| CID 24754886 | IC50 | 38.0 [1], 46.2 [2], 60.0 [3] |
| CID 24754886 | Ki | 0.8 [1], 1.0 [2], 6.7 [3], 6.8 [4], 18.0 [5] |
| (3S,6S,10As)-N-[(S)-[1-[4-[4-[4-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]butyl]phenyl]butyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | IC50 | 1.0 [1], 4.6 [2], 5.7 [3] |
| (3S,6S,10As)-N-[(S)-[1-[4-[4-[4-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]butyl]phenyl]butyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | Ki | 0.5 [1], 1.0 [2], 1.5 [3] |
| Lcl-161 | IC50 | 0.4 [1], 58.0 [2], 61.0 [3], 2140.0 [4], 2720.0 [5] |
| (3S,6S,10As)-N-[(S)-[1-[4-[4-[4-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]butyl]phenyl]butyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | IC50 | 10000.0 [1], 50000.0 [2] |
| (3S,6S,10As)-N-[(S)-[1-[4-[4-[4-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]butyl]phenyl]butyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | Ki | 3000.0 [1], 9000.0 [2] |
| (3S,6S,10As)-N-[(S)-[1-[[4-[[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]methyl]phenyl]methyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | IC50 | 8.8 [1], 10.0 [2] |
| (3S,6S,10As)-N-[(S)-[1-[[4-[[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]methyl]phenyl]methyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | Ki | 2.0 [1] |
| (3S,6S,10As)-N-[(S)-[1-[2-[4-[2-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]ethyl]phenyl]ethyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | IC50 | 5.7 [1], 6.2 [2] |
| (3S,6S,10As)-N-[(S)-[1-[2-[4-[2-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]ethyl]phenyl]ethyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | Ki | 1.0 [1], 1.5 [2] |
| (3S,6S,10As)-N-[(S)-[1-[3-[4-[3-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]propyl]phenyl]propyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | IC50 | 2.6 [1], 3.6 [2] |
| (3S,6S,10As)-N-[(S)-[1-[3-[4-[3-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]propyl]phenyl]propyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | Ki | 1.0 [1] |
| (3S,6S,10As)-N-[(S)-[1-[6-[4-[6-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]hexyl]phenyl]hexyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | IC50 | 5.4 [1], 9.5 [2] |
| (3S,6S,10As)-N-[(S)-[1-[6-[4-[6-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]hexyl]phenyl]hexyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | Ki | 1.0 [1], 3.0 [2] |
| (3S,6S,10As)-N-[(S)-[1-[8-[4-[8-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]octyl]phenyl]octyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | IC50 | 7.3 [1], 13.0 [2] |
| (3S,6S,10As)-N-[(S)-[1-[8-[4-[8-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]octyl]phenyl]octyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | Ki | 2.0 [1], 2.5 [2] |
| (3S,6S,10As)-N-[(S)-[1-[10-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]decyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | IC50 | 2.8 [1], 9.0 [2] |
| (3S,6S,10As)-N-[(S)-[1-[10-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]decyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | Ki | 1.0 [1], 3.0 [2] |
| (3S,6S,10As)-N-[(S)-[1-[12-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]dodecyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | IC50 | 3.2 [1], 9.2 [2] |
| (3S,6S,10As)-N-[(S)-[1-[12-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]dodecyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | Ki | 1.0 [1], 3.0 [2] |
| (3S,6S,10As)-N-[(S)-[1-[4-[1-[4-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]butyl]triazol-4-yl]butyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | IC50 | 6.2 [1], 6.5 [2] |
| (3S,6S,10As)-N-[(S)-[1-[4-[1-[4-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]butyl]triazol-4-yl]butyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | Ki | 1.0 [1], 2.0 [2] |
| (3S,6S,10As)-N-[(S)-[1-[4-[4-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]butylcarbamoylamino]butyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | IC50 | 6.8 [1], 7.4 [2] |
| (3S,6S,10As)-N-[(S)-[1-[4-[4-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]butylcarbamoylamino]butyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | Ki | 1.0 [1], 2.0 [2] |
| (3S,6S,10As)-N-[(S)-[1-[5-[5-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]pentoxy]pentyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | IC50 | 4.9 [1], 7.4 [2] |
| (3S,6S,10As)-N-[(S)-[1-[5-[5-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]pentoxy]pentyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | Ki | 1.0 [1], 2.0 [2] |
| (3S,6S,10As)-N-[(S)-[1-[2-[4-[2-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]ethoxy]butoxy]ethyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | IC50 | 7.5 [1], 9.8 [2] |
| (3S,6S,10As)-N-[(S)-[1-[2-[4-[2-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]ethoxy]butoxy]ethyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | Ki | 1.0 [1], 3.0 [2] |
| (3S,6S,10As)-N-[(S)-[1-[2-[2-[2-[2-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | IC50 | 13.0 [1], 14.0 [2] |
| (3S,6S,10As)-N-[(S)-[1-[2-[2-[2-[2-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]ethoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | Ki | 2.0 [1], 3.0 [2] |
| (3S,6S,10As)-N-[(S)-[1-[4-[4-[4-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]butyl]phenyl]butyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | IC50 | 16.0 [1], 23.0 [2] |
| (3S,6S,10As)-N-[(S)-[1-[4-[4-[4-[4-[(S)-[[(3S,6S,10aS)-6-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carbonyl]amino]-phenylmethyl]triazol-1-yl]butyl]phenyl]butyl]triazol-4-yl]-phenylmethyl]-6-[[(2S)-2-(methylamino)propanoyl]amino]-5-oxo-2,3,6,7,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a]azocine-3-carboxamide | Ki | 3.0 [1], 6.0 [2] |
| Gdc-0152 | IC50 | 10.4 [1] |
| Gdc-0152 | Ki | 17.0 [1], 14500.0 [2] |
| CID 25172871 | IC50 | 9.0 [1] |
| CID 25172871 | Ki | 1.5 [1] |
| (5S,8S,10Ar)-3-acetyl-N-benzhydryl-5-[[(2S)-2-(methylamino)propanoyl]amino]-6-oxo-1,2,4,5,8,9,10,10a-octahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide | Ki | 1.1 [1], 1.3 [2] |
| (8S,11S,14S,17S,29S,32S,35S,38S)-10,31-Bis[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-14,35-bis(naphthalen-2-ylmethyl)-12,15,33,36-tetraoxo-2,23-dioxa-5,6,7,10,13,16,26,27,28,31,34,37-dodecazaheptacyclo[38.2.2.219,22.14,7.18,11.125,28.129,32]pentaconta-1(43),4(50),5,19,21,25(46),26,40(44),41,47-decaene-17,38-dicarboxylic acid | IC50 | 5.0 [1], 22.0 [2] |
| 4-N-[(3S)-2-[(2S)-3,3-Dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-3-[[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]carbamoyl]-3,4-dihydro-1H-isoquinolin-7-yl]-1-N-[(3S,5S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-5-[[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]carbamoyl]pyrrolidin-3-yl]benzene-1,4-dicarboxamide | IC50 | 10.0 [1], 15.0 [2] |
| 1-(6-Benzyl-3,3-dimethyl-2H-pyrrolo[3,2-c]pyridin-1-yl)-2-[(2R,5R)-2-(methoxymethyl)-5-methylpiperazin-1-yl]ethanone | IC50 | 10.0 [1] |
| 1-(3,3-Dimethyl-6-chloroindoline-1-yl)-2-((3R)-3-methylpiperazine-1-yl)ethanone | IC50 | 3700.0 [1] |
| 1-[6-Chloro-2,3-dihydro-1H-pyrrolo[3,2-c]pyridine-1-yl]-2-[(3R)-3-methylpiperazino]ethanone | IC50 | 20000.0 [1] |
| 1-(3,3-Dimethyl-6-chloroindoline-1-yl)-2-((3R,6R)-3-methyl-6-methoxymethylpiperazine-1-yl)ethanone | IC50 | 650.0 [1] |
| (2S,5S,8S,11S,17S,20S,23S,26S)-4,19-Bis[(2S)-3-methyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-8,23-bis(naphthalen-2-ylmethyl)-6,9,21,24-tetraoxo-1,4,7,10,14,15,16,19,22,25,29,30-dodecazapentacyclo[26.2.1.12,5.113,16.117,20]tetratriaconta-13(33),14,28(31),29-tetraene-11,26-dicarboxylic acid | IC50 | 3.0 [1], 9.0 [2] |
| (2S)-N-[(3S,4S)-5-Acetyl-7-cyano-4-methyl-1-[(2-methylnaphthalen-1-yl)methyl]-2-oxo-3,4-dihydro-1,5-benzodiazepin-3-yl]-2-(methylamino)propanamide | IC50 | 2640.0 [1], 54800.0 [2] |
| (2S)-N-[(3S)-5-[[2-Cyano-1-(2-cyanophenyl)indol-3-yl]methyl]-4-oxospiro[3H-1,5-benzoxazepine-2,4'-oxane]-3-yl]-2-(methylamino)propanamide;hydrochloride | IC50 | 271.0 [1], 55000.0 [2] |
| (8S,11S,14S,17S,29S,32S,35S,38S)-10,31-Bis[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-14,35-bis(naphthalen-2-ylmethyl)-12,15,33,36-tetraoxo-2,23-dioxa-5,6,7,10,13,16,26,27,28,31,34,37-dodecazaheptacyclo[38.2.2.219,22.14,7.18,11.125,28.129,32]pentaconta-1(43),4(50),5,19,21,25(46),26,40(44),41,47-decaene-17,38-dicarboxylic acid | IC50 | 7.0 [1], 24.0 [2] |
| 1-(6-Benzyl-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl)-2-[(2R,5R)-2-(methoxymethyl)-5-methylpiperazin-1-yl]ethanone | IC50 | 14.0 [1] |
| 1-(6-Chloro-3,3-dimethyl-2H-pyrrolo[3,2-c]pyridin-1-yl)-2-[(2R,5R)-2-(methoxymethyl)-5-methylpiperazin-1-yl]ethanone | IC50 | 320.0 [1] |
| (5S,10Ar)-3-N-[6-[[(5S,8S,10aR)-5-[[(2S)-2-(methylamino)propanoyl]amino]-6-oxo-8-[(3-phenylcyclobutyl)carbamoyl]-1,2,4,5,8,9,10,10a-octahydropyrrolo[1,2-a][1,5]diazocine-3-carbonyl]amino]hexyl]-5-[[(2S)-2-(methylamino)propanoyl]amino]-6-oxo-8-N-(3-phenylcyclobutyl)-1,2,4,5,8,9,10,10a-octahydropyrrolo[1,2-a][1,5]diazocine-3,8-dicarboxamide | IC50 | 1000.0 [1] |
| Birinapant | IC50 | 50.0 [1] |
| AT-406 | Ki | 1.9 [1] |
| (2S)-N-[(1S)-2-[(3Ar,7aS)-6-(2-phenylethyl)-3,3a,4,5,7,7a-hexahydro-2H-pyrrolo[2,3-c]pyridin-1-yl]-1-cyclohexyl-2-oxoethyl]-2-(methylamino)propanamide | IC50 | 27.0 [1] |
| Bestatin Methyl Ester | IC50 | 690.0 [1] |
| Nvp-cgm097 | IC50 | 50000.0 [1] |
| CID 49847690 | IC50 | 15.0 [1] |
| (2S,3S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-Aminopropanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoic acid | IC50 | 0.32 [1] |
| L-Alanyl-L-valyl-L-prolyl-L-isoleucinamide | Ki | 188.0 [1] |
| AT-Iap | IC50 | 0.32 [1] |
| LCL161-O-Me | IC50 | 4.8 [1] |
| (5S,8S,10Ar)-N-benzhydryl-5-[[(2S)-2-(methylamino)propanoyl]amino]-6-oxo-2,3,4,5,8,9,10,10a-octahydro-1H-pyrrolo[1,2-a][1,5]diazocine-8-carboxamide | Ki | 1.2 [1] |
| (3S,6S,7R,9As)-N-benzhydryl-7-[2-(benzylamino)ethyl]-6-[[(2S)-2-(methylamino)butanoyl]amino]-5-oxo-1,2,3,6,7,8,9,9a-octahydropyrrolo[1,2-a]azepine-3-carboxamide | IC50 | 2.0 [1] |
| (5S,8S,10Ar)-3-[5-[4-[5-[(5S,8S,10aR)-8-(benzhydrylcarbamoyl)-5-[[(2S)-2-(methylamino)propanoyl]amino]-6-oxo-1,2,4,5,8,9,10,10a-octahydropyrrolo[1,2-a][1,5]diazocin-3-yl]-5-oxopentyl]phenyl]pentanoyl]-N-benzhydryl-5-[[(2S)-2-(methylamino)propanoyl]amino]-6-oxo-1,2,4,5,8,9,10,10a-octahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide | Ki | 2.9 [1] |
| (2S,4S,6R,9S)-8-[(2S)-2-Cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-[(4R)-3,4-dihydro-2H-chromen-4-yl]-1,8-diazatricyclo[4.4.0.02,4]decane-9-carboxamide;dihydrochloride | IC50 | 3.5 [1] |
| (2R,4R,6R,9S)-8-[(2S)-2-Cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-[(4R)-3,4-dihydro-2H-chromen-4-yl]-1,8-diazatricyclo[4.4.0.02,4]decane-9-carboxamide;dihydrochloride | IC50 | 28.0 [1] |
| (3S,8Ar)-2-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-[(4R)-3,4-dihydro-2H-chromen-4-yl]-3,4,6,7,8,8a-hexahydro-1H-pyrrolo[1,2-a]pyrazine-3-carboxamide;dihydrochloride | IC50 | 2.1 [1] |
| (2S)-2-[[(2S)-2-Aminopropanoyl]amino]-3-methylbutanamide | IC50 | 24000.0 [1] |
| (3S)-2-[(2S)-3,3-Dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-7-[[(3S,5S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-5-[[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]carbamoyl]pyrrolidin-3-yl]amino]-N-[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]-3,4-dihydro-1H-isoquinoline-3-carboxamide | IC50 | 3.4 [1] |
| 1-[6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl]-2-[(2R,5R)-5-methyl-2-[[(3R)-3-methylmorpholin-4-yl]methyl]piperazin-1-yl]ethanone | IC50 | 0.22 [1] |
| (3S)-2-[(2S)-3,3-Dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-N-[[4-[[(3S,5S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-5-[[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]carbamoyl]pyrrolidin-3-yl]carbamoyl]phenyl]methyl]-N-[(1S)-1,2,3,4-tetrahydronaphthalen-1-yl]-3,4-dihydro-1H-isoquinoline-3-carboxamide | IC50 | 25.0 [1] |
| N'-[(3S)-2-[(2S)-3,3-Dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-3-[[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]carbamoyl]-3,4-dihydro-1H-isoquinolin-7-yl]-N-[(3S,5S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-5-[[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]carbamoyl]pyrrolidin-3-yl]pentanediamide | IC50 | 3.4 [1] |
| (3S)-2-[(2S)-3,3-Dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-7-N-[5-[[(3S,5S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-5-[[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]carbamoyl]pyrrolidin-3-yl]carbamoyl]-1,3-benzothiazol-2-yl]-3-N-[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]-3,4-dihydro-1H-isoquinoline-3,7-dicarboxamide | IC50 | 11.0 [1] |
| 2-[(2R,5R)-2-[[(2R,5R)-2,5-Dimethylmorpholin-4-yl]methyl]-5-methylpiperazin-1-yl]-1-[6-[(4-fluorophenyl)methyl]-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl]ethanone | IC50 | 4.2 [1] |
| 2-[(2R,5R)-2-[[(3R,5S)-3,5-Dimethylmorpholin-4-yl]methyl]-5-methylpiperazin-1-yl]-1-[6-[(4-fluorophenyl)methyl]-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl]ethanone | IC50 | 0.62 [1] |
| 2-[(2R,5R)-2-[[(3R,5R)-3,5-Dimethylmorpholin-4-yl]methyl]-5-methylpiperazin-1-yl]-1-[6-[(R)-(4-fluorophenyl)-hydroxymethyl]-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl]ethanone | IC50 | 2.3 [1] |
| (3S)-2-[(2S)-3,3-Dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-N-[[4-[[(3S,5S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-5-[[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]carbamoyl]pyrrolidin-3-yl]carbamoyl]phenyl]methyl]-N-[(1S)-2-methoxy-1-phenylethyl]-3,4-dihydro-1H-isoquinoline-3-carboxamide | IC50 | 8.0 [1] |
| (3S)-2-[(2S)-3,3-Dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-7-[[4-[2-[[(3S,5S)-1-[(2S)-3,3-dimethyl-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]-5-[[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]carbamoyl]pyrrolidin-3-yl]amino]ethyl]benzoyl]amino]-N-[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]-3,4-dihydro-1H-isoquinoline-3-carboxamide | IC50 | 4.2 [1] |
| 1-[2-[(2R,5R)-2-[[(3R,5R)-3,5-Dimethylmorpholin-4-yl]methyl]-5-methylpiperazin-1-yl]acetyl]-6-[(4-fluorophenyl)methyl]-3,3-dimethyl-2,4-dihydropyrrolo[3,2-b]pyridin-5-one | IC50 | 0.13 [1] |
| 2-[(2R,5R)-2-[[(3R,5R)-3,5-Dimethylmorpholin-4-yl]methyl]-5-methylpiperazin-1-yl]-1-[6-[(4-fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl]ethanone | IC50 | 0.1 [1] |
| 1-[2-[(2R,5R)-2-[[(3R,5R)-3,5-Dimethylmorpholin-4-yl]methyl]-5-methylpiperazin-1-yl]acetyl]-6-[(4-fluorophenyl)methyl]-3,3,4-trimethyl-2H-pyrrolo[3,2-b]pyridin-5-one | IC50 | 0.18 [1] |
| 1-[2-[(2R,5R)-2-[[(3R,5R)-3,5-Dimethylmorpholin-4-yl]methyl]-5-methylpiperazin-1-yl]acetyl]-6-[(4-fluorophenyl)methyl]-3,3-dimethyl-2H-pyrrolo[2,3-c]pyridin-5-one | IC50 | 0.7 [1] |
| N-[2-[2-[2-[3-[2-[(2S)-1-[(2S)-2-Cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]pyrrolidin-2-yl]-1,3-thiazole-4-carbonyl]phenoxy]ethoxy]ethoxy]ethyl]-3-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]benzamide | IC50 | 220.0 [1] |
| (3S,6S,7R,9As)-N-benzhydryl-7-[[3-[[2-[bis(pyridin-2-ylmethyl)amino]acetyl]amino]propanoylamino]methyl]-6-[[(2S)-2-(methylamino)butanoyl]amino]-5-oxo-1,2,3,6,7,8,9,9a-octahydropyrrolo[1,2-a]azepine-3-carboxamide | IC50 | 1.35 [1] |
| (3S,6S,7R,9As)-N-benzhydryl-7-[[[2-[bis(pyridin-2-ylmethyl)amino]acetyl]amino]methyl]-6-[[(2S)-2-(methylamino)butanoyl]amino]-5-oxo-1,2,3,6,7,8,9,9a-octahydropyrrolo[1,2-a]azepine-3-carboxamide | IC50 | 1.52 [1] |
| (3S,6S,7R,9As)-N-benzhydryl-7-[[11-[[2-[bis(pyridin-2-ylmethyl)amino]acetyl]amino]undecanoylamino]methyl]-6-[[(2S)-2-(methylamino)butanoyl]amino]-5-oxo-1,2,3,6,7,8,9,9a-octahydropyrrolo[1,2-a]azepine-3-carboxamide | IC50 | 6.08 [1] |
| (3S,6S,7R,9As)-N-benzhydryl-7-[[[2-[2-[2-[[2-[bis(pyridin-2-ylmethyl)amino]acetyl]amino]ethoxy]ethoxy]acetyl]amino]methyl]-6-[[(2S)-2-(methylamino)butanoyl]amino]-5-oxo-1,2,3,6,7,8,9,9a-octahydropyrrolo[1,2-a]azepine-3-carboxamide | IC50 | 1.66 [1] |
| (3S,6S,7R,9As)-7-(benzamidomethyl)-N-[(1S)-2-[2-[bis(pyridin-2-ylmethyl)amino]ethylamino]-2-oxo-1-phenylethyl]-6-[[(2S)-2-(methylamino)butanoyl]amino]-5-oxo-1,2,3,6,7,8,9,9a-octahydropyrrolo[1,2-a]azepine-3-carboxamide | IC50 | 1.09 [1] |
| Sniper(abl)-062 | IC50 | 86.0 [1] |
| 4-[(2S)-3-[(2R)-2-(6-Benzylpyrazin-2-yl)pyrrolidin-1-yl]-2-[[(2S)-2-(methylamino)propanoyl]amino]-3-oxopropyl]benzenesulfonic acid | IC50 | 1000.0 [1] |
| 4-[(2S)-3-[(2S)-2-(2,3-Dihydro-1H-inden-2-ylcarbamoyl)pyrrolidin-1-yl]-2-[[(2S)-2-(methylamino)propanoyl]amino]-3-oxopropyl]benzenesulfonic acid | IC50 | 1000.0 [1] |
| (2S)-N-[(2S)-1-[(2R)-2-(6-Benzylpyrazin-2-yl)pyrrolidin-1-yl]-3-[3-chloro-4-(trifluoromethyl)phenyl]-1-oxopropan-2-yl]-2-(methylamino)propanamide | IC50 | 352.6 [1] |
| (2S)-N-[(2S)-4-Amino-1-[2-(1H-benzimidazol-2-yl)pyrrolidin-1-yl]-1-oxobutan-2-yl]-2-(methylamino)propanamide | IC50 | 16000.0 [1] |
| (2S)-N-[(2S)-1-[2-(1H-Benzimidazol-2-yl)pyrrolidin-1-yl]-3-[4-(diaminomethylideneamino)phenyl]-1-oxopropan-2-yl]-2-(methylamino)propanamide | IC50 | 5000.0 [1] |
| [4-[(2S)-3-[(2R)-2-(6-Benzylpyrazin-2-yl)pyrrolidin-1-yl]-2-[[(2S)-2-(methylamino)propanoyl]amino]-3-oxopropyl]phenyl]methylphosphonic acid | IC50 | 2000.0 [1] |
| N-[4-[Chloro(difluoro)methoxy]phenyl]-6-[3-[2-[2-[2-[3-[2-[(2S)-1-[(2S)-2-cyclohexyl-2-[methyl-[(2S)-2-(methylamino)propanoyl]amino]acetyl]pyrrolidin-2-yl]-1,3-thiazole-4-carbonyl]phenoxy]ethoxy]ethoxy]ethylcarbamoyl]pyrrolidin-1-yl]-5-(1H-pyrazol-5-yl)pyridine-3-carboxamide | IC50 | 1000.0 [1] |
| 2-[(2R,5R)-2-[[(3R,5R)-3,5-Dimethylmorpholin-4-yl]methyl]-5-methylpiperazin-1-yl]-1-[6-[(4-fluoro-2-hydroxyphenyl)methyl]-3,3-dimethyl-2H-pyrrolo[3,2-b]pyridin-1-yl]ethanone | IC50 | 0.59 [1] |
| 4-[[(2S)-3-[(2R)-2-[6-[(3-Fluorophenyl)methyl]pyrazin-2-yl]pyrrolidin-1-yl]-2-[[(2S)-2-(methylamino)propanoyl]amino]-3-oxopropyl]carbamoyl]benzenesulfonyl fluoride | IC50 | 200.0 [1] |
| (2S)-N-[(1R)-4-Fluoro-2,3-dihydro-1H-inden-1-yl]-1-[(2S)-2-[[(2S)-2-(methylamino)propanoyl]amino]-3-(4-nitrophenyl)propanoyl]pyrrolidine-2-carboxamide | IC50 | 23.9 [1] |
| 4-[[(2S)-3-[(2S)-2-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-[[(2S)-2-(methylamino)propanoyl]amino]-3-oxopropyl]carbamoyl]benzenesulfonyl fluoride | IC50 | 181.0 [1] |