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Cholecystokinin A receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
Unii-1fgz6L9SF2Ki24.55 [1], 165.96 [2]
(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-oneKi28.84 [1], 213.8 [2], 912.01 [3]
Tert-butyl N-[(2S)-1-[[(4aS,5R)-2-naphthalen-1-yl-1,3-dioxo-4,4a,5,6,7,8-hexahydropyrido[1,2-c]pyrimidin-5-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]carbamateIC508.9 [1]
Tert-butyl N-[(2S)-1-[[(4aS,5R)-1,3-dioxo-2-phenyl-4,4a,5,6,7,8-hexahydropyrido[1,2-c]pyrimidin-5-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]carbamateIC5035.2 [1]
Tert-butyl N-[(2S)-1-[[(4aS,5R)-2-benzyl-3-oxo-1-sulfanyl-4,4a,5,6,7,8-hexahydro-1H-pyrido[1,2-c]pyrimidin-5-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]carbamateIC5027.5 [1]
SincalideKi0.28 [1]
DevazepideIC500.08 [1], 0.49 [2]
DevazepideKi0.02 [1], 1.82 [2]
2-[2,4-Dioxo-5-phenyl-3-(phenylcarbamoylamino)-1,5-benzodiazepin-1-yl]-N-phenyl-N-propan-2-ylacetamideIC5050.12 [1], 54.95 [2]
2-[2,4-Dioxo-5-phenyl-3-(phenylcarbamoylamino)-1,5-benzodiazepin-1-yl]-N-phenyl-N-propan-2-ylacetamideKi50.12 [1]
NetazepideKi28.84 [1], 30.2 [2], 31.62 [3]
Gski181771XIC50105.0 [1], 128.0 [2], 131.0 [3]
2-(2-(1H-Indole-2-carboxamido)benzamido)-3-phenylpropanoic acidIC50197.0 [1]
2-(2-(1H-Indole-2-carboxamido)benzamido)-3-phenylpropanoic acidKi31.62 [1], 59.8 [2]
3-[[2-[5-Cyclohexyl-1-(3,3-dimethyl-2-oxobutyl)-2-oxo-1,3,4-benzotriazepin-3-yl]acetyl]amino]benzoic acidKi10000.0 [1], 11220.18 [2]
N-[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)ureaIC50158.49 [1]
N-[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)ureaKi173.78 [1]
AsperlicinIC501400.0 [1]
CID 5311148IC5022.91 [1]
Tert-butyl N-[(2S)-1-[[(4aS,5S)-2-benzyl-1,3-dioxo-4,4a,5,6,7,8-hexahydropyrido[1,2-c]pyrimidin-5-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]carbamateIC506850.0 [1], 20860.0 [2]
N-[4-Chloro-2-(piperidin-1-ylcarbonyl)phenyl]-2,1,3-benzothiadiazole-4-sulfonamideKi10000.0 [1]
4-[4-Iodo-2-[(5-quinoxalinylsulfonyl)amino]benzoyl]-morpholineKi10000.0 [1]
1-[2-[(2,1,3-Benzothiadiazol-4-ylsulfonyl)amino]-4-bromobenzoyl]-piperidineKi10000.0 [1]
2-[3-Methyl-2,4-dioxo-1-[2-oxo-2-(N-propan-2-ylanilino)ethyl]-5-phenyl-1,5-benzodiazepin-3-yl]-N-phenylacetamideIC5075.86 [1]
N-(4-Methoxyphenyl)-2-[3-[(1-methylindazol-3-yl)methyl]-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-propan-2-ylacetamideIC5042.66 [1]
2-[3-[(1-Benzylindazol-3-yl)methyl]-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-(4-methoxyphenyl)-N-propan-2-ylacetamideIC50309.03 [1]
2-[3-(1H-Indol-3-ylmethyl)-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-(4-methoxyphenyl)-N-propan-2-ylacetamideIC5010.81 [1], 10.96 [2]
2-[3-(2H-Indazol-3-ylmethyl)-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-phenyl-N-propan-2-ylacetamideIC5087.1 [1]
2-[2,4-Dioxo-1-[2-oxo-2-(N-propan-2-ylanilino)ethyl]-5-phenyl-1,5-benzodiazepin-3-yl]-N-phenylacetamideIC50154.88 [1]
2-[2,4-Dioxo-1-[2-oxo-2-(N-propan-2-ylanilino)ethyl]-5-phenyl-1,5-benzodiazepin-3-yl]-N-phenylacetamideKi158.49 [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-ylacetamideIC5013.18 [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-ylacetamideIC508.32 [1]
1-[2-[(2,1,3-Benzothiadiazol-4-ylsulfonyl)amino]-4-chlorobenzoyl]-piperidineKi10000.0 [1]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2Ki32.0 [1], 320.0 [2]
1-[2-[(2,1,3-Benzooxadiazol-4-ylsulfonyl)amino]-4-chlorobenzoyl]-piperidineKi10000.0 [1]
N-(5-Bromo-2-(piperidine-1-carbonyl)phenyl)isoquinoline-5-sulfonamideKi10000.0 [1]
2-[(2,1,3-Benzothiadiazol-4-ylsulfonyl)amino]-4-chloro-N-(phenylmethyl)-benzamideKi10000.0 [1]
N-(5-Chloro-2-(piperidine-1-carbonyl)phenyl)quinoline-8-sulfonamideKi10000.0 [1]
1-[4-Bromo-2-[(quinolin-5-ylsulfonyl)amino]-benzoyl]-piperidineKi10000.0 [1]
1-[4-Bromo-2-[[naphthalen-1-ylsulfonyl]amino]benzoyl]-piperidineKi10000.0 [1]
3-[4-[1-(3-Ethoxyphenyl)-2-(4-methylphenyl)imidazole-4-carbonyl]piperazin-1-yl]naphthalene-1-carboxylic acidIC500.12 [1]
3-[4-[1-(3-Ethoxyphenyl)-2-(2-fluoro-4-methylphenyl)imidazole-4-carbonyl]piperazin-1-yl]naphthalene-1-carboxylic acidIC500.04 [1], 0.06 [2]
[1-(3-Ethoxyphenyl)-2-(4-methylphenyl)imidazol-4-yl]-(4-quinolin-3-ylpiperazin-1-yl)methanoneIC500.45 [1]
3-[[2,4-Dioxo-1-[2-oxo-2-(N-propan-2-ylanilino)ethyl]-5-phenyl-1,5-benzodiazepin-3-yl]carbamoylamino]benzoic acidIC50125.89 [1]
3-[[2,4-Dioxo-1-[2-oxo-2-(N-propan-2-ylanilino)ethyl]-5-phenyl-1,5-benzodiazepin-3-yl]carbamoylamino]benzoic acidKi125.89 [1]
1-[(3S)-5-Cyclohexyl-2,4-dioxo-1-(2-oxo-2-pyrrolidin-1-ylethyl)-1,5-benzodiazepin-3-yl]-3-(4-fluorophenyl)ureaKi79.43 [1]
PropranololIC505011.87 [1]
PaclitaxelKi2276.0 [1]
LoxiglumideIC50195.0 [1]
CID 108187IC501047.13 [1]
5-(4-Chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamideIC502000.0 [1]
LintitriptIC500.56 [1]
CipargaminIC5030000.0 [1]
CID 121964IC501900.0 [1]
DevazepidaKi10.4 [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 acidKi3200.0 [1]
4-[2-[(2,1,3-Benzothiadiazol-4-ylsulfonyl)amino]benzoyl]-morpholineKi10000.0 [1]
3-{[5-(Adamantan-1-yloxymethyl)-2-cyclohexyl-1H-imidazole-4-carbonyl]-amino}-benzoic acidKi10000.0 [1]
(3S)-3-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-Amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]-3-(1H-indol-3-yl)propanoyl]-methylamino]hexanoyl]amino]-4-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-oxobutanoic acidKi1080.0 [1]
(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 acidIC5019.95 [1]
2-[2,4-Dioxo-5-phenyl-3-(phenylcarbamoylamino)-1,5-benzodiazepin-1-yl]-N-(4-methoxyphenyl)-N-propan-2-ylacetamideIC5079.43 [1]
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2Ki1100.0 [1]
Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2Ki870.0 [1]
3-Phenyl-2-[[2-[[(E)-3-phenylprop-2-enoyl]amino]benzoyl]amino]propanoic acidIC504000.0 [1]
2-(1-(3,4-Difluorophenylsulfonyl)-2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)acetic acidIC508100.0 [1]
2-[5-Cyclohexyl-1-(2-cyclopentyl-2-oxoethyl)-2-oxo-1,3,4-benzotriazepin-3-yl]-N-[3-(5-oxo-4H-1,2,4-oxadiazol-3-yl)phenyl]acetamideKi467.74 [1]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-[[(2S)-2-[3-(4-sulfooxyphenyl)propanoylamino]hexanoyl]amino]acetyl]amino]propanoyl]amino]hexanoyl]amino]-4-oxobutanoic acidIC500.99 [1]
1-[2-[(2,1,3-Benzothiadiazol-5-ylsulfonyl)amino]-4-bromobenzoyl]-piperidineKi10000.0 [1]
2-[[2-(1H-Indole-2-carbonylamino)benzoyl]amino]-4-phenylbutanoic acidKi3.9 [1]
2-[[2-(1H-Indole-2-carbonylamino)benzoyl]amino]propanoic acidIC502800.0 [1]
(2S)-2-[[2-(2,1,3-Benzothiadiazol-4-ylsulfonylamino)-4-chlorobenzoyl]amino]-3-(3,4-dichlorophenyl)propanoic acidKi251.19 [1]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-2-[[(2S)-3-(1H-indol-3-yl)-2-[[2-[[(2S)-2-[3-(4-sulfooxyphenyl)propanoylamino]hexanoyl]amino]acetyl]amino]propanoyl]amino]hexanoyl]-methylamino]-4-oxobutanoic acidIC500.5 [1]
4-[[(2R)-1-[[(2R)-2-(2-Adamantyloxycarbonylamino)-3-(1H-indol-3-yl)-2-methylpropanoyl]amino]-6-[(2-methylphenyl)carbamoylamino]hexan-2-yl]amino]-4-oxobutanoic acidIC5012.02 [1]
4-[[(2R)-1-[[(2S)-2-(2-Adamantyloxycarbonylamino)-3-(1H-indol-3-yl)-2-methylpropanoyl]amino]-6-[(2-methylphenyl)carbamoylamino]hexan-2-yl]amino]-4-oxobutanoic acidIC50229.09 [1]
3-[1-(4-Methoxyphenyl)-5-(4-methylphenyl)pyrazol-3-yl]-2-(4-methylphenyl)propanoic acidKi25.12 [1]
2-(3-Chlorophenyl)-3-[1-(4-methoxyphenyl)-5-(4-methylphenyl)pyrazol-3-yl]propanoic acidKi25.12 [1]
4-[[(2S)-2-[[(2S)-2-(2-Adamantyloxycarbonylamino)-3-(1H-indol-3-yl)-2-methylpropanoyl]amino]-6-[(2-methylphenyl)carbamoylamino]hexyl]amino]-4-oxobutanoic acidIC50724.44 [1]
2-(4-Methoxyphenyl)-3-[1-(4-methoxyphenyl)-5-(4-methylphenyl)pyrazol-3-yl]propanoic acidKi25.12 [1]
2-(3-Methoxyphenyl)-3-[1-(4-methoxyphenyl)-5-(4-methylphenyl)pyrazol-3-yl]propanoic acidKi25.12 [1]
2-[2,4-Dioxo-5-phenyl-3-(phenylcarbamoylamino)-1,5-benzodiazepin-1-yl]-N-(4-hydroxyphenyl)-N-propan-2-ylacetamideIC5039.81 [1]
2-(4-Chlorophenyl)-3-[1-(4-methoxyphenyl)-5-(4-methylphenyl)pyrazol-3-yl]propanoic acidKi25.12 [1]
[[3-(2-Naphthyl)-2-methyl-2-[[(2-adamantyloxy)carbonyl]amino]propionyl]phenethylamino]acetic acidKi3006.0 [1]
N-[2,4-Dioxo-1-[2-oxo-2-(N-propan-2-ylanilino)ethyl]-5-phenyl-1,5-benzodiazepin-3-yl]-1H-indole-2-carboxamideIC5015.85 [1]
2-[3-Methyl-2,4-dioxo-5-phenyl-3-(phenylcarbamoylamino)-1,5-benzodiazepin-1-yl]-N-phenyl-N-propan-2-ylacetamideIC501318.26 [1]
2-[3-(2H-Indazol-3-ylmethyl)-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-(2-methoxyphenyl)-N-propan-2-ylacetamideIC501584.89 [1]
N-(4-Fluorophenyl)-2-[3-(2H-indazol-3-ylmethyl)-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-propan-2-ylacetamideIC50138.04 [1]
2-[3-Ethyl-2,4-dioxo-1-[2-oxo-2-(N-propan-2-ylanilino)ethyl]-5-phenyl-1,5-benzodiazepin-3-yl]-N-phenylacetamideIC5036.31 [1]
2-[3-(1H-Indol-3-ylmethyl)-3-methoxy-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-(4-methoxyphenyl)-N-propan-2-ylacetamideIC5013.8 [1]
2-[3-Benzyl-2,4-dioxo-1-[2-oxo-2-(N-propan-2-ylanilino)ethyl]-5-phenyl-1,5-benzodiazepin-3-yl]-N-phenylacetamideIC50389.05 [1]
2-[3-[(4-Fluoro-2H-indazol-3-yl)methyl]-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-(4-methoxyphenyl)-N-propan-2-ylacetamideIC5017.38 [1]
2-[3-[(7-Fluoro-2H-indazol-3-yl)methyl]-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-(4-methoxyphenyl)-N-propan-2-ylacetamideIC5020.89 [1]
N-Cyclopropyl-2-[3-(2H-indazol-3-ylmethyl)-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-phenylacetamideIC50524.81 [1]
N-Tert-butyl-2-[3-(2H-indazol-3-ylmethyl)-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-phenylacetamideIC50891.25 [1]
2-[3-(2H-Indazol-3-ylmethyl)-3-methoxy-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-(4-methoxyphenyl)-N-propan-2-ylacetamideIC5014.45 [1]
2-[3-[(6-Fluoro-2H-indazol-3-yl)methyl]-2,4-dioxo-5-phenyl-1,5-benzodiazepin-1-yl]-N-(4-methoxyphenyl)-N-propan-2-ylacetamideIC5029.51 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Cholecystokinin A receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.10 May2024https://www.aatbio.com/data-sets/cholecystokinin-a-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 10). Quest Database™ Cholecystokinin A receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/cholecystokinin-a-receptor-inhibitors-ic50-ki.
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