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Somatostatin receptor 1 Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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SomatostatinIC500.14 [1], 1.6 [2], 1.9 [3]
SomatostatinKi0.29 [1], 0.36 [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 acidIC503.2 [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 acidKi1.9 [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 acidIC5027.0 [1]
(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 acidIC503.2 [1], 3.6 [2], 3.8 [3], 3.9 [4]
(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-carboxamideKi251.19 [1], 300.0 [2], 875.0 [3]
CID 5311374IC501000.0 [1]
(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 acidIC505.3 [1]
H-DPhe-c[Cys-Phe-DTrp-Lys-Thr-Cys]-Thr-NH2IC501000.0 [1]
SeglitideIC501000.0 [1]
SeglitideKi1000.0 [1]
Cyclo(Pro-Phe-D-Trp-Lys-Thr-Phe)Ki630.96 [1], 1000.0 [2]
8-D-Tryptophan-somatostatinIC502.3 [1]
8-D-Tryptophan-somatostatinKi0.32 [1]
2-(1-(4-Amino-3,5-diethoxybenzyl)piperidin-4-ylamino)benzo[d]oxazole-5-sulfonamideKi1750.0 [1], 10000.0 [2]
(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-carboxamideKi1000.0 [1]
(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 acidIC501000.0 [1]
(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 acidIC501000.0 [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 acidIC50410.0 [1], 10000.0 [2]
Des-AA1,2,5-[IAmp9,Tyr11]-SRIFIC5015.0 [1], 17.1 [2]
(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 acidIC5014.0 [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 acidIC501000.0 [1]
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-oneIC501330.0 [1], 5776.0 [2]
(4R,7S,10S,13R,16S,19R)-19-[[(2S)-2-Amino-3-(4-hydroxy-2-iodophenyl)propanoyl]amino]-N-[(2R,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-7,16-dibenzyl-13-[methyl(naphthalene-2-carbonyl)amino]-6,9,12,15,18-pentaoxo-10-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamideIC500.8 [1], 1.0 [2]
LanreotideKi501.19 [1]
PasireotideKi6.31 [1]
EdotreotideIC5010000.0 [1]
VapreotideKi158.49 [1]
(4R,7S,10S,13S,16S,19S,22R,25S,28S,31S,34R)-34-Amino-31-(4-aminobutyl)-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 acidIC5031.0 [1]
CID 15965425Ki2392.0 [1]
CID 56927659IC502362.0 [1]
5-{3,4,5-Tris-benzyloxy-6-[2-(1H-indol-3-yl)-ethoxy]-tetrahydro-pyran-2-ylmethoxy}-pentylamineKi4000.0 [1]
(1R,3R)-1-(Oxan-4-yl)-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indoleIC501000.0 [1]
(3R)-1,1-Dibutyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indoleKi3700.0 [1]
(2R,5R)-5-(4-Aminobutyl)-2-(1H-indol-3-ylmethyl)-7-(naphthalen-1-ylmethyl)-1,4,7-thiadiazonane-3,6-dioneIC50501.0 [1]
H-c[Cys-Phe-DTrp-Lys-Thr-Cys]-OHIC501000.0 [1]
(3S)-1,1-Dibutyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indoleKi10000.0 [1]
N-(1-(4-Chloro-3-ethoxybenzyl)piperidin-4-yl)-5-methylnicotinamideKi5100.0 [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-oxadiazoleIC502300.0 [1]
N-[1-[[3,5-Diethoxy-4-(4-fluorophenyl)phenyl]methyl]piperidin-4-yl]-5-methylpyridine-3-carboxamideIC50300.0 [1]
(4R,7S,10S,13S,16S,19S,22R,25S,28S,31S,34S,37R)-19,34-Bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-37-[[2-[[(2S)-2-aminopropanoyl]amino]acetyl]amino]-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-[(4-hydroxyphenyl)methyl]-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 acidIC50140.0 [1]
5-[[(2R,3S,5R,6R)-6-[2-(1H-Indol-3-yl)ethoxy]-3,5-bis(phenylmethoxy)oxan-2-yl]methoxy]pentan-1-amineKi4100.0 [1]
5-[[(2S,3S,4R,5R,6S)-5-(1H-Imidazol-5-ylmethoxy)-6-[2-(1H-indol-3-yl)ethoxy]-3,4-bis(phenylmethoxy)oxan-2-yl]methoxy]pentan-1-amineKi300.0 [1]
N-[(R)-2-(1H-Indol-3-yl)-1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-4-methoxy-benzamidineKi2310.0 [1]
2-[8-(3-Aminopropyl)-6-(1-benzothiophen-3-yl)imidazo[1,2-a]pyrazin-2-yl]-N-cyclohexyl-2-methylpropanamideKi9700.0 [1]
4-Chloro-N'-[(1R)-2-(1H-indol-3-yl)-1-(5-phenyl-1H-imidazol-2-yl)ethyl]benzenecarboximidamideKi1730.0 [1]
[(R)-1-(4-Phenyl-1H-imidazole-2-yl)-2-(1H-indole-3-yl)ethyl]carbamic acid tert-butyl esterKi10000.0 [1]
(3S,6S,9S,12R,15S,18R)-9-(4-Aminobutyl)-3-benzyl-15-[(4-hydroxyphenyl)methyl]-12-(1H-indol-3-ylmethyl)-1,18-dimethyl-6-propan-2-yl-1,4,7,10,13,16-hexazacyclooctadecane-2,5,8,11,14,17-hexoneIC501000.0 [1]
2,4-Difluoro-N'-[(1R)-2-(1H-indol-3-yl)-1-(5-phenyl-1H-imidazol-2-yl)ethyl]benzenecarboximidamideKi1550.0 [1]
3-[6-(3-Nitrophenyl)-2-phenylimidazo[1,2-a]pyrazin-8-yl]propan-1-amineKi3400.0 [1]
[(R)-1-(4-Phenyl-1H-imidazole-2-yl)-2-(1H-indole-3-yl)ethyl]carbamic acid benzyl esterKi1400.0 [1]
5-((2R,3R,4S,5R,6R)-3,4,5-Tris-benzyloxy-6-methoxy-tetrahydro-pyran-2-ylmethoxy)-pentylamineKi2400.0 [1]
1-[(R)-1-(4-Phenyl-1H-imidazole-2-yl)-2-(1H-indole-3-yl)ethyl]-3-(2,4-difluorophenyl)ureaKi2600.0 [1]
(4R,7S,10S,13R,16S,19S)-10-(4-Aminobutyl)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-7-ethyl-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-carboxamideIC501000.0 [1]
5-[[(2R,3S,5R,6R)-5-(1H-Imidazol-5-ylmethoxy)-6-[2-(1H-indol-3-yl)ethoxy]-3-phenylmethoxyoxan-2-yl]methoxy]pentan-1-amineKi6800.0 [1]
N'-[[(2R,3R,4S,5R,6R)-6-[2-(1H-Indol-3-yl)ethoxy]-3,4,5-tris(phenylmethoxy)oxan-2-yl]methyl]pentane-1,5-diamineKi2100.0 [1]
5-[[(2S,3S,4R,5S,6S)-6-[2-(1H-Indol-3-yl)ethoxy]-3,4,5-tris(phenylmethoxy)oxan-2-yl]methoxy]pentan-1-amineKi4400.0 [1]
(4R,7S,10S,13R,16S,19S)-10-(4-Aminobutyl)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2S)-2-amino-3-phenylpropanoyl]amino]-7-[(1R)-1-hydroxyethyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-16-(pyridin-3-ylmethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamideIC501000.0 [1]
(4R,7S,10S,13R,16S,19S)-10-(4-Aminobutyl)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-7-[(1R)-1-hydroxyethyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-16-(pyridin-3-ylmethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamideIC501000.0 [1]
(4R,7S,10S,13R,16S,19S)-10-(4-Aminobutyl)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2R)-2-amino-3-naphthalen-2-ylpropanoyl]amino]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamideIC501580.0 [1]
(4R,7S,10S,13R,16S,19S)-10-(4-Aminobutyl)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2S)-2-amino-3-naphthalen-2-ylpropanoyl]amino]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamideIC502163.0 [1]
(4R,7S,10S,13R,16S,19S)-10-(4-Aminobutyl)-N-[(2S)-1-amino-3-naphthalen-2-yl-1-oxopropan-2-yl]-19-[[(2S)-2-amino-3-naphthalen-2-ylpropanoyl]amino]-16-(1H-imidazol-5-ylmethyl)-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamideIC501000.0 [1]
5-[[(2S,3S,4R,5R,6S)-6-[2-(1H-Indol-3-yl)ethoxy]-3,4,5-tris(phenylmethoxy)oxan-2-yl]methoxy]pentan-1-amineKi4000.0 [1]
(4R,7S,10S,13R,16S,19S)-10-(4-Aminobutyl)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-7-[(1R)-1-hydroxyethyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-16-(pyridin-3-ylmethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamideIC501000.0 [1]
(4R,7S,10S,13R,16S,19S)-10-(4-Aminobutyl)-N-[(2S)-1-amino-3-naphthalen-2-yl-1-oxopropan-2-yl]-19-[[(2S)-2-amino-3-phenylpropanoyl]amino]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-16-(pyridin-3-ylmethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamideIC50535.0 [1]
(4S,7S,10S,13R,16S,19R)-10-(4-Aminobutyl)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2R)-2-amino-3-naphthalen-2-ylpropanoyl]amino]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamideIC504843.0 [1]
(4R,7S,10S,13R,16S,19S)-19-Acetamido-10-(4-aminobutyl)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamideIC501000.0 [1]
(2S)-6-Amino-N-[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]-2-[[(2R)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]hexanamideIC501000.0 [1]
[(3S,6S,9S,12R,15S,18S,20R)-9-(4-Aminobutyl)-3,15-dibenzyl-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-(5-aminopentyl)carbamateKi10.0 [1]
[(3S,6S,9S,12R,15S,18S,20R)-9-(4-Aminobutyl)-3-benzyl-15-[3-(diaminomethylideneamino)propyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-(2-aminoethyl)carbamateKi6.31 [1]
[(3S,6S,9S,12R,15S,18S,20R)-9-(4-Aminobutyl)-3,15-dibenzyl-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-[2-(dimethylamino)ethyl]carbamateKi1.58 [1]
(3S,6S,9S,12R,15S,18S,20R)-9-(4-Aminobutyl)-3,15-dibenzyl-20-hydroxy-12-(1H-indol-3-ylmethyl)-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosane-2,5,8,11,14,17-hexoneKi63.1 [1]
[(3S,6S,9S,12R,15S,18S,20R)-9-(4-Aminobutyl)-3-benzyl-15-(1H-imidazol-5-ylmethyl)-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-(2-aminoethyl)carbamateKi3.98 [1]
(4R,7S,10S,13S,16S,19S,22S,25R)-13-(4-Aminobutyl)-19-[(4-aminophenyl)methyl]-22-benzyl-25-(carbamoylamino)-10-[(1R)-1-hydroxyethyl]-7-[(4-hydroxyphenyl)methyl]-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 acidIC50757.0 [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-(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 acidIC50117.0 [1]
DotatateIC5010000.0 [1]
(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-[(1R)-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 acidIC50410.0 [1]
(4R,7S,10S,13S,16R,19S,22S,25R)-25-Amino-13-(4-aminobutyl)-19-[(4-aminophenyl)methyl]-7,22-dibenzyl-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 acidIC50450.0 [1]
(4R,7S,10S,13S,16S,19S,22S,25R)-25-Amino-13-(4-aminobutyl)-19-[(4-aminophenyl)methyl]-22-benzyl-10-[(1R)-1-hydroxyethyl]-7-[(4-hydroxyphenyl)methyl]-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 acidIC50327.0 [1]
(4R,7S,10S,13S,16S,19S,22S,25R)-25-Amino-13-(4-aminobutyl)-7,19,22-tribenzyl-10-[(1R)-1-hydroxyethyl]-16-[(1S)-1-(1H-indol-3-yl)ethyl]-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acidIC5021.0 [1]
(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-(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 acidIC5027.0 [1]
(4R,7S,10S,13S,16R,19S,22S,25R)-25-Amino-13-(4-aminobutyl)-19,22-dibenzyl-10-[(1R)-1-hydroxyethyl]-7-[(4-hydroxyphenyl)methyl]-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 acidIC5010.3 [1]
(4R,7S,10S,13S,16R,19S,22S,25R)-13-(4-Aminobutyl)-19-[(4-aminophenyl)methyl]-22-benzyl-25-(carbamoylamino)-10-[(1R)-1-hydroxyethyl]-7-[(4-hydroxyphenyl)methyl]-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 acidIC501000.0 [1]
(4R,7S,10S,13S,16R,19S,22S,25R)-25-Amino-13-(4-aminobutyl)-7,19,22-tribenzyl-10-[(1R)-1-hydroxyethyl]-16-(naphthalen-2-ylmethyl)-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acidIC50607.0 [1]
(4R,7S,10S,13S,16S,19S,22S,25R)-13-(4-Aminobutyl)-25-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-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 acidIC501000.0 [1]
(4R,7S,10S,13S,16S,19S,22S,25R)-13-(4-Aminobutyl)-19-[(4-aminophenyl)methyl]-7,22-dibenzyl-25-(carbamoylamino)-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 acidIC50650.0 [1]
(4R,7S,10S,13S,16R,19S,22S,25R)-13-(4-Aminobutyl)-25-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-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 acidIC50330.0 [1]
(4R,7S,10S,13S,16R,19S,22S,25R)-25-Amino-13-(4-aminobutyl)-7,19,22-tribenzyl-10-[(1R)-1-hydroxyethyl]-16-[(1R)-1-(1H-indol-3-yl)ethyl]-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acidIC5049.0 [1]
(4R,7S,10S,13S,16S,19S,22S,25R)-25-Amino-13-(4-aminobutyl)-19-[(4-aminophenyl)methyl]-7,22-dibenzyl-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 acidIC50213.0 [1]
(4R,7S,10S,13S,16R,19S,22S,25R)-13-(4-Aminobutyl)-19-[(4-aminophenyl)methyl]-7,22-dibenzyl-25-(carbamoylamino)-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 acidIC50840.0 [1]
(4R,7S,10S,13S,16S,19S,22S,25R)-25-Amino-13-(4-aminobutyl)-22-benzyl-10-[(1R)-1-hydroxyethyl]-16-(1H-indol-3-ylmethyl)-7,19-dimethyl-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acidIC5010000.0 [1]
(4R,7S,10S,13S,16S,19S,22S,25R)-25-Amino-13-(4-aminobutyl)-19,22-dibenzyl-10-[(1R)-1-hydroxyethyl]-7-[(4-hydroxyphenyl)methyl]-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 acidIC506.5 [1]
(4R,7S,10S,13S,16R,19S,22S,25R)-13-(4-Aminobutyl)-19,22-dibenzyl-25-(carbamoylamino)-10-[(1R)-1-hydroxyethyl]-7-[(4-hydroxyphenyl)methyl]-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 acidIC5055.0 [1]
(4R,7S,10S,13S,16R,19S,22S,25S)-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 acidIC50545.0 [1]
(2S,5R,8S,11S,14S,19S)-8-(4-Aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-2-benzyl-N-[(2R,3R)-1,3-dihydroxybutan-2-yl]-11-[(1R)-1-hydroxyethyl]-5-(1H-indol-3-ylmethyl)-3,6,9,12,20-pentaoxo-1,4,7,10,13-pentazacycloicosane-14-carboxamideIC501000.0 [1]
N-[(2R,3S)-1-[5-[(Dimethylamino)methyl]-2-(trifluoromethoxy)anilino]-3-(1H-indol-3-yl)-1-oxobutan-2-yl]-4-(4-fluoro-2-methylphenyl)-3-oxopiperazine-1-carboxamideIC505100.0 [1]
3-Amino-N-[(2S,3R,4S,5S,6R)-6-[(4-chlorophenyl)methoxymethyl]-5-hydroxy-2-methylsulfanyl-4-(naphthalen-2-ylmethoxy)oxan-3-yl]propanamideIC509590.0 [1]
4-Amino-N-[(2R,3R,4R,5S,6R)-4-[(4-chlorophenyl)methoxy]-5-hydroxy-6-(methoxymethyl)-2-(naphthalen-2-ylmethoxy)oxan-3-yl]butanamideIC5010000.0 [1]
3-[[4-(4-Aminobutyl)-5-quinolin-2-yl-1,2,4-triazol-3-yl]sulfanyl]-1-(7-methyl-1H-indol-3-yl)propan-1-oneKi530.0 [1]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Somatostatin receptor 1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 22 Feb. 2025, https://www.aatbio.com/data-sets/somatostatin-receptor-1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2025, February 22). Quest Database™ Somatostatin receptor 1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/somatostatin-receptor-1-inhibitors-ic50-ki.
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