(3-Methoxyphenyl)methyl]-3-[(3S)-1-methylpyrrolidin-3-yl]oxy-4-(trifluoromethyl)anilineIC50691.0 [1], 1130.0 [2]



References

This online tool may be cited as follows

MLA

"Quest Database™ Urotensin II receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.9 May2024https://www.aatbio.com/data-sets/urotensin-ii-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 9). Quest Database™ Urotensin II receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/urotensin-ii-receptor-inhibitors-ic50-ki.
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