 | Endothelin | IC50 | 0.05 [1], 0.2 [2], 0.38 [3] |
| Endothelin | Ki | 0.14 [1] |
 | Bosentan | IC50 | 40.0 [1] |
| Bosentan | Ki | 6.5 [1], 8.0 [2] |
 | 5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide | IC50 | 5.8 [1], 50.12 [2], 150.0 [3], 570.0 [4] |
| 5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide | Ki | 48.0 [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-one | IC50 | 0.3 [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-one | Ki | 0.17 [1] |
 | (1,1'-Biphenyl)-2-sulfonamide, N-(3,4-dimethyl-5-isoxazolyl)-4'-(2-oxazolyl)- | Ki | 1.4 [1] |
 | Atrasentan | IC50 | 0.03 [1], 0.08 [2], 0.31 [3] |
| Atrasentan | Ki | 0.03 [1] |
 | Sitaxentan | IC50 | 1.4 [1] |
| Sitaxentan | Ki | 0.43 [1] |
 | Bms-248360 | IC50 | 2.0 [1] |
| Bms-248360 | Ki | 1.9 [1], 2.0 [2] |
 | Sulfisoxazole | IC50 | 780.0 [1], 850.0 [2] |
| Sulfisoxazole | Ki | 13465.0 [1] |
 | A-216546 Free base | IC50 | 0.49 [1], 24900.0 [2] |
| A-216546 Free base | Ki | 0.46 [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 acid | IC50 | 15.0 [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-carboxamide | IC50 | 0.15 [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 acid | IC50 | 8900.0 [1], 9500.0 [2] |
 | 3-Benzo[1,3]dioxol-5-yl-4-benzyl-5-(4-chloro-phenyl)-5-hydroxy-5H-furan-2-one | IC50 | 430.0 [1], 2200.0 [2], 3800.0 [3] |
 | 5-Benzyloxy-3-isopropoxy-benzo[b]thiophene-2-carboxylic acid | IC50 | 6000.0 [1], 8800.0 [2] |
 | Irbesartan | Ki | 0.0 [1], 10000.0 [2] |
 | Cyclo(D-trp-D-asp-pro-D-val-leu) | IC50 | 20.5 [1], 24.8 [2], 37.0 [3] |
 | Unii-0I32bcl40Z | Ki | 0.2 [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 acid | IC50 | 0.08 [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 acid | IC50 | 50000.0 [1] |
 | 3-[(4-Chloro-3-methyl-1,2-oxazol-5-yl)sulfamoyl]-N-(4-methylphenyl)thiophene-2-carboxamide | IC50 | 15.0 [1] |
 | N-(1,3-Benzodioxol-5-yl)-3-[(4-bromo-3-methyl-1,2-oxazol-5-yl)sulfamoyl]thiophene-2-carboxamide | IC50 | 19.0 [1] |
 | 5-Hydroxy-4-(4-methoxy-benzyl)-5-(4-methoxy-phenyl)-3-phenyl-5H-furan-2-one | IC50 | 2000.0 [1], 2200.0 [2] |
 | 3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-(3,4-dichlorophenyl)-5-hydroxyfuran-2-one | IC50 | 400.0 [1], 560.0 [2] |
 | 5-Hydroxy-4-(4-methoxy-benzyl)-5-(4-methoxy-phenyl)-3-p-tolyl-5H-furan-2-one | IC50 | 570.0 [1], 750.0 [2] |
 | 3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-hydroxy-5-(4-methoxy-3-methylphenyl)furan-2-one | IC50 | 12.0 [1] |
 | 5-Hydroxy-4-(4-methoxy-benzyl)-3,5-bis-(4-methoxy-phenyl)-5H-furan-2-one | IC50 | 190.0 [1], 310.0 [2] |
 | 3-(3,4-Dichlorophenyl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methoxyphenyl)methyl]furan-2-one | IC50 | 170.0 [1], 310.0 [2] |
 | 3-Benzo[1,3]dioxol-5-yl-4-benzyl-5-hydroxy-5-(4-methoxy-phenyl)-5H-furan-2-one | IC50 | 7.4 [1], 50.0 [2] |
 | 3-(1,3-Benzodioxol-5-yl)-4-[(4-chlorophenyl)methyl]-5-hydroxy-5-(4-methoxyphenyl)furan-2-one | IC50 | 110.0 [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 acid | IC50 | 1800.0 [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 acid | IC50 | 0.11 [1], 4.0 [2], 4.2 [3] |
 | 3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-hydroxy-5-phenylfuran-2-one | IC50 | 600.0 [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 acid | IC50 | 3.5 [1], 4.0 [2], 4.9 [3] |
 | 3-(1,3-Benzodioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methylphenyl)methyl]furan-2-one | IC50 | 50.0 [1], 51.0 [2] |
 | 3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-hydroxy-5-(4-methylphenyl)furan-2-one | IC50 | 1200.0 [1], 4900.0 [2] |
 | 3-(1,3-Benzodioxol-5-yl)-5-hydroxy-4-[(4-methoxy-3-methylphenyl)methyl]-5-(4-methoxyphenyl)furan-2-one | IC50 | 2.4 [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)sulfonylacetamide | IC50 | 24.0 [1] |
 | 3-(1,3-Benzodioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methoxyphenyl)methyl]furan-2-one | IC50 | 1.8 [1], 9.0 [2] |
 | 3-(4-Chlorophenyl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methoxyphenyl)methyl]furan-2-one | IC50 | 700.0 [1], 960.0 [2] |
 | Methyl 2-(1,3-benzodioxol-5-yl)-2-(1,2,3,4-tetrahydroacridin-9-yl)acetate | IC50 | 7300.0 [1], 11000.0 [2], 12000.0 [3] |
 | 2-Acridin-9-yl-2-benzo[1,3]dioxol-5-yl-ethanol | IC50 | 900.0 [1], 10000.0 [2] |
 | 2-Acridin-9-yl-2-benzo[1,3]dioxol-5-yl-acetamide | IC50 | 7900.0 [1], 8500.0 [2], 77000.0 [3] |
 | Acridin-9-yl-benzo[1,3]dioxol-5-yl-acetic acid methyl ester | IC50 | 2800.0 [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-carboxylate | IC50 | 8.9 [1], 8900.0 [2] |
 | Endothelin-1 | IC50 | 0.02 [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 acid | IC50 | 22.0 [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 acid | Ki | 18.0 [1] |
 | Sodium;(Z)-2-(1,3-benzodioxol-5-yl)-4-(4-methoxyphenyl)-4-oxo-3-[(3,4,5-trimethoxyphenyl)methyl]but-2-enoate | IC50 | 0.31 [1] |
| Sodium;(Z)-2-(1,3-benzodioxol-5-yl)-4-(4-methoxyphenyl)-4-oxo-3-[(3,4,5-trimethoxyphenyl)methyl]but-2-enoate | Ki | 0.17 [1] |
 | Acetyldiphenylalanyl-leucyl-aspartyl-isoleucyl-isoleucyl-tryptophan | IC50 | 3500.0 [1], 4400.0 [2] |
 | Enrasentan | Ki | 1.1 [1] |
 | Histidyl-leucyl-aspartyl-isoleucyl-isoleucyl-tryptophan | IC50 | 50000.0 [1] |
 | 3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-6-hydroxy-4-oxoquinoline-2-carboxylic acid | IC50 | 37.01 [1], 38.9 [2] |
 | N-(2-Acetyl-4,6-dimethylphenyl)-3-[(4-chloro-3-methyl-1,2-oxazol-5-yl)sulfamoyl]thiophene-2-carboxamide | IC50 | 0.04 [1] |
 | Sparsentan | Ki | 9.3 [1] |
 | 4-[1-(1,3-Benzodioxol-5-yl)-2-oxo-2-[(4-propan-2-ylphenyl)sulfonylamino]ethoxy]-3-propylbenzoic acid | IC50 | 0.26 [1] |
| 4-[1-(1,3-Benzodioxol-5-yl)-2-oxo-2-[(4-propan-2-ylphenyl)sulfonylamino]ethoxy]-3-propylbenzoic acid | Ki | 0.13 [1] |
 | N-(3,4-Dimethyl-1,2-oxazol-5-yl)naphthalene-1-sulfonamide | IC50 | 440.0 [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]acetamide | Ki | 0.2 [1] |
 | 2-[2-(1,3-Benzodioxol-5-yl)acetyl]-N-(4-chloro-3-methyl-1,2-oxazol-5-yl)thiophene-3-sulfonamide | IC50 | 18.0 [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 acid | IC50 | 0.04 [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-carboxamide | IC50 | 3.4 [1] |
 | N-(3,4-Dimethyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamide | IC50 | 3.3 [1] |
 | 3-[(4-Chloro-3-methyl-1,2-oxazol-5-yl)sulfamoyl]-N-(4-methoxy-2-methylphenyl)thiophene-2-carboxamide | IC50 | 2.6 [1] |
 | N-(6-Acetyl-1,3-benzodioxol-5-yl)-3-[(4-chloro-3-methyl-1,2-oxazol-5-yl)sulfamoyl]thiophene-2-carboxamide | IC50 | 10.0 [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 acid | IC50 | 1000.0 [1] |
 | 3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxo-6-prop-2-enoxyquinoline-2-carboxylic acid | IC50 | 38.1 [1] |
 | 3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-6-(methoxymethoxy)-4-oxoquinoline-2-carboxylic acid | IC50 | 24.4 [1] |
 | 6-Butoxy-3-[(3-carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxoquinoline-2-carboxylic acid | IC50 | 1.44 [1], 1.88 [2] |
 | 3-(1,3-Benzodioxol-5-yl)-1-(1,3-benzodioxol-5-ylmethyl)-5-propoxyindole-2-carboxylic acid | IC50 | 80.0 [1], 250.0 [2] |
 | 3-(1,3-Benzodioxol-5-yl)-1-(1,3-benzodioxol-5-ylmethyl)-5,6-dimethoxyindole-2-carboxylic acid | IC50 | 60.0 [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 acid | IC50 | 400.0 [1], 7000.0 [2] |
 | 3-[(3-Carboxyphenyl)methyl]-6-ethoxy-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxoquinoline-2-carboxylic acid | IC50 | 6.6 [1] |
 | 3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-6-(2-methylpropoxy)-4-oxoquinoline-2-carboxylic acid | IC50 | 6.3 [1], 9.9 [2] |
 | 3-[(3-Carboxyphenyl)methyl]-6-(cyclopropylmethoxy)-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxoquinoline-2-carboxylic acid | IC50 | 115.9 [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-trimethylbenzamide | Ki | 1.5 [1], 1.8 [2] |
 | Darusentan, (+/-)- | Ki | 6.0 [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 acid | IC50 | 430.0 [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]benzenesulfonamide | IC50 | 14.0 [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]benzenesulfonamide | Ki | 14.0 [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]benzenesulfonamide | IC50 | 13.0 [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]benzenesulfonamide | Ki | 13.0 [1] |
 | (2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-2-(3-fluoro-4-methoxyphenyl)-1-[2-[hexylsulfonyl(propyl)amino]ethyl]pyrrolidine-3-carboxylic acid | IC50 | 0.08 [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-carboxamide | IC50 | 415.0 [1] |
| 2-Butyl-5-chloro-3-[[4-[2-[(3,4-dimethyl-1,2-oxazol-5-yl)sulfamoyl]phenyl]phenyl]methyl]imidazole-4-carboxamide | Ki | 415.0 [1] |
 | 3-[1-(1,3-Benzodioxol-5-yl)-2-[(2-methoxy-4-methylphenyl)sulfonylamino]-2-oxoethyl]-1-methylindole-6-carboxamide | IC50 | 1.1 [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 acid | IC50 | 4.0 [1], 14.0 [2] |
 | 3-[(4-Bromo-3-methyl-1,2-oxazol-5-yl)sulfamoyl]-N-phenylthiophene-2-carboxamide | IC50 | 166.0 [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 acid | IC50 | 0.07 [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 acid | IC50 | 0.06 [1], 1.66 [2] |
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