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Cholecystokinin B receptor 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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N-[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)ureaIC504.0 [1]
N-[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)ureaKi1.58 [1], 1.8 [2], 2.95 [3]
SincalideKi0.28 [1], 0.3 [2], 0.64 [3], 0.65 [4]
DevazepideIC50245.0 [1]
DevazepideKi3.69 [1], 29.51 [2], 51.29 [3], 62.0 [4], 87.1 [5]
(4S)-6-[2-[(2R)-2-[(3,5-Dimethylphenyl)methyl]piperidin-1-yl]-2-oxoethyl]-4-(2H-indazol-3-ylmethyl)-1-phenyl-4H-[1,2,4]triazolo[3,4-d][1,5]benzodiazepin-5-oneKi69.18 [1], 213.8 [2], 1412.54 [3]
Unii-1fgz6L9SF2Ki24.55 [1], 70.79 [2], 1000.0 [3]
Boc-trp-met-asp-phe-NH2IC5025.0 [1]
Boc-trp-met-asp-phe-NH2Ki42.0 [1]
(3S)-1-Methyl-3-[3-(3-methylphenyl)ureido]-5-phenyl-1H-1,4-benzodiazepin-2(3H)-oneIC50130.0 [1], 150.0 [2], 151.0 [3], 280.0 [4]
CID 108187IC500.14 [1]
CID 108187Ki0.35 [1], 0.4 [2], 0.98 [3], 1.86 [4]
2-[2,4-Dioxo-5-phenyl-3-(phenylcarbamoylamino)-1,5-benzodiazepin-1-yl]-N-phenyl-N-propan-2-ylacetamideIC5023.99 [1], 25.12 [2]
2-[2,4-Dioxo-5-phenyl-3-(phenylcarbamoylamino)-1,5-benzodiazepin-1-yl]-N-phenyl-N-propan-2-ylacetamideKi25.12 [1]
1-(4-Chlorophenyl)-3-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]ureaIC50410.0 [1], 540.0 [2], 1100.0 [3]
1-(4-Chloro-phenyl)-3-((R)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-ureaIC505.5 [1], 12.0 [2], 19.6 [3]
1-(4-Chlorophenyl)-3-[2-oxo-1-(2-oxo-2-pyrrolidin-1-ylethyl)-5-phenyl-3H-1,4-benzodiazepin-3-yl]ureaIC500.28 [1], 0.5 [2], 1.6 [3]
Ethyl 2-[3-[(4-chlorophenyl)carbamoylamino]-2-oxo-5-phenyl-3H-1,4-benzodiazepin-1-yl]acetateIC501.0 [1], 3.3 [2]
PentagastrinIC506000.0 [1]
PentagastrinKi14.5 [1], 22.0 [2], 52.0 [3]
Cholecystokinin (27-33), tert-butyloxycarbonyl-nle(28,31)-IC500.2 [1], 0.29 [2]
Cholecystokinin (27-33), tert-butyloxycarbonyl-nle(28,31)-Ki0.23 [1]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-6-[(2-methylphenyl)carbamoylamino]hexanoyl]-methylamino]-4-oxobutanoic acidIC504500.0 [1], 4700.0 [2], 10000.0 [3]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-6-[(2-methylphenyl)carbamoylamino]hexanoyl]amino]-4-oxobutanoic acidIC501400.0 [1], 1500.0 [2]
Ethyl 2-[3-[(4-chlorobenzoyl)amino]-5-(2-fluorophenyl)-2-oxo-3H-1,4-benzodiazepin-1-yl]acetateIC50690.0 [1], 1900.0 [2]
1-[1-(1-Adamantylmethyl)-2,4-dioxo-5-phenyl-1,5-benzodiazepin-3-yl]-3-phenylureaKi0.37 [1], 0.71 [2], 2.29 [3], 83.18 [4]
1-[(3R)-5-Cyclohexyl-1-methyl-2-oxo-3H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)ureaIC500.28 [1]
TetragastrinKi10.4 [1], 19.5 [2]
1-(1-Methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl)-3-(3-methylphenyl)ureaIC503.1 [1], 5.2 [2], 7.1 [3]
LorglumideIC501000.0 [1], 1900.0 [2], 25000.0 [3]
NetazepideKi0.08 [1], 0.14 [2]
2-[2-(5-Bromo-1H-indol-3-YL)ethyl]-3-[3-(1-methylethoxy)phenyl]-4-(3H)-quinazolinoneIC5081.0 [1], 160.0 [2]
SpiroglumideIC501223.0 [1], 1400.0 [2]
3-[[2-[5-Cyclohexyl-1-(3,3-dimethyl-2-oxobutyl)-2-oxo-1,3,4-benzotriazepin-3-yl]acetyl]amino]benzoic acidKi1.0 [1], 5.13 [2]
4-Chloro-N-[(3S)-5-(2-fluorophenyl)-1-methyl-2-oxo-3H-1,4-benzodiazepin-3-yl]benzamideIC50800.0 [1], 2500.0 [2], 2900.0 [3]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-6-[(3-methylphenyl)carbamoylamino]hexanoyl]amino]-4-oxobutanoic acidIC501900.0 [1]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-6-[(4-methylphenyl)carbamoylamino]hexanoyl]amino]-4-oxobutanoic acidIC501200.0 [1]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-6-[(2-methoxyphenyl)carbamoylamino]hexanoyl]amino]-4-oxobutanoic acidIC503400.0 [1], 3800.0 [2]
1-[2-[(2,1,3-Benzothiadiazol-4-ylsulfonyl)amino]-4-bromobenzoyl]-piperidineKi25.12 [1]
1-(4-Chlorophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)ureaIC5022.0 [1], 23.0 [2], 81.3 [3]
Ethyl 2-[3-[(4-chlorophenyl)carbamoylamino]-5-(2-fluorophenyl)-2-oxo-3H-1,4-benzodiazepin-1-yl]acetateIC501.2 [1], 4.1 [2]
4-Chloro-N-[(3R)-5-(2-fluorophenyl)-1-methyl-2-oxo-3H-1,4-benzodiazepin-3-yl]benzamideIC505200.0 [1], 7600.0 [2], 11000.0 [3]
1-Methyl-N-(1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl)indole-2-carboxamideIC502000.0 [1], 15000.0 [2]
4-Chloro-N-(1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl)benzamideIC506700.0 [1], 40000.0 [2]
1-(4-Chlorophenyl)-3-[1-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]ureaIC500.8 [1], 2.6 [2], 8.0 [3]
1-[1-[2-(3-Azabicyclo[3.2.2]nonan-3-yl)-2-oxoethyl]-5-(2-fluorophenyl)-9-methyl-2-oxo-3H-1,4-benzodiazepin-3-yl]-3-[3-(2H-tetrazol-5-yl)phenyl]ureaIC500.38 [1], 0.68 [2]
(3S)-3-[[(2S)-2-[[(2R)-3-(1H-Indol-3-yl)-2-[[2-[[(2S)-2-[[(2S)-2-[(2-methylpropan-2-yl)oxycarbonylamino]-3-(4-sulfophenyl)propanoyl]amino]-4-methylsulfanylbutanoyl]amino]acetyl]amino]propanoyl]amino]hexanoyl]amino]-4-oxo-4-(2-phenylethoxy)butanoic acidIC507.0 [1], 210.0 [2], 500.0 [3]
(2R,4R)-1-[(2R)-2-(2-Azatricyclo[3.3.1.13,7]decan-2-yloxycarbonylamino)-3-(1H-indol-3-yl)-2-methylpropanoyl]-4-(2,4-difluorophenoxy)pyrrolidine-2-carboxylic acidKi6.8 [1], 17.6 [2], 324.3 [3]
(2R,4R)-1-[(2R)-2-(2-Azatricyclo[3.3.1.13,7]decan-2-yloxycarbonylamino)-3-(1H-indol-3-yl)-2-methylpropanoyl]-4-(2,4-dichlorophenoxy)pyrrolidine-2-carboxylic acidKi1.9 [1], 30.4 [2], 45.7 [3]
(2R,4R)-1-[(2R)-2-(2-Azatricyclo[3.3.1.13,7]decan-2-yloxycarbonylamino)-3-(1H-indol-3-yl)-2-methylpropanoyl]-4-(4-nitrophenoxy)pyrrolidine-2-carboxylic acidKi0.5 [1], 26.3 [2], 75.5 [3]
2-[2-[2-[2-[2-[[(4R,4As,7S,7aR,12bS)-4a,10-dihydroxy-3-methyl-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]amino]-2-oxoethoxy]acetyl]hydrazinyl]-2-oxoethoxy]-N-[2-[3-[[(3R)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]carbamoylamino]phenoxy]ethyl]acetamideKi3.9 [1], 57.0 [2], 356.0 [3]
N-[2-[[2-[2-[[(4R,4As,7S,7aR,12bS)-4a,10-dihydroxy-3-methyl-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]amino]-2-oxoethoxy]acetyl]amino]ethyl]-2-[2-[2-[3-[[(3R)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]carbamoylamino]phenoxy]ethylamino]-2-oxoethoxy]acetamideKi7.3 [1], 33.0 [2], 71.0 [3]
N-[6-[[2-[2-[[(4R,4As,7S,7aR,12bS)-4a,10-dihydroxy-3-methyl-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]amino]-2-oxoethoxy]acetyl]amino]hexyl]-2-[2-[2-[3-[[(3R)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]carbamoylamino]phenoxy]ethylamino]-2-oxoethoxy]acetamideKi16.3 [1], 77.0 [2], 260.0 [3]
2-[2-[[(4R,4As,7S,7aR,12bS)-4a,10-dihydroxy-3-methyl-1,2,4,5,6,7,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinolin-7-yl]amino]-2-oxoethoxy]-N-[2-[3-[[(3R)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]carbamoylamino]phenoxy]ethyl]acetamideKi14.2 [1], 210.0 [2], 223.0 [3]
(R)-3-Amino-1-methyl-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-oneIC50100000.0 [1]
(R)-3-Amino-1-methyl-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-oneIC50100000.0 [1]
Tert-butyl 2-[3-[(3-methylphenyl)carbamoylamino]-2-oxo-4,5-dihydro-3H-1-benzazepin-1-yl]acetateIC5018.0 [1], 110.0 [2]
ProglumideIC50900000.0 [1], 2500000.0 [2]
beta-Carboline-3-carboxylic acid methyl esterIC50100000.0 [1], 150000.0 [2]
TifluadomIC50100000.0 [1]
TifluadomKi100000.0 [1]
CID 132980IC500.1 [1]
DevazepidaIC50720.0 [1]
DevazepidaKi169.0 [1]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoic acidIC50300.0 [1], 500.0 [2]
Gski181771XIC502.7 [1], 5.6 [2]
(3S)-3-Amino-4-[[(2S)-1-[[(2R)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]-methylamino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-4-oxobutanoic acidIC500.79 [1]
(3S)-3-Amino-4-[[(2S)-1-[[(2R)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]-methylamino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-4-oxobutanoic acidKi2.1 [1]
2-(2-(1H-Indole-2-carboxamido)benzamido)-3-phenylpropanoic acidKi10000.0 [1], 22000.0 [2]
9H-Pyrido[3,4-b]indol-3-amineIC50100000.0 [1]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]-methylamino]hexanoyl]amino]-4-oxobutanoic acidKi0.8 [1]
CID 5311148IC501000.0 [1]
N-[4-Chloro-2-(piperidin-1-ylcarbonyl)phenyl]-2,1,3-benzothiadiazole-4-sulfonamideKi398.11 [1]
4-[4-Iodo-2-[(5-quinoxalinylsulfonyl)amino]benzoyl]-morpholineKi31.62 [1]
N-[(3R)-1-Methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamideIC501400.0 [1], 3700.0 [2]
2-[3-Methyl-2,4-dioxo-1-[2-oxo-2-(N-propan-2-ylanilino)ethyl]-5-phenyl-1,5-benzodiazepin-3-yl]-N-phenylacetamideIC508317.64 [1]
N,N-Diethyl-2-[3-[(3-methylphenyl)carbamoylamino]-2-oxo-5-pyridin-2-yl-3H-1,4-benzodiazepin-1-yl]acetamideIC500.56 [1]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]hexanoyl]amino]-4-oxobutanoic acidIC5065.0 [1]
1-(1-Methyl-2-oxo-5-pyridin-2-yl-3H-1,4-benzodiazepin-3-yl)-3-(3-methylphenyl)ureaIC5066.0 [1]
1-(5-Azepan-1-yl-1-methyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-3-m-tolyl-ureaIC501.25 [1], 1.3 [2]
(3S)-3-[[(2S)-2-[[(2S)-2-Acetamido-3-(1H-indol-3-yl)propanoyl]amino]-6-[(2-methylphenyl)carbamoylamino]hexanoyl]amino]-4-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-4-oxobutanoic acidIC505011.87 [1], 6400.0 [2]
1-(1-Methyl-2-oxo-5-pyrrolidin-1-yl-3H-1,4-benzodiazepin-3-yl)-3-(3-methylphenyl)ureaIC50137.0 [1]
N-(4-Methoxyphenyl)-2-[3-[(1-methylindazol-3-yl)methyl]-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-propan-2-ylacetamideIC502398.83 [1]
2-[3-[(1-Benzylindazol-3-yl)methyl]-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-(4-methoxyphenyl)-N-propan-2-ylacetamideIC50100000.0 [1]
2-[3-(1H-Indol-3-ylmethyl)-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-(4-methoxyphenyl)-N-propan-2-ylacetamideIC505248.07 [1]
2-[2,4-Dioxo-5-phenyl-3-(phenylcarbamoylamino)-1,5-benzodiazepin-1-yl]-N-phenylacetamideIC5031.7 [1], 450.0 [2]
2-[3-(2H-Indazol-3-ylmethyl)-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-phenyl-N-propan-2-ylacetamideIC50177.83 [1]
2-[2,4-Dioxo-1-[2-oxo-2-(N-propan-2-ylanilino)ethyl]-5-phenyl-1,5-benzodiazepin-3-yl]-N-phenylacetamideIC50831.76 [1]
2-[2,4-Dioxo-1-[2-oxo-2-(N-propan-2-ylanilino)ethyl]-5-phenyl-1,5-benzodiazepin-3-yl]-N-phenylacetamideKi794.33 [1]
2-[3-(2H-Indazol-3-ylmethyl)-3-methyl-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-(4-methoxyphenyl)-N-propan-2-ylacetamideIC5069183.1 [1]
2-[3-(1H-Indol-3-ylmethyl)-3-methyl-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-(4-methoxyphenyl)-N-propan-2-ylacetamideIC5017378.01 [1]
Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2Ki1.3 [1], 4.8 [2]
1-[2-[(2,1,3-Benzothiadiazol-4-ylsulfonyl)amino]-4-chlorobenzoyl]-piperidineKi39.81 [1]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2Ki1.3 [1], 1.5 [2]
(4R)-6-(2-Fluorophenyl)-4-(1H-indol-3-ylmethyl)-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepineIC5012000.0 [1]
N-[(3S)-1-Methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-4-(trifluoromethyl)benzamideIC504600.0 [1], 6200.0 [2]
(3R)-1-Methyl-3-[[4-(trifluoromethyl)benzoyl]amino]-5-phenyl-1H-1,4-benzodiazepin-2(3H)-oneIC503300.0 [1], 4200.0 [2]
Items per page: 1 - 10 of 97
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References

This online tool may be cited as follows

MLA

"Quest Database™ Cholecystokinin B receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Dec. 2024, https://www.aatbio.com/data-sets/cholecystokinin-b-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, December 21). Quest Database™ Cholecystokinin B receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/cholecystokinin-b-receptor-inhibitors-ic50-ki.
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