| Somatostatin | IC50 | 0.4 [1], 3.1 [2], 3.3 [3] |
| Somatostatin | Ki | 0.1 [1], 0.14 [2] |
| (4R,7S,10R,13S,16R,19S,22R,25S,28R,31S,34R,37S)-37-[[2-[[(2S)-2-[[(2S)-6-Amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]propanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-carboxybutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]propanoyl]amino]acetyl]amino]-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carboxylic acid | IC50 | 3.7 [1] |
| (4R,7S,10R,13S,16R,19S,22R,25S,28R,31S,34R,37S)-37-[[2-[[(2S)-2-[[(2S)-6-Amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]propanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-carboxybutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]propanoyl]amino]acetyl]amino]-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carboxylic acid | Ki | 1.3 [1] |
| CID 56927659 | IC50 | 0.95 [1] |
| (4R,7S,10S,13S,16R,19S,22S,25R)-25-Amino-13-(4-aminobutyl)-7,19,22-tribenzyl-10-[(1R)-1-hydroxyethyl]-16-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid | IC50 | 13.0 [1] |
| (1R,3R)-1-(Oxan-4-yl)-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole | IC50 | 11.0 [1], 14.0 [2], 22.0 [3] |
| (3R)-1-Cyclohexyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole | IC50 | 0.8 [1], 26.0 [2], 26.1 [3] |
| (3R)-1-Cyclohexyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole | Ki | 1.7 [1] |
| (4R,7S,10S,13R,16S,19R)-10-(4-Aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-N-[(2S,3R)-1,3-dihydroxybutan-2-yl]-7-[(1R)-1-hydroxyethyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide | IC50 | 92.9 [1] |
| (4R,7S,10S,13R,16S,19R)-10-(4-Aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-N-[(2S,3R)-1,3-dihydroxybutan-2-yl]-7-[(1R)-1-hydroxyethyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide | Ki | 5.01 [1], 15.2 [2], 26.8 [3] |
| (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R)-37-[[2-[[(2S)-2-[[(2S)-6-Amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]propanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-carboxybutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]propanoyl]amino]acetyl]amino]-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-13,25,28-tribenzyl-10,16-bis[(1S)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-2-ylmethyl)-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carboxylic acid | IC50 | 3.2 [1], 3.5 [2], 4.9 [3], 7.1 [4] |
| (3S)-1,1-Dibutyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indole | IC50 | 2.7 [1], 6.8 [2] |
| (3S)-1,1-Dibutyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indole | Ki | 0.64 [1], 3.4 [2] |
| 6-[(1R,3R)-3-[5-(4-Fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-3-carboxylic acid | IC50 | 2.4 [1], 7.9 [2], 23.7 [3], 87.2 [4] |
| CID 5311374 | IC50 | 1000.0 [1], 10000.0 [2] |
| (4R,7S,10S,13S,16S,19S,22S,25R)-25-Amino-13-(4-aminobutyl)-7,19,22-tribenzyl-10-[(1R)-1-hydroxyethyl]-16-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid | IC50 | 13.0 [1] |
| H-DPhe-c[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-NH2 | IC50 | 38.0 [1], 39.0 [2] |
| (3R)-1,1-Dibutyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indole | IC50 | 2.7 [1] |
| (3R)-1,1-Dibutyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indole | Ki | 0.64 [1] |
| 3-[(1R,3R)-3-[5-(5-Fluoropyridin-2-yl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,2,4-oxadiazole | IC50 | 2.5 [1], 3.0 [2], 3.6 [3] |
| (1R,3R)-3-[5-(4-Fluorophenyl)-1H-imidazol-2-yl]-1-(oxan-4-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole | IC50 | 2.8 [1], 5.7 [2] |
| Seglitide | IC50 | 105.0 [1] |
| Seglitide | Ki | 31.62 [1] |
| Cyclo(Pro-Phe-D-Trp-Lys-Thr-Phe) | Ki | 125.89 [1], 129.0 [2] |
| 8-D-Tryptophan-somatostatin | IC50 | 2.4 [1] |
| 8-D-Tryptophan-somatostatin | Ki | 0.61 [1] |
| 2-(1-(4-Amino-3,5-diethoxybenzyl)piperidin-4-ylamino)benzo[d]oxazole-5-sulfonamide | Ki | 10000.0 [1] |
| (4R,7S,10S,13R,16S,19S)-10-(4-Aminobutyl)-19-[[(2S)-2-amino-3-(4-chlorophenyl)propanoyl]amino]-N-[(2S)-1-amino-3-naphthalen-2-yl-1-oxopropan-2-yl]-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide | Ki | 93.0 [1], 115.1 [2] |
| (4R,7S,10S,13S,16S,19S,22S,25R)-25-Amino-13-(4-aminobutyl)-7,22-dibenzyl-10-[(1R)-1-hydroxyethyl]-19-[(4-hydroxyphenyl)methyl]-16-[(1S)-1-naphthalen-2-ylethyl]-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid | IC50 | 600.0 [1], 825.0 [2] |
| (4R,7S,10S,13S,16R,19S,22S,25R)-25-Amino-13-(4-aminobutyl)-7,22-dibenzyl-10-[(1R)-1-hydroxyethyl]-16-(1H-indol-3-ylmethyl)-19-methyl-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid | IC50 | 897.0 [1] |
| (4R,7S,10S,13S,16R,19S,22S,25R)-25-Amino-13-(4-aminobutyl)-7,22-dibenzyl-10-[(1R)-1-hydroxyethyl]-19-[(4-hydroxyphenyl)methyl]-16-[(1S)-1-naphthalen-2-ylethyl]-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid | IC50 | 18.0 [1], 664.0 [2] |
| Des-AA1,2,5-[IAmp9,Tyr11]-SRIF | IC50 | 1000.0 [1] |
| (4R,7S,10R,13S,16R,19S,22S,25S,28R,31R,34S)-31-(4-Aminobutyl)-34-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33-decaoxo-19-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decazacyclopentatriacontane-4-carboxylic acid | IC50 | 1000.0 [1] |
| (4R,7S,10S,13S,16S,19S,22S,25R)-25-Amino-13-(4-aminobutyl)-7,22-dibenzyl-10-[(1R)-1-hydroxyethyl]-16-(1H-indol-3-ylmethyl)-19-methyl-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid | IC50 | 750.0 [1] |
| 6-Methyl-1,1-dipentyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indole | IC50 | 450.0 [1] |
| 6-Methyl-1,1-dipentyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indole | Ki | 6.9 [1] |
| 1,1-Dibutyl-6-chloro-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indole | IC50 | 43.0 [1] |
| 1,1-Dibutyl-6-chloro-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indole | Ki | 3.4 [1] |
| Ethyl 6-[(1R,3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-2-carboxylate | IC50 | 0.83 [1], 1.97 [2] |
| Ethyl 6-[(1S,3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-2-carboxylate | IC50 | 1.52 [1], 5.36 [2] |
| Ethyl 2-[(1R,3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-4-carboxylate | IC50 | 0.64 [1], 0.78 [2] |
| Ethyl 2-[(1S,3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-4-carboxylate | IC50 | 4.87 [1], 47.1 [2] |
| Ethyl 5-[(1R,3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-3-carboxylate | IC50 | 0.15 [1], 0.78 [2] |
| Ethyl 5-[(1S,3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-3-carboxylate | IC50 | 3.36 [1], 24.0 [2] |
| Ethyl 6-[(1R,3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-3-carboxylate | IC50 | 1.72 [1], 5.25 [2] |
| Ethyl 6-[(1S,3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-3-carboxylate | IC50 | 2.91 [1], 31.6 [2] |
| 6-[(1R,3R)-3-[5-(4-Fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-2-carboxylic acid | IC50 | 4.41 [1], 67.0 [2] |
| 6-[(1S,3R)-3-[5-(4-Fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-2-carboxylic acid | IC50 | 74.7 [1], 105.0 [2] |
| 2-[(1S,3R)-3-[5-(4-Fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-4-carboxylic acid | IC50 | 52.3 [1], 72.7 [2] |
| 5-[(1R,3R)-3-[5-(4-Fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-3-carboxylic acid | IC50 | 0.52 [1], 1.22 [2] |
| 5-[(1S,3R)-3-[5-(4-Fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-3-carboxylic acid | IC50 | 6.12 [1], 10.8 [2] |
| 6-[(1S,3R)-3-[5-(4-Fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-3-carboxylic acid | IC50 | 409.0 [1], 2000.0 [2] |
| (3R)-3-[5-(4-Fluorophenyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole | IC50 | 11.4 [1], 15.0 [2] |
| (3R)-3-[5-(4-Fluorophenyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydro-1H-carbazole | IC50 | 24.9 [1], 538.6 [2] |
| (3R)-1-Cyclohexyl-3-(5-phenyl-1H-imidazol-2-yl)-1,3,4,9-tetrahydropyrano[3,4-b]indole | IC50 | 25.3 [1], 156.6 [2] |
| (3R)-3-[5-(4-Fluorophenyl)-1H-imidazol-2-yl]-1-methyl-1-phenyl-2,3,4,9-tetrahydropyrido[3,4-b]indole | IC50 | 4.6 [1], 15.7 [2] |
| (3R)-3-[5-(4-Fluorophenyl)-1H-imidazol-2-yl]-1-phenyl-1-(trifluoromethyl)-2,3,4,9-tetrahydropyrido[3,4-b]indole | IC50 | 2.1 [1], 13.3 [2] |
| (3R)-1-Cyclohexyl-3-(5-pyridin-2-yl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole | IC50 | 11.3 [1], 28.1 [2] |
| (3R)-1-Cyclohexyl-3-(5-pyridin-3-yl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole | IC50 | 20.0 [1], 28.6 [2] |
| (3R)-1-Cyclohexyl-3-(5-pyridin-4-yl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole | IC50 | 11.5 [1], 17.2 [2] |
| (3R)-1-Cyclohexyl-3-(5-pyrazin-2-yl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole | IC50 | 53.3 [1], 134.6 [2] |
| (3R)-1-Cyclohexyl-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole | IC50 | 2.6 [1], 4.8 [2] |
| 3-[(1R,3R)-3-[5-(5-Fluoropyridin-2-yl)-1H-imidazol-2-yl]-1-(1H-pyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,2,4-oxadiazole | IC50 | 11.0 [1], 20.4 [2] |
| 3-[(1R,3R)-1-(1-Ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,2,4-oxadiazole | IC50 | 1.2 [1], 2.2 [2] |
| 5-Ethyl-3-[(1R,3R)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-1,2,4-oxadiazole | IC50 | 1.2 [1], 2.9 [2] |
| 3-[(1R,3R)-1-[1-(Cyclopropylmethyl)pyrazol-4-yl]-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,2,4-oxadiazole | IC50 | 0.4 [1], 1.1 [2] |
| [3-[(1R,3R)-3-[5-(5-Fluoropyridin-2-yl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-1,2,4-oxadiazol-5-yl]methanamine | IC50 | 11.1 [1], 13.7 [2] |
| 2-[(1R,3R)-3-[5-(5-Fluoropyridin-2-yl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,3,4-oxadiazole | IC50 | 4.9 [1], 6.9 [2] |
| 2-Ethyl-5-[(1R,3R)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-1,3,4-oxadiazole | IC50 | 4.6 [1], 5.1 [2] |
| 2-[(1R,3R)-1-(1-Ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,3,4-oxadiazole | IC50 | 2.2 [1], 4.8 [2] |
| 5-[(1R,3R)-1-(1-Ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-3H-1,3,4-oxadiazol-2-one | IC50 | 3.5 [1], 5.4 [2] |
| 5-[(1R,3R)-1-(1-Ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-3H-1,3,4-oxadiazole-2-thione | IC50 | 3.3 [1], 7.6 [2] |
| 2-[(1R,3R)-1-(1-Ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methylsulfanyl-1,3,4-oxadiazole | IC50 | 0.7 [1], 1.9 [2] |
| 5-[(1R,3R)-3-[5-(5-Fluoropyridin-2-yl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-1,3,4-oxadiazol-2-amine | IC50 | 5.3 [1], 5.6 [2] |
| 5-[(1R,3R)-1-(1-Ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-N-methyl-1,3,4-oxadiazol-2-amine | IC50 | 2.2 [1], 3.5 [2] |
| 5-[(1R,3R)-1-(1-Ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-N,N-dimethyl-1,3,4-oxadiazol-2-amine | IC50 | 4.6 [1], 4.7 [2] |
| 5-[(1R,3R)-3-[5-(5-Fluoropyridin-2-yl)-1H-imidazol-2-yl]-1-(1H-pyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-3-methyl-1,3,4-oxadiazol-2-one | IC50 | 17.3 [1], 17.5 [2] |
| 5-[(1R,3R)-3-[5-(5-Fluoropyridin-2-yl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-3-methyl-1,3,4-oxadiazol-2-one | IC50 | 4.3 [1], 4.5 [2] |
| 3-Ethyl-5-[(1R,3R)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-1,3,4-oxadiazol-2-one | IC50 | 1.6 [1], 2.9 [2] |
| 5-[(1R,3R)-3-[5-(5-Fluoropyridin-2-yl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-3-propan-2-yl-1,3,4-oxadiazol-2-one | IC50 | 0.8 [1], 2.0 [2] |
| 5-[(1R,3R)-1-(1-Ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-3-methyl-1,3,4-oxadiazol-2-one | IC50 | 1.1 [1], 2.3 [2] |
| 3-Ethyl-5-[(1R,3R)-1-(1-ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-1,3,4-oxadiazol-2-one | IC50 | 0.4 [1], 3.0 [2] |
| 5-[(1R,3R)-1-(1-Ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-3-propan-2-yl-1,3,4-oxadiazol-2-one | IC50 | 1.0 [1], 2.1 [2] |
| 3-(Cyclopropylmethyl)-5-[(1R,3R)-1-(1-ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-1,3,4-oxadiazol-2-one | IC50 | 1.3 [1], 1.4 [2] |
| 3-[2-(Dimethylamino)ethyl]-5-[(1R,3R)-1-(1-ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-1,3,4-oxadiazol-2-one | IC50 | 0.5 [1], 2.1 [2] |
| 2-[5-[(1R,3R)-1-(1-Ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-2-oxo-1,3,4-oxadiazol-3-yl]acetic acid | IC50 | 0.8 [1], 4.9 [2] |
| 2-[5-[(1R,3R)-1-(1-Ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-2-oxo-1,3,4-oxadiazol-3-yl]acetamide | IC50 | 0.3 [1], 2.4 [2] |
| 3-[(1R,3R)-3-[5-(5-Fluoropyridin-2-yl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-4H-1,2,4-oxadiazol-5-one | IC50 | 888.4 [1], 1948.0 [2] |
| Methyl 4-[(3R)-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl]piperidine-1-carboxylate | IC50 | 4.0 [1], 66.0 [2] |
| (4R,7S,10S,13R,16S,19S)-10-(4-Aminobutyl)-19-[[(2R)-2-amino-3-(4-chlorophenyl)propanoyl]amino]-N-[(2S)-1-amino-3-naphthalen-2-yl-1-oxopropan-2-yl]-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide | IC50 | 112.0 [1] |
| (4R,7S,10S,13R,16S,19S)-10-(4-Aminobutyl)-19-[[(2R)-2-amino-3-(4-chlorophenyl)propanoyl]amino]-N-[(2S)-1-amino-3-naphthalen-2-yl-1-oxopropan-2-yl]-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide | Ki | 93.0 [1] |
| (4R,7S,10S,13R,16S,19S)-19-[[(2R)-2-Amino-3-(4-chlorophenyl)propanoyl]amino]-N-[(2S)-1-amino-3-naphthalen-2-yl-1-oxopropan-2-yl]-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-10-[4-(methylamino)butyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide | IC50 | 61.0 [1] |
| (4R,7S,10S,13R,16S,19S)-19-[[(2R)-2-Amino-3-(4-chlorophenyl)propanoyl]amino]-N-[(2S)-1-amino-3-naphthalen-2-yl-1-oxopropan-2-yl]-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-10-[4-(methylamino)butyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide | Ki | 50.0 [1] |
| 5-[(3R)-1-(1-Ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-3-methyl-1,3,4-oxadiazol-2-one | IC50 | 24.2 [1], 137.9 [2] |
| 1-Cyclohexyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole;oxalic acid | IC50 | 19.0 [1] |
| 1-Cyclohexyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole;oxalic acid | Ki | 1.7 [1] |
| 5-[1-(1-Ethylpyrazol-4-yl)-3-[5-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-3-methyl-1,3,4-oxadiazol-2-one | IC50 | 75.4 [1], 76.7 [2] |
| Tert-butyl 4-[(3R)-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl]piperidine-1-carboxylate | IC50 | 7.0 [1], 1000.0 [2] |
| 1-[4-[(3R)-3-(5-Phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl]piperidin-1-yl]ethanone | IC50 | 16.0 [1], 46.0 [2] |