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Cholecystokinin receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
(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 acidIC503.7 [1], 4300.0 [2]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-6-[[(E)-3-(4-hydroxyphenyl)prop-2-enoyl]amino]-2-[[3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]hexanoyl]-methylamino]-4-oxobutanoic acidIC505.0 [1], 5810.0 [2]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-[[(2S)-6-[[(E)-3-(4-hydroxyphenyl)prop-2-enoyl]amino]-2-[[3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]hexanoyl]amino]-4-oxobutanoic acidIC504.2 [1], 710.0 [2]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-2-[[3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-6-[[(E)-3-pyridin-3-ylprop-2-enoyl]amino]hexanoyl]-methylamino]-4-oxobutanoic acidIC5041.0 [1], 10400.0 [2]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-[[(2S)-6-[[(E)-3-(4-hydroxyphenyl)prop-2-enoyl]amino]-2-[[3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]hexanoyl]-methylamino]-4-oxobutanoic acidIC509.0 [1], 13600.0 [2]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-[[(2S)-2-[[3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-6-[[(E)-3-thiophen-2-ylprop-2-enoyl]amino]hexanoyl]-methylamino]-4-oxobutanoic acidIC5032.0 [1], 10900.0 [2]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-2-[[3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-6-[[(E)-3-thiophen-2-ylprop-2-enoyl]amino]hexanoyl]-methylamino]-4-oxobutanoic acidIC5035.0 [1], 4577.0 [2]
(3S)-4-[[(2S)-1-Amino-1-oxo-3-phenylpropan-2-yl]-methylamino]-3-[[(2S)-2-[[3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]amino]-6-[[(E)-3-thiophen-2-ylprop-2-enoyl]amino]hexanoyl]amino]-4-oxobutanoic acidIC5018.0 [1], 731.0 [2]
DiazepamIC50100000.0 [1]
ClonazepamIC50100000.0 [1]
ChlordiazepoxideIC50100000.0 [1]
FlunitrazepamIC50100000.0 [1]
DevazepideIC50270.0 [1]
NaluzotanKi2000.0 [1]
Cholecystokinin (27-33), tert-butyloxycarbonyl-nle(28,31)-IC500.3 [1]
DevazepidaIC50800.0 [1]
1-Methyl-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-oneIC50100000.0 [1]
5-(2-Fluorophenyl)-1,3-dihydro-1-methyl-2H-1,4-benzodiazepin-2-oneIC50100000.0 [1]
1-Methyl-3-(4-bromobenzoyl)amino-5-phenyl-3H-1,4-benzodiazepin-2-oneIC502400.0 [1]
N-(2-Oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl)-1H-indole-2-carboxamideIC508000.0 [1]
N-[(3R)-1-Methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamideIC503700.0 [1]
4-Chloro-N-[(3S)-5-(2-fluorophenyl)-1-methyl-2-oxo-3H-1,4-benzodiazepin-3-yl]benzamideIC502900.0 [1]
Ethyl 2-[3-[(4-chlorobenzoyl)amino]-5-(2-fluorophenyl)-2-oxo-3H-1,4-benzodiazepin-1-yl]acetateIC501900.0 [1]
2-(1H-Indol-3-yl)-N-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-acetamideIC5011000.0 [1]
N-[5-(2-Fluorophenyl)-1-methyl-2-oxo-3H-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamideIC50300.0 [1]
N-[5-(2-Fluoro-phenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-benzamideIC5040000.0 [1]
4-Chloro-N-[(3R)-5-(2-fluorophenyl)-1-methyl-2-oxo-3H-1,4-benzodiazepin-3-yl]benzamideIC5011000.0 [1]
4-Chloro-N-[5-(2-fluoro-phenyl)-1-methyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-benzamideIC503400.0 [1]
N-[5-(2-Fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamideIC503000.0 [1]
N-(2-Oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl)-1H-indole-3-carboxamideIC508400.0 [1]
3-(1H-Indol-3-yl)-N-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-propionamideIC50100000.0 [1]
4-(1H-Indol-3-yl)-N-(2-oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl)butanamideIC50100000.0 [1]
4-Chloro-N-[5-(2-fluoro-phenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-benzamideIC5040000.0 [1]
N-[5-(2-Fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepin-3-yl]quinazoline-2-carboxamideIC5080000.0 [1]
N-[5-(2-Fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepin-3-yl]-1-benzofuran-2-carboxamideIC5032000.0 [1]
N-[5-(2-Fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepin-3-yl]-1H-pyrrole-2-carboxamideIC50100000.0 [1]
N-(2-Oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl)naphthalene-2-carboxamideIC5012000.0 [1]
N-(2-Oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl)naphthalene-1-carboxamideIC5012000.0 [1]
N-[(3S)-5-(2-Fluorophenyl)-1-methyl-2-oxo-3H-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamideIC50300.0 [1]
N-[5-(2-Fluorophenyl)-1-methyl-2-oxo-3H-1,4-benzodiazepin-3-yl]-1-methylindole-2-carboxamideIC501000.0 [1]
5-Fluoro-N-[5-(2-fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamideIC5012000.0 [1]
5-Chloro-N-[5-(2-fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamideIC5038000.0 [1]
1-Methyl-N-(1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl)indole-2-carboxamideIC5015000.0 [1]
5-Bromo-N-[5-(2-fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamideIC5050000.0 [1]
N-[5-(2-Fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepin-3-yl]-5-hydroxy-1H-indole-2-carboxamideIC5016000.0 [1]
N-[5-(2-Fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepin-3-yl]-5-methoxy-1H-indole-2-carboxamideIC5029000.0 [1]
N-[5-(2-Fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepin-3-yl]-1-methylindole-2-carboxamideIC507000.0 [1]
N-[5-(2-Fluoro-phenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-4-nitro-benzamideIC5050000.0 [1]
4-Chloro-N-(1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl)benzamideIC5040000.0 [1]
4-Chloro-N-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-benzamideIC5040000.0 [1]
2-Chloro-N-[5-(2-fluoro-phenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-benzamideIC5040000.0 [1]
N-[5-(2-Fluoro-phenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-4-trifluoromethyl-benzamideIC5040000.0 [1]
N-[5-(2-Fluoro-phenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-4-methyl-benzamideIC5014000.0 [1]
2-Chloro-N-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-benzamideIC50100000.0 [1]
2-Chloro-N-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]benzamideIC5083000.0 [1]
3-Chloro-N-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-benzamideIC5075000.0 [1]
N-[5-(2-Fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepin-3-yl]-4-methoxybenzamideIC5040000.0 [1]
4-Dimethylamino-N-[5-(2-fluoro-phenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-benzamideIC50100000.0 [1]
N-[5-(2-Fluoro-phenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-3,4-dimethoxy-benzamideIC5040000.0 [1]
4-Fluoro-N-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-benzamideIC5043000.0 [1]
N-(2-Oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl)-4-(trifluoromethyl)benzamideIC5065000.0 [1]
N-(2-Oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl)-4-phenylbenzamideIC5018000.0 [1]
4-Tert-Butyl-N-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-benzamideIC50100000.0 [1]
3,5-Dichloro-N-(2-oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl)benzamideIC50100000.0 [1]
4-Hydroxy-N-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-benzamideIC50100000.0 [1]
4-Cyano-N-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-benzamideIC50100000.0 [1]
2-Amino-4-chloro-N-(1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl)benzamideIC502400.0 [1]
4-Bromo-N-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]benzamideIC501600.0 [1]
N-[5-(2-Fluorophenyl)-1-methyl-2-oxo-3H-1,4-benzodiazepin-3-yl]-4-(trifluoromethyl)benzamideIC501800.0 [1]
N-[(3S)-5-(2-Fluorophenyl)-1-methyl-2-oxo-3H-1,4-benzodiazepin-3-yl]-4-(trifluoromethyl)benzamideIC501400.0 [1]
4-Tert-butyl-N-[5-(2-fluorophenyl)-1-methyl-2-oxo-3H-1,4-benzodiazepin-3-yl]benzamideIC502300.0 [1]
4-Tert-butyl-N-[(3S)-5-(2-fluorophenyl)-1-methyl-2-oxo-3H-1,4-benzodiazepin-3-yl]benzamideIC508000.0 [1]
N-[5-(2-Fluorophenyl)-1-methyl-2-oxo-3H-1,4-benzodiazepin-3-yl]-3-iodobenzamideIC501700.0 [1]
N-[(3S)-1-Methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-4-pentylbenzamideIC50100000.0 [1]
N-[(3S)-1-Methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-4-(trifluoromethyl)benzamideIC504600.0 [1]
(3R)-1-Methyl-3-[[4-(trifluoromethyl)benzoyl]amino]-5-phenyl-1H-1,4-benzodiazepin-2(3H)-oneIC503300.0 [1]
Ethyl 2-[3-[(2-chlorobenzoyl)amino]-5-(2-fluorophenyl)-2-oxo-3H-1,4-benzodiazepin-1-yl]acetateIC503200.0 [1]
(2R)-2-Amino-N-[(3R)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-3-phenylpropanamideIC50100000.0 [1]
3,4-Dichloro-N-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-benzamideIC5040000.0 [1]
2-Chloro-N-(2-oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl)benzamideIC5040000.0 [1]
4-Methylsulfanyl-N-(2-oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl)benzamideIC5023000.0 [1]
7-Chloro-3-(1H-indol-3-ylmethyl)-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-oneIC50100000.0 [1]
N-[5-(2-Fluoro-phenyl)-1-methyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-4-pentyl-benzamideIC50100000.0 [1]
1-[4-[4-[2-Tert-butyl-6-(trifluoromethyl)pyrimidin-4-yl]piperazin-1-yl]butyl]-3,4-dihydro-1-benzazepine-2,5-dioneIC5010000.0 [1]
Ethyl 2-[[(3R)-5-(2-fluorophenyl)-3-(1H-indol-3-ylmethyl)-1,3-dihydro-1,4-benzodiazepin-2-ylidene]amino]acetateIC5049000.0 [1]
2-[[(3R)-5-(2-Fluorophenyl)-3-(1H-indol-3-ylmethyl)-1,3-dihydro-1,4-benzodiazepin-2-ylidene]amino]acetic acidIC507000.0 [1]
(3R)-5-(2-Fluorophenyl)-3-(1H-indol-3-ylmethyl)-N-methyl-1,3-dihydro-1,4-benzodiazepin-2-imineIC50100000.0 [1]
2-[(3R)-3-(1H-Indol-3-ylmethyl)-2-methylimino-1,3-dihydro-1,4-benzodiazepin-5-yl]-N-methylanilineIC50100000.0 [1]
(3R)-5-(2-Fluorophenyl)-3-(1H-indol-3-ylmethyl)-N-propyl-1,3-dihydro-1,4-benzodiazepin-2-imineIC50100000.0 [1]
Tert-butyl N-[(2R)-1-[(1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl)amino]-1-oxo-3-phenylpropan-2-yl]carbamateIC5013000.0 [1]
(2R)-2-Amino-N-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-3-phenylpropanamideIC5040000.0 [1]
(3R)-5-(2-Fluorophenyl)-3-(1H-indol-3-ylmethyl)-N-phenyl-3H-1,4-benzodiazepin-2-amineIC50100000.0 [1]
Tert-butyl N-[(2S)-3-(1H-indol-3-yl)-1-oxo-1-[(2-oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl)amino]propan-2-yl]carbamateIC50100000.0 [1]
Tert-butyl N-[(2R)-3-(1H-indol-3-yl)-1-oxo-1-[(2-oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl)amino]propan-2-yl]carbamateIC5020000.0 [1]
2-(1-Benzothiophen-4-yl)-N-[5-(2-fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepin-3-yl]acetamideIC503300.0 [1]
N-[5-(2-Fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepin-3-yl]-2-hydroxy-2-phenylacetamideIC5080000.0 [1]
(E)-N-[5-(2-Fluorophenyl)-2-oxo-1,3-dihydro-1,4-benzodiazepin-3-yl]-3-phenylprop-2-enamideIC505500.0 [1]
N-[5-(2-Fluoro-phenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-acetamideIC5040000.0 [1]
N-(2-Oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl)-2,3-dihydro-1H-indole-2-carboxamideIC5040000.0 [1]
N-[5-(2-Fluorophenyl)-1-methyl-2-oxo-3H-1,4-benzodiazepin-3-yl]thiophene-3-carboxamideIC5026000.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Cholecystokinin receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.9 May2024https://www.aatbio.com/data-sets/cholecystokinin-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 9). Quest Database™ Cholecystokinin receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/cholecystokinin-receptor-inhibitors-ic50-ki.
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