 | 3-Benzo[1,3]dioxol-5-yl-5-hydroxy-5-(4-methoxy-phenyl)-4-(3,4,5-trimethoxy-benzyl)-5H-furan-2-one | IC50 | 120.0 [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-one | Ki | 139.0 [1] |
 | Bosentan | IC50 | 95.0 [1], 150.0 [2], 202.0 [3], 280.0 [4] |
| Bosentan | Ki | 80.0 [1], 340.0 [2] |
 | (1,1'-Biphenyl)-2-sulfonamide, N-(3,4-dimethyl-5-isoxazolyl)-4'-(2-oxazolyl)- | Ki | 18700.0 [1] |
 | A-216546 Free base | IC50 | 13000.0 [1], 15400.0 [2], 16700.0 [3] |
| A-216546 Free base | Ki | 13000.0 [1] |
 | Atrasentan | IC50 | 63.3 [1], 88.0 [2], 515.0 [3] |
 | Unii-0I32bcl40Z | Ki | 14.7 [1], 18.0 [2] |
 | 5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide | IC50 | 14000.0 [1] |
| 5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide | Ki | 50000.0 [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 acid | IC50 | 0.03 [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 acid | Ki | 0.05 [1] |
 | 3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxo-6-propoxyquinoline-2-carboxylic acid | IC50 | 913.4 [1], 2868.4 [2], 2870.0 [3] |
 | Darusentan, (+/-)- | Ki | 371.0 [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 acid | IC50 | 10.0 [1], 7600.0 [2], 16000.0 [3] |
 | Endothelin | IC50 | 0.13 [1], 0.2 [2] |
 | Sitaxentan | IC50 | 9.8 [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-enoate | IC50 | 417.0 [1] |
| Sodium;(Z)-2-(1,3-benzodioxol-5-yl)-4-(4-methoxyphenyl)-4-oxo-3-[(3,4,5-trimethoxyphenyl)methyl]but-2-enoate | Ki | 139.0 [1] |
 | Enrasentan | Ki | 110.0 [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]sulfonylazanide | IC50 | 8.3 [1] |
| Sodium;[6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-5-(4-methylphenyl)pyrimidin-4-yl]-[4-(1-hydroxy-2-methylpropan-2-yl)phenyl]sulfonylazanide | Ki | 41.0 [1] |
 | 3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-6-hydroxy-4-oxoquinoline-2-carboxylic acid | IC50 | 15561.5 [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 acid | IC50 | 0.28 [1], 1.28 [2] |
 | 4-[1-(1,3-Benzodioxol-5-yl)-2-oxo-2-[(4-propan-2-ylphenyl)sulfonylamino]ethoxy]-3-propylbenzoic acid | IC50 | 4.4 [1] |
| 4-[1-(1,3-Benzodioxol-5-yl)-2-oxo-2-[(4-propan-2-ylphenyl)sulfonylamino]ethoxy]-3-propylbenzoic acid | Ki | 5.4 [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 acid | IC50 | 60.0 [1], 960.0 [2] |
 | N-[6-[2-(5-Bromopyrimidin-2-yl)oxyethoxy]-5-(4-methylphenyl)pyrimidin-4-yl]-4-tert-butylbenzenesulfonamide | IC50 | 38.0 [1] |
| N-[6-[2-(5-Bromopyrimidin-2-yl)oxyethoxy]-5-(4-methylphenyl)pyrimidin-4-yl]-4-tert-butylbenzenesulfonamide | Ki | 130.0 [1] |
 | 3-[(4-Chloro-3-methyl-1,2-oxazol-5-yl)sulfamoyl]-N-(4-methylphenyl)thiophene-2-carboxamide | IC50 | 14100.0 [1] |
 | N-(1,3-Benzodioxol-5-yl)-3-[(4-bromo-3-methyl-1,2-oxazol-5-yl)sulfamoyl]thiophene-2-carboxamide | IC50 | 10100.0 [1] |
 | N-[[2-[2-[(3,4-Dimethyl-1,2-oxazol-5-yl)sulfamoyl]phenyl]-5-(1,3-oxazol-2-yl)phenyl]methyl]acetamide | Ki | 4400.0 [1] |
 | 5-Hydroxy-4-(4-methoxy-benzyl)-5-(4-methoxy-phenyl)-3-phenyl-5H-furan-2-one | IC50 | 2500.0 [1] |
 | 3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-(3,4-dichlorophenyl)-5-hydroxyfuran-2-one | IC50 | 25000.0 [1] |
 | 5-Hydroxy-4-(4-methoxy-benzyl)-5-(4-methoxy-phenyl)-3-p-tolyl-5H-furan-2-one | IC50 | 2500.0 [1], 2700.0 [2] |
 | 3-Benzo[1,3]dioxol-5-yl-4-benzyl-5-(4-chloro-phenyl)-5-hydroxy-5H-furan-2-one | IC50 | 2700.0 [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 acid | IC50 | 0.47 [1], 0.6 [2] |
 | 3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-hydroxy-5-(4-methoxy-3-methylphenyl)furan-2-one | IC50 | 1750.0 [1] |
 | 5-Hydroxy-4-(4-methoxy-benzyl)-3,5-bis-(4-methoxy-phenyl)-5H-furan-2-one | IC50 | 2500.0 [1], 9000.0 [2] |
 | 3-(3,4-Dichlorophenyl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methoxyphenyl)methyl]furan-2-one | IC50 | 2500.0 [1], 2700.0 [2] |
 | 3-[(4-Chloro-3-methyl-1,2-oxazol-5-yl)sulfamoyl]-N-(4-methoxy-2-methylphenyl)thiophene-2-carboxamide | IC50 | 14000.0 [1] |
 | 3-Benzo[1,3]dioxol-5-yl-4-benzyl-5-hydroxy-5-(4-methoxy-phenyl)-5H-furan-2-one | IC50 | 4550.0 [1] |
 | 3-(1,3-Benzodioxol-5-yl)-4-[(4-chlorophenyl)methyl]-5-hydroxy-5-(4-methoxyphenyl)furan-2-one | IC50 | 2500.0 [1] |
 | 3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-hydroxy-5-phenylfuran-2-one | IC50 | 30000.0 [1] |
 | 3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxo-6-prop-2-enoxyquinoline-2-carboxylic acid | IC50 | 1131.0 [1], 1131.2 [2] |
 | 3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-6-(methoxymethoxy)-4-oxoquinoline-2-carboxylic acid | IC50 | 1030.0 [1], 1030.2 [2] |
 | 6-Butoxy-3-[(3-carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxoquinoline-2-carboxylic acid | IC50 | 548.2 [1] |
 | 3-(1,3-Benzodioxol-5-yl)-1-(1,3-benzodioxol-5-ylmethyl)-5-propoxyindole-2-carboxylic acid | IC50 | 850.0 [1], 1600.0 [2] |
 | 3-(1,3-Benzodioxol-5-yl)-1-(1,3-benzodioxol-5-ylmethyl)-5,6-dimethoxyindole-2-carboxylic acid | IC50 | 1200.0 [1], 1400.0 [2] |
 | Bosentan sodium | IC50 | 310.0 [1] |
| Bosentan sodium | Ki | 140.0 [1] |
 | 3-[(3-Carboxyphenyl)methyl]-6-ethoxy-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-4-oxoquinoline-2-carboxylic acid | IC50 | 3119.0 [1] |
 | 3-[(3-Carboxyphenyl)methyl]-1-[(6-ethyl-1,3-benzodioxol-5-yl)methyl]-6-(2-methylpropoxy)-4-oxoquinoline-2-carboxylic acid | IC50 | 713.0 [1], 1983.0 [2] |
 | 3-(1,3-Benzodioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methylphenyl)methyl]furan-2-one | IC50 | 390.0 [1], 2500.0 [2] |
 | 3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-hydroxy-5-(4-methylphenyl)furan-2-one | IC50 | 25000.0 [1] |
 | 3-(1,3-Benzodioxol-5-yl)-5-hydroxy-4-[(4-methoxy-3-methylphenyl)methyl]-5-(4-methoxyphenyl)furan-2-one | IC50 | 1140.0 [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)sulfonylacetamide | IC50 | 60.0 [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-trimethylbenzamide | Ki | 1.2 [1] |
 | 3-(1,3-Benzodioxol-5-yl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methoxyphenyl)methyl]furan-2-one | IC50 | 1550.0 [1] |
 | 3-(4-Chlorophenyl)-5-hydroxy-5-(4-methoxyphenyl)-4-[(4-methoxyphenyl)methyl]furan-2-one | IC50 | 2500.0 [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 | 0.48 [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 acid | IC50 | 2800.0 [1], 62000.0 [2] |
 | 3-[1-(1,3-Benzodioxol-5-yl)-2-[(2-methoxy-4-methylphenyl)sulfonylamino]-2-oxoethyl]-1-methylindole-6-carboxamide | IC50 | 275.0 [1], 302.0 [2] |
 | 3-Methoxy-2-[(4-methoxy-6,7-dihydro-5H-cyclopenta[d]pyrimidin-2-yl)oxy]-3,3-diphenylpropanoic acid | Ki | 20.4 [1], 56.0 [2] |
 | 3-[(4-Bromo-3-methyl-1,2-oxazol-5-yl)sulfamoyl]-N-phenylthiophene-2-carboxamide | IC50 | 77600.0 [1] |
 | (2S,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(2-pyrazol-1-ylethyl)pyrrolidine-3-carboxylic acid | IC50 | 28600.0 [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 acid | IC50 | 0.14 [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 acid | IC50 | 0.2 [1], 1.46 [2] |
 | 3-(1,3-Benzodioxol-5-yl)-4-benzyl-5-methoxy-5-(4-methoxyphenyl)furan-2(5H)-one | IC50 | 25000.0 [1] |
 | 3-[1-(1,3-Benzodioxol-5-yl)-2-oxo-2-[(4-propan-2-ylphenyl)sulfonylamino]ethyl]-1-ethylindole-6-carboxylic acid | IC50 | 69.0 [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 acid | IC50 | 31000.0 [1] |
 | 3-[1-(1,3-Benzodioxol-5-yl)-2-oxo-2-[(4-propan-2-ylphenyl)sulfonylamino]ethyl]-1-methylindole-6-carboxamide | IC50 | 15.0 [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 acid | IC50 | 39700.0 [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 acid | IC50 | 92700.0 [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-dienoate | IC50 | 70000.0 [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-trienoate | IC50 | 21000.0 [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-trienoate | IC50 | 50000.0 [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 acid | IC50 | 18000.0 [1], 65400.0 [2] |
 | 3-Methoxy-3,3-diphenyl-2-[(4-methoxy-6-methylpyrimidin-2-yl)oxy]propanoic acid | Ki | 19.7 [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 acid | IC50 | 26000.0 [1], 32000.0 [2] |
 | 4-Benzo[1,3]dioxol-5-yl-1-dibutylcarbamoylmethyl-2-(4-methoxy-phenyl)-pyrrolidine-3-carboxylic acid | IC50 | 98.0 [1] |
| 4-Benzo[1,3]dioxol-5-yl-1-dibutylcarbamoylmethyl-2-(4-methoxy-phenyl)-pyrrolidine-3-carboxylic acid | Ki | 139.0 [1] |
 | 3-[1-(1,3-Benzodioxol-5-yl)-2-[(2-ethoxy-4-methylphenyl)sulfonylamino]-2-oxoethyl]-1-methylindole-6-carboxamide | IC50 | 397.0 [1] |
 | 3-Methoxy-2-(4-methoxy-5,6-dihydro-furo[2,3-d]pyrimidin-2-yloxy)-3,3-diphenyl-propionic acid | Ki | 24.5 [1], 57.0 [2] |
 | 5-Benzyloxy-3-isopropoxy-benzo[b]thiophene-2-carboxylic acid | IC50 | 100000.0 [1] |
 | 1-Benzo[1,3]dioxol-5-ylmethyl-5,6-dimethoxy-3-(3-methoxy-phenylsulfanyl)-1H-indole-2-carboxylic acid | IC50 | 210.0 [1], 1100.0 [2] |
 | N-(4-Bromo-3-methyl-1,2-oxazol-5-yl)-2-phenylbenzenesulfonamide | IC50 | 7900.0 [1], 100000.0 [2] |
 | N-(4-Bromo-3-methyl-isoxazol-5-yl)-benzenesulfonamide | IC50 | 20000.0 [1], 100000.0 [2] |
 | 1-(1,3-Benzodioxol-5-ylmethyl)-3-(1,3-benzodioxol-5-ylsulfanyl)-5-methoxy-6-phenylmethoxyindole-2-carboxylic acid | IC50 | 490.0 [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 acid | IC50 | 170.0 [1], 230.0 [2] |
 | 5-(1,3-Benzodioxol-5-ylmethyl)-7-(3,4-dimethoxyphenyl)sulfanyl-[1,3]dioxolo[4,5-f]indole-6-carboxylic acid | IC50 | 170.0 [1] |
 | 1-(1,3-Benzodioxol-5-ylmethyl)-5,6-dimethoxy-3-(3,4,5-trimethoxyphenyl)sulfanylindole-2-carboxylic acid | IC50 | 380.0 [1], 440.0 [2] |
 | 1,3-Benzodioxol-5-yl 3-[(4-bromo-3-methyl-1,2-oxazol-5-yl)sulfamoyl]thiophene-2-carboxylate | IC50 | 5700.0 [1], 5740.0 [2] |
 | 1-(1,3-Benzodioxol-5-ylmethyl)-3-(1,3-benzodioxol-5-ylsulfanyl)-5,6-dimethoxyindole-2-carboxylic acid | IC50 | 280.0 [1], 1100.0 [2] |
 | Cyclo(D-trp-D-asp-pro-D-val-leu) | IC50 | 1000.0 [1] |
 | Sulfisoxazole | IC50 | 24000.0 [1] |
 | Ambrisentan | IC50 | 1190.0 [1] |
 | Darusentan | IC50 | 16.0 [1] |
 | (+/-)-Ambrisentan | Ki | 195.0 [1] |
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