 | Sufugolix | IC50 | 0.6 [1] |
| Sufugolix | Ki | 0.2 [1] |
 | Nbi-42902 | IC50 | 2.8 [1], 3.0 [2] |
 | 1-[4-[5-[[Benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-3-ethylurea | IC50 | 0.07 [1], 0.1 [2], 0.3 [3], 7.0 [4] |
| 1-[4-[5-[[Benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-3-ethylurea | Ki | 0.4 [1] |
 | Unii-F1klt23O3A | IC50 | 0.6 [1] |
| Unii-F1klt23O3A | Ki | 0.1 [1], 0.2 [2] |
 | 6-(4-Aminophenyl)-5-[[benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-3-phenylthieno[2,3-d]pyrimidine-2,4-dione | Ki | 36.0 [1] |
 | N-[4-[5-[[Benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]benzamide | IC50 | 1.0 [1] |
 | 5-[[Benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-6-(4-nitrophenyl)-3-phenylthieno[2,3-d]pyrimidine-2,4-dione | Ki | 180.0 [1] |
 | 1-[(2,6-Difluorophenyl)methyl]-5-[[methyl(2-pyridin-2-ylethyl)amino]methyl]-6-(4-nitrophenyl)-3-phenylthieno[2,3-d]pyrimidine-2,4-dione | Ki | 0.6 [1] |
 | 1-[(2,6-Difluorophenyl)methyl]-5-[[methyl(2-phenylethyl)amino]methyl]-6-(4-nitrophenyl)-3-phenylthieno[2,3-d]pyrimidine-2,4-dione | Ki | 170.0 [1] |
 | N-[4-[5-[[Benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]acetamide | Ki | 4.1 [1] |
 | 4-[2-[(2S)-Azetidin-2-yl]ethoxy]-7-chloro-2-oxo-N-pyrimidin-4-yl-3-(3,4,5-trimethylphenyl)-1H-quinoline-6-carboxamide | IC50 | 0.44 [1], 0.5 [2], 0.9 [3], 60.0 [4] |
| 4-[2-[(2S)-Azetidin-2-yl]ethoxy]-7-chloro-2-oxo-N-pyrimidin-4-yl-3-(3,4,5-trimethylphenyl)-1H-quinoline-6-carboxamide | Ki | 0.4 [1] |
 | 1-[(2,6-Difluorophenyl)methyl]-5-(3-methoxyphenyl)-6-methyl-3-[2-[methyl(2-pyridin-2-ylethyl)amino]ethyl]pyrimidine-2,4-dione | IC50 | 16.0 [1] |
| 1-[(2,6-Difluorophenyl)methyl]-5-(3-methoxyphenyl)-6-methyl-3-[2-[methyl(2-pyridin-2-ylethyl)amino]ethyl]pyrimidine-2,4-dione | Ki | 34.0 [1], 610.0 [2] |
 | 3-[(2R)-2-Amino-2-phenylethyl]-1-[(2,6-difluorophenyl)methyl]-5-(3-methoxyphenyl)-6-methylpyrimidine-2,4-dione | IC50 | 5.0 [1] |
| 3-[(2R)-2-Amino-2-phenylethyl]-1-[(2,6-difluorophenyl)methyl]-5-(3-methoxyphenyl)-6-methylpyrimidine-2,4-dione | Ki | 2.3 [1], 3.2 [2], 45.0 [3] |
 | 3-[(2S)-2-(Cyclopentylamino)propyl]-1-[(2,6-difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4-dione | IC50 | 5.5 [1], 8.2 [2] |
| 3-[(2S)-2-(Cyclopentylamino)propyl]-1-[(2,6-difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4-dione | Ki | 4.5 [1], 50.0 [2] |
 | N-[4-[5-[[Benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]propanamide | IC50 | 0.3 [1], 4.0 [2], 9.0 [3], 300.0 [4] |
| N-[4-[5-[[Benzyl(methyl)amino]methyl]-1-[(2,6-difluorophenyl)methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]propanamide | Ki | 0.8 [1] |
 | 1-[(2,6-Difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyl-3-[(2S)-2-(methylamino)-3-phenylpropyl]pyrimidine-2,4-dione | IC50 | 20.0 [1] |
| 1-[(2,6-Difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyl-3-[(2S)-2-(methylamino)-3-phenylpropyl]pyrimidine-2,4-dione | Ki | 8.1 [1], 200.0 [2] |
 | Relugolix | IC50 | 0.08 [1], 0.33 [2], 0.82 [3], 18.0 [4] |
 | 3-[(2R)-2-Amino-2-phenylethyl]-1-[(2,6-difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)pyrimidine-2,4-dione | Ki | 5.3 [1], 5.6 [2] |
 | 3-[(2R)-2-Amino-2-phenylethyl]-5-(2-fluoro-3-methoxyphenyl)-1-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]pyrimidine-2,4-dione | Ki | 0.6 [1], 0.64 [2] |
 | 1-[(2,6-Difluorophenyl)methyl]-5-(3-methoxyphenyl)-6-methyl-3-[(2R)-2-[methyl(pyridin-2-ylmethyl)amino]propyl]pyrimidine-2,4-dione | Ki | 5.0 [1], 5.5 [2], 102.0 [3] |
 | 4-[[(1R)-2-[5-(2-Fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-2,6-dioxopyrimidin-1-yl]-1-phenylethyl]amino]butanoic acid | IC50 | 4.9 [1], 47.0 [2] |
| 4-[[(1R)-2-[5-(2-Fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-2,6-dioxopyrimidin-1-yl]-1-phenylethyl]amino]butanoic acid | Ki | 1.2 [1], 2.0 [2] |
 | 5-[[4-[2-(4-Tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl]methyl]-1-ethylpyrimidine-2,4-dione | IC50 | 1.6 [1], 1.7 [2], 4.0 [3] |
 | N-[[4-[(Diaminomethylideneamino)methyl]cyclohexyl]methyl]-5-[(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)methyl]furan-2-carboxamide | Ki | 16.0 [1], 40.0 [2] |
 | 1-[4-[1-[(2,6-Difluorophenyl)methyl]-5-[[2-methoxyethyl(methyl)amino]methyl]-2,4-dioxo-3-pyridin-2-ylthieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea | IC50 | 0.2 [1], 0.3 [2], 0.83 [3], 13.0 [4] |
 | Leuprorelin | IC50 | 0.29 [1], 0.3 [2], 0.8 [3] |
 | CID 11496610 | IC50 | 12.0 [1], 28.0 [2] |
 | 7-Chloro-2-oxo-4-[2-[(2S)-piperidin-2-yl]ethoxy]-N-pyrimidin-4-yl-3-(3,4,5-trimethylphenyl)-1H-quinoline-6-carboxamide | IC50 | 0.3 [1], 2.2 [2] |
 | 3-[(2R)-2-Amino-2-phenylethyl]-1-[(2-chloro-6-fluorophenyl)methyl]-5-(2-fluorophenyl)-6-methylpyrimidine-2,4-dione | IC50 | 2.8 [1] |
| 3-[(2R)-2-Amino-2-phenylethyl]-1-[(2-chloro-6-fluorophenyl)methyl]-5-(2-fluorophenyl)-6-methylpyrimidine-2,4-dione | Ki | 0.61 [1], 0.7 [2], 6.4 [3] |
 | 3-[(2R)-2-Amino-2-cyclohexylethyl]-1-[(2,6-difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4-dione | IC50 | 6.5 [1] |
| 3-[(2R)-2-Amino-2-cyclohexylethyl]-1-[(2,6-difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4-dione | Ki | 6.5 [1], 120.0 [2] |
 | 1-[(2,6-Difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-3-[(2R)-1-[(2-methoxyphenyl)methylamino]propan-2-yl]-6-methylpyrimidine-2,4-dione | IC50 | 5.7 [1] |
| 1-[(2,6-Difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-3-[(2R)-1-[(2-methoxyphenyl)methylamino]propan-2-yl]-6-methylpyrimidine-2,4-dione | Ki | 3.7 [1], 3.9 [2], 30.0 [3] |
 | 3-[(2S)-2-(Benzylamino)propyl]-1-[(2,6-difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4-dione | IC50 | 38.0 [1] |
| 3-[(2S)-2-(Benzylamino)propyl]-1-[(2,6-difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4-dione | Ki | 25.0 [1], 51.0 [2], 550.0 [3] |
 | 1-[(2,6-Difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyl-3-[(2R)-2-(pyridin-2-ylmethylamino)propyl]pyrimidine-2,4-dione | IC50 | 0.5 [1] |
| 1-[(2,6-Difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyl-3-[(2R)-2-(pyridin-2-ylmethylamino)propyl]pyrimidine-2,4-dione | Ki | 1.1 [1], 43.0 [2] |
 | 2-(4-Tert-butylphenyl)-4-[4-[(1-ethyl-5-methylimidazol-4-yl)methyl]piperazin-1-yl]-1H-benzimidazole | IC50 | 5.8 [1], 7.0 [2], 14.0 [3], 15.0 [4] |
 | 6-[[4-[2-(4-Tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl]methyl]-1,4-dihydroquinoxaline-2,3-dione | IC50 | 4.9 [1], 9.4 [2] |
 | 1-(7-Azabicyclo[2.2.1]heptan-7-yl)-2-[2-(3,5-dimethylphenyl)-3-[(2S)-1-(4-pyridin-4-ylbutylamino)propan-2-yl]-1H-indol-5-yl]-2-methylpropan-1-one | IC50 | 0.7 [1], 5.7 [2] |
 | 1-[4-[1-[(2,6-Difluorophenyl)methyl]-5-[[2-methoxyethyl(methyl)amino]methyl]-3-(4-methoxyphenyl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea | IC50 | 0.07 [1], 0.17 [2], 0.29 [3], 0.43 [4] |
 | 1-[4-[1-[(2,6-Difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea | IC50 | 0.12 [1], 0.26 [2], 0.55 [3], 0.95 [4] |
 | 3-[(2S)-2-(Cyclobutylamino)propyl]-1-[(2,6-difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4-dione | IC50 | 10.0 [1] |
| 3-[(2S)-2-(Cyclobutylamino)propyl]-1-[(2,6-difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4-dione | Ki | 3.6 [1], 5.0 [2], 87.0 [3] |
 | 1-[4-[1-[(2,6-Difluorophenyl)methyl]-5-[[2-methoxyethyl(methyl)amino]methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea | IC50 | 0.08 [1], 0.1 [2], 0.5 [3], 1.4 [4] |
 | N-[4-[3-[[Benzyl(methyl)amino]methyl]-7-[(2,6-difluorophenyl)methyl]-5-(2-methylpropanoyl)-4-oxothieno[2,3-b]pyridin-2-yl]phenyl]-2-hydroxybutanamide | IC50 | 0.1 [1], 0.9 [2], 15.0 [3] |
 | 1-[4-[1-[(2,6-Difluorophenyl)methyl]-5-[[2-methoxyethyl(methyl)amino]methyl]-3-(5-methylpyridin-2-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea | IC50 | 0.1 [1], 0.18 [2], 0.3 [3], 1.3 [4] |
 | 1-[4-[1-[(2,6-Difluorophenyl)methyl]-5-[[2-methoxyethyl(methyl)amino]methyl]-3-(6-methoxypyridin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea | IC50 | 0.07 [1], 0.2 [2], 0.49 [3], 0.8 [4] |
 | 1-[4-[1-[(2,6-Difluorophenyl)methyl]-5-[[2-methoxyethyl(methyl)amino]methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea | IC50 | 0.08 [1], 0.24 [2], 0.26 [3], 0.94 [4] |
 | Degarelix | IC50 | 0.58 [1], 1.64 [2], 8.8 [3] |
 | Acyline | IC50 | 0.52 [1], 0.69 [2], 6.8 [3] |
 | Furan-1 | Ki | 6.0 [1], 19.0 [2] |
 | N-[4-(4-{2-[2-(3,5-Dimethyl-phenyl)-1H-indol-3-yl]-ethylamino}-butyl)-phenyl]-methanesulfonamide | IC50 | 7.0 [1], 170.0 [2] |
 | [(1S,2R,5R,6S,7S,8R,9S,11R,13R,14R)-8-[(2S,3R,4S,6R)-4-[Cyclopropylmethyl(methyl)amino]-3-hydroxy-6-methyloxan-2-yl]oxy-15-[2-(3,4-dichlorophenyl)ethyl]-2-ethyl-9-methoxy-1,5,7,9,11,13-hexamethyl-4,12,16-trioxo-3,17-dioxa-15-azabicyclo[12.3.0]heptadecan-6-yl] (4S)-4-methyl-2-oxo-1,3-oxazolidine-3-carboxylate | Ki | 1.86 [1], 2.0 [2] |
 | Pentan-3-yl 2-[4-(butanoylamino)phenyl]-8-[(2-fluorophenyl)methyl]-3-[[methyl(2-pyridin-2-ylethyl)amino]methyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate | Ki | 7.5 [1] |
 | 1-[(2,6-Difluorophenyl)methyl]-5-(2,3-dihydro-1,4-benzodioxin-6-yl)-6-methyl-3-[2-[methyl(2-pyridin-2-ylethyl)amino]ethyl]pyrimidine-2,4-dione | Ki | 24.0 [1] |
 | 1-[(2R)-2-Amino-2-phenylethyl]-3-[(2,6-difluorophenyl)methyl]-5-(3-methoxyphenyl)-1,3,5-triazinane-2,4,6-trione | Ki | 37.0 [1] |
 | 1-Benzyl-2-(2-pyridin-3-yl-ethylsulfanyl)-1H-benzoimidazole-5-sulfonic acid 4-fluoro-benzylamide | IC50 | 120.0 [1] |
 | 1-(2,6-Difluorobenzyl)-3-[(R)-2-(2-pyridinylmethylamino)propyl]-5-(3-methoxyphenyl)-6-methyluracil | Ki | 15.0 [1] |
 | 1-[(2,6-Difluorophenyl)methyl]-5-(3-methoxyphenyl)-6-methyl-3-[(2S)-2-[methyl(2-pyridin-2-ylethyl)amino]propyl]pyrimidine-2,4-dione | Ki | 5.0 [1], 470.0 [2], 890.0 [3] |
 | 1-[(2,6-Difluorophenyl)methyl]-5-(3-methoxyphenyl)-6-methyl-3-[(2R)-2-[methyl(2-pyridin-2-ylethyl)amino]propyl]pyrimidine-2,4-dione | Ki | 1.1 [1], 5.2 [2] |
 | Prazarelix acetate | IC50 | 1.36 [1], 1.4 [2], 6.9 [3] |
 | 1-[(2,6-Difluorophenyl)methyl]-5-(3-methoxyphenyl)-3-[(2R)-1-[(2-methoxyphenyl)methylamino]propan-2-yl]-6-methylpyrimidine-2,4-dione | Ki | 20.0 [1], 160.0 [2] |
 | 3-[(2R)-2-Amino-2-phenylethyl]-5-(2-fluoro-3-methoxyphenyl)-1-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-6-methylpyrimidine-2,4-dione | IC50 | 0.5 [1] |
| 3-[(2R)-2-Amino-2-phenylethyl]-5-(2-fluoro-3-methoxyphenyl)-1-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-6-methylpyrimidine-2,4-dione | Ki | 0.5 [1] |
 | 3-[(2R)-2-Amino-2-phenylethyl]-5-(2-fluorophenyl)-1-[(2-fluorophenyl)methyl]-6-methylpyrimidine-2,4-dione | Ki | 19.0 [1], 20.0 [2] |
 | 2-(4-Tert-butylphenyl)-4-[4-[(2-methyl-1-propylimidazol-4-yl)methyl]piperazin-1-yl]-1H-benzimidazole | IC50 | 18.0 [1], 43.0 [2] |
 | 1-(7-Azabicyclo[2.2.1]heptan-7-yl)-2-[2-(3,5-dimethylphenyl)-3-[2-(4-pyridin-4-ylbutylamino)ethyl]-1H-indol-5-yl]-2-methylpropan-1-one | IC50 | 1.4 [1], 18.0 [2] |
 | 2-(4-Tert-butylphenyl)-4-[4-[(2-ethyl-5-methyl-1H-imidazol-4-yl)methyl]piperazin-1-yl]-1H-benzimidazole | IC50 | 6.6 [1], 10.0 [2], 18.0 [3] |
 | 4-[2-[4-[2-(Trifluoromethyl)-1H-benzimidazol-4-yl]piperazin-1-yl]ethoxy]-1,3-dihydrobenzimidazole-2-thione | IC50 | 790.0 [1], 800.0 [2], 4500.0 [3] |
 | Ethyl 3-[[benzyl(methyl)amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate | IC50 | 0.5 [1], 70.79 [2] |
| Ethyl 3-[[benzyl(methyl)amino]methyl]-8-[(2,6-difluorophenyl)methyl]-2-[4-(ethylcarbamoylamino)phenyl]-5-oxoimidazo[1,2-a]pyrimidine-6-carboxylate | Ki | 4.79 [1] |
 | 3-[(2R)-2-Amino-2-phenylethyl]-1-[(2,6-difluorophenyl)methyl]-5-(2,3-dihydro-1,4-benzodioxin-6-yl)-6-methylpyrimidine-2,4-dione | IC50 | 10.0 [1] |
| 3-[(2R)-2-Amino-2-phenylethyl]-1-[(2,6-difluorophenyl)methyl]-5-(2,3-dihydro-1,4-benzodioxin-6-yl)-6-methylpyrimidine-2,4-dione | Ki | 5.1 [1], 74.0 [2] |
 | 1-[(2,6-Difluorophenyl)methyl]-3-[(2S)-2-[(5-ethylfuran-2-yl)methylamino]propyl]-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4-dione | IC50 | 27.0 [1] |
| 1-[(2,6-Difluorophenyl)methyl]-3-[(2S)-2-[(5-ethylfuran-2-yl)methylamino]propyl]-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4-dione | Ki | 15.0 [1] |
 | 1-[(2,6-Difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyl-3-[(2S)-2-[(3-methylthiophen-2-yl)methylamino]propyl]pyrimidine-2,4-dione | IC50 | 4.0 [1] |
| 1-[(2,6-Difluorophenyl)methyl]-5-(2-fluoro-3-methoxyphenyl)-6-methyl-3-[(2S)-2-[(3-methylthiophen-2-yl)methylamino]propyl]pyrimidine-2,4-dione | Ki | 4.0 [1], 87.0 [2] |
 | 1-[(2,6-Difluorophenyl)methyl]-3-[(2R)-2-(dimethylamino)-2-phenylethyl]-5-(2-fluoro-3-methoxyphenyl)-6-methylpyrimidine-2,4-dione | IC50 | 49.0 [1] |
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