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Endothelin receptor ET-A 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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▼
EndothelinIC500.05 [1], 0.2 [2], 0.38 [3]
EndothelinKi0.14 [1]
BosentanIC5040.0 [1]
BosentanKi6.5 [1], 8.0 [2]
5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamideIC505.8 [1], 50.12 [2], 150.0 [3], 570.0 [4]
5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamideKi48.0 [1], 55.0 [2]
3-Benzo[1,3]dioxol-5-yl-5-hydroxy-5-(4-methoxy-phenyl)-4-(3,4,5-trimethoxy-benzyl)-5H-furan-2-oneIC500.3 [1], 0.37 [2], 1.1 [3]
3-Benzo[1,3]dioxol-5-yl-5-hydroxy-5-(4-methoxy-phenyl)-4-(3,4,5-trimethoxy-benzyl)-5H-furan-2-oneKi0.17 [1]
(1,1'-Biphenyl)-2-sulfonamide, N-(3,4-dimethyl-5-isoxazolyl)-4'-(2-oxazolyl)-Ki1.4 [1]
AtrasentanIC500.03 [1], 0.08 [2], 0.31 [3]
AtrasentanKi0.03 [1]
SitaxentanIC501.4 [1]
SitaxentanKi0.43 [1]
Bms-248360IC502.0 [1]
Bms-248360Ki1.9 [1], 2.0 [2]
SulfisoxazoleIC50780.0 [1], 850.0 [2]
SulfisoxazoleKi13465.0 [1]
A-216546 Free baseIC500.49 [1], 24900.0 [2]
A-216546 Free baseKi0.46 [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 acidIC5015.0 [1], 40.0 [2], 58.0 [3], 70.0 [4]
3-[(4-Chloro-3-methyl-1,2-oxazol-5-yl)sulfamoyl]-N-(2,4,6-trimethylphenyl)thiophene-2-carboxamideIC500.15 [1], 0.17 [2], 0.63 [3], 630.0 [4]
(3S)-3-[[(2S)-2-[[(2R)-2-Acetamido-3-(1H-imidazol-5-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 acidIC508900.0 [1], 9500.0 [2]
3-Benzo[1,3]dioxol-5-yl-4-benzyl-5-(4-chloro-phenyl)-5-hydroxy-5H-furan-2-oneIC50430.0 [1], 2200.0 [2], 3800.0 [3]
5-Benzyloxy-3-isopropoxy-benzo[b]thiophene-2-carboxylic acidIC506000.0 [1], 8800.0 [2]
IrbesartanKi0.0 [1], 10000.0 [2]
Cyclo(D-trp-D-asp-pro-D-val-leu)IC5020.5 [1], 24.8 [2], 37.0 [3]
Unii-0I32bcl40ZKi0.2 [1], 0.43 [2]
(2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-2-(3-fluoro-4-methoxyphenyl)-1-[2-[pentylsulfonyl(propyl)amino]ethyl]pyrrolidine-3-carboxylic acidIC500.08 [1], 0.48 [2]
(3S)-3-[[(2S)-2-[[(2S)-2-Acetamido-3-(1H-imidazol-5-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 acidIC5050000.0 [1]
3-[(4-Chloro-3-methyl-1,2-oxazol-5-yl)sulfamoyl]-N-(4-methylphenyl)thiophene-2-carboxamideIC5015.0 [1]
N-(1,3-Benzodioxol-5-yl)-3-[(4-bromo-3-methyl-1,2-oxazol-5-yl)sulfamoyl]thiophene-2-carboxamideIC5019.0 [1]
5-Hydroxy-4-(4-methoxy-benzyl)-5-(4-methoxy-phenyl)-3-phenyl-5H-furan-2-oneIC502000.0 [1], 2200.0 [2]
3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-(3,4-dichlorophenyl)-5-hydroxyfuran-2-oneIC50400.0 [1], 560.0 [2]
5-Hydroxy-4-(4-methoxy-benzyl)-5-(4-methoxy-phenyl)-3-p-tolyl-5H-furan-2-oneIC50570.0 [1], 750.0 [2]
3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-hydroxy-5-(4-methoxy-3-methylphenyl)furan-2-oneIC5012.0 [1]
5-Hydroxy-4-(4-methoxy-benzyl)-3,5-bis-(4-methoxy-phenyl)-5H-furan-2-oneIC50190.0 [1], 310.0 [2]
3-(3,4-Dichlorophenyl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methoxyphenyl)methyl]furan-2-oneIC50170.0 [1], 310.0 [2]
3-Benzo[1,3]dioxol-5-yl-4-benzyl-5-hydroxy-5-(4-methoxy-phenyl)-5H-furan-2-oneIC507.4 [1], 50.0 [2]
3-(1,3-Benzodioxol-5-yl)-4-[(4-chlorophenyl)methyl]-5-hydroxy-5-(4-methoxyphenyl)furan-2-oneIC50110.0 [1], 140.0 [2]
(3S)-3-[[(2S)-2-[[(2R)-2-Acetamido-3-phenylpropanoyl]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 acidIC501800.0 [1], 2800.0 [2], 10000.0 [3]
3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxo-6-propoxyquinoline-2-carboxylic acidIC500.11 [1], 4.0 [2], 4.2 [3]
3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-hydroxy-5-phenylfuran-2-oneIC50600.0 [1], 1300.0 [2]
(3S)-3-[[(2S)-2-[[(2S)-2-Acetamido-2-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,11,13-hexaenyl)acetyl]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 acidIC503.5 [1], 4.0 [2], 4.9 [3]
3-(1,3-Benzodioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methylphenyl)methyl]furan-2-oneIC5050.0 [1], 51.0 [2]
3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-hydroxy-5-(4-methylphenyl)furan-2-oneIC501200.0 [1], 4900.0 [2]
3-(1,3-Benzodioxol-5-yl)-5-hydroxy-4-[(4-methoxy-3-methylphenyl)methyl]-5-(4-methoxyphenyl)furan-2-oneIC502.4 [1], 6.0 [2]
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)sulfonylacetamideIC5024.0 [1]
3-(1,3-Benzodioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methoxyphenyl)methyl]furan-2-oneIC501.8 [1], 9.0 [2]
3-(4-Chlorophenyl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methoxyphenyl)methyl]furan-2-oneIC50700.0 [1], 960.0 [2]
Methyl 2-(1,3-benzodioxol-5-yl)-2-(1,2,3,4-tetrahydroacridin-9-yl)acetateIC507300.0 [1], 11000.0 [2], 12000.0 [3]
2-Acridin-9-yl-2-benzo[1,3]dioxol-5-yl-ethanolIC50900.0 [1], 10000.0 [2]
2-Acridin-9-yl-2-benzo[1,3]dioxol-5-yl-acetamideIC507900.0 [1], 8500.0 [2], 77000.0 [3]
Acridin-9-yl-benzo[1,3]dioxol-5-yl-acetic acid methyl esterIC502800.0 [1], 4300.0 [2], 5800.0 [3]
1,3-Benzodioxol-5-yl 3-[(4-bromo-3-methyl-1,2-oxazol-5-yl)sulfamoyl]thiophene-2-carboxylateIC508.9 [1], 8900.0 [2]
Endothelin-1IC500.02 [1]
2-[(3S,6R,9S,12R,15S)-6-(1H-Indol-3-ylmethyl)-9-(2-methylpropyl)-2,5,8,11,14-pentaoxo-12-propan-2-yl-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-3-yl]acetic acidIC5022.0 [1]
2-[(3S,6R,9S,12R,15S)-6-(1H-Indol-3-ylmethyl)-9-(2-methylpropyl)-2,5,8,11,14-pentaoxo-12-propan-2-yl-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-3-yl]acetic acidKi18.0 [1]
Sodium;(Z)-2-(1,3-benzodioxol-5-yl)-4-(4-methoxyphenyl)-4-oxo-3-[(3,4,5-trimethoxyphenyl)methyl]but-2-enoateIC500.31 [1]
Sodium;(Z)-2-(1,3-benzodioxol-5-yl)-4-(4-methoxyphenyl)-4-oxo-3-[(3,4,5-trimethoxyphenyl)methyl]but-2-enoateKi0.17 [1]
Acetyldiphenylalanyl-leucyl-aspartyl-isoleucyl-isoleucyl-tryptophanIC503500.0 [1], 4400.0 [2]
EnrasentanKi1.1 [1]
Histidyl-leucyl-aspartyl-isoleucyl-isoleucyl-tryptophanIC5050000.0 [1]
3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-6-hydroxy-4-oxoquinoline-2-carboxylic acidIC5037.01 [1], 38.9 [2]
N-(2-Acetyl-4,6-dimethylphenyl)-3-[(4-chloro-3-methyl-1,2-oxazol-5-yl)sulfamoyl]thiophene-2-carboxamideIC500.04 [1]
SparsentanKi9.3 [1]
4-[1-(1,3-Benzodioxol-5-yl)-2-oxo-2-[(4-propan-2-ylphenyl)sulfonylamino]ethoxy]-3-propylbenzoic acidIC500.26 [1]
4-[1-(1,3-Benzodioxol-5-yl)-2-oxo-2-[(4-propan-2-ylphenyl)sulfonylamino]ethoxy]-3-propylbenzoic acidKi0.13 [1]
N-(3,4-Dimethyl-1,2-oxazol-5-yl)naphthalene-1-sulfonamideIC50440.0 [1], 20000.0 [2]
N-[[2-[2-[(3,4-Dimethyl-1,2-oxazol-5-yl)sulfamoyl]phenyl]-5-(1,3-oxazol-2-yl)phenyl]methyl]acetamideKi0.2 [1]
2-[2-(1,3-Benzodioxol-5-yl)acetyl]-N-(4-chloro-3-methyl-1,2-oxazol-5-yl)thiophene-3-sulfonamideIC5018.0 [1], 21.0 [2]
(2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-[butylsulfonyl(propyl)amino]ethyl]-2-(3-fluoro-4-methoxyphenyl)pyrrolidine-3-carboxylic acidIC500.04 [1], 0.38 [2]
3-[(4-Chloro-3-methyl-1,2-oxazol-5-yl)sulfamoyl]-N-(6-cyano-1,3-benzodioxol-5-yl)thiophene-2-carboxamideIC503.4 [1]
N-(3,4-Dimethyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamideIC503.3 [1]
3-[(4-Chloro-3-methyl-1,2-oxazol-5-yl)sulfamoyl]-N-(4-methoxy-2-methylphenyl)thiophene-2-carboxamideIC502.6 [1]
N-(6-Acetyl-1,3-benzodioxol-5-yl)-3-[(4-chloro-3-methyl-1,2-oxazol-5-yl)sulfamoyl]thiophene-2-carboxamideIC5010.0 [1]
(3S)-3-[[(2S)-2-[[(2R)-2-Acetamido-3-naphthalen-2-ylpropanoyl]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 acidIC501000.0 [1]
3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxo-6-prop-2-enoxyquinoline-2-carboxylic acidIC5038.1 [1]
3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-6-(methoxymethoxy)-4-oxoquinoline-2-carboxylic acidIC5024.4 [1]
6-Butoxy-3-[(3-carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxoquinoline-2-carboxylic acidIC501.44 [1], 1.88 [2]
3-(1,3-Benzodioxol-5-yl)-1-(1,3-benzodioxol-5-ylmethyl)-5-propoxyindole-2-carboxylic acidIC5080.0 [1], 250.0 [2]
3-(1,3-Benzodioxol-5-yl)-1-(1,3-benzodioxol-5-ylmethyl)-5,6-dimethoxyindole-2-carboxylic acidIC5060.0 [1], 150.0 [2]
(3S)-3-[[(2S)-2-[[(2R)-2-Acetamido-3-(4-hydroxyphenyl)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 acidIC50400.0 [1], 7000.0 [2]
3-[(3-Carboxyphenyl)methyl]-6-ethoxy-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxoquinoline-2-carboxylic acidIC506.6 [1]
3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-6-(2-methylpropoxy)-4-oxoquinoline-2-carboxylic acidIC506.3 [1], 9.9 [2]
3-[(3-Carboxyphenyl)methyl]-6-(cyclopropylmethoxy)-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxoquinoline-2-carboxylic acidIC50115.9 [1], 121.3 [2]
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-trimethylbenzamideKi1.5 [1], 1.8 [2]
Darusentan, (+/-)-Ki6.0 [1]
(2S)-2-[[(2S,3S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-Acetamido-3,3-diphenylpropanoyl]amino]-4-methylpentanoyl]amino]-6-aminohexanoyl]amino]-3-methylpentanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-indol-3-yl)propanoic acidIC50430.0 [1], 480.0 [2]
N-(3,4-Dimethyl-1,2-oxazol-5-yl)-2-[2-(hydroxymethyl)-4-[(4-oxo-2-propyl-5,6,7,8-tetrahydrocyclohepta[d]imidazol-3-yl)methyl]phenyl]benzenesulfonamideIC5014.0 [1]
N-(3,4-Dimethyl-1,2-oxazol-5-yl)-2-[2-(hydroxymethyl)-4-[(4-oxo-2-propyl-5,6,7,8-tetrahydrocyclohepta[d]imidazol-3-yl)methyl]phenyl]benzenesulfonamideKi14.0 [1]
N-(3,4-Dimethyl-1,2-oxazol-5-yl)-2-[2-methyl-4-[(4-oxo-2-propyl-5,6,7,8-tetrahydrocyclohepta[d]imidazol-3-yl)methyl]phenyl]benzenesulfonamideIC5013.0 [1]
N-(3,4-Dimethyl-1,2-oxazol-5-yl)-2-[2-methyl-4-[(4-oxo-2-propyl-5,6,7,8-tetrahydrocyclohepta[d]imidazol-3-yl)methyl]phenyl]benzenesulfonamideKi13.0 [1]
(2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-2-(3-fluoro-4-methoxyphenyl)-1-[2-[hexylsulfonyl(propyl)amino]ethyl]pyrrolidine-3-carboxylic acidIC500.08 [1], 0.14 [2]
2-Butyl-5-chloro-3-[[4-[2-[(3,4-dimethyl-1,2-oxazol-5-yl)sulfamoyl]phenyl]phenyl]methyl]imidazole-4-carboxamideIC50415.0 [1]
2-Butyl-5-chloro-3-[[4-[2-[(3,4-dimethyl-1,2-oxazol-5-yl)sulfamoyl]phenyl]phenyl]methyl]imidazole-4-carboxamideKi415.0 [1]
3-[1-(1,3-Benzodioxol-5-yl)-2-[(2-methoxy-4-methylphenyl)sulfonylamino]-2-oxoethyl]-1-methylindole-6-carboxamideIC501.1 [1]
(3S)-3-[[(2S)-2-[[(2S)-2-Acetamido-3,3-diphenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]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 acidIC504.0 [1], 14.0 [2]
3-[(4-Bromo-3-methyl-1,2-oxazol-5-yl)sulfamoyl]-N-phenylthiophene-2-carboxamideIC50166.0 [1]
(2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-[3-chloropropylsulfonyl(propyl)amino]ethyl]-2-(3-fluoro-4-methoxyphenyl)pyrrolidine-3-carboxylic acidIC500.07 [1], 0.55 [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 acidIC500.06 [1], 1.66 [2]
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-A Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Dec. 2024, https://www.aatbio.com/data-sets/endothelin-receptor-et-a-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, December 21). Quest Database™ Endothelin receptor ET-A Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/endothelin-receptor-et-a-inhibitors-ic50-ki.
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