 | Aliskiren | IC50 | 0.6 [1] |
 | Pepstatin | IC50 | 6000.0 [1] |
 | Pepstatin | Ki | 100.0 [1], 13000.0 [2] |
 | (2S)-1-[(2S)-2-[[(2S)-2-Amino-2-methylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]-N-[(2S)-1-[[(2S)-1-[[1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]pyrrolidine-2-carboxamide | IC50 | 3.0 [1], 13.0 [2], 31.0 [3], 32.0 [4] |
 | (2S)-1-[(2S)-2-[[(2S)-2-Amino-2-methylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]-N-[(2S)-1-[[(2S)-1-[[1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]pyrrolidine-2-carboxamide | Ki | 10.0 [1] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-(benzylamino)-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | IC50 | 25.0 [1] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-(benzylamino)-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | Ki | 18.0 [1], 55.0 [2], 70.0 [3] |
 | Methyl (4S)-3-hydroxy-4-[[(2S)-2-[[(4S)-3-hydroxy-4-[[(2S)-3-(1H-imidazol-5-yl)-2-[[(2S)-2-[(2-methylpropan-2-yl)oxycarbonylamino]-3-phenylpropanoyl]amino]propanoyl]amino]-6-methylheptanoyl]amino]propanoyl]amino]-6-methylheptanoate | IC50 | 27.0 [1] |
 | Isovaleryl-phe-nle-sta-ala-sta-OH | IC50 | 28.18 [1] |
 | (3R)-3-[(1S)-1-(3-Chlorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide | IC50 | 0.5 [1] |
 | Methyl (4S)-3-hydroxy-4-[[(2S)-2-[[(4S)-3-hydroxy-6-methyl-4-[[(2S)-3-methyl-2-[[(2S)-3-phenyl-2-(phenylmethoxycarbonylamino)propanoyl]amino]butanoyl]amino]heptanoyl]amino]propanoyl]amino]-6-methylheptanoate | IC50 | 93.0 [1] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | IC50 | 63.0 [1], 140.0 [2], 290.0 [3] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | Ki | 190.0 [1] |
 | (2S,5S)-5-[[(2S)-2-[(2-Benzyl-3-tert-butylsulfonylpropanoyl)amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-N-butyl-6-cyclohexyl-4-hydroxy-2-propan-2-ylhexanamide | IC50 | 2.0 [1] |
 | (2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-5-[[(2S)-1-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-cyclohexyl-3-hydroxy-5-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-1-[(2S)-3-(1H-imidazol-5-yl)-2-(3-methylbutanoylamino)propanoyl]pyrrolidine-2-carboxamide | IC50 | 0.17 [1], 1.9 [2] |
 | (2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-5-[[(2S)-1-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-cyclohexyl-3-hydroxy-5-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-1-[(2S)-3-(1H-imidazol-5-yl)-2-(3-methylbutanoylamino)propanoyl]pyrrolidine-2-carboxamide | Ki | 0.16 [1], 0.19 [2], 0.54 [3], 3.7 [4] |
 | (2R)-4-(4-Aminopiperidin-1-yl)-2-benzyl-N-[(2S)-1-[[(2S,3R,4S)-1-cyclohexyl-3,4-dihydroxy-6-pyridin-2-ylhexan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-4-oxobutanamide | IC50 | 0.38 [1], 0.39 [2] |
 | Enalkiren | IC50 | 0.75 [1], 0.76 [2], 2.3 [3], 14.0 [4] |
 | Zankiren | IC50 | 0.2 [1], 0.24 [2], 1.1 [3], 110.0 [4] |
 | Vtp-27999 | IC50 | 0.3 [1], 0.47 [2], 0.5 [3], 1.1 [4], 10.0 [5] |
 | (2S)-6-Amino-2-[[(2S)-3-(4-hydroxyphenyl)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-4-yl)-2-[[(2S)-2-[[(2S)-1-[(2S)-3-(1H-imidazol-4-yl)-2-[[(2S)-pyrrolidine-2-carbonyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]hexanoic acid | IC50 | 5200.0 [1], 7000.0 [2], 8000.0 [3], 9400.0 [4], 9410.0 [5] |
 | (2S)-N-[(2S)-3-(2-Amino-1,3-thiazol-4-yl)-1-[[(2S,3R,4S)-1-cyclohexyl-3,4-dihydroxy-6-methylheptan-2-yl]amino]-1-oxopropan-2-yl]-2-(morpholin-4-ylsulfonylamino)-3-phenylpropanamide | IC50 | 0.36 [1], 0.37 [2], 0.57 [3], 1.96 [4] |
 | Methyl (3S,4S)-3-hydroxy-4-[[(2S)-2-[[(3S,4S)-3-hydroxy-4-[[(2S)-3-(1H-indol-3-yl)-2-[[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]propanoyl]amino]-6-methylheptanoyl]amino]propanoyl]amino]-6-methylheptanoate | IC50 | 17.0 [1], 150.0 [2], 151.36 [3], 170.0 [4], 150000.0 [5] |
 | (2R)-2-Benzyl-N-[(2S)-1-[[(1R,2S)-3-cyclohexyl-1-[(5S)-3-ethyl-2-oxo-1,3-oxazolidin-5-yl]-1-hydroxypropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-4-morpholin-4-yl-4-oxobutanamide | IC50 | 0.99 [1], 1.3 [2] |
 | (3R,4R)-4-{4-[3-(Benzyloxy)propoxy]phenyl}-3-(2-naphthylmethoxy)piperidine | IC50 | 5.0 [1], 8.0 [2], 1300.0 [3] |
 | Methyl N-[2-[(R)-(3-chlorophenyl)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl]carbamate | IC50 | 0.48 [1], 0.8 [2], 0.82 [3] |
 | Cbz-Trp-Val-Sta-Ala-Sta-OMe | IC50 | 25.0 [1], 42.0 [2], 150.0 [3], 151.36 [4] |
 | (2S,4S,5S)-6-Cyclohexyl-4-hydroxy-N-(3-imidazol-1-ylpropyl)-5-[[(2S)-2-[[(2S)-1-[4-(methoxymethoxy)piperidin-1-yl]-1-oxo-3-phenylpropan-2-yl]amino]hexanoyl]amino]-2-propan-2-ylhexanamide | IC50 | 2.0 [1], 7.6 [2], 24.0 [3], 330.0 [4] |
 | (2S,4S,5S)-6-Cyclohexyl-4-hydroxy-5-[[(2S)-2-[[(2S)-1-[4-(methoxymethoxy)piperidin-1-yl]-1-oxo-3-phenylpropan-2-yl]amino]hexanoyl]amino]-N-(3-morpholin-4-ylpropyl)-2-propan-2-ylhexanamide | IC50 | 3.3 [1], 7.3 [2], 16.0 [3], 290.0 [4] |
 | Methyl (3S,4S)-3-hydroxy-4-[[(2S)-2-[[(3S,4S)-3-hydroxy-6-methyl-4-[[(2S)-2-[[(2S)-2-[(2-methylpropan-2-yl)oxycarbonylamino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]heptanoyl]amino]propanoyl]amino]-6-methylheptanoate | IC50 | 76.0 [1], 130.0 [2], 190.0 [3], 190.55 [4], 1000.0 [5] |
 | 2-Tert-butyl-4-(3-methoxypropylamino)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholine-4-carbonyl)piperidin-3-yl]pyrimidine-5-carboxamide | IC50 | 0.38 [1], 0.79 [2], 1.5 [3] |
 | (2S)-N-[(2S)-1-[[(2S)-1-[[1-[[(2S,3S)-1-[[(2S)-2-Amino-3-phenylpropanoyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-1-[(2S)-3-(1H-imidazol-5-yl)-2-[[(2S)-pyrrolidine-2-carbonyl]amino]propanoyl]pyrrolidine-2-carboxamide | IC50 | 3.0 [1], 50.0 [2], 81.0 [3], 200.0 [4] |
 | 2-Tert-butyl-4-hexyl-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholine-4-carbonyl)piperidin-3-yl]pyrimidine-5-carboxamide | IC50 | 10.0 [1], 24.0 [2], 29.0 [3] |
 | (2S)-6-Amino-2-[[(2S)-2-[[(2S)-2-[[(3S,4S)-3-hydroxy-4-[[(2S)-3-(1H-imidazol-5-yl)-2-[[(2S)-2-[[(2S)-1-[(2S)-3-(1H-imidazol-5-yl)-2-[[(2S)-pyrrolidine-2-carbonyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoyl]amino]propanoyl]amino]-6-methylheptanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]hexanoic acid | IC50 | 10.0 [1], 37.0 [2], 90.0 [3], 100.0 [4] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | IC50 | 63.0 [1], 140.0 [2] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | Ki | 70.0 [1], 190.0 [2], 1000.0 [3] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[1-[[(2S)-1-[(4-chlorophenyl)methylamino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | IC50 | 5.0 [1], 81.0 [2] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[1-[[(2S)-1-[(4-chlorophenyl)methylamino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | Ki | 50.0 [1], 240.0 [2], 280.0 [3] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[3-hydroxy-1-[[(2S)-1-[(2-hydroxy-1,2-diphenylethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | IC50 | 24.0 [1], 841.0 [2] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[3-hydroxy-1-[[(2S)-1-[(2-hydroxy-1,2-diphenylethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | Ki | 28.0 [1], 47.0 [2], 350.0 [3] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[3-hydroxy-6-methyl-1-[[(2S)-4-methyl-1-(1-naphthalen-2-ylethylamino)-1-oxopentan-2-yl]amino]-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | IC50 | 14.0 [1], 51.0 [2] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[3-hydroxy-6-methyl-1-[[(2S)-4-methyl-1-(1-naphthalen-2-ylethylamino)-1-oxopentan-2-yl]amino]-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | Ki | 0.98 [1], 13.0 [2], 140.0 [3] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[1-[[(2S)-1-(1,2-diphenylethylamino)-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | IC50 | 6.9 [1], 151.0 [2] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[1-[[(2S)-1-(1,2-diphenylethylamino)-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | Ki | 29.0 [1], 38.0 [2], 280.0 [3] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[1-[[(2S)-1-[(1-benzylpiperidin-4-yl)amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | IC50 | 127.0 [1], 280.0 [2] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[1-[[(2S)-1-[(1-benzylpiperidin-4-yl)amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | Ki | 0.04 [1], 0.06 [2], 97.0 [3] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[3-hydroxy-1-[[(2S)-1-[(1-hydroxy-1-phenylpropan-2-yl)amino]-4-methyl-1-oxopentan-2-yl]amino]-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | IC50 | 178.0 [1], 480.0 [2] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[3-hydroxy-1-[[(2S)-1-[(1-hydroxy-1-phenylpropan-2-yl)amino]-4-methyl-1-oxopentan-2-yl]amino]-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | Ki | 36.0 [1], 67.0 [2], 220.0 [3] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[3-hydroxy-6-methyl-1-[[(2S)-4-methyl-1-[(2-methylidene-9-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,11,13-hexaenyl)amino]-1-oxopentan-2-yl]amino]-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | IC50 | 5.8 [1], 569.0 [2] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[3-hydroxy-6-methyl-1-[[(2S)-4-methyl-1-[(2-methylidene-9-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,11,13-hexaenyl)amino]-1-oxopentan-2-yl]amino]-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | Ki | 120.0 [1], 320.0 [2], 520.0 [3] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[3-hydroxy-6-methyl-1-[[(2S)-4-methyl-1-oxo-1-(1-phenylethylamino)pentan-2-yl]amino]-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | IC50 | 14.0 [1], 49.0 [2] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[3-hydroxy-6-methyl-1-[[(2S)-4-methyl-1-oxo-1-(1-phenylethylamino)pentan-2-yl]amino]-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | Ki | 6.0 [1], 19.0 [2], 100.0 [3] |
 | 2-Benzyl-3-tert-butylsulfonyl-N-[1-[[(2S,3R,4R,5R,6R)-1-cyclohexyl-3,4,5,6,7-pentahydroxyheptan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]propanamide | IC50 | 4.4 [1], 4.5 [2], 11.0 [3], 100.0 [4], 110.0 [5] |
 | (2S)-6-Amino-2-[[(2S)-2-[[(2S,3S)-2-[[(3S,4S)-3-hydroxy-4-[[(2S)-3-(1H-imidazol-5-yl)-2-[[(2S)-2-[[(2S)-1-[(2S)-3-(1H-imidazol-5-yl)-2-[[(2S)-pyrrolidine-2-carbonyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoyl]amino]propanoyl]amino]-6-methylheptanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]hexanoic acid | IC50 | 8.0 [1], 500.0 [2], 1250.0 [3], 2000.0 [4] |
 | Ditekiren | IC50 | 0.0 [1], 0.11 [2], 0.26 [3] |
 | Ditekiren | Ki | 0.04 [1] |
 | (2S)-6-Amino-2-[[(2S)-3-(1H-imidazol-5-yl)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-[[(2S)-2-[[(2S)-1-[(2S)-3-(1H-imidazol-5-yl)-2-[[(2S)-pyrrolidine-2-carbonyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]hexanoic acid | IC50 | 1.0 [1], 10.0 [2] |
 | Terlakiren | IC50 | 0.2 [1], 0.3 [2], 0.5 [3], 0.7 [4] |
 | (2S,4S,5S)-5-[[(2S)-2-[[(2S)-2-Benzyl-3-tert-butylsulfonylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-N-butyl-6-cyclohexyl-4-hydroxy-2-propan-2-ylhexanamide | IC50 | 0.83 [1], 1.6 [2] |
 | (2S,4S,5S)-5-[[(2S)-2-[[(2S)-2-Benzyl-3-tert-butylsulfonylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-N-butyl-6-cyclohexyl-4-hydroxy-2-propan-2-ylhexanamide | Ki | 0.7 [1] |
 | 5-{4-[(3,5-Difluorobenzyl)amino]phenyl}-6-ethylpyrimidine-2,4-diamine | IC50 | 4000.0 [1], 6600.0 [2] |
 | 6-(2,4-Diamino-6-ethylpyrimidin-5-yl)-2-(3,5-difluorophenyl)-4-(3-methoxypropyl)-2-methyl-1,4-benzoxazin-3-one | IC50 | 7.0 [1], 7.1 [2] |
 | (2R)-1-Methoxy-3-[(3S,4R,5R)-5-[(4-methoxynaphthalen-2-yl)methoxy]-4-[4-[3-[(2-methoxyphenyl)methoxy]propoxy]phenyl]piperidin-3-yl]oxypropan-2-ol | IC50 | 0.07 [1], 8.9 [2] |
 | (2R)-2-Benzyl-N-[(2S)-1-[[(1R,2S)-3-cyclohexyl-1-[(5S)-3-ethyl-2-oxo-1,3-oxazolidin-5-yl]-1-hydroxypropan-2-yl]amino]-1-oxo-3-(1,3-thiazol-4-yl)propan-2-yl]-4-morpholin-4-yl-4-oxobutanamide | IC50 | 0.6 [1], 8.1 [2] |
 | N-[2-[6-(2,4-Diamino-6-ethylpyrimidin-5-yl)-2,2-dimethyl-3-oxo-1,4-benzoxazin-4-yl]ethyl]acetamide | IC50 | 20.0 [1], 147.0 [2] |
 | (3R,4S)-N-[[2-Chloro-5-(3-methoxypropyl)phenyl]methyl]-N-cyclopropyl-4-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl]piperidine-3-carboxamide | IC50 | 0.22 [1], 0.33 [2], 11.8 [3], 12.3 [4] |
 | (3R,4S)-N-[[2-Chloro-5-[(3,3,3-trifluoropropanoylamino)methyl]phenyl]methyl]-N-cyclopropyl-4-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl]piperidine-3-carboxamide | IC50 | 0.27 [1], 0.38 [2], 6.9 [3] |
 | (3R,4S)-N-[[5-(2-Acetamidoethyl)-2-chlorophenyl]methyl]-N-cyclopropyl-4-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl]piperidine-3-carboxamide | IC50 | 0.18 [1], 1.4 [2] |
 | Methyl (3S,4S)-3-hydroxy-4-[[(2S)-2-[[(3S,4S)-3-hydroxy-4-[[(2S)-3-(1H-imidazol-5-yl)-2-[[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]propanoyl]amino]-6-methylheptanoyl]amino]propanoyl]amino]-6-methylheptanoate | IC50 | 110.0 [1], 140.0 [2], 141.25 [3] |
 | (2S,4S,5S)-N-Butyl-6-cyclohexyl-4-hydroxy-5-[[(2S)-2-[[(2S)-1-[4-(methoxymethoxy)piperidin-1-yl]-1-oxo-3-phenylpropan-2-yl]amino]hexanoyl]amino]-2-propan-2-ylhexanamide | IC50 | 0.9 [1], 1.8 [2], 8.7 [3] |
 | (2S,4S,5S)-N-Butyl-6-cyclohexyl-4-hydroxy-5-[[(2S)-2-[(2S)-1-[4-(methoxymethoxy)piperidin-1-yl]-1-oxo-3-phenylpropan-2-yl]oxyhexanoyl]amino]-2-propan-2-ylhexanamide | IC50 | 1.2 [1], 1.5 [2], 8.2 [3] |
 | (1R,5S)-7-[4-[3-(2-Chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-[(2,3-dichlorophenyl)methyl]-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide | IC50 | 0.4 [1], 36.0 [2] |
 | (2R,4S,5S,7S)-5-Amino-N-butyl-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-2,8-dimethylnonanamide;hydrochloride | IC50 | 1.0 [1] |
 | (2R,4S,5S,7S)-5-Amino-N-(3-amino-3-oxopropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-2,8-dimethylnonanamide;hydrochloride | IC50 | 7.0 [1], 17.0 [2] |
 | (3R,4S)-N-[[5-Chloro-2-(3-methoxypropyl)pyridin-4-yl]methyl]-N-cyclopropyl-4-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl]piperidine-3-carboxamide | IC50 | 0.28 [1], 3.5 [2] |
 | (3S,4R)-N-[[2-Chloro-5-(2-methoxyethyl)phenyl]methyl]-N-cyclopropyl-4-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl]-4-hydroxypiperidine-3-carboxamide | IC50 | 0.24 [1], 5.6 [2] |
 | 7-[[(3R,4R)-4-[4-[3-[(2-Methoxyphenyl)methoxy]propoxy]phenyl]piperidin-3-yl]oxymethyl]-1,2,3,4-tetrahydroquinoline | IC50 | 0.21 [1], 0.67 [2], 31.0 [3], 37.0 [4] |
 | (3S,4R)-N-Cyclopropyl-4-hydroxy-N-[[3-(2-methoxyethoxy)-5-(3-methoxypropyl)phenyl]methyl]-4-phenylpiperidine-3-carboxamide | IC50 | 318.0 [1], 320.0 [2], 990.0 [3] |
 | (3S,4R)-N-Cyclopropyl-4-(3,4-difluorophenyl)-4-hydroxy-N-[[3-(2-methoxyethoxy)-5-(3-methoxypropyl)phenyl]methyl]piperidine-3-carboxamide | IC50 | 6.4 [1], 13.0 [2], 42.0 [3], 97.0 [4] |
 | (3R)-N-[(2S)-1-Cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-3-ethoxypropoxy(phenyl)methyl]piperidine-1-carboxamide | IC50 | 40.0 [1], 447.0 [2] |
 | (3R)-3-[(1S)-1-(3-Chlorophenyl)-1,5-dihydroxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide | IC50 | 21.0 [1], 315.0 [2] |
 | (3R)-3-[(1S)-1-(3-Chloro-2-fluorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide | IC50 | 0.1 [1], 0.73 [2], 9.4 [3], 27.0 [4] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[(4S)-1-[[(2S)-1-(benzylamino)-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | IC50 | 18.0 [1], 150.0 [2], 1900.0 [3] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[(4S)-1-[[(2S)-1-(benzylamino)-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | Ki | 43.0 [1] |
 | N-[2-[2-[3-Chloro-4-[(3S,4S)-4-(3,4-difluorophenyl)piperidin-3-yl]phenyl]phenyl]ethyl]acetamide | IC50 | 0.5 [1], 7.5 [2] |
 | (2R)-2-(Aminomethyl)-N-[[2-chloro-5-(3-methoxypropyl)phenyl]methyl]-N-cyclopropyl-3-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl]propanamide | IC50 | 0.09 [1], 2.4 [2] |
 | Methyl N-[[4-chloro-3-[[cyclopropyl-[(3R,4S)-4-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl]piperidine-3-carbonyl]amino]methyl]phenyl]methyl]carbamate | IC50 | 0.09 [1], 2.0 [2] |
 | (3R,4S)-N-Cyclopropyl-4-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl]-N-[[3-(2-methoxyethoxy)-5-(3-methoxypropyl)phenyl]methyl]piperidine-3-carboxamide | IC50 | 0.02 [1], 4.4 [2], 5.0 [3] |
 | (3R,4S)-N-Cyclopropyl-N-[[3-(2-methoxyethoxy)-5-(3-methoxypropyl)phenyl]methyl]-4-(1-methyl-2-oxopyridin-4-yl)piperidine-3-carboxamide | IC50 | 12.0 [1], 31.0 [2] |
 | (2S)-N-[(2S,3R,4S)-1-Cyclohexyl-3,4-dihydroxy-6-methylheptan-2-yl]-2-[(2S)-1-[4-(methoxymethoxy)piperidin-1-yl]-1-oxo-3-phenylpropan-2-yl]oxypropanamide | IC50 | 1.3 [1], 7.0 [2], 27.0 [3], 340.0 [4] |
 | (2S)-N-[(2S,3R,4S)-1-Cyclohexyl-3,4-dihydroxy-6-methylheptan-2-yl]-2-[(2S)-1-[4-(methoxymethoxy)piperidin-1-yl]-1-oxo-3-phenylpropan-2-yl]oxypentanamide | IC50 | 1.4 [1], 3.3 [2], 5.5 [3], 31.0 [4] |
 | (2S)-N-[(2S,3R,4S)-1-Cyclohexyl-3,4-dihydroxy-6-methylheptan-2-yl]-2-[(2S)-1-[4-(methoxymethoxy)piperidin-1-yl]-1-oxo-3-phenylpropan-2-yl]oxybutanamide | IC50 | 0.9 [1], 5.4 [2], 7.9 [3], 120.0 [4] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[3-hydroxy-1-[[(2S)-1-[(4-methoxyphenyl)methylamino]-4-methyl-1-oxopentan-2-yl]amino]-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | IC50 | 6.7 [1], 33.0 [2] |
 | Tert-butyl N-[(2S)-1-[[(2S)-1-[[3-hydroxy-1-[[(2S)-1-[(4-methoxyphenyl)methylamino]-4-methyl-1-oxopentan-2-yl]amino]-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate | Ki | 12.0 [1], 100.0 [2] |
 | Methyl (3S,4S)-3-hydroxy-4-[[(2S)-2-[[(3S,4S)-3-hydroxy-6-methyl-4-[[(2S)-1-[[(2S)-1-(3-methylbutanoylamino)-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopentan-2-yl]amino]heptanoyl]amino]propanoyl]amino]-6-methylheptanoate | IC50 | 30.0 [1], 42.0 [2], 58.0 [3], 420.0 [4] |
 | N-[(2S)-1-[[(2S,3S,5S)-1-Cyclohexyl-3,5-dihydroxy-6-methylheptan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-1H-indole-2-carboxamide | IC50 | 42.0 [1], 45.0 [2], 93.0 [3], 3500.0 [4] |
 | (2R,4S,5S,7S)-5-Amino-N-(4-amino-4-oxobutyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-2,8-dimethylnonanamide | IC50 | 1.0 [1], 3.0 [2] |
 | (2S,4S,5S)-6-Cyclohexyl-4-hydroxy-5-[[(2S)-2-[(2S)-1-[4-(methoxymethoxy)piperidin-1-yl]-1-oxo-3-phenylpropan-2-yl]oxyhexanoyl]amino]-N-(3-morpholin-4-ylpropyl)-2-propan-2-ylhexanamide | IC50 | 2.4 [1], 2.8 [2] |