| 5-[(3As,4S,6aR)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]-N-[4-[[4-[[2-[[(2R,5S,8S,11S,14S,17S,23S,26S,29S,32S)-17-ethyl-14-[(E,1R,2R)-1-hydroxy-2-methylhex-4-enyl]-4,7,10,13,19,22,28,32-octamethyl-5,8,23,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-11,26-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacont-2-yl]methoxy]acetyl]amino]phenyl]diazenyl]phenyl]pentanamide | IC50 | 89.0 [1], 135.0 [2], 1400.0 [3], 16400.0 [4] |
| Methylsulfanylmethyl (E,5R,6R)-6-[(2S,5R,11S,14S,17R,20R,23S,26S,29S,32R)-5-ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacont-2-yl]-6-hydroxy-5-methylhex-2-enoate | IC50 | 348.0 [1], 2147.0 [2] |
| Methoxymethyl (E,5R,6R)-6-[(2S,5R,11S,14S,17R,20R,23S,26S,29S,32R)-5-ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacont-2-yl]-6-hydroxy-5-methylhex-2-enoate | IC50 | 742.0 [1], 1916.0 [2] |
| 2-[[(2R,5S,8S,11S,14S,17S,23S,26S,29S,32S)-17-Ethyl-14-[(E,1R,2R)-1-hydroxy-2-methylhex-4-enyl]-4,7,10,13,19,22,28,32-octamethyl-5,8,23,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-11,26-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacont-2-yl]methoxy]-N-[4-[[4-[[2-[[(2R,5S,8S,11S,14S,17S,23S,26S,29S,32S)-17-ethyl-14-[(E,1R,2R)-1-hydroxy-2-methylhex-4-enyl]-4,7,10,13,19,22,28,32-octamethyl-5,8,23,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-11,26-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacont-2-yl]methoxy]acetyl]amino]phenyl]diazenyl]phenyl]acetamide | IC50 | 140.0 [1], 358.0 [2] |
| 2-[[(2R,5S,8S,11S,14S,17S,23S,26S,29S,32S)-17-Ethyl-14-[(E,1R,2R)-1-hydroxy-2-methylhex-4-enyl]-4,7,10,13,19,22,28,32-octamethyl-5,8,23,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-11,26-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacont-2-yl]methoxy]-N-(4-phenyldiazenylphenyl)acetamide | IC50 | 49.0 [1], 75.0 [2] |
| Cyclosporin A | IC50 | 183.0 [1] |
| Tacrolimus | IC50 | 14.8 [1] |
| 2-[4-[(2S)-3-[4-(3-Hydroxy-2-methoxycarbonylphenoxy)butylamino]-3-oxo-2-(prop-2-enoxycarbonylamino)propyl]-N-oxaloanilino]benzoic acid | Ki | 200000.0 [1] |
| 2-[[4-[2-Acetamido-3-oxo-3-(pentylamino)propyl]naphthalen-1-yl]-oxaloamino]benzoic acid | Ki | 300000.0 [1] |
| 2-[4-[2-Acetamido-3-[4-(5-chloro-3-hydroxy-2-methoxycarbonylphenoxy)butylamino]-3-oxopropyl]-2-ethyl-N-oxaloanilino]benzoic acid | Ki | 3000.0 [1] |
| (1R,9S,12S,13R,14R,17R,18E,21S,23S,24R,25S,27R)-17-Ethyl-1,14-dihydroxy-12-[(E)-1-[(3R,4R)-4-[(2S)-2-hydroxy-2-naphthalen-2-ylethoxy]-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | IC50 | 2.8 [1] |
| (1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-17-Ethyl-1,14-dihydroxy-23,25-dimethoxy-12-[(E)-1-[(1R,3R,4R)-3-methoxy-4-(2-phenylethoxy)cyclohexyl]prop-1-en-2-yl]-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | IC50 | 7.2 [1] |
| (1R,9S,12S,13R,14R,17R,18E,21S,23S,24R,25S,27R)-17-Ethyl-1,14-dihydroxy-12-[(E)-1-[(3R,4R)-4-[(2R)-2-hydroxy-2-naphthalen-2-ylethoxy]-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | IC50 | 7.32 [1] |
| (1R,9S,12S,13R,14R,17R,18E,21S,23S,24R,25S,27R)-12-[(E)-1-[(3R,4R)-4-[(2S)-2-(1-Benzothiophen-2-yl)-2-hydroxyethoxy]-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | IC50 | 4.17 [1] |
| (1R,9S,12S,13R,14R,17R,18E,21S,23S,24R,25S,27R)-12-[(E)-1-[(3R,4R)-4-[(2R)-2-(3,4-Difluorophenyl)-2-hydroxyethoxy]-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | IC50 | 8.65 [1] |
| (1R,9S,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-17-Ethyl-1,14-dihydroxy-23,25-dimethoxy-12-[(E)-1-[(1R,3R,4R)-3-methoxy-4-(3-phenylpropoxy)cyclohexyl]prop-1-en-2-yl]-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | IC50 | 14.0 [1] |
| (1R,9S,12S,13R,14R,17R,18E,21S,23S,24R,25S,27R)-12-[(E)-1-[(3R,4R)-4-[(2R)-2-(3,5-Dimethylphenyl)-2-hydroxyethoxy]-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | IC50 | 8.7 [1] |
| (1R,9S,12S,13R,14R,17R,18E,21S,23S,24R,25S,27R)-17-Ethyl-1,14-dihydroxy-12-[(E)-1-[(3R,4R)-4-[(2R)-2-hydroxy-2-[3-(trifluoromethyl)phenyl]ethoxy]-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | IC50 | 5.85 [1] |
| (1R,9S,12S,13R,14R,17R,18E,21S,23S,24R,25S,27R)-12-[(E)-1-[(3R,4R)-4-[(2S)-2-(3,4-Difluorophenyl)-2-hydroxyethoxy]-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | IC50 | 7.25 [1] |
| (1R,9S,12S,13R,14R,17R,18E,21S,23S,24R,25S,27R)-17-Ethyl-1,14-dihydroxy-12-[(E)-1-[(3R,4R)-4-[(2S)-2-hydroxy-2-[3-(trifluoromethyl)phenyl]ethoxy]-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | IC50 | 4.93 [1] |
| (1R,9S,12S,13R,14R,17R,18E,21S,23S,24R,25S,27R)-12-[(E)-1-[(3R,4R)-4-[(2S)-2-(3,5-Dimethylphenyl)-2-hydroxyethoxy]-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | IC50 | 7.91 [1] |
| (1R,9S,12S,13R,14R,17R,18E,21S,23S,24R,25S,27R)-12-[(E)-1-[(3R,4R)-4-[(2R)-2-(1-Benzothiophen-2-yl)-2-hydroxyethoxy]-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone | IC50 | 3.96 [1] |
| (E,5R,6R)-6-[(2S,5R,11S,14S,17R,20R,23S,26S,29S,32R)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacont-2-yl]-6-hydroxy-5-methylhex-2-enoic acid | IC50 | 5000.0 [1] |
| Ethyl (E,5R,6R)-6-[(2S,5R,11S,14S,17R,20R,23S,26S,29S,32R)-5-ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacont-2-yl]-6-hydroxy-5-methylhex-2-enoate | IC50 | 363.0 [1] |
| Methyl (5R,6R)-6-[(2S,5R,11S,14S,17R,20R,23S,26S,29S,32R)-5-ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacont-2-yl]-6-hydroxy-5-methylhexanoate | IC50 | 890.0 [1] |
| Methylsulfanylmethyl (5R,6R)-6-[(2S,5R,11S,14S,17R,20R,23S,26S,29S,32R)-5-ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacont-2-yl]-6-hydroxy-5-methylhexanoate | IC50 | 5000.0 [1] |
| 2-Fluoroethyl (5R,6R)-6-[(2S,5R,11S,14S,17R,20R,23S,26S,29S,32R)-5-ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacont-2-yl]-6-hydroxy-5-methylhexanoate | IC50 | 1539.0 [1] |
| Methyl (E,5R,6R)-6-[(2S,5R,11S,14S,17R,20R,23S,26S,29S,32R)-5-ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacont-2-yl]-6-hydroxy-5-methylhex-2-enoate | IC50 | 581.0 [1] |
| 2-Fluoroethyl (E,5R,6R)-6-[(2S,5R,11S,14S,17R,20R,23S,26S,29S,32R)-5-ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacont-2-yl]-6-hydroxy-5-methylhex-2-enoate | IC50 | 636.0 [1] |
| Ethyl (5R,6R)-6-[(2S,5R,11S,14S,17R,20R,23S,26S,29S,32R)-5-ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacont-2-yl]-6-hydroxy-5-methylhexanoate | IC50 | 840.0 [1] |