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Endothelin receptor ET-B Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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3-Benzo[1,3]dioxol-5-yl-5-hydroxy-5-(4-methoxy-phenyl)-4-(3,4,5-trimethoxy-benzyl)-5H-furan-2-oneIC50120.0 [1], 300.0 [2], 780.0 [3]
3-Benzo[1,3]dioxol-5-yl-5-hydroxy-5-(4-methoxy-phenyl)-4-(3,4,5-trimethoxy-benzyl)-5H-furan-2-oneKi139.0 [1]
BosentanIC5095.0 [1], 150.0 [2], 202.0 [3], 280.0 [4]
BosentanKi80.0 [1], 340.0 [2]
(1,1'-Biphenyl)-2-sulfonamide, N-(3,4-dimethyl-5-isoxazolyl)-4'-(2-oxazolyl)-Ki18700.0 [1]
A-216546 Free baseIC5013000.0 [1], 15400.0 [2], 16700.0 [3]
A-216546 Free baseKi13000.0 [1]
AtrasentanIC5063.3 [1], 88.0 [2], 515.0 [3]
Unii-0I32bcl40ZKi14.7 [1], 18.0 [2]
5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamideIC5014000.0 [1]
5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamideKi50000.0 [1]
(3S)-3-[[(2S)-2-[[(2S)-2-[[(1S,4S,7S,10R,13S,16R,19S,22R,25R,28R,31S,36R,39S,42R,45S)-31-Amino-7,13-bis(4-aminobutyl)-22-benzyl-4-(2-carboxyethyl)-10-(carboxymethyl)-28-[(1R)-1-hydroxyethyl]-19-[(1S)-1-hydroxyethyl]-16-[2-(4-hydroxyphenyl)ethyl]-39,42-bis[(4-hydroxyphenyl)methyl]-3,6,9,12,15,18,21,24,27,30,38,41,44,47-tetradecaoxo-45-propan-2-yl-33,34,49,50-tetrathia-2,5,8,11,14,17,20,23,26,29,37,40,43,46-tetradecazabicyclo[23.22.4]henpentacontane-36-carbonyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-[[(2S,3S)-1-[[(2S,3S)-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-oxobutanoic acidIC500.03 [1], 0.04 [2]
(3S)-3-[[(2S)-2-[[(2S)-2-[[(1S,4S,7S,10R,13S,16R,19S,22R,25R,28R,31S,36R,39S,42R,45S)-31-Amino-7,13-bis(4-aminobutyl)-22-benzyl-4-(2-carboxyethyl)-10-(carboxymethyl)-28-[(1R)-1-hydroxyethyl]-19-[(1S)-1-hydroxyethyl]-16-[2-(4-hydroxyphenyl)ethyl]-39,42-bis[(4-hydroxyphenyl)methyl]-3,6,9,12,15,18,21,24,27,30,38,41,44,47-tetradecaoxo-45-propan-2-yl-33,34,49,50-tetrathia-2,5,8,11,14,17,20,23,26,29,37,40,43,46-tetradecazabicyclo[23.22.4]henpentacontane-36-carbonyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-[[(2S,3S)-1-[[(2S,3S)-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-oxobutanoic acidKi0.05 [1]
3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxo-6-propoxyquinoline-2-carboxylic acidIC50913.4 [1], 2868.4 [2], 2870.0 [3]
Darusentan, (+/-)-Ki371.0 [1], 1000.0 [2]
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-Amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[(3S,6R,12R,15S,18R,24S,27R)-18-(2-amino-2-oxoethyl)-6-[(1R)-1-hydroxyethyl]-12-(1H-imidazol-4-ylmethyl)-15-(1H-indol-3-ylmethyl)-3-methyl-2,5,8,11,14,17,20,23,26-nonaoxo-1,4,7,10,13,16,19,22,25-nonazabicyclo[25.3.0]triacontan-24-yl]acetyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(1H-indol-3-yl)propanoic acidIC5010.0 [1], 7600.0 [2], 16000.0 [3]
EndothelinIC500.13 [1], 0.2 [2]
SitaxentanIC509.8 [1], 9800.0 [2]
Sodium;(Z)-2-(1,3-benzodioxol-5-yl)-4-(4-methoxyphenyl)-4-oxo-3-[(3,4,5-trimethoxyphenyl)methyl]but-2-enoateIC50417.0 [1]
Sodium;(Z)-2-(1,3-benzodioxol-5-yl)-4-(4-methoxyphenyl)-4-oxo-3-[(3,4,5-trimethoxyphenyl)methyl]but-2-enoateKi139.0 [1]
EnrasentanKi110.0 [1], 111.0 [2]
Sodium;[6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-5-(4-methylphenyl)pyrimidin-4-yl]-[4-(1-hydroxy-2-methylpropan-2-yl)phenyl]sulfonylazanideIC508.3 [1]
Sodium;[6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-5-(4-methylphenyl)pyrimidin-4-yl]-[4-(1-hydroxy-2-methylpropan-2-yl)phenyl]sulfonylazanideKi41.0 [1]
3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-6-hydroxy-4-oxoquinoline-2-carboxylic acidIC5015561.5 [1], 15602.3 [2]
(2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-2-(3-fluoro-4-methoxyphenyl)-1-[2-[pentylsulfonyl(propyl)amino]ethyl]pyrrolidine-3-carboxylic acidIC500.28 [1], 1.28 [2]
4-[1-(1,3-Benzodioxol-5-yl)-2-oxo-2-[(4-propan-2-ylphenyl)sulfonylamino]ethoxy]-3-propylbenzoic acidIC504.4 [1]
4-[1-(1,3-Benzodioxol-5-yl)-2-oxo-2-[(4-propan-2-ylphenyl)sulfonylamino]ethoxy]-3-propylbenzoic acidKi5.4 [1]
(3S)-3-[[(2S)-2-[[(2S)-2-Acetamido-3,3-diphenylpropanoyl]amino]-4-methylpentanoyl]amino]-4-[[(2S,3S)-1-[[(2S,3S)-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-oxobutanoic acidIC5060.0 [1], 960.0 [2]
N-[6-[2-(5-Bromopyrimidin-2-yl)oxyethoxy]-5-(4-methylphenyl)pyrimidin-4-yl]-4-tert-butylbenzenesulfonamideIC5038.0 [1]
N-[6-[2-(5-Bromopyrimidin-2-yl)oxyethoxy]-5-(4-methylphenyl)pyrimidin-4-yl]-4-tert-butylbenzenesulfonamideKi130.0 [1]
3-[(4-Chloro-3-methyl-1,2-oxazol-5-yl)sulfamoyl]-N-(4-methylphenyl)thiophene-2-carboxamideIC5014100.0 [1]
N-(1,3-Benzodioxol-5-yl)-3-[(4-bromo-3-methyl-1,2-oxazol-5-yl)sulfamoyl]thiophene-2-carboxamideIC5010100.0 [1]
N-[[2-[2-[(3,4-Dimethyl-1,2-oxazol-5-yl)sulfamoyl]phenyl]-5-(1,3-oxazol-2-yl)phenyl]methyl]acetamideKi4400.0 [1]
5-Hydroxy-4-(4-methoxy-benzyl)-5-(4-methoxy-phenyl)-3-phenyl-5H-furan-2-oneIC502500.0 [1]
3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-(3,4-dichlorophenyl)-5-hydroxyfuran-2-oneIC5025000.0 [1]
5-Hydroxy-4-(4-methoxy-benzyl)-5-(4-methoxy-phenyl)-3-p-tolyl-5H-furan-2-oneIC502500.0 [1], 2700.0 [2]
3-Benzo[1,3]dioxol-5-yl-4-benzyl-5-(4-chloro-phenyl)-5-hydroxy-5H-furan-2-oneIC502700.0 [1], 27000.0 [2]
(2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-[butylsulfonyl(propyl)amino]ethyl]-2-(3-fluoro-4-methoxyphenyl)pyrrolidine-3-carboxylic acidIC500.47 [1], 0.6 [2]
3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-hydroxy-5-(4-methoxy-3-methylphenyl)furan-2-oneIC501750.0 [1]
5-Hydroxy-4-(4-methoxy-benzyl)-3,5-bis-(4-methoxy-phenyl)-5H-furan-2-oneIC502500.0 [1], 9000.0 [2]
3-(3,4-Dichlorophenyl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methoxyphenyl)methyl]furan-2-oneIC502500.0 [1], 2700.0 [2]
3-[(4-Chloro-3-methyl-1,2-oxazol-5-yl)sulfamoyl]-N-(4-methoxy-2-methylphenyl)thiophene-2-carboxamideIC5014000.0 [1]
3-Benzo[1,3]dioxol-5-yl-4-benzyl-5-hydroxy-5-(4-methoxy-phenyl)-5H-furan-2-oneIC504550.0 [1]
3-(1,3-Benzodioxol-5-yl)-4-[(4-chlorophenyl)methyl]-5-hydroxy-5-(4-methoxyphenyl)furan-2-oneIC502500.0 [1]
3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-hydroxy-5-phenylfuran-2-oneIC5030000.0 [1]
3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxo-6-prop-2-enoxyquinoline-2-carboxylic acidIC501131.0 [1], 1131.2 [2]
3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-6-(methoxymethoxy)-4-oxoquinoline-2-carboxylic acidIC501030.0 [1], 1030.2 [2]
6-Butoxy-3-[(3-carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxoquinoline-2-carboxylic acidIC50548.2 [1]
3-(1,3-Benzodioxol-5-yl)-1-(1,3-benzodioxol-5-ylmethyl)-5-propoxyindole-2-carboxylic acidIC50850.0 [1], 1600.0 [2]
3-(1,3-Benzodioxol-5-yl)-1-(1,3-benzodioxol-5-ylmethyl)-5,6-dimethoxyindole-2-carboxylic acidIC501200.0 [1], 1400.0 [2]
Bosentan sodiumIC50310.0 [1]
Bosentan sodiumKi140.0 [1]
3-[(3-Carboxyphenyl)methyl]-6-ethoxy-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxoquinoline-2-carboxylic acidIC503119.0 [1]
3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-6-(2-methylpropoxy)-4-oxoquinoline-2-carboxylic acidIC50713.0 [1], 1983.0 [2]
3-(1,3-Benzodioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methylphenyl)methyl]furan-2-oneIC50390.0 [1], 2500.0 [2]
3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-hydroxy-5-(4-methylphenyl)furan-2-oneIC5025000.0 [1]
3-(1,3-Benzodioxol-5-yl)-5-hydroxy-4-[(4-methoxy-3-methylphenyl)methyl]-5-(4-methoxyphenyl)furan-2-oneIC501140.0 [1]
2-(1,3-Benzodioxol-5-yl)-2-[4-[(2-ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]-2-propylphenoxy]-N-(4-propan-2-ylphenyl)sulfonylacetamideIC5060.0 [1]
N-[(2R)-1-[[(2S)-1-(Butylsulfonylamino)-3-methyl-1-oxobutan-2-yl]amino]-3-[4-(1,2-oxazol-5-yl)phenyl]-1-oxopropan-2-yl]-N,3,5-trimethylbenzamideKi1.2 [1]
3-(1,3-Benzodioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methoxyphenyl)methyl]furan-2-oneIC501550.0 [1]
3-(4-Chlorophenyl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methoxyphenyl)methyl]furan-2-oneIC502500.0 [1]
(2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-2-(3-fluoro-4-methoxyphenyl)-1-[2-[hexylsulfonyl(propyl)amino]ethyl]pyrrolidine-3-carboxylic acidIC500.48 [1], 1.12 [2]
(2S,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(2,2-dimethylpentyl)pyrrolidine-3-carboxylic acidIC502800.0 [1], 62000.0 [2]
3-[1-(1,3-Benzodioxol-5-yl)-2-[(2-methoxy-4-methylphenyl)sulfonylamino]-2-oxoethyl]-1-methylindole-6-carboxamideIC50275.0 [1], 302.0 [2]
3-Methoxy-2-[(4-methoxy-6,7-dihydro-5H-cyclopenta[d]pyrimidin-2-yl)oxy]-3,3-diphenylpropanoic acidKi20.4 [1], 56.0 [2]
3-[(4-Bromo-3-methyl-1,2-oxazol-5-yl)sulfamoyl]-N-phenylthiophene-2-carboxamideIC5077600.0 [1]
(2S,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(2-pyrazol-1-ylethyl)pyrrolidine-3-carboxylic acidIC5028600.0 [1], 42000.0 [2]
(2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-[3-chloropropylsulfonyl(propyl)amino]ethyl]-2-(3-fluoro-4-methoxyphenyl)pyrrolidine-3-carboxylic acidIC500.14 [1], 0.83 [2]
(2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-2-(3-fluoro-4-methoxyphenyl)-1-[2-[propyl(4,4,4-trifluorobutylsulfonyl)amino]ethyl]pyrrolidine-3-carboxylic acidIC500.2 [1], 1.46 [2]
3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-methoxy-5-(4-methoxyphenyl)furan-2(5H)-oneIC5025000.0 [1]
3-[1-(1,3-Benzodioxol-5-yl)-2-oxo-2-[(4-propan-2-ylphenyl)sulfonylamino]ethyl]-1-ethylindole-6-carboxylic acidIC5069.0 [1], 2200.0 [2]
2-(2,5-Dibromo-3,4-dimethoxyphenyl)-2-[4-[(2-ethyl-5,7-dimethylimidazo[4,5-b]pyridin-3-yl)methyl]-2,6-dipropylphenoxy]acetic acidIC5031000.0 [1]
3-[1-(1,3-Benzodioxol-5-yl)-2-oxo-2-[(4-propan-2-ylphenyl)sulfonylamino]ethyl]-1-methylindole-6-carboxamideIC5015.0 [1], 34.0 [2]
(2S,3R,4S)-1-[2-(Dibutylamino)-2-oxoethyl]-2-[(Z)-2,2-dimethylpent-3-enyl]-4-(7-methoxy-1,3-benzodioxol-5-yl)pyrrolidine-3-carboxylic acidIC5039700.0 [1], 45300.0 [2]
(2S,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-[(Z)-2,2-dimethylpent-3-enyl]pyrrolidine-3-carboxylic acidIC5092700.0 [1], 100000.0 [2]
[(5R,9As,9bS)-1,9b-dihydroxy-6,6,9a-trimethyl-3,5,5a,7,8,9-hexahydro-1H-benzo[e][2]benzofuran-5-yl] (2E,4E)-hexa-2,4-dienoateIC5070000.0 [1], 148000.0 [2]
[(5R,9As,9bS)-1,9b-dihydroxy-6,6,9a-trimethyl-3,5,5a,7,8,9-hexahydro-1H-benzo[e][2]benzofuran-5-yl] (2E,4E,6E)-octa-2,4,6-trienoateIC5021000.0 [1], 41000.0 [2]
[(5R,9As,9bS)-9b-hydroxy-6,6,9a-trimethyl-1-oxo-3,5,5a,7,8,9-hexahydrobenzo[e][2]benzofuran-5-yl] (2E,4E,6E)-octa-2,4,6-trienoateIC5050000.0 [1], 73000.0 [2]
(2S,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-[2-(2-oxopyrrolidin-1-yl)ethyl]pyrrolidine-3-carboxylic acidIC5018000.0 [1], 65400.0 [2]
3-Methoxy-3,3-diphenyl-2-[(4-methoxy-6-methylpyrimidin-2-yl)oxy]propanoic acidKi19.7 [1], 29.0 [2]
(2S,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(2-pyridin-2-ylethyl)pyrrolidine-3-carboxylic acidIC5026000.0 [1], 32000.0 [2]
4-Benzo[1,3]dioxol-5-yl-1-dibutylcarbamoylmethyl-2-(4-methoxy-phenyl)-pyrrolidine-3-carboxylic acidIC5098.0 [1]
4-Benzo[1,3]dioxol-5-yl-1-dibutylcarbamoylmethyl-2-(4-methoxy-phenyl)-pyrrolidine-3-carboxylic acidKi139.0 [1]
3-[1-(1,3-Benzodioxol-5-yl)-2-[(2-ethoxy-4-methylphenyl)sulfonylamino]-2-oxoethyl]-1-methylindole-6-carboxamideIC50397.0 [1]
3-Methoxy-2-(4-methoxy-5,6-dihydro-furo[2,3-d]pyrimidin-2-yloxy)-3,3-diphenyl-propionic acidKi24.5 [1], 57.0 [2]
5-Benzyloxy-3-isopropoxy-benzo[b]thiophene-2-carboxylic acidIC50100000.0 [1]
1-Benzo[1,3]dioxol-5-ylmethyl-5,6-dimethoxy-3-(3-methoxy-phenylsulfanyl)-1H-indole-2-carboxylic acidIC50210.0 [1], 1100.0 [2]
N-(4-Bromo-3-methyl-1,2-oxazol-5-yl)-2-phenylbenzenesulfonamideIC507900.0 [1], 100000.0 [2]
N-(4-Bromo-3-methyl-isoxazol-5-yl)-benzenesulfonamideIC5020000.0 [1], 100000.0 [2]
1-(1,3-Benzodioxol-5-ylmethyl)-3-(1,3-benzodioxol-5-ylsulfanyl)-5-methoxy-6-phenylmethoxyindole-2-carboxylic acidIC50490.0 [1], 740.0 [2]
5-(1,3-Benzodioxol-5-ylmethyl)-7-(3,4,5-trimethoxyphenyl)sulfanyl-[1,3]dioxolo[4,5-f]indole-6-carboxylic acidIC50170.0 [1], 230.0 [2]
5-(1,3-Benzodioxol-5-ylmethyl)-7-(3,4-dimethoxyphenyl)sulfanyl-[1,3]dioxolo[4,5-f]indole-6-carboxylic acidIC50170.0 [1]
1-(1,3-Benzodioxol-5-ylmethyl)-5,6-dimethoxy-3-(3,4,5-trimethoxyphenyl)sulfanylindole-2-carboxylic acidIC50380.0 [1], 440.0 [2]
1,3-Benzodioxol-5-yl 3-[(4-bromo-3-methyl-1,2-oxazol-5-yl)sulfamoyl]thiophene-2-carboxylateIC505700.0 [1], 5740.0 [2]
1-(1,3-Benzodioxol-5-ylmethyl)-3-(1,3-benzodioxol-5-ylsulfanyl)-5,6-dimethoxyindole-2-carboxylic acidIC50280.0 [1], 1100.0 [2]
Cyclo(D-trp-D-asp-pro-D-val-leu)IC501000.0 [1]
SulfisoxazoleIC5024000.0 [1]
AmbrisentanIC501190.0 [1]
DarusentanIC5016.0 [1]
(+/-)-AmbrisentanKi195.0 [1]
Items per page: 1 - 10 of 100
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References

This online tool may be cited as follows

MLA

"Quest Database™ Endothelin receptor ET-B Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 20 Nov. 2024, https://www.aatbio.com/data-sets/endothelin-receptor-et-b-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, November 20). Quest Database™ Endothelin receptor ET-B Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/endothelin-receptor-et-b-inhibitors-ic50-ki.
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