Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type

 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
51353551 18141 None 18 Human Functional pEC50 = 11 11.0 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.1 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.1 nM (Rvb = 7 to 14 pM)
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL1269257 18141 None 18 Human Functional pEC50 = 11 11.0 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.1 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.1 nM (Rvb = 7 to 14 pM)
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
51353551 18141 None 18 Human Functional pEC50 = 10.9 10.9 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.01 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.01 nM (Rvb = 7 to 14 pM)
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL1269257 18141 None 18 Human Functional pEC50 = 10.9 10.9 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.01 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.01 nM (Rvb = 7 to 14 pM)
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
10649606 49630 None 0 Human Functional pEC50 = 10.9 10.9 4 2
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49630 None 0 Human Functional pEC50 = 10.9 10.9 4 2
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
10649606 49630 None 0 Human Functional pEC50 = 10.7 10.7 4 2
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49630 None 0 Human Functional pEC50 = 10.7 10.7 4 2
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
44336539 5146 None 0 Human Functional pEC50 = 10.7 10.7 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5146 None 0 Human Functional pEC50 = 10.7 10.7 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 10 nM (Rvb = 7 to 14 pM)
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
10819755 165537 None 0 Human Functional pEC50 = 10.6 10.6 218776 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL423907 165537 None 0 Human Functional pEC50 = 10.6 10.6 218776 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24769543 188811 None 0 Human Functional pEC50 = 10.5 10.5 2 2
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 649 9 2 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504406 188811 None 0 Human Functional pEC50 = 10.5 10.5 2 2
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 649 9 2 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
44562302 188297 None 0 Human Functional pEC50 = 10.5 10.5 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 666 11 2 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL498958 188297 None 0 Human Functional pEC50 = 10.5 10.5 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 666 11 2 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
24769604 188796 None 0 Mouse Functional pEC50 = 10.5 10.5 -1 2
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 663 9 2 7 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504114 188796 None 0 Mouse Functional pEC50 = 10.5 10.5 -1 2
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 663 9 2 7 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
10649606 49630 None 0 Human Functional pEC50 = 10.4 10.4 4 2
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49630 None 0 Human Functional pEC50 = 10.4 10.4 4 2
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
44562297 188730 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 631 9 2 7 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL502974 188730 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 631 9 2 7 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
4627 822 None 42 Human Functional pEC50 = 10.4 10.4 -1 6
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
864 822 None 42 Human Functional pEC50 = 10.4 10.4 -1 6
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
9833444 822 None 42 Human Functional pEC50 = 10.4 10.4 -1 6
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
CHEMBL1121 822 None 42 Human Functional pEC50 = 10.4 10.4 -1 6
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
DB09142 822 None 42 Human Functional pEC50 = 10.4 10.4 -1 6
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
24861113 188296 None 0 Human Functional pEC50 = 10.3 10.3 24 2
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 564 7 1 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL498942 188296 None 0 Human Functional pEC50 = 10.3 10.3 24 2
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 564 7 1 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL506201 188296 None 0 Human Functional pEC50 = 10.3 10.3 24 2
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 564 7 1 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
44336539 5146 None 0 Human Functional pEC50 = 10.3 10.3 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5146 None 0 Human Functional pEC50 = 10.3 10.3 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 100 nM (Rvb = 7 to 14 pM)
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
24861114 189248 None 4 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 582 7 1 6 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL510690 189248 None 4 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 582 7 1 6 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
44562301 189159 None 0 Human Functional pEC50 = 10.3 10.3 3 2
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL509464 189159 None 0 Human Functional pEC50 = 10.3 10.3 3 2
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24861060 188834 None 0 Human Functional pEC50 = 10.3 10.3 5 3
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL446789 188834 None 0 Human Functional pEC50 = 10.3 10.3 5 3
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504861 188834 None 0 Human Functional pEC50 = 10.3 10.3 5 3
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
24861060 188834 None 0 Human Functional pEC50 = 10.3 10.3 5 3
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL446789 188834 None 0 Human Functional pEC50 = 10.3 10.3 5 3
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL504861 188834 None 0 Human Functional pEC50 = 10.3 10.3 5 3
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
155530671 171665 None 0 Human Functional pEC50 = 10.2 10.2 47863 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1627 65 14 19 4.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4464703 171665 None 0 Human Functional pEC50 = 10.2 10.2 47863 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1627 65 14 19 4.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
46869398 61944 None 0 Human Functional pEC50 = 10.2 10.2 5 3
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 576 6 1 6 6.1 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774043 61944 None 0 Human Functional pEC50 = 10.2 10.2 5 3
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 576 6 1 6 6.1 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
24769605 178824 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL468372 178824 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
53233689 61876 None 0 Human Functional pEC50 = 10.2 10.2 2 3
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 604 5 1 7 5.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773877 61876 None 0 Human Functional pEC50 = 10.2 10.2 2 3
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 604 5 1 7 5.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2011.03.069
155524181 170956 None 0 Human Functional pEC50 = 10.2 10.2 4 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1820 71 18 22 2.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4453982 170956 None 0 Human Functional pEC50 = 10.2 10.2 4 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1820 71 18 22 2.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24769604 188796 None 0 Human Functional pEC50 = 10.2 10.2 1 2
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 663 9 2 7 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504114 188796 None 0 Human Functional pEC50 = 10.2 10.2 1 2
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 663 9 2 7 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
44562304 188983 None 0 Human Functional pEC50 = 10.1 10.1 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 664 9 3 7 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(=O)NC)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL507094 188983 None 0 Human Functional pEC50 = 10.1 10.1 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 664 9 3 7 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(=O)NC)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
24861394 189163 None 0 Human Functional pEC50 = 10.1 10.1 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 592 5 1 7 5.6 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL509519 189163 None 0 Human Functional pEC50 = 10.1 10.1 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 592 5 1 7 5.6 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2008.06.057
44578457 172574 None 0 Human Functional pEC50 = 10.1 10.1 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL448221 172574 None 0 Human Functional pEC50 = 10.1 10.1 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44562300 188744 None 0 Human Functional pEC50 = 10.1 10.1 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL503107 188744 None 0 Human Functional pEC50 = 10.1 10.1 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24769546 172792 None 0 Human Functional pEC50 = 10.1 10.1 2 2
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 618 9 2 8 4.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL450105 172792 None 0 Human Functional pEC50 = 10.1 10.1 2 2
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 618 9 2 8 4.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24861391 188859 None 0 Human Functional pEC50 = 10.0 10.0 2 2
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 578 5 1 7 5.3 O=C(O)c1cc(N2CCN(C(=O)c3cn(-c4ccc5c(c4)OCCO5)c(-c4ccc(F)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2008.06.057
CHEMBL505225 188859 None 0 Human Functional pEC50 = 10.0 10.0 2 2
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 578 5 1 7 5.3 O=C(O)c1cc(N2CCN(C(=O)c3cn(-c4ccc5c(c4)OCCO5)c(-c4ccc(F)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2008.06.057
CHEMBL505969 188859 None 0 Human Functional pEC50 = 10.0 10.0 2 2
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 578 5 1 7 5.3 O=C(O)c1cc(N2CCN(C(=O)c3cn(-c4ccc5c(c4)OCCO5)c(-c4ccc(F)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2008.06.057
16755781 188893 None 9 Human Functional pEC50 = 10.0 10.0 9 3
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL443189 188893 None 9 Human Functional pEC50 = 10.0 10.0 9 3
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL505409 188893 None 9 Human Functional pEC50 = 10.0 10.0 9 3
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL505727 188893 None 9 Human Functional pEC50 = 10.0 10.0 9 3
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
16755781 188893 None 9 Human Functional pEC50 = 10.0 10.0 9 3
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL443189 188893 None 9 Human Functional pEC50 = 10.0 10.0 9 3
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505409 188893 None 9 Human Functional pEC50 = 10.0 10.0 9 3
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505727 188893 None 9 Human Functional pEC50 = 10.0 10.0 9 3
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562298 171554 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 667 10 2 8 5.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL446324 171554 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 667 10 2 8 5.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562312 188752 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL503331 188752 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562306 189037 None 0 Human Functional pEC50 = 10.0 10.0 8 2
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL508004 189037 None 0 Human Functional pEC50 = 10.0 10.0 8 2
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562296 189111 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 648 11 2 8 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL508772 189111 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 648 11 2 8 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562307 172809 None 0 Human Functional pEC50 = 10 10.0 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL450443 172809 None 0 Human Functional pEC50 = 10 10.0 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562303 172891 None 0 Human Functional pEC50 = 10 10.0 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 685 10 2 8 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL451342 172891 None 0 Human Functional pEC50 = 10 10.0 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 685 10 2 8 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL386682 214847 None 0 Guinea pig Functional pEC50 = 10 10.0 60 2
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CN(C)C(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
155535107 172117 None 0 Human Functional pEC50 = 10.0 10.0 323 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1904 73 19 22 4.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4471525 172117 None 0 Human Functional pEC50 = 10.0 10.0 323 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1904 73 19 22 4.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155537344 172421 None 0 Human Functional pEC50 = 10.0 10.0 46773 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4475304 172421 None 0 Human Functional pEC50 = 10.0 10.0 46773 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155532425 171851 None 0 Human Functional pEC50 = 10.0 10.0 3 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01558
CHEMBL4467338 171851 None 0 Human Functional pEC50 = 10.0 10.0 3 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01558
24769546 172792 None 0 Mouse Functional pEC50 = 10.0 10.0 -2 2
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 618 9 2 8 4.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL450105 172792 None 0 Mouse Functional pEC50 = 10.0 10.0 -2 2
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 618 9 2 8 4.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562301 189159 None 0 Mouse Functional pEC50 = 10.0 10.0 -3 2
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL509464 189159 None 0 Mouse Functional pEC50 = 10.0 10.0 -3 2
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155555346 174476 None 0 Human Functional pEC50 = 9.9 9.9 3 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4551834 174476 None 0 Human Functional pEC50 = 9.9 9.9 3 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155557064 174696 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1998 75 18 24 4.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4557012 174696 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1998 75 18 24 4.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44336539 5146 None 0 Human Functional pEC50 = 9.9 9.9 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5146 None 0 Human Functional pEC50 = 9.9 9.9 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1000 nM (Rvb = 7 to 14 pM)
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
44578729 189740 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 531 4 0 7 5.1 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL514953 189740 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 531 4 0 7 5.1 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
53233689 61876 None 0 Mouse Functional pEC50 = 9.9 9.9 -2 3
Agonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 604 5 1 7 5.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773877 61876 None 0 Mouse Functional pEC50 = 9.9 9.9 -2 3
Agonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 604 5 1 7 5.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2011.03.069
46235271 73674 None 2 Human Functional pEC50 = 9.9 9.9 3 3
Agonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73674 None 2 Human Functional pEC50 = 9.9 9.9 3 3
Agonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
155516677 170192 None 0 Human Functional pEC50 = 9.9 9.9 1 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 72 18 23 2.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4443415 170192 None 0 Human Functional pEC50 = 9.9 9.9 1 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 72 18 23 2.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155544674 175040 None 0 Human Functional pEC50 = 9.9 9.9 1 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4565336 175040 None 0 Human Functional pEC50 = 9.9 9.9 1 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44578728 179564 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 535 6 0 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL474067 179564 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 535 6 0 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
44562299 188977 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 646 9 3 7 5.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL507051 188977 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 646 9 3 7 5.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24769543 188811 None 0 Mouse Functional pEC50 = 9.9 9.9 -2 2
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 649 9 2 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504406 188811 None 0 Mouse Functional pEC50 = 9.9 9.9 -2 2
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 649 9 2 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
155536333 172275 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1865 71 17 24 1.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4473468 172275 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1865 71 17 24 1.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24861392 173021 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 574 5 1 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL451644 173021 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 574 5 1 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
44562314 188870 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505432 188870 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155564421 175372 None 0 Human Functional pEC50 = 9.8 9.8 12302 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1770 69 16 21 3.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4572516 175372 None 0 Human Functional pEC50 = 9.8 9.8 12302 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1770 69 16 21 3.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155524770 171041 None 0 Human Functional pEC50 = 9.8 9.8 12882 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1641 66 14 19 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4455361 171041 None 0 Human Functional pEC50 = 9.8 9.8 12882 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1641 66 14 19 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44562309 171685 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 603 8 2 7 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL446502 171685 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 603 8 2 7 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155526914 171305 None 0 Human Functional pEC50 = 9.8 9.8 2 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1837 72 19 24 0.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4459331 171305 None 0 Human Functional pEC50 = 9.8 9.8 2 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1837 72 19 24 0.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155559320 174968 None 0 Human Functional pEC50 = 9.8 9.8 1 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1872 72 18 23 3.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4563364 174968 None 0 Human Functional pEC50 = 9.8 9.8 1 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1872 72 18 23 3.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
155533399 171948 None 0 Human Functional pEC50 = 9.8 9.8 -2 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1838 72 19 24 1.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4468861 171948 None 0 Human Functional pEC50 = 9.8 9.8 -2 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1838 72 19 24 1.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155535249 172106 None 0 Human Functional pEC50 = 9.8 9.8 2754 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1808 68 16 23 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4471373 172106 None 0 Human Functional pEC50 = 9.8 9.8 2754 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1808 68 16 23 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155535579 172153 None 0 Human Functional pEC50 = 9.8 9.8 158 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4471871 172153 None 0 Human Functional pEC50 = 9.8 9.8 158 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44562310 172756 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL449681 172756 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155552556 174172 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1792 67 16 22 1.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4544208 174172 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1792 67 16 22 1.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
51353551 18141 None 18 Human Functional pEC50 = 9.7 9.7 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1 nM (Rvb = 7 to 14 pM)
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL1269257 18141 None 18 Human Functional pEC50 = 9.7 9.7 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1 nM (Rvb = 7 to 14 pM)Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1 nM (Rvb = 7 to 14 pM)
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
155542488 173237 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1820 69 16 22 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4520976 173237 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1820 69 16 22 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
54583298 61943 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 558 6 1 6 5.9 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774042 61943 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 558 6 1 6 5.9 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
44562308 172759 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL449725 172759 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155514270 169973 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL4440419 169973 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
155514432 169968 None 0 Human Functional pEC50 = 9.7 9.7 1096 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 2121 86 19 27 2.3 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4440303 169968 None 0 Human Functional pEC50 = 9.7 9.7 1096 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 2121 86 19 27 2.3 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155551968 174121 None 0 Human Functional pEC50 = 9.7 9.7 9772 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1793 69 16 20 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4542927 174121 None 0 Human Functional pEC50 = 9.7 9.7 9772 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1793 69 16 20 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
54583296 61934 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 533 5 0 6 5.8 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774033 61934 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 533 5 0 6 5.8 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
155540739 172610 None 0 Human Functional pEC50 = 9.6 9.6 3388 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1907 74 17 24 2.5 CCCC[C@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4483457 172610 None 0 Human Functional pEC50 = 9.6 9.6 3388 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1907 74 17 24 2.5 CCCC[C@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44578686 179479 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473865 179479 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
44562305 188727 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL502924 188727 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155514270 169973 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4440419 169973 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44578764 180918 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 535 4 0 7 5.0 O=C(c1cn(-c2ccc3c(c2)OCCO3)c(-c2ccc(F)cc2)n1)N1CCN(c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2008.06.057
CHEMBL475679 180918 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 535 4 0 7 5.0 O=C(c1cn(-c2ccc3c(c2)OCCO3)c(-c2ccc(F)cc2)n1)N1CCN(c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2008.06.057
46235271 73674 None 2 Human Functional pEC50 = 9.5 9.5 3 3
Agonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73674 None 2 Human Functional pEC50 = 9.5 9.5 3 3
Agonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
155539345 172936 None 0 Human Functional pEC50 = 9.5 9.5 3235 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1850 72 16 23 3.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4514283 172936 None 0 Human Functional pEC50 = 9.5 9.5 3235 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1850 72 16 23 3.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155543163 173390 None 0 Human Functional pEC50 = 9.5 9.5 8709 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1886 72 16 25 2.5 CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4525615 173390 None 0 Human Functional pEC50 = 9.5 9.5 8709 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1886 72 16 25 2.5 CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24861060 188834 None 0 Mouse Functional pEC50 = 9.5 9.5 -5 3
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL446789 188834 None 0 Mouse Functional pEC50 = 9.5 9.5 -5 3
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504861 188834 None 0 Mouse Functional pEC50 = 9.5 9.5 -5 3
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
155517239 170260 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 2582 122 16 39 4.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4444353 170260 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 2582 122 16 39 4.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155547906 173780 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)C[C@H](NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4534977 173780 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)C[C@H](NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155546692 173746 None 0 Human Functional pEC50 = 9.5 9.5 -3 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1861 72 19 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4534236 173746 None 0 Human Functional pEC50 = 9.5 9.5 -3 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1861 72 19 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
46235271 73674 None 2 Human Functional pEC50 = 9.5 9.5 3 3
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73674 None 2 Human Functional pEC50 = 9.5 9.5 3 3
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
155515427 170052 None 0 Human Functional pEC50 = 9.4 9.4 1819 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4441596 170052 None 0 Human Functional pEC50 = 9.4 9.4 1819 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
155566319 175844 None 0 Human Functional pEC50 = 9.4 9.4 4677 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1850 71 16 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4583158 175844 None 0 Human Functional pEC50 = 9.4 9.4 4677 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1850 71 16 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155543995 173427 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1876 73 16 22 4.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4526455 173427 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1876 73 16 22 4.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155548381 173836 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1720 69 15 20 3.8 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)[C@@H](C)CC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4536393 173836 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1720 69 15 20 3.8 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)[C@@H](C)CC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24861174 174711 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL455742 174711 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
155562281 175945 None 0 Human Functional pEC50 = 9.4 9.4 4168 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4585323 175945 None 0 Human Functional pEC50 = 9.4 9.4 4168 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
155555065 174438 None 0 Human Functional pEC50 = 9.4 9.4 4168 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4550876 174438 None 0 Human Functional pEC50 = 9.4 9.4 4168 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44562313 172561 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL448118 172561 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
46235271 73674 None 2 Human Functional pEC50 = 9.3 9.3 3 3
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73674 None 2 Human Functional pEC50 = 9.3 9.3 3 3
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
44562306 189037 None 0 Mouse Functional pEC50 = 9.3 9.3 -8 2
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL508004 189037 None 0 Mouse Functional pEC50 = 9.3 9.3 -8 2
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155517761 170326 None 0 Human Functional pEC50 = 9.3 9.3 416 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4445529 170326 None 0 Human Functional pEC50 = 9.3 9.3 416 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
155560670 175196 None 0 Human Functional pEC50 = 9.3 9.3 72 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4568746 175196 None 0 Human Functional pEC50 = 9.3 9.3 72 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
155568312 176182 None 0 Human Functional pEC50 = 9.3 9.3 36 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 72 17 23 3.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4591101 176182 None 0 Human Functional pEC50 = 9.3 9.3 36 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 72 17 23 3.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
52949124 876 None 4 Human Functional pEC50 = 9.3 9.3 2 3
Agonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 876 None 4 Human Functional pEC50 = 9.3 9.3 2 3
Agonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 876 None 4 Human Functional pEC50 = 9.3 9.3 2 3
Agonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 876 None 4 Human Functional pEC50 = 9.3 9.3 2 3
Agonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R N2.61T mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
44578727 189859 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL515887 189859 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
46869398 61944 None 0 Mouse Functional pEC50 = 9.2 9.2 -5 3
Agonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 576 6 1 6 6.1 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774043 61944 None 0 Mouse Functional pEC50 = 9.2 9.2 -5 3
Agonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at mouse CCK1 receptor expressed in CHO Flip cells assessed as increase in radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 576 6 1 6 6.1 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
54580295 61933 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774032 61933 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)cc1 10.1016/j.bmcl.2011.03.069
155532759 171858 None 0 Human Functional pEC50 = 9.1 9.1 27542 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1431 50 12 15 5.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4467402 171858 None 0 Human Functional pEC50 = 9.1 9.1 27542 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1431 50 12 15 5.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44578767 173620 None 0 Human Functional pEC50 = 9.1 9.1 3 2
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL453083 173620 None 0 Human Functional pEC50 = 9.1 9.1 3 2
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL503822 173620 None 0 Human Functional pEC50 = 9.1 9.1 3 2
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44578767 173620 None 0 Human Functional pEC50 = 9.1 9.1 3 2
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL453083 173620 None 0 Human Functional pEC50 = 9.1 9.1 3 2
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL503822 173620 None 0 Human Functional pEC50 = 9.1 9.1 3 2
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
54586148 61888 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 543 4 0 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773891 61888 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 543 4 0 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2011.03.069
44562311 188825 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504707 188825 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human CCK1 receptorAgonist activity at human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
51353551 18141 None 18 Human Functional pEC50 = 9.1 9.1 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responsesActivity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responses
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL1269257 18141 None 18 Human Functional pEC50 = 9.1 9.1 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responsesActivity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responses
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
168277247 190818 None 0 Human Functional pEC50 = 9.1 9.1 -12 2
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5585 206 67 76 -9.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL5182331 190818 None 0 Human Functional pEC50 = 9.1 9.1 -12 2
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5585 206 67 76 -9.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
168281017 191023 None 0 Human Functional pEC50 = 9.0 9.0 -10 2
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 4869 167 62 67 -13.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL5185239 191023 None 0 Human Functional pEC50 = 9.0 9.0 -10 2
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 4869 167 62 67 -13.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
155543846 173315 None 0 Human Functional pEC50 = 9.0 9.0 -14 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1838 72 19 24 2.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4522865 173315 None 0 Human Functional pEC50 = 9.0 9.0 -14 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1838 72 19 24 2.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24785705 182392 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL478398 182392 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
168280134 190850 None 0 Human Functional pEC50 = 9.0 9.0 -3 2
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5585 206 67 76 -9.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL5182775 190850 None 0 Human Functional pEC50 = 9.0 9.0 -3 2
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5585 206 67 76 -9.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
16755782 179457 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473663 179457 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
44578424 183032 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL479256 183032 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
155540394 173039 None 0 Human Functional pEC50 = 9.0 9.0 58 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1820 69 17 23 2.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4516794 173039 None 0 Human Functional pEC50 = 9.0 9.0 58 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1820 69 17 23 2.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
168273900 190807 None 0 Human Functional pEC50 = 8.9 8.9 -7 2
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 4701 158 61 64 -14.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL5182173 190807 None 0 Human Functional pEC50 = 8.9 8.9 -7 2
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 4701 158 61 64 -14.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
168277239 190817 None 0 Human Functional pEC50 = 8.9 8.9 -2 2
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5417 197 66 73 -11.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL5182323 190817 None 0 Human Functional pEC50 = 8.9 8.9 -2 2
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5417 197 66 73 -11.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL409529 215227 None 2 Guinea pig Functional pEC50 = 8.9 8.9 11 2
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
168276807 190745 None 0 Human Functional pEC50 = 8.9 8.9 -9 2
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5417 197 66 73 -11.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
CHEMBL5181266 190745 None 0 Human Functional pEC50 = 8.9 8.9 -9 2
Agonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assayAgonist activity at human CCK1R expressed in HEK293 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by AlphaScreen assay
ChEMBL 5417 197 66 73 -11.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.ejmech.2022.114214
54587150 61884 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773887 61884 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
16755781 188893 None 9 Mouse Functional pEC50 = 8.9 8.9 -12 3
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL443189 188893 None 9 Mouse Functional pEC50 = 8.9 8.9 -12 3
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505409 188893 None 9 Mouse Functional pEC50 = 8.9 8.9 -12 3
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505727 188893 None 9 Mouse Functional pEC50 = 8.9 8.9 -12 3
Agonist activity at mouse CCK1 receptorAgonist activity at mouse CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
52949124 876 None 4 Human Functional pEC50 = 8.9 8.9 2 3
Agonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 876 None 4 Human Functional pEC50 = 8.9 8.9 2 3
Agonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 876 None 4 Human Functional pEC50 = 8.9 8.9 2 3
Agonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 876 None 4 Human Functional pEC50 = 8.9 8.9 2 3
Agonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R T3.28V, T3.29S mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL414592 215605 None 0 Guinea pig Functional pEC50 = 8.9 8.9 8 2
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)N(C)C(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
52949124 876 None 4 Human Functional pEC50 = 8.8 8.8 2 3
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 876 None 4 Human Functional pEC50 = 8.8 8.8 2 3
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 876 None 4 Human Functional pEC50 = 8.8 8.8 2 3
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 876 None 4 Human Functional pEC50 = 8.8 8.8 2 3
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
10700916 174540 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4553223 174540 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155550911 174032 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1884 70 16 23 3.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4540877 174032 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1884 70 16 23 3.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
54583260 61893 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773896 61893 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2011.03.069
52949124 876 None 4 Human Functional pEC50 = 8.7 8.7 2 3
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 876 None 4 Human Functional pEC50 = 8.7 8.7 2 3
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 876 None 4 Human Functional pEC50 = 8.7 8.7 2 3
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 876 None 4 Human Functional pEC50 = 8.7 8.7 2 3
Agonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at wild-type human CCK1R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
24785703 179458 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 534 6 0 5 6.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473664 179458 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 534 6 0 5 6.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
54586175 61938 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 504 5 0 6 5.8 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ccoc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774037 61938 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 504 5 0 6 5.8 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ccoc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
44578611 189767 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2cccc(F)c2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL515160 189767 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2cccc(F)c2)c1 10.1016/j.bmcl.2008.06.057
44578456 189705 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5cnccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL514716 189705 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5cnccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
155531277 171734 None 0 Human Functional pEC50 = 7.9 7.9 2 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1821 72 18 23 2.1 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4465747 171734 None 0 Human Functional pEC50 = 7.9 7.9 2 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1821 72 18 23 2.1 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155553502 174279 None 0 Human Functional pEC50 = 7.9 7.9 -26 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 72 19 22 3.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OP(=O)(O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4547294 174279 None 0 Human Functional pEC50 = 7.9 7.9 -26 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1822 72 19 22 3.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OP(=O)(O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155564367 175260 None 0 Human Functional pEC50 = 6.9 6.9 -457 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 72 18 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4570130 175260 None 0 Human Functional pEC50 = 6.9 6.9 -457 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1836 72 18 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
70691750 73672 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 621 7 1 6 6.1 O=C1[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017833 73672 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 621 7 1 6 6.1 O=C1[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccc1 10.1016/j.bmcl.2012.02.049
52949124 876 None 4 Human Functional pEC50 = 6.9 6.9 2 3
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
9055 876 None 4 Human Functional pEC50 = 6.9 6.9 2 3
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
CHEMBL1269258 876 None 4 Human Functional pEC50 = 6.9 6.9 2 3
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
DB12694 876 None 4 Human Functional pEC50 = 6.9 6.9 2 3
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
10507109 109283 None 0 Guinea pig Functional pEC50 = 5.9 5.9 -51 4
Agonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladderAgonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladder
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
CHEMBL321761 109283 None 0 Guinea pig Functional pEC50 = 5.9 5.9 -51 4
Agonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladderAgonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladder
ChEMBL 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
70683295 73622 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 606 7 1 5 6.2 O=C(CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21)N1CCC(Cc2ccccc2)C1 10.1016/j.bmcl.2012.02.049
CHEMBL2017692 73622 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 606 7 1 5 6.2 O=C(CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21)N1CCC(Cc2ccccc2)C1 10.1016/j.bmcl.2012.02.049
44578531 172665 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 570 6 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OCC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL448597 172665 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 570 6 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OCC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
11571172 140671 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Intrinsic agonistic activity at CCK receptor in SD rat at 1 uM expressed in pancreatic acinar cell lineIntrinsic agonistic activity at CCK receptor in SD rat at 1 uM expressed in pancreatic acinar cell line
ChEMBL 695 10 2 6 6.6 COc1ccc(N(C(=O)CN2C(=O)[C@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm049072h
CHEMBL381347 140671 None 0 Rat Functional pEC50 = 6.8 6.8 - 1
Intrinsic agonistic activity at CCK receptor in SD rat at 1 uM expressed in pancreatic acinar cell lineIntrinsic agonistic activity at CCK receptor in SD rat at 1 uM expressed in pancreatic acinar cell line
ChEMBL 695 10 2 6 6.6 COc1ccc(N(C(=O)CN2C(=O)[C@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm049072h
52944224 18142 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 586 8 2 7 5.6 CC(C)N(C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
CHEMBL1269259 18142 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 586 8 2 7 5.6 CC(C)N(C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
70685411 73663 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 606 6 1 5 6.8 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017824 73663 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 606 6 1 5 6.8 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
54580296 61936 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774035 61936 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
24785432 181667 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 7 0 5 6.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(CC)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476725 181667 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 7 0 5 6.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(CC)cc2)c1 10.1016/j.bmcl.2008.06.057
52945789 18291 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 541 7 0 5 6.0 CC(C)N(C(=O)CN1C(=O)C(Cc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
CHEMBL1270487 18291 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 541 7 0 5 6.0 CC(C)N(C(=O)CN1C(=O)C(Cc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
54586149 61891 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2cccc(C)c2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773894 61891 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2cccc(C)c2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL217236 211831 None 0 Guinea pig Functional pEC50 = 8.7 8.7 4 2
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
46235272 73671 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 589 8 1 7 4.9 COCCC1CCCCN1C(=O)CN1C(=O)[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL2017832 73671 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 589 8 1 7 4.9 COCCC1CCCCN1C(=O)CN1C(=O)[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
24785178 181645 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476530 181645 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
24785177 189890 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1ccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL516113 189890 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1ccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL266839 213163 None 0 Guinea pig Functional pEC50 = 7.7 7.7 7 2
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
54580266 61885 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 529 6 0 6 6.0 CCOc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773888 61885 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 529 6 0 6 6.0 CCOc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
70689619 73664 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 592 6 1 5 6.5 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017825 73664 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 592 6 1 5 6.5 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
155557285 174622 None 0 Human Functional pEC50 = 6.6 6.6 -295 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1779 74 19 22 1.6 CCCC[C@H](NC(=O)[C@H](CNC(=O)CCCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4555341 174622 None 0 Human Functional pEC50 = 6.6 6.6 -295 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1779 74 19 22 1.6 CCCC[C@H](NC(=O)[C@H](CNC(=O)CCCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155553269 174231 None 0 Human Functional pEC50 = 6.6 6.6 53 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1818 68 15 22 3.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N1CCC[C@@H]1C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4545970 174231 None 0 Human Functional pEC50 = 6.6 6.6 53 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1818 68 15 22 3.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N1CCC[C@@H]1C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44578305 181276 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 5 0 5 6.1 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc(Cl)c(Cl)c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476095 181276 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 5 0 5 6.1 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc(Cl)c(Cl)c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
46235271 73674 None 2 Human Functional pEC50 = 7.6 7.6 3 3
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
CHEMBL2017835 73674 None 2 Human Functional pEC50 = 7.6 7.6 3 3
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
CHEMBL208479 211658 None 0 Human Functional pEC50 = 5.6 5.6 -30 5
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
CHEMBL208479 211658 None 0 Human Functional pEC50 = 5.6 5.6 -30 5
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
46234969 73667 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 626 7 1 5 7.4 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1CC1CCCCC1 10.1016/j.bmcl.2012.02.049
CHEMBL2017828 73667 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 626 7 1 5 7.4 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1CC1CCCCC1 10.1016/j.bmcl.2012.02.049
54587151 61886 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 545 6 0 7 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1OC 10.1016/j.bmcl.2011.03.069
CHEMBL1773889 61886 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 545 6 0 7 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1OC 10.1016/j.bmcl.2011.03.069
101823779 1396 None 27 Human Functional pEC50 = 6.6 6.6 -354 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
16162108 1396 None 27 Human Functional pEC50 = 6.6 6.6 -354 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
8408 1396 None 27 Human Functional pEC50 = 6.6 6.6 -354 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
CHEMBL4451154 1396 None 27 Human Functional pEC50 = 6.6 6.6 -354 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
54586174 61935 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 514 5 0 5 6.2 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774034 61935 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 514 5 0 5 6.2 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL375360 214678 None 3 Human Functional pEC50 = 7.6 7.6 -1 2
Activity at human CCK1 receptor expressed in HEK293 cells assessed as level of [3H]inositol produced relative to controlActivity at human CCK1 receptor expressed in HEK293 cells assessed as level of [3H]inositol produced relative to control
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm061268p
4627 822 None 42 Human Functional pEC50 = 7.6 7.6 -1 6
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
864 822 None 42 Human Functional pEC50 = 7.6 7.6 -1 6
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
9833444 822 None 42 Human Functional pEC50 = 7.6 7.6 -1 6
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
CHEMBL1121 822 None 42 Human Functional pEC50 = 7.6 7.6 -1 6
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
DB09142 822 None 42 Human Functional pEC50 = 7.6 7.6 -1 6
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
4627 822 None 42 Human Functional pEC50 = 7.6 7.6 -1 6
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
864 822 None 42 Human Functional pEC50 = 7.6 7.6 -1 6
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
9833444 822 None 42 Human Functional pEC50 = 7.6 7.6 -1 6
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
CHEMBL1121 822 None 42 Human Functional pEC50 = 7.6 7.6 -1 6
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
DB09142 822 None 42 Human Functional pEC50 = 7.6 7.6 -1 6
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None None 10.1021/jm050921q
51353551 18141 None 18 Human Functional pEC50 = 6.6 6.6 1 3
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
CHEMBL1269257 18141 None 18 Human Functional pEC50 = 6.6 6.6 1 3
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
54580265 61881 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccccc1-c1cnc(C(=O)N2CCN(c3cnc4ccccc4c3)CC2)nc1-c1ccc(C)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773884 61881 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccccc1-c1cnc(C(=O)N2CCN(c3cnc4ccccc4c3)CC2)nc1-c1ccc(C)cc1 10.1016/j.bmcl.2011.03.069
52942901 18144 None 0 Rat Functional pEC50 = 6.5 6.5 1 2
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269261 18144 None 0 Rat Functional pEC50 = 6.5 6.5 1 2
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL382051 214753 None 0 Human Functional pEC50 = 6.5 6.5 -331 5
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
CHEMBL217609 211838 None 0 Guinea pig Functional pEC50 = 8.5 8.5 6 2
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
46235271 73674 None 2 Human Functional pEC50 = 8.5 8.5 3 3
Agonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73674 None 2 Human Functional pEC50 = 8.5 8.5 3 3
Agonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
155542545 173222 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1770 70 16 21 3.9 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4520699 173222 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1770 70 16 21 3.9 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL382051 214753 None 0 Human Functional pEC50 = 6.5 6.5 -331 5
Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assayAntagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
44578772 182902 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 486 5 0 5 5.5 COc1cccc(-c2cc(C(=O)N3CCN(c4cccc(Cl)c4)CC3)nn2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL479063 182902 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 486 5 0 5 5.5 COc1cccc(-c2cc(C(=O)N3CCN(c4cccc(Cl)c4)CC3)nn2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
70681224 73668 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 621 7 1 6 6.1 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccn1 10.1016/j.bmcl.2012.02.049
CHEMBL2017829 73668 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 621 7 1 6 6.1 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccn1 10.1016/j.bmcl.2012.02.049
52949124 876 None 4 Human Functional pEC50 = 6.5 6.5 2 3
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
9055 876 None 4 Human Functional pEC50 = 6.5 6.5 2 3
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
CHEMBL1269258 876 None 4 Human Functional pEC50 = 6.5 6.5 2 3
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
DB12694 876 None 4 Human Functional pEC50 = 6.5 6.5 2 3
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
44578530 188793 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 556 5 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL504024 188793 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 556 5 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
54581261 61883 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 529 6 0 6 6.0 CCOc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773886 61883 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 529 6 0 6 6.0 CCOc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
54582288 61890 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2C)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773893 61890 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2C)cc1 10.1016/j.bmcl.2011.03.069
54580263 61877 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2cccc(F)c2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773878 61877 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2cccc(F)c2)cc1 10.1016/j.bmcl.2011.03.069
70695934 73670 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 595 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL2017831 73670 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 595 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)[C@@H](Cc2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
9960432 39435 None 7 Guinea pig Functional pEC50 = 7.4 7.4 -3 3
Agonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladderAgonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladder
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
CHEMBL147186 39435 None 7 Guinea pig Functional pEC50 = 7.4 7.4 -3 3
Agonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladderAgonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladder
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
10698109 107352 None 0 Guinea pig Functional pEC50 = 6.4 6.4 -2 3
Agonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladderAgonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladder
ChEMBL 560 8 1 4 5.8 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
CHEMBL317181 107352 None 0 Guinea pig Functional pEC50 = 6.4 6.4 -2 3
Agonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladderAgonist activity at CCK1 receptor assessed as stimulation of contraction in guinea pig gallbladder
ChEMBL 560 8 1 4 5.8 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmc.2007.12.047
44578647 179434 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2c(F)cccc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473457 179434 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2c(F)cccc2F)c1 10.1016/j.bmcl.2008.06.057
70695922 73621 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 558 6 1 5 5.9 CCC1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL2017691 73621 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 558 6 1 5 5.9 CCC1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
54581301 61939 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 503 5 1 5 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5cc[nH]c5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774038 61939 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 503 5 1 5 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5cc[nH]c5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
52949124 876 None 4 Human Functional pEC50 = 7.4 7.4 2 3
Agonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 876 None 4 Human Functional pEC50 = 7.4 7.4 2 3
Agonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 876 None 4 Human Functional pEC50 = 7.4 7.4 2 3
Agonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 876 None 4 Human Functional pEC50 = 7.4 7.4 2 3
Agonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
54586147 61882 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773885 61882 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
70693814 73669 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 621 7 1 6 6.1 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccncc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017830 73669 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 621 7 1 6 6.1 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccncc1 10.1016/j.bmcl.2012.02.049
52946666 18143 None 0 Rat Functional pEC50 = 6.4 6.4 2 2
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 600 9 2 7 5.6 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269260 18143 None 0 Rat Functional pEC50 = 6.4 6.4 2 2
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 600 9 2 7 5.6 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
44578422 181668 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5n4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476739 181668 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5n4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
52949124 876 None 4 Rat Functional pEC50 = 6.4 6.4 -2 3
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
9055 876 None 4 Rat Functional pEC50 = 6.4 6.4 -2 3
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
CHEMBL1269258 876 None 4 Rat Functional pEC50 = 6.4 6.4 -2 3
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
DB12694 876 None 4 Rat Functional pEC50 = 6.4 6.4 -2 3
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
44578562 181640 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc3c2OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL476519 181640 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc3c2OCCO3)cc1 10.1016/j.bmcl.2008.06.057
52940616 18146 None 0 Rat Functional pEC50 = 6.3 6.3 1 2
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 581 7 1 6 5.7 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(c2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269263 18146 None 0 Rat Functional pEC50 = 6.3 6.3 1 2
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 581 7 1 6 5.7 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(c2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
46234820 73665 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 572 6 1 5 6.1 CC(C)C1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL2017826 73665 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 572 6 1 5 6.1 CC(C)C1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
46235271 73674 None 2 Human Functional pEC50 = 8.3 8.3 3 3
Agonist activity at human CCK1R W6.48A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R W6.48A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73674 None 2 Human Functional pEC50 = 8.3 8.3 3 3
Agonist activity at human CCK1R W6.48A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R W6.48A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
24785180 181646 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 536 6 0 5 6.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476531 181646 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 536 6 0 5 6.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2008.06.057
54582313 61940 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 572 6 0 7 6.0 COC(=O)c1cc2ccccc2cc1N1CCN(C(=O)c2ncc(-c3ccc(OC)cc3)c(-c3ccc(C)cc3)n2)CC1 10.1016/j.bmcl.2011.03.069
CHEMBL1774039 61940 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 572 6 0 7 6.0 COC(=O)c1cc2ccccc2cc1N1CCN(C(=O)c2ncc(-c3ccc(OC)cc3)c(-c3ccc(C)cc3)n2)CC1 10.1016/j.bmcl.2011.03.069
70689603 73620 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 588 8 1 6 5.5 COCCC1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
CHEMBL2017690 73620 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 588 8 1 6 5.5 COCCC1CCCCN1C(=O)CN1C(=O)C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2012.02.049
52940616 18146 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 581 7 1 6 5.7 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(c2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269263 18146 None 0 Human Functional pEC50 = 6.3 6.3 -1 2
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 581 7 1 6 5.7 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(c2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
24785430 182390 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 6 0 5 6.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OC(C)C)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL478397 182390 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 6 0 5 6.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OC(C)C)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL269185 213239 None 0 Guinea pig Functional pEC50 = 7.3 7.3 5 2
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)NCC(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
44578398 181890 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1cccc(-n2cc(C(=O)N3CCN(c4cccc5ccccc45)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL477784 181890 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1cccc(-n2cc(C(=O)N3CCN(c4cccc5ccccc45)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
70695933 73662 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 607 7 1 6 5.7 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCC1Cc1ccccn1 10.1016/j.bmcl.2012.02.049
CHEMBL2017823 73662 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 607 7 1 6 5.7 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCC1Cc1ccccn1 10.1016/j.bmcl.2012.02.049
54583297 61941 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 558 6 1 6 5.9 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774040 61941 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 558 6 1 6 5.9 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
54582287 61889 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 501 5 0 6 5.3 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773892 61889 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 501 5 0 6 5.3 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2)cc1 10.1016/j.bmcl.2011.03.069
24785431 189919 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL516355 189919 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
24784941 189827 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 516 6 0 5 6.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL515616 189827 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 516 6 0 5 6.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL2370248 212273 None 0 Guinea pig Functional pEC50 = 7.2 7.2 -1 2
In vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptorIn vitro smooth muscle contraction activity in guinea pig gall bladder cholecystokinin type A receptor
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00093a013
155540415 173042 None 0 Human Functional pEC50 = 6.2 6.2 -1584 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1862 71 17 23 3.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4516868 173042 None 0 Human Functional pEC50 = 6.2 6.2 -1584 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1862 71 17 23 3.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
54580267 61892 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 535 5 0 6 6.0 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2Cl)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773895 61892 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 535 5 0 6 6.0 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2Cl)cc1 10.1016/j.bmcl.2011.03.069
52943046 18145 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 557 8 0 6 5.8 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Oc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269262 18145 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 557 8 0 6 5.8 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Oc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
51353551 18141 None 18 Rat Functional pEC50 = 7.2 7.2 -18 3
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
CHEMBL1269257 18141 None 18 Rat Functional pEC50 = 7.2 7.2 -18 3
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
52946666 18143 None 0 Human Functional pEC50 = 6.2 6.2 -2 2
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 600 9 2 7 5.6 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269260 18143 None 0 Human Functional pEC50 = 6.2 6.2 -2 2
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 600 9 2 7 5.6 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
24785176 181669 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 500 5 0 4 6.5 CCc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476747 181669 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 500 5 0 4 6.5 CCc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
70683305 73673 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 635 7 1 6 6.4 Cc1cccc(CC2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
CHEMBL2017834 73673 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 635 7 1 6 6.4 Cc1cccc(CC2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
46235271 73674 None 2 Human Functional pEC50 = 7.2 7.2 3 3
Agonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73674 None 2 Human Functional pEC50 = 7.2 7.2 3 3
Agonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
24785179 181642 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 6 0 5 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccccc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476520 181642 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 6 0 5 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccccc2)c1 10.1016/j.bmcl.2008.06.057
54584255 61937 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ncccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774036 61937 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ncccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
44578251 182538 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 486 5 0 5 5.5 COc1cccc(-n2cc(C(=O)N3CCN(c4cccc(Cl)c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL478604 182538 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 486 5 0 5 5.5 COc1cccc(-n2cc(C(=O)N3CCN(c4cccc(Cl)c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44578423 189768 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL515161 189768 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
155533520 171931 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 910 26 8 9 2.5 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4468598 171931 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 910 26 8 9 2.5 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24784942 181449 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 488 4 1 5 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(O)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL476297 181449 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 488 4 1 5 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(O)c2)cc1 10.1016/j.bmcl.2008.06.057
46234970 73666 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 620 7 1 5 6.7 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017827 73666 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assayAgonist activity at human CCK1 receptor assessed as increase in CCK8-induced calcium release incubated in dark for 30 mins followed by light incubation for 30 mins measured by FLIPR assay
ChEMBL 620 7 1 5 6.7 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccc1 10.1016/j.bmcl.2012.02.049
136000594 61887 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 517 4 2 7 5.0 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc(O)c(O)c2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773890 61887 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 517 4 2 7 5.0 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc(O)c(O)c2)cc1 10.1016/j.bmcl.2011.03.069
44578399 182060 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 492 5 1 6 4.7 COc1cccc(-n2cc(C(=O)N3CCN(c4nc5ccccc5[nH]4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL477996 182060 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 492 5 1 6 4.7 COc1cccc(-n2cc(C(=O)N3CCN(c4nc5ccccc5[nH]4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
10509945 89418 None 0 Human Functional pEC50 = 8.0 8.0 63 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL2369816 89418 None 0 Human Functional pEC50 = 8.0 8.0 63 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44578455 182561 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ncccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL478630 182561 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ncccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
24784940 182893 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL479046 182893 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
54581302 61942 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 572 6 0 7 6.0 COC(=O)c1cc(N2CCN(C(=O)c3ncc(-c4ccc(OC)cc4)c(-c4ccc(C)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2011.03.069
CHEMBL1774041 61942 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysisAgonist activity at human CCK1 receptor expressed in CHO Flip cells assessed as increase of radio labeled inositol phosphate accumulation by Wallac microbeta analysis
ChEMBL 572 6 0 7 6.0 COC(=O)c1cc(N2CCN(C(=O)c3ncc(-c4ccc(OC)cc4)c(-c4ccc(C)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2011.03.069
44336539 5146 None 0 Human Functional pEC50 = 7.1 7.1 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responsesActivity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responses
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5146 None 0 Human Functional pEC50 = 7.1 7.1 1 3
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responsesActivity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responses
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
52942901 18144 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269261 18144 None 0 Human Functional pEC50 = 7.0 7.0 -1 2
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assayAgonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
155517868 170314 None 0 Human Functional pEC50 = 6.0 6.0 -457 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1893 76 19 24 3.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4445353 170314 None 0 Human Functional pEC50 = 6.0 6.0 -457 2
Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assayAgonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay
ChEMBL 1893 76 19 24 3.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44578529 182880 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 7 0 5 6.8 CCCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL479030 182880 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity against human CCK1 receptorAgonist activity against human CCK1 receptor
ChEMBL 530 7 0 5 6.8 CCCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
443375 210065 None 33 Human Functional pIC50 = 10.1 10.1 2 9
Antagonistic activity against cholecystokinin type A receptorAntagonistic activity against cholecystokinin type A receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00067a001
CHEMBL9506 210065 None 33 Human Functional pIC50 = 10.1 10.1 2 9
Antagonistic activity against cholecystokinin type A receptorAntagonistic activity against cholecystokinin type A receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00067a001
44398261 124453 None 0 Human Functional pIC50 = 7.9 7.9 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 124453 None 0 Human Functional pIC50 = 7.9 7.9 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67553 None 0 Human Functional pIC50 = 6.0 6.0 -100 2
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67553 None 0 Human Functional pIC50 = 6.0 6.0 -100 2
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 124453 None 0 Human Functional pIC50 = 6.9 6.9 -91 2
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 124453 None 0 Human Functional pIC50 = 6.9 6.9 -91 2
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
3035433 99522 None 8 Human Functional pIC50 = 5.9 5.9 - 1
Antagonistic activity against cholecystokinin type A receptorAntagonistic activity against cholecystokinin type A receptor
ChEMBL 535 4 3 7 3.1 CC(C)C[C@@H]1N[C@H]2N(C1=O)c1ccccc1[C@@]2(O)C[C@@H]1NC(=O)c2ccccc2-n2c1nc1ccccc1c2=O 10.1021/jm00067a001
CHEMBL283117 99522 None 8 Human Functional pIC50 = 5.9 5.9 - 1
Antagonistic activity against cholecystokinin type A receptorAntagonistic activity against cholecystokinin type A receptor
ChEMBL 535 4 3 7 3.1 CC(C)C[C@@H]1N[C@H]2N(C1=O)c1ccccc1[C@@]2(O)C[C@@H]1NC(=O)c2ccccc2-n2c1nc1ccccc1c2=O 10.1021/jm00067a001
44398261 124453 None 0 Human Functional pIC50 = 6.7 6.7 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 124453 None 0 Human Functional pIC50 = 6.7 6.7 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 124453 None 0 Human Functional pIC50 = 5.7 5.7 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 124453 None 0 Human Functional pIC50 = 5.7 5.7 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10507071 113674 None 0 Human Functional pIC50 = 4.7 4.7 -524 4
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL332261 113674 None 0 Human Functional pIC50 = 4.7 4.7 -524 4
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127683 None 0 Human Functional pIC50 = 6.6 6.6 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127683 None 0 Human Functional pIC50 = 6.6 6.6 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67553 None 0 Human Functional pIC50 = 5.6 5.6 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67553 None 0 Human Functional pIC50 = 5.6 5.6 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67553 None 0 Human Functional pIC50 = 7.6 7.6 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67553 None 0 Human Functional pIC50 = 7.6 7.6 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67553 None 0 Human Functional pIC50 = 7.6 7.6 -100 2
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67553 None 0 Human Functional pIC50 = 7.6 7.6 -100 2
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127683 None 0 Human Functional pIC50 = 7.6 7.6 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127683 None 0 Human Functional pIC50 = 7.6 7.6 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127683 None 0 Human Functional pIC50 = 7.6 7.6 -7 2
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127683 None 0 Human Functional pIC50 = 7.6 7.6 -7 2
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 124453 None 0 Human Functional pIC50 = 7.6 7.6 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 124453 None 0 Human Functional pIC50 = 7.6 7.6 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL375360 214678 None 3 Human Functional pIC50 = 7.6 7.6 -1 2
Activity at human CCK1 receptor expressed in HEK293 cells assessed as level of [3H]inositol produced relative to controlActivity at human CCK1 receptor expressed in HEK293 cells assessed as level of [3H]inositol produced relative to control
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm061268p
44398261 124453 None 0 Human Functional pIC50 = 7.6 7.6 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 124453 None 0 Human Functional pIC50 = 7.6 7.6 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
52949124 876 None 4 Human Functional pIC50 = 8.5 8.5 2 3
Agonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 876 None 4 Human Functional pIC50 = 8.5 8.5 2 3
Agonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 876 None 4 Human Functional pIC50 = 8.5 8.5 2 3
Agonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 876 None 4 Human Functional pIC50 = 8.5 8.5 2 3
Agonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysisAgonist activity at human CCK1R V3.36A mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
10008654 127683 None 0 Human Functional pIC50 = 8.4 8.4 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127683 None 0 Human Functional pIC50 = 8.4 8.4 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 124453 None 0 Human Functional pIC50 = 7.5 7.5 -91 2
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 124453 None 0 Human Functional pIC50 = 7.5 7.5 -91 2
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (F107A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67553 None 0 Human Functional pIC50 = 7.5 7.5 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67553 None 0 Human Functional pIC50 = 7.5 7.5 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67553 None 0 Human Functional pIC50 = 7.5 7.5 -100 2
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67553 None 0 Human Functional pIC50 = 7.5 7.5 -100 2
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67553 None 0 Human Functional pIC50 = 7.5 7.5 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67553 None 0 Human Functional pIC50 = 7.5 7.5 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67553 None 0 Human Functional pIC50 = 7.4 7.4 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67553 None 0 Human Functional pIC50 = 7.4 7.4 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67553 None 0 Human Functional pIC50 = 5.3 5.3 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67553 None 0 Human Functional pIC50 = 5.3 5.3 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127683 None 0 Human Functional pIC50 = 8.3 8.3 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127683 None 0 Human Functional pIC50 = 8.3 8.3 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 124453 None 0 Human Functional pIC50 = 8.2 8.2 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 124453 None 0 Human Functional pIC50 = 8.2 8.2 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S348A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 124453 None 0 Human Functional pIC50 = 8.2 8.2 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 124453 None 0 Human Functional pIC50 = 8.2 8.2 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (M195L)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67553 None 0 Human Functional pIC50 = 6.3 6.3 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67553 None 0 Human Functional pIC50 = 6.3 6.3 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127683 None 0 Human Functional pIC50 = 6.2 6.2 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127683 None 0 Human Functional pIC50 = 6.2 6.2 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R336M)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 124453 None 0 Human Functional pIC50 = 8.1 8.1 -91 2
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 124453 None 0 Human Functional pIC50 = 8.1 8.1 -91 2
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127683 None 0 Human Functional pIC50 = 8.1 8.1 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127683 None 0 Human Functional pIC50 = 8.1 8.1 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (S342A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
11027990 67553 None 0 Human Functional pIC50 = 7.1 7.1 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL189634 67553 None 0 Human Functional pIC50 = 7.1 7.1 -100 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (T117A)
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127683 None 0 Human Functional pIC50 = 8.1 8.1 -7 2
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127683 None 0 Human Functional pIC50 = 8.1 8.1 -7 2
Inhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1RInhibition of CCK-Induced inositol phosphate production in Cos-7 cells expressing human CCK1R
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127683 None 0 Human Functional pIC50 = 8.1 8.1 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127683 None 0 Human Functional pIC50 = 8.1 8.1 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (R197M)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127683 None 0 Human Functional pIC50 = 6.1 6.1 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127683 None 0 Human Functional pIC50 = 6.1 6.1 -7 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329F)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
44398261 124453 None 0 Human Functional pIC50 = 6.1 6.1 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 124453 None 0 Human Functional pIC50 = 6.1 6.1 -91 2
Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)Inhibition of CCK-Induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I352A)
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127683 None 0 Human Functional pIC50 = 8.0 8.0 -7 2
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127683 None 0 Human Functional pIC50 = 8.0 8.0 -7 2
Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)Inhibition of CCK-induced inositol phosphate in Cos-7 cells expressing mutant CCK1R (I329A)
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
44306887 102116 None 0 Guinea pig Functional pKd = 7.4 7.4 - 2
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1cccc(NC(=O)Nc2ccccc2C)c1)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL302027 102116 None 0 Guinea pig Functional pKd = 7.4 7.4 - 2
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1cccc(NC(=O)Nc2ccccc2C)c1)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
44306360 157967 None 0 Guinea pig Functional pKd = 7.4 7.4 - 2
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1ccc(NC(=O)Nc2ccccc2C)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL408395 157967 None 0 Guinea pig Functional pKd = 7.4 7.4 - 2
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1ccc(NC(=O)Nc2ccccc2C)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
44458112 98761 None 0 Guinea pig Functional pKd = 8.2 8.2 - 1
Compound was tested for competitive blocking of guinea pig ileal smooth muscle strip contraction to cholecystokinin-8 (CCK-8) receptorCompound was tested for competitive blocking of guinea pig ileal smooth muscle strip contraction to cholecystokinin-8 (CCK-8) receptor
ChEMBL 374 4 2 3 2.7 O=C(N[C@@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
CHEMBL277661 98761 None 0 Guinea pig Functional pKd = 8.2 8.2 - 1
Compound was tested for competitive blocking of guinea pig ileal smooth muscle strip contraction to cholecystokinin-8 (CCK-8) receptorCompound was tested for competitive blocking of guinea pig ileal smooth muscle strip contraction to cholecystokinin-8 (CCK-8) receptor
ChEMBL 374 4 2 3 2.7 O=C(N[C@@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
44306888 102385 None 0 Guinea pig Functional pKd = 7.2 7.2 - 2
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1cccc(NC(=O)Nc2ccccc2C)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL303635 102385 None 0 Guinea pig Functional pKd = 7.2 7.2 - 2
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1cccc(NC(=O)Nc2ccccc2C)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
44306868 102138 None 0 Guinea pig Functional pKd = 7.1 7.1 - 2
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 836 18 9 7 3.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1ccc(NC(=O)Nc2ccccc2Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL302150 102138 None 0 Guinea pig Functional pKd = 7.1 7.1 - 2
Antagonist activity against CCK-8 induced responses in guinea pig gall bladder was determinedAntagonist activity against CCK-8 induced responses in guinea pig gall bladder was determined
ChEMBL 836 18 9 7 3.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1ccc(NC(=O)Nc2ccccc2Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
2360 3297 None 0 Rat Functional pIC50 = 8.4 8.4 - 1
NoneNone
Drug Central 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 None
5042 3297 None 0 Rat Functional pIC50 = 8.4 8.4 - 1
NoneNone
Drug Central 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 None
871 3297 None 0 Rat Functional pIC50 = 8.4 8.4 - 1
NoneNone
Drug Central 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 None
CHEMBL1697771 3297 None 0 Rat Functional pIC50 = 8.4 8.4 - 1
NoneNone
Drug Central 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 None
DB11656 3297 None 0 Rat Functional pIC50 = 8.4 8.4 - 1
NoneNone
Drug Central 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 None
1614 2349 None 53 Rat Functional pIC50 = 8.2 8.2 -1 2
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
60182 2349 None 53 Rat Functional pIC50 = 8.2 8.2 -1 2
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
892 2349 None 53 Rat Functional pIC50 = 8.2 8.2 -1 2
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
CHEMBL206025 2349 None 53 Rat Functional pIC50 = 8.2 8.2 -1 2
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
65937 1403 None 0 Human Functional pIC50 = 8.2 8.2 - 1
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
834 1403 None 0 Human Functional pIC50 = 8.2 8.2 - 1
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
889 1403 None 0 Human Functional pIC50 = 8.2 8.2 - 1
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
CHEMBL550781 1403 None 0 Human Functional pIC50 = 8.2 8.2 - 1
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
DB04856 1403 None 0 Human Functional pIC50 = 8.2 8.2 - 1
NoneNone
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
4329839 819 None 0 Rat Functional pIC50 = 5.3 5.3 -158 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
861 819 None 0 Rat Functional pIC50 = 5.3 5.3 -158 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
16168172 1771 None 0 Rat Functional pIC50 = 6.1 6.1 -158 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
3559 1771 None 0 Rat Functional pIC50 = 6.1 6.1 -158 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
444007 3043 None 0 Rat Functional pIC50 = 6.2 6.2 -794 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
870 3043 None 0 Rat Functional pIC50 = 6.2 6.2 -794 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
DB00183 3043 None 0 Rat Functional pIC50 = 6.2 6.2 -794 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
3960 2345 None 18 Rat Functional pIC50 = 7.5 7.5 53 4
UnclassifiedUnclassified
Guide to Pharmacology 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 1975695
3960 2345 None 18 Rat Functional pIC50 = 7.5 7.5 53 4
UnclassifiedUnclassified
Guide to Pharmacology 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 2437574
891 2345 None 18 Rat Functional pIC50 = 7.5 7.5 53 4
UnclassifiedUnclassified
Guide to Pharmacology 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 1975695
891 2345 None 18 Rat Functional pIC50 = 7.5 7.5 53 4
UnclassifiedUnclassified
Guide to Pharmacology 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 2437574
CHEMBL24938 2345 None 18 Rat Functional pIC50 = 7.5 7.5 53 4
UnclassifiedUnclassified
Guide to Pharmacology 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 1975695
CHEMBL24938 2345 None 18 Rat Functional pIC50 = 7.5 7.5 53 4
UnclassifiedUnclassified
Guide to Pharmacology 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 2437574
52949124 876 None 4 Human Functional pIC50 = 7.5 7.5 2 3
UnclassifiedUnclassified
Guide to Pharmacology 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 20851601
9055 876 None 4 Human Functional pIC50 = 7.5 7.5 2 3
UnclassifiedUnclassified
Guide to Pharmacology 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 20851601
CHEMBL1269258 876 None 4 Human Functional pIC50 = 7.5 7.5 2 3
UnclassifiedUnclassified
Guide to Pharmacology 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 20851601
DB12694 876 None 4 Human Functional pIC50 = 7.5 7.5 2 3
UnclassifiedUnclassified
Guide to Pharmacology 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 20851601
5311148 1896 None 8 Human Functional pIC50 = 7.6 7.6 41 2
UnclassifiedUnclassified
Guide to Pharmacology 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 9276016
865 1896 None 8 Human Functional pIC50 = 7.6 7.6 41 2
UnclassifiedUnclassified
Guide to Pharmacology 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 9276016
CHEMBL293226 1896 None 8 Human Functional pIC50 = 7.6 7.6 41 2
UnclassifiedUnclassified
Guide to Pharmacology 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 9276016
3888 2122 None 0 Human Functional pIC50 = 8.3 8.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7654246
5311196 2122 None 0 Human Functional pIC50 = 8.3 8.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7654246
122077 2322 None 40 Human Functional pIC50 = 8.3 8.3 -8 2
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10988332
890 2322 None 40 Human Functional pIC50 = 8.3 8.3 -8 2
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10988332
CHEMBL249973 2322 None 40 Human Functional pIC50 = 8.3 8.3 -8 2
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10988332
DB04867 2322 None 40 Human Functional pIC50 = 8.3 8.3 -8 2
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10988332
121964 207 None 26 Rat Functional pIC50 = 8.4 8.4 4265 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1636779
858 207 None 26 Rat Functional pIC50 = 8.4 8.4 4265 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1636779
CHEMBL323521 207 None 26 Rat Functional pIC50 = 8.4 8.4 4265 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1636779
904 3026 None 12 Rat Functional pIC50 = 8.6 8.6 3 3
UnclassifiedUnclassified
Guide to Pharmacology 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 8605955
9915756 3026 None 12 Rat Functional pIC50 = 8.6 8.6 3 3
UnclassifiedUnclassified
Guide to Pharmacology 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 8605955
CHEMBL2111204 3026 None 12 Rat Functional pIC50 = 8.6 8.6 3 3
UnclassifiedUnclassified
Guide to Pharmacology 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 8605955
CHEMBL356898 3026 None 12 Rat Functional pIC50 = 8.6 8.6 3 3
UnclassifiedUnclassified
Guide to Pharmacology 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 8605955
862 821 None 0 Mouse Functional pIC50 = 9.2 9.2 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12370550
127948 3719 None 0 Rat Functional pIC50 = 9.6 9.6 79432 2
UnclassifiedUnclassified
Guide to Pharmacology 502 7 2 4 4.5 COc1ccc2c(c1)N(c1ccccc1F)C(=O)[C@@]2(CCC(=O)O)NC(=O)C1CCc2c(C1)cccc2 8813597
884 3719 None 0 Rat Functional pIC50 = 9.6 9.6 79432 2
UnclassifiedUnclassified
Guide to Pharmacology 502 7 2 4 4.5 COc1ccc2c(c1)N(c1ccccc1F)C(=O)[C@@]2(CCC(=O)O)NC(=O)C1CCc2c(C1)cccc2 8813597
3476 1400 None 2 Rat Functional pIC50 = 9.7 9.7 870 2
UnclassifiedUnclassified
Guide to Pharmacology 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
59751 1400 None 2 Rat Functional pIC50 = 9.7 9.7 870 2
UnclassifiedUnclassified
Guide to Pharmacology 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
878 1400 None 2 Rat Functional pIC50 = 9.7 9.7 870 2
UnclassifiedUnclassified
Guide to Pharmacology 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
CHEMBL39263 1400 None 2 Rat Functional pIC50 = 9.7 9.7 870 2
UnclassifiedUnclassified
Guide to Pharmacology 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
4627 822 None 42 Rat Functional pIC50 = 9.9 9.9 -2 6
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
864 822 None 42 Rat Functional pIC50 = 9.9 9.9 -2 6
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
9833444 822 None 42 Rat Functional pIC50 = 9.9 9.9 -2 6
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
CHEMBL1121 822 None 42 Rat Functional pIC50 = 9.9 9.9 -2 6
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
DB09142 822 None 42 Rat Functional pIC50 = 9.9 9.9 -2 6
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
2281 3175 None 47 Rat Functional pIC50 None 2.2 2.2 -2454 2
UnclassifiedUnclassified
Guide to Pharmacology 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 3440035
4922 3175 None 47 Rat Functional pIC50 None 2.2 2.2 -2454 2
UnclassifiedUnclassified
Guide to Pharmacology 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 3440035
893 3175 None 47 Rat Functional pIC50 None 2.2 2.2 -2454 2
UnclassifiedUnclassified
Guide to Pharmacology 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 3440035
CHEMBL316561 3175 None 47 Rat Functional pIC50 None 2.2 2.2 -2454 2
UnclassifiedUnclassified
Guide to Pharmacology 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 3440035
DB13431 3175 None 47 Rat Functional pIC50 None 2.2 2.2 -2454 2
UnclassifiedUnclassified
Guide to Pharmacology 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 3440035
2360 3297 None 0 Rat Functional pIC50 None 4.4 4.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 15556137
5042 3297 None 0 Rat Functional pIC50 None 4.4 4.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 15556137
871 3297 None 0 Rat Functional pIC50 None 4.4 4.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 15556137
CHEMBL1697771 3297 None 0 Rat Functional pIC50 None 4.4 4.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 15556137
DB11656 3297 None 0 Rat Functional pIC50 None 4.4 4.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 15556137
108187 926 None 30 Rat Functional pIC50 None 5.6 5.6 -794 5
UnclassifiedUnclassified
Guide to Pharmacology 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 1975695
873 926 None 30 Rat Functional pIC50 None 5.6 5.6 -794 5
UnclassifiedUnclassified
Guide to Pharmacology 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 1975695
CHEMBL2062154 926 None 30 Rat Functional pIC50 None 5.6 5.6 -794 5
UnclassifiedUnclassified
Guide to Pharmacology 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 1975695
CHEMBL287735 926 None 30 Rat Functional pIC50 None 5.6 5.6 -794 5
UnclassifiedUnclassified
Guide to Pharmacology 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 1975695
122119 3023 None 0 Rat Functional pIC50 None 5.9 5.9 -1000 2
UnclassifiedUnclassified
Guide to Pharmacology 618 12 5 6 5.1 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](CC1CNc2c1cccc2)(NC(=O)OC1C[C@H]2C([C@]1(C)CC2)(C)C)C)CCC(=O)O 1975695
882 3023 None 0 Rat Functional pIC50 None 5.9 5.9 -1000 2
UnclassifiedUnclassified
Guide to Pharmacology 618 12 5 6 5.1 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](CC1CNc2c1cccc2)(NC(=O)OC1C[C@H]2C([C@]1(C)CC2)(C)C)C)CCC(=O)O 1975695
880 2239 None 6 Rat Functional pIC50 None 6.4 6.4 -7413 2
UnclassifiedUnclassified
Guide to Pharmacology 487 5 3 7 3.5 O=C(N[C@@H]1N=C(C2CCCCC2)c2c(N(C1=O)C)cccc2)Nc1cccc(c1)N(c1n[nH]nn1)C 8632408
9935175 2239 None 6 Rat Functional pIC50 None 6.4 6.4 -7413 2
UnclassifiedUnclassified
Guide to Pharmacology 487 5 3 7 3.5 O=C(N[C@@H]1N=C(C2CCCCC2)c2c(N(C1=O)C)cccc2)Nc1cccc(c1)N(c1n[nH]nn1)C 8632408
CHEMBL2093059 2239 None 6 Rat Functional pIC50 None 6.4 6.4 -7413 2
UnclassifiedUnclassified
Guide to Pharmacology 487 5 3 7 3.5 O=C(N[C@@H]1N=C(C2CCCCC2)c2c(N(C1=O)C)cccc2)Nc1cccc(c1)N(c1n[nH]nn1)C 8632408
1614 2349 None 53 Rat Functional pIC50 None 6.5 6.5 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 3663268
60182 2349 None 53 Rat Functional pIC50 None 6.5 6.5 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 3663268
892 2349 None 53 Rat Functional pIC50 None 6.5 6.5 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 3663268
CHEMBL206025 2349 None 53 Rat Functional pIC50 None 6.5 6.5 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 3663268
104929 2219 None 5 Rat Functional pIC50 None 6.6 6.6 -12 3
UnclassifiedUnclassified
Guide to Pharmacology 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
3477 2219 None 5 Rat Functional pIC50 None 6.6 6.6 -12 3
UnclassifiedUnclassified
Guide to Pharmacology 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
879 2219 None 5 Rat Functional pIC50 None 6.6 6.6 -12 3
UnclassifiedUnclassified
Guide to Pharmacology 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
CHEMBL289498 2219 None 5 Rat Functional pIC50 None 6.6 6.6 -12 3
UnclassifiedUnclassified
Guide to Pharmacology 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 1975695
10742947 3999 None 0 Rat Functional pIC50 None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 469 8 6 4 3.7 OC(=O)CC(c1ccccc1)NC(=O)c1cccc(c1)NC(=O)c1cc2c([nH]1)ccc(c2)C(=N)N 12538004
886 3999 None 0 Rat Functional pIC50 None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 469 8 6 4 3.7 OC(=O)CC(c1ccccc1)NC(=O)c1cccc(c1)NC(=O)c1cc2c([nH]1)ccc(c2)C(=N)N 12538004
CHEMBL137814 3999 None 0 Rat Functional pIC50 None 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 469 8 6 4 3.7 OC(=O)CC(c1ccccc1)NC(=O)c1cccc(c1)NC(=O)c1cc2c([nH]1)ccc(c2)C(=N)N 12538004
887 4110 None 30 Rat Functional pIC50 None 6.9 6.9 -2511 3
UnclassifiedUnclassified
Guide to Pharmacology 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 9022799
9870520 4110 None 30 Rat Functional pIC50 None 6.9 6.9 -2511 3
UnclassifiedUnclassified
Guide to Pharmacology 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 9022799
9870520.0 4110 None 30 Rat Functional pIC50 None 6.9 6.9 -2511 3
UnclassifiedUnclassified
Guide to Pharmacology 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 9022799
CHEMBL324547 4110 None 30 Rat Functional pIC50 None 6.9 6.9 -2511 3
UnclassifiedUnclassified
Guide to Pharmacology 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 9022799
DB12355 4110 None 30 Rat Functional pIC50 None 6.9 6.9 -2511 3
UnclassifiedUnclassified
Guide to Pharmacology 498 6 3 6 4.1 CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2 9022799
4627 822 None 42 Rat Functional pIC50 None 7.2 7.2 -2 6
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
864 822 None 42 Rat Functional pIC50 None 7.2 7.2 -2 6
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
9833444 822 None 42 Rat Functional pIC50 None 7.2 7.2 -2 6
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
CHEMBL1121 822 None 42 Rat Functional pIC50 None 7.2 7.2 -2 6
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
DB09142 822 None 42 Rat Functional pIC50 None 7.2 7.2 -2 6
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
10348659 1804 None 0 Human Functional pIC50 None 7.2 7.2 3 2
UnclassifiedUnclassified
Guide to Pharmacology 604 8 2 5 5.4 O=C(NC1C(=O)N(c2ccccc2)c2c(N(C1=O)CC(=O)N(c1ccc(cc1)N(C)C)C(C)C)cccc2)Nc1ccccc1 8558528
866 1804 None 0 Human Functional pIC50 None 7.2 7.2 3 2
UnclassifiedUnclassified
Guide to Pharmacology 604 8 2 5 5.4 O=C(NC1C(=O)N(c2ccccc2)c2c(N(C1=O)CC(=O)N(c1ccc(cc1)N(C)C)C(C)C)cccc2)Nc1ccccc1 8558528
CHEMBL1184355 1804 None 0 Human Functional pIC50 None 7.2 7.2 3 2
UnclassifiedUnclassified
Guide to Pharmacology 604 8 2 5 5.4 O=C(NC1C(=O)N(c2ccccc2)c2c(N(C1=O)CC(=O)N(c1ccc(cc1)N(C)C)C(C)C)cccc2)Nc1ccccc1 8558528
19023535 3540 None 0 Rat Functional pIC50 None 7.8 7.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 363 4 3 3 2.0 OC(=O)C1CN(C(=O)C1NC(=O)c1c[nH]c2c1cccc2)c1ccccc1 None
883 3540 None 0 Rat Functional pIC50 None 7.8 7.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 363 4 3 3 2.0 OC(=O)C1CN(C(=O)C1NC(=O)c1c[nH]c2c1cccc2)c1ccccc1 None
11757476 2064 None 1 Rat Functional pIC50 None 9 9.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 558 7 4 4 3.7 O=C(NC(C)(C)C)N[C@H](C(=O)N[C@@H]1CCCN2[C@H]1CC(=O)N(C2=O)Cc1ccccc1)Cc1c[nH]c2c1cccc2 15331911
876 2064 None 1 Rat Functional pIC50 None 9 9.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 558 7 4 4 3.7 O=C(NC(C)(C)C)N[C@H](C(=O)N[C@@H]1CCCN2[C@H]1CC(=O)N(C2=O)Cc1ccccc1)Cc1c[nH]c2c1cccc2 15331911
CHEMBL2112828 2064 None 1 Rat Functional pIC50 None 9 9.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 558 7 4 4 3.7 O=C(NC(C)(C)C)N[C@H](C(=O)N[C@@H]1CCCN2[C@H]1CC(=O)N(C2=O)Cc1ccccc1)Cc1c[nH]c2c1cccc2 15331911
868 3667 None 0 Human Functional pIC50 None 9.3 9.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 609 10 2 7 7.9 COc1cc(Cl)c(cc1c1nc(sc1CCC1CCCCC1)NC(=O)c1cc2c(n1CC(=O)O)c(C)cc(c2)C)OC 10215648
9852833 3667 None 0 Human Functional pIC50 None 9.3 9.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 609 10 2 7 7.9 COc1cc(Cl)c(cc1c1nc(sc1CCC1CCCCC1)NC(=O)c1cc2c(n1CC(=O)O)c(C)cc(c2)C)OC 10215648
CHEMBL3302616 3667 None 0 Human Functional pIC50 None 9.3 9.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 609 10 2 7 7.9 COc1cc(Cl)c(cc1c1nc(sc1CCC1CCCCC1)NC(=O)c1cc2c(n1CC(=O)O)c(C)cc(c2)C)OC 10215648
132916 3161 None 15 Rat Functional pIC50 None 9.4 9.4 602 2
UnclassifiedUnclassified
Guide to Pharmacology 438 3 2 3 3.8 O=C(c1cc2c([nH]1)cccc2)N[C@H]1N=C(c2ccccc2F)c2c3N(C1=O)CCc3ccc2 7509389
874 3161 None 15 Rat Functional pIC50 None 9.4 9.4 602 2
UnclassifiedUnclassified
Guide to Pharmacology 438 3 2 3 3.8 O=C(c1cc2c([nH]1)cccc2)N[C@H]1N=C(c2ccccc2F)c2c3N(C1=O)CCc3ccc2 7509389
CHEMBL300072 3161 None 15 Rat Functional pIC50 None 9.4 9.4 602 2
UnclassifiedUnclassified
Guide to Pharmacology 438 3 2 3 3.8 O=C(c1cc2c([nH]1)cccc2)N[C@H]1N=C(c2ccccc2F)c2c3N(C1=O)CCc3ccc2 7509389
122077 2322 None 40 Rat Functional pIC50 None 9.7 9.7 8 2
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 7681406
890 2322 None 40 Rat Functional pIC50 None 9.7 9.7 8 2
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 7681406
CHEMBL249973 2322 None 40 Rat Functional pIC50 None 9.7 9.7 8 2
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 7681406
DB04867 2322 None 40 Rat Functional pIC50 None 9.7 9.7 8 2
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 7681406


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
45138674 16653 None 45 Human Binding pAC50 = 5 5.0 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 572 6 1 7 5.7 COc1cccc(N2CCN(C3=Nc4c(F)cccc4[C@H](CC(=O)O)N3c3cc(C(F)(F)F)ccc3OC)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1241951 16653 None 45 Human Binding pAC50 = 5 5.0 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 572 6 1 7 5.7 COc1cccc(N2CCN(C3=Nc4c(F)cccc4[C@H](CC(=O)O)N3c3cc(C(F)(F)F)ccc3OC)CC2)c1 10.1038/s41467-023-40064-9
25181577 78248 None 44 Human Binding pAC50 = 5 5.0 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
CHEMBL2105695 78248 None 44 Human Binding pAC50 = 5 5.0 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
3062316 33583 None 70 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 487 7 3 9 3.3 Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1 10.1038/s41467-023-40064-9
CHEMBL1421 33583 None 70 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 487 7 3 9 3.3 Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1 10.1038/s41467-023-40064-9
CHEMBL5416410 33583 None 70 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 487 7 3 9 3.3 Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1 10.1038/s41467-023-40064-9
10184653 11001 None 62 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 8 2 7 4.4 CN(C)C/C=C/C(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1O[C@H]1CCOC1 10.1038/s41467-023-40064-9
CHEMBL1173655 11001 None 62 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 8 2 7 4.4 CN(C)C/C=C/C(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1O[C@H]1CCOC1 10.1038/s41467-023-40064-9
25025298 78180 None 37 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 546 8 3 8 4.5 Cc1ccn(-c2cc(Cl)ccc2[C@@H](Oc2cc(-c3ccc(C[C@H](N)C(=O)O)cc3)nc(N)n2)C(F)(F)F)n1 10.1038/s41467-023-40064-9
CHEMBL2103855 78180 None 37 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 546 8 3 8 4.5 Cc1ccn(-c2cc(Cl)ccc2[C@@H](Oc2cc(-c3ccc(C[C@H](N)C(=O)O)cc3)nc(N)n2)C(F)(F)F)n1 10.1038/s41467-023-40064-9
213046 2385 None 44 Human Binding pAC50 = 4.9 4.9 - 8
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
213046.0 2385 None 44 Human Binding pAC50 = 4.9 4.9 - 8
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
4168 2385 None 44 Human Binding pAC50 = 4.9 4.9 - 8
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
7461 2385 None 44 Human Binding pAC50 = 4.9 4.9 - 8
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
CHEMBL1237021 2385 None 44 Human Binding pAC50 = 4.9 4.9 - 8
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
DB08815 2385 None 44 Human Binding pAC50 = 4.9 4.9 - 8
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
392622 56328 None 57 Human Binding pAC50 = 4.9 4.9 - 4
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
CHEMBL163 56328 None 57 Human Binding pAC50 = 4.9 4.9 - 4
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
6436173 55132 None 30 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL1617 55132 None 30 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
1890 2759 None 31 Human Binding pAC50 = 4.9 4.9 - 26
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
4449 2759 None 31 Human Binding pAC50 = 4.9 4.9 - 26
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
7247 2759 None 31 Human Binding pAC50 = 4.9 4.9 - 26
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
CHEMBL623 2759 None 31 Human Binding pAC50 = 4.9 4.9 - 26
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
DB01149 2759 None 31 Human Binding pAC50 = 4.9 4.9 - 26
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
10831 117027 None 19 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 397 7 2 5 4.3 O=C(Nc1ccccc1)OCC(CN1CCCCC1)OC(=O)Nc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL338667 117027 None 19 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 397 7 2 5 4.3 O=C(Nc1ccccc1)OCC(CN1CCCCC1)OC(=O)Nc1ccccc1 10.1038/s41467-023-40064-9
2713 207729 None 57 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353524 207729 None 57 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5360566 207729 None 57 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
88536661 207729 None 57 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
9552079 207729 None 57 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1330113 207729 None 57 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL790 207729 None 57 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353627 84575 None 8 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 411 8 3 4 4.6 CC(C)n1c(/C=C/C(O)CC(O)CC(=O)O)c(-c2ccc(F)cc2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL2220442 84575 None 8 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 411 8 3 4 4.6 CC(C)n1c(/C=C/C(O)CC(O)CC(=O)O)c(-c2ccc(F)cc2)c2ccccc21 10.1038/s41467-023-40064-9
104850 3330 None 58 Human Binding pAC50 = 4.8 4.8 - 6
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
4150 3330 None 58 Human Binding pAC50 = 4.8 4.8 - 6
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
743 3330 None 58 Human Binding pAC50 = 4.8 4.8 - 6
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL111 3330 None 58 Human Binding pAC50 = 4.8 4.8 - 6
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
DB06155 3330 None 58 Human Binding pAC50 = 4.8 4.8 - 6
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
135398735 137055 None 20 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
136262914 137055 None 20 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL374478 137055 None 20 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
148192 10423 None 49 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 704 14 5 9 4.2 COC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)[C@@H](O)CN(Cc1ccc(-c2ccccn2)cc1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL1163 10423 None 49 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 704 14 5 9 4.2 COC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)[C@@H](O)CN(Cc1ccc(-c2ccccn2)cc1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C(C)(C)C 10.1038/s41467-023-40064-9
4150 788 None 26 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
5288 788 None 26 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
644019 788 None 26 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
644019.0 788 None 26 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
CHEMBL190461 788 None 26 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
DB09061 788 None 26 Human Binding pAC50 = 4.7 4.7 - 12
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
135564886 14499 None 5 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
135673376 14499 None 5 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
137157436 14499 None 5 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
145948239 14499 None 5 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
71587099 14499 None 5 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
CHEMBL1201304 14499 None 5 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
2540 4402 None 68 Human Binding pAC50 = 4.7 4.7 - 4
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
CHEMBL1014 4402 None 68 Human Binding pAC50 = 4.7 4.7 - 4
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
2179 167616 None 49 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL1256655 167616 None 49 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL43 167616 None 49 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
2351 4301 None 35 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1008 4301 None 35 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1257078 4301 None 35 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
30323 62505 None 35 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL1563 62505 None 35 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL178 62505 None 35 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
2583 3776 None 69 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
592 3776 None 69 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
65999 3776 None 69 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
65999.0 3776 None 69 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
CHEMBL1017 3776 None 69 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
DB00966 3776 None 69 Human Binding pAC50 = 5.6 5.6 - 1
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
123879 3287 None 57 Human Binding pAC50 = 4.6 4.6 - 4
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
123879.0 3287 None 57 Human Binding pAC50 = 4.6 4.6 - 4
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
1910 3287 None 57 Human Binding pAC50 = 4.6 4.6 - 4
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
1911 3287 None 57 Human Binding pAC50 = 4.6 4.6 - 4
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
2354 3287 None 57 Human Binding pAC50 = 4.6 4.6 - 4
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
CHEMBL361812 3287 None 57 Human Binding pAC50 = 4.6 4.6 - 4
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
DB13036 3287 None 57 Human Binding pAC50 = 4.6 4.6 - 4
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
54682461 84720 None 41 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 602 11 2 6 7.3 CCC[C@@]1(CCc2ccccc2)CC(O)=C([C@H](CC)c2cccc(NS(=O)(=O)c3ccc(C(F)(F)F)cn3)c2)C(=O)O1 10.1038/s41467-023-40064-9
CHEMBL222559 84720 None 41 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 602 11 2 6 7.3 CCC[C@@]1(CCc2ccccc2)CC(O)=C([C@H](CC)c2cccc(NS(=O)(=O)c3ccc(C(F)(F)F)cn3)c2)C(=O)O1 10.1038/s41467-023-40064-9
CHEMBL2103737 78169 None 0 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
8550 14429 None 40 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 578 7 1 9 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC 10.1038/s41467-023-40064-9
CHEMBL1200515 14429 None 40 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 578 7 1 9 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC 10.1038/s41467-023-40064-9
4846 27995 None 38 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 1 2 6 2.2 O=C(O)c1cc(O)c2c3nc4ccccc4oc-3cc(=O)c2n1 10.1038/s41467-023-40064-9
CHEMBL1372341 27995 None 38 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 1 2 6 2.2 O=C(O)c1cc(O)c2c3nc4ccccc4oc-3cc(=O)c2n1 10.1038/s41467-023-40064-9
4495 198991 None 63 Human Binding pAC50 = 5.2 5.2 - 30
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL56367 198991 None 63 Human Binding pAC50 = 5.2 5.2 - 30
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 10.1038/s41467-023-40064-9
16362 3125 None 49 Human Binding pAC50 = 5.2 5.2 - 29
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
16362.0 3125 None 49 Human Binding pAC50 = 5.2 5.2 - 29
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 3125 None 49 Human Binding pAC50 = 5.2 5.2 - 29
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 3125 None 49 Human Binding pAC50 = 5.2 5.2 - 29
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 3125 None 49 Human Binding pAC50 = 5.2 5.2 - 29
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 3125 None 49 Human Binding pAC50 = 5.2 5.2 - 29
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
41684 31229 None 62 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
CHEMBL1401 31229 None 62 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
5329102 194838 None 50 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 194838 None 50 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
71496458 115628 None 61 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
CHEMBL3353410 115628 None 61 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
176870 197941 None 62 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 10 1 7 3.4 C#Cc1cccc(Nc2ncnc3cc(OCCOC)c(OCCOC)cc23)c1 10.1038/s41467-023-40064-9
CHEMBL553 197941 None 62 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 10 1 7 3.4 C#Cc1cccc(Nc2ncnc3cc(OCCOC)c(OCCOC)cc23)c1 10.1038/s41467-023-40064-9
4627 822 None 42 Human Binding pEC50 = 10 10.0 -2 5
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00017a022
864 822 None 42 Human Binding pEC50 = 10 10.0 -2 5
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00017a022
9833444 822 None 42 Human Binding pEC50 = 10 10.0 -2 5
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00017a022
CHEMBL1121 822 None 42 Human Binding pEC50 = 10 10.0 -2 5
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00017a022
DB09142 822 None 42 Human Binding pEC50 = 10 10.0 -2 5
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00017a022
10032955 168138 None 0 Human Binding pEC50 = 8.5 8.5 - 0
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)NC(=O)CCC(=O)O 10.1021/jm00017a022
CHEMBL432256 168138 None 0 Human Binding pEC50 = 8.5 8.5 - 0
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)NC(=O)CCC(=O)O 10.1021/jm00017a022
CHEMBL319438 213676 None 0 Human Binding pEC50 = 8.4 8.4 - 0
Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptorCompound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00017a022
24769604 188796 None 0 Human Binding pIC50 = 11 11.0 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 663 9 2 7 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504114 188796 None 0 Human Binding pIC50 = 11 11.0 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 663 9 2 7 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
44562301 189159 None 0 Human Binding pIC50 = 10.8 10.8 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL509464 189159 None 0 Human Binding pIC50 = 10.8 10.8 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24769546 172792 None 0 Human Binding pIC50 = 10.7 10.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 618 9 2 8 4.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL450105 172792 None 0 Human Binding pIC50 = 10.7 10.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 618 9 2 8 4.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24861391 188859 None 0 Human Binding pIC50 = 10.5 10.5 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 5 1 7 5.3 O=C(O)c1cc(N2CCN(C(=O)c3cn(-c4ccc5c(c4)OCCO5)c(-c4ccc(F)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2008.06.057
CHEMBL505225 188859 None 0 Human Binding pIC50 = 10.5 10.5 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 5 1 7 5.3 O=C(O)c1cc(N2CCN(C(=O)c3cn(-c4ccc5c(c4)OCCO5)c(-c4ccc(F)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2008.06.057
CHEMBL505969 188859 None 0 Human Binding pIC50 = 10.5 10.5 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 5 1 7 5.3 O=C(O)c1cc(N2CCN(C(=O)c3cn(-c4ccc5c(c4)OCCO5)c(-c4ccc(F)cc4)n3)CC2)cc2ccccc12 10.1016/j.bmcl.2008.06.057
24861394 189163 None 0 Human Binding pIC50 = 10.5 10.5 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 592 5 1 7 5.6 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL509519 189163 None 0 Human Binding pIC50 = 10.5 10.5 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 592 5 1 7 5.6 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2008.06.057
53233689 61876 None 0 Human Binding pIC50 = 10.5 10.5 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 604 5 1 7 5.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773877 61876 None 0 Human Binding pIC50 = 10.5 10.5 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 604 5 1 7 5.8 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)c(F)c1 10.1016/j.bmcl.2011.03.069
44562306 189037 None 0 Human Binding pIC50 = 10.4 10.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL508004 189037 None 0 Human Binding pIC50 = 10.4 10.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24861060 188834 None 0 Human Binding pIC50 = 10.4 10.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL446789 188834 None 0 Human Binding pIC50 = 10.4 10.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504861 188834 None 0 Human Binding pIC50 = 10.4 10.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
155543995 173427 None 0 Human Binding pIC50 = 10.4 10.4 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1876 73 16 22 4.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4526455 173427 None 0 Human Binding pIC50 = 10.4 10.4 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1876 73 16 22 4.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44562302 188297 None 0 Human Binding pIC50 = 10.4 10.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 666 11 2 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL498958 188297 None 0 Human Binding pIC50 = 10.4 10.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 666 11 2 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
155562281 175945 None 0 Human Binding pIC50 = 10.4 10.4 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4585323 175945 None 0 Human Binding pIC50 = 10.4 10.4 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
10819755 165537 None 0 Human Binding pIC50 = 10.4 10.4 - 2
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL423907 165537 None 0 Human Binding pIC50 = 10.4 10.4 - 2
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 976 28 9 11 1.6 CCCC[C@H](NC(=O)Cc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL411079 215322 None 0 Rat Binding pIC50 = 10.3 10.3 - 0
Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N1CSC(C)(C)[C@@H]1C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00100a033
121964 207 None 26 Rat Binding pIC50 = 10.3 10.3 831 2
Inhibitory activity against cholecystokinin type A receptor from rat pancreas binding assayInhibitory activity against cholecystokinin type A receptor from rat pancreas binding assay
ChEMBL None None None None 10.1021/jm00100a033
858 207 None 26 Rat Binding pIC50 = 10.3 10.3 831 2
Inhibitory activity against cholecystokinin type A receptor from rat pancreas binding assayInhibitory activity against cholecystokinin type A receptor from rat pancreas binding assay
ChEMBL None None None None 10.1021/jm00100a033
CHEMBL323521 207 None 26 Rat Binding pIC50 = 10.3 10.3 831 2
Inhibitory activity against cholecystokinin type A receptor from rat pancreas binding assayInhibitory activity against cholecystokinin type A receptor from rat pancreas binding assay
ChEMBL None None None None 10.1021/jm00100a033
155543163 173390 None 0 Human Binding pIC50 = 10.3 10.3 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1886 72 16 25 2.5 CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4525615 173390 None 0 Human Binding pIC50 = 10.3 10.3 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1886 72 16 25 2.5 CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24769605 178824 None 0 Human Binding pIC50 = 10.3 10.3 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL468372 178824 None 0 Human Binding pIC50 = 10.3 10.3 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 605 10 1 8 5.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155514270 169973 None 0 Human Binding pIC50 = 10.3 10.3 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4440419 169973 None 0 Human Binding pIC50 = 10.3 10.3 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
24769543 188811 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 649 9 2 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504406 188811 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 649 9 2 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
24861060 188834 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL446789 188834 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL504861 188834 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 578 7 1 6 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
155539345 172936 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1850 72 16 23 3.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4514283 172936 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1850 72 16 23 3.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155514432 169968 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 2121 86 19 27 2.3 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4440303 169968 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 2121 86 19 27 2.3 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)[C@H](CCCCN)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155540739 172610 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1907 74 17 24 2.5 CCCC[C@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4483457 172610 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1907 74 17 24 2.5 CCCC[C@H](NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44562303 172891 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 685 10 2 8 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL451342 172891 None 0 Human Binding pIC50 = 10.2 10.2 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 685 10 2 8 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
24861114 189248 None 4 Human Binding pIC50 = 10.2 10.2 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 582 7 1 6 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL510690 189248 None 4 Human Binding pIC50 = 10.2 10.2 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 582 7 1 6 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
155515427 170052 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4441596 170052 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
155566319 175844 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1850 71 16 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4583158 175844 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1850 71 16 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155559320 174968 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1872 72 18 23 3.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4563364 174968 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1872 72 18 23 3.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
443375 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL9506 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
155547906 173780 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)C[C@H](NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4534977 173780 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)C[C@H](NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155560670 175196 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4568746 175196 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1886 72 17 23 4.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
443375 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80683-6
CHEMBL9506 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80683-6
443375 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Concentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissueConcentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm020424z
CHEMBL9506 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Concentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissueConcentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm020424z
443375 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
CHEMBL9506 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
443375 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm000937a
CHEMBL9506 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm000937a
443375 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL9506 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
443375 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00609-9
CHEMBL9506 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00609-9
443375 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00164a020
CHEMBL9506 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00164a020
443375 210065 None 33 Human Binding pIC50 = 10.1 10.1 -2 5
Inhibition of cholecystokinin A receptorInhibition of cholecystokinin A receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/np9800102
CHEMBL9506 210065 None 33 Human Binding pIC50 = 10.1 10.1 -2 5
Inhibition of cholecystokinin A receptorInhibition of cholecystokinin A receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/np9800102
24861113 188296 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 564 7 1 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL498942 188296 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 564 7 1 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL506201 188296 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 564 7 1 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
44562297 188730 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 631 9 2 7 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL502974 188730 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 631 9 2 7 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562299 188977 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 646 9 3 7 5.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL507051 188977 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 646 9 3 7 5.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
443375 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80684-8
CHEMBL9506 210065 None 33 Rat Binding pIC50 = 10.1 10.1 -3 5
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80684-8
155536333 172275 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1865 71 17 24 1.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4473468 172275 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1865 71 17 24 1.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155555346 174476 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4551834 174476 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155535579 172153 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4471871 172153 None 0 Human Binding pIC50 = 10.1 10.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44398261 124453 None 0 Rat Binding pIC50 = 10.1 10.1 - 0
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 124453 None 0 Rat Binding pIC50 = 10.1 10.1 - 0
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
10460766 115520 None 0 Rat Binding pIC50 = 10.1 10.1 - 0
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 7 3 5 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm010898i
CHEMBL3350858 115520 None 0 Rat Binding pIC50 = 10.1 10.1 - 0
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 7 3 5 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm010898i
44562304 188983 None 0 Human Binding pIC50 = 10.0 10.0 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 664 9 3 7 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(=O)NC)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
CHEMBL507094 188983 None 0 Human Binding pIC50 = 10.0 10.0 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 664 9 3 7 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@H]3CNC(=O)NC)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.07.083
155555065 174438 None 0 Human Binding pIC50 = 10.0 10.0 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4550876 174438 None 0 Human Binding pIC50 = 10.0 10.0 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 71 17 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL269098 213237 None 0 Rat Binding pIC50 = 10 10.0 - 0
Compound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasCompound was tested for the inhibition of specific binding of [125I]bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(01)81250-6
4627 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL None None None None 10.1021/jm00092a007
864 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL None None None None 10.1021/jm00092a007
9833444 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL None None None None 10.1021/jm00092a007
CHEMBL1121 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL None None None None 10.1021/jm00092a007
DB09142 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL None None None None 10.1021/jm00092a007
4627 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00105a062
864 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00105a062
9833444 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00105a062
CHEMBL1121 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00105a062
DB09142 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00105a062
443375 210065 None 33 Rat Binding pIC50 = 10 10.0 -3 5
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00105a062
CHEMBL9506 210065 None 33 Rat Binding pIC50 = 10 10.0 -3 5
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00105a062
4627 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1016/S0960-894X(00)80687-3
864 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1016/S0960-894X(00)80687-3
9833444 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1016/S0960-894X(00)80687-3
CHEMBL1121 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1016/S0960-894X(00)80687-3
DB09142 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1016/S0960-894X(00)80687-3
443375 210065 None 33 Rat Binding pIC50 = 10 10.0 -3 5
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80687-3
CHEMBL9506 210065 None 33 Rat Binding pIC50 = 10 10.0 -3 5
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80687-3
4627 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL None None None None 10.1021/jm00057a005
864 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL None None None None 10.1021/jm00057a005
9833444 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL None None None None 10.1021/jm00057a005
CHEMBL1121 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL None None None None 10.1021/jm00057a005
DB09142 822 None 42 Rat Binding pIC50 = 10 10.0 -1 5
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL None None None None 10.1021/jm00057a005
443375 210065 None 33 Rat Binding pIC50 = 10 10.0 -3 5
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00057a005
CHEMBL9506 210065 None 33 Rat Binding pIC50 = 10 10.0 -3 5
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00057a005
155532759 171858 None 0 Human Binding pIC50 = 10.0 10.0 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1431 50 12 15 5.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4467402 171858 None 0 Human Binding pIC50 = 10.0 10.0 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1431 50 12 15 5.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155517239 170260 None 0 Human Binding pIC50 = 10.0 10.0 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 2582 122 16 39 4.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4444353 170260 None 0 Human Binding pIC50 = 10.0 10.0 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 2582 122 16 39 4.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44562300 188744 None 0 Human Binding pIC50 = 10.0 10.0 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL503107 188744 None 0 Human Binding pIC50 = 10.0 10.0 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 645 9 2 7 6.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
4627 822 None 42 Human Binding pIC50 = 10.0 10.0 -2 5
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
864 822 None 42 Human Binding pIC50 = 10.0 10.0 -2 5
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
9833444 822 None 42 Human Binding pIC50 = 10.0 10.0 -2 5
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
CHEMBL1121 822 None 42 Human Binding pIC50 = 10.0 10.0 -2 5
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
DB09142 822 None 42 Human Binding pIC50 = 10.0 10.0 -2 5
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL None None None None 10.1021/acs.jmedchem.8b01558
155517761 170326 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4445529 170326 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1900 71 16 23 4.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
72548703 161661 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor after 60 mins by scintillation counting analysisDisplacement of [125I]CCK-8s from human recombinant CCK1 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161661 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor after 60 mins by scintillation counting analysisDisplacement of [125I]CCK-8s from human recombinant CCK1 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
44562298 171554 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 667 10 2 8 5.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL446324 171554 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 667 10 2 8 5.0 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44578764 180918 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 535 4 0 7 5.0 O=C(c1cn(-c2ccc3c(c2)OCCO3)c(-c2ccc(F)cc2)n1)N1CCN(c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2008.06.057
CHEMBL475679 180918 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 535 4 0 7 5.0 O=C(c1cn(-c2ccc3c(c2)OCCO3)c(-c2ccc(F)cc2)n1)N1CCN(c2cnc3ccccc3c2)CC1 10.1016/j.bmcl.2008.06.057
16755781 188893 None 9 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
16755781 188893 None 9 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL443189 188893 None 9 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL443189 188893 None 9 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505409 188893 None 9 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL505409 188893 None 9 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505727 188893 None 9 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL505727 188893 None 9 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 560 7 1 6 6.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
4627 822 None 42 Human Binding pIC50 = 9.9 9.9 -2 5
Displacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cellsDisplacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
864 822 None 42 Human Binding pIC50 = 9.9 9.9 -2 5
Displacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cellsDisplacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
9833444 822 None 42 Human Binding pIC50 = 9.9 9.9 -2 5
Displacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cellsDisplacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
CHEMBL1121 822 None 42 Human Binding pIC50 = 9.9 9.9 -2 5
Displacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cellsDisplacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
DB09142 822 None 42 Human Binding pIC50 = 9.9 9.9 -2 5
Displacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cellsDisplacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
4627 822 None 42 Human Binding pIC50 = 9.9 9.9 -2 5
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2016.11.014
864 822 None 42 Human Binding pIC50 = 9.9 9.9 -2 5
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2016.11.014
9833444 822 None 42 Human Binding pIC50 = 9.9 9.9 -2 5
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2016.11.014
CHEMBL1121 822 None 42 Human Binding pIC50 = 9.9 9.9 -2 5
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2016.11.014
DB09142 822 None 42 Human Binding pIC50 = 9.9 9.9 -2 5
Displacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL None None None None 10.1016/j.bmc.2016.11.014
44578457 172574 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL448221 172574 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
24861392 173021 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 574 5 1 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL451644 173021 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 574 5 1 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
44562296 189111 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 648 11 2 8 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL508772 189111 None 0 Human Binding pIC50 = 9.9 9.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 648 11 2 8 5.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)C[C@@H]3COCC(=O)O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155552556 174172 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1792 67 16 22 1.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4544208 174172 None 0 Human Binding pIC50 = 9.8 9.8 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1792 67 16 22 1.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
54586148 61888 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 543 4 0 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773891 61888 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 543 4 0 7 5.4 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2011.03.069
155542488 173237 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1820 69 16 22 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4520976 173237 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1820 69 16 22 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL413654 215539 None 0 Rat Binding pIC50 = 9.7 9.7 - 2
Compound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptorCompound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](C)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H](N)CCC(=O)O)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm00378a012
13822923 194928 None 0 Rat Binding pIC50 = 9.7 9.7 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 450 3 2 5 4.5 Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=NC2NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00396a028
CHEMBL53907 194928 None 0 Rat Binding pIC50 = 9.7 9.7 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 450 3 2 5 4.5 Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=NC2NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00396a028
44578729 189740 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 531 4 0 7 5.1 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL514953 189740 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 531 4 0 7 5.1 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
44562310 172756 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL449681 172756 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
46869398 61944 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 576 6 1 6 6.1 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774043 61944 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 576 6 1 6 6.1 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
44578728 179564 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 535 6 0 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL474067 179564 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 535 6 0 6 5.9 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
44562305 188727 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL502924 188727 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44562314 188870 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL505432 188870 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 602 8 1 7 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3C(=O)NC(C)C)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155516677 170192 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1822 72 18 23 2.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4443415 170192 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1822 72 18 23 2.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155524181 170956 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1820 71 18 22 2.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4453982 170956 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1820 71 18 22 2.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
14888734 167949 None 0 Rat Binding pIC50 = 9.6 9.6 - 0
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1012 29 10 13 0.8 CSCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL430906 167949 None 0 Rat Binding pIC50 = 9.6 9.6 - 0
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1012 29 10 13 0.8 CSCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
44562307 172809 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL450443 172809 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
54583296 61934 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 533 5 0 6 5.8 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774033 61934 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 533 5 0 6 5.8 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)cc1 10.1016/j.bmcl.2011.03.069
10477146 78544 None 0 Rat Binding pIC50 = 9.6 9.6 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2111920 78544 None 0 Rat Binding pIC50 = 9.6 9.6 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
155568312 176182 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 72 17 23 3.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4591101 176182 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 72 17 23 3.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155544674 175040 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4565336 175040 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
4627 822 None 42 Guinea pig Binding pIC50 = 9.6 9.6 -1 5
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(00)80680-0
864 822 None 42 Guinea pig Binding pIC50 = 9.6 9.6 -1 5
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(00)80680-0
9833444 822 None 42 Guinea pig Binding pIC50 = 9.6 9.6 -1 5
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(00)80680-0
CHEMBL1121 822 None 42 Guinea pig Binding pIC50 = 9.6 9.6 -1 5
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(00)80680-0
DB09142 822 None 42 Guinea pig Binding pIC50 = 9.6 9.6 -1 5
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(00)80680-0
14208286 67705 None 0 Rat Binding pIC50 = 9.5 9.5 - 0
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 395 4 1 3 3.7 CN1C(=O)[C@@H](NC(=O)/C=C/c2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL1907661 67705 None 0 Rat Binding pIC50 = 9.5 9.5 - 0
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 395 4 1 3 3.7 CN1C(=O)[C@@H](NC(=O)/C=C/c2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
155537344 172421 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4475304 172421 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1848 72 16 22 3.6 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155535107 172117 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1904 73 19 22 4.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4471525 172117 None 0 Human Binding pIC50 = 9.5 9.5 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1904 73 19 22 4.7 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
4627 822 None 42 Human Binding pIC50 = 9.4 9.4 -2 5
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
ChEMBL None None None None 10.1021/jm8007618
864 822 None 42 Human Binding pIC50 = 9.4 9.4 -2 5
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
ChEMBL None None None None 10.1021/jm8007618
9833444 822 None 42 Human Binding pIC50 = 9.4 9.4 -2 5
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
ChEMBL None None None None 10.1021/jm8007618
CHEMBL1121 822 None 42 Human Binding pIC50 = 9.4 9.4 -2 5
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
ChEMBL None None None None 10.1021/jm8007618
DB09142 822 None 42 Human Binding pIC50 = 9.4 9.4 -2 5
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
ChEMBL None None None None 10.1021/jm8007618
4627 822 None 42 Human Binding pIC50 = 9.4 9.4 -2 5
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm00017a022
864 822 None 42 Human Binding pIC50 = 9.4 9.4 -2 5
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm00017a022
9833444 822 None 42 Human Binding pIC50 = 9.4 9.4 -2 5
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm00017a022
CHEMBL1121 822 None 42 Human Binding pIC50 = 9.4 9.4 -2 5
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm00017a022
DB09142 822 None 42 Human Binding pIC50 = 9.4 9.4 -2 5
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm00017a022
14208241 67772 None 0 Rat Binding pIC50 = 9.4 9.4 - 0
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
CHEMBL1907852 67772 None 0 Rat Binding pIC50 = 9.4 9.4 - 0
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
44562312 188752 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL503331 188752 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 588 8 1 7 5.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
14208244 58885 None 0 Rat Binding pIC50 = 9.4 9.4 - 0
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80684-8
CHEMBL168852 58885 None 0 Rat Binding pIC50 = 9.4 9.4 - 0
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80684-8
4627 822 None 42 Human Binding pIC50 = 9.4 9.4 -2 5
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00001a027
864 822 None 42 Human Binding pIC50 = 9.4 9.4 -2 5
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00001a027
9833444 822 None 42 Human Binding pIC50 = 9.4 9.4 -2 5
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00001a027
CHEMBL1121 822 None 42 Human Binding pIC50 = 9.4 9.4 -2 5
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00001a027
DB09142 822 None 42 Human Binding pIC50 = 9.4 9.4 -2 5
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm00001a027
4627 822 None 42 Guinea pig Binding pIC50 = 9.4 9.4 -1 5
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None None 10.1021/jm00173a006
864 822 None 42 Guinea pig Binding pIC50 = 9.4 9.4 -1 5
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None None 10.1021/jm00173a006
9833444 822 None 42 Guinea pig Binding pIC50 = 9.4 9.4 -1 5
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None None 10.1021/jm00173a006
CHEMBL1121 822 None 42 Guinea pig Binding pIC50 = 9.4 9.4 -1 5
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None None 10.1021/jm00173a006
DB09142 822 None 42 Guinea pig Binding pIC50 = 9.4 9.4 -1 5
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None None 10.1021/jm00173a006
24785705 182392 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL478398 182392 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2ccc3c(c2)OCCO3)cc1 10.1016/j.bmcl.2008.06.057
44562308 172759 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL449725 172759 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
44578767 173620 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44578767 173620 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL453083 173620 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL453083 173620 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL503822 173620 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL503822 173620 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 517 6 0 6 5.8 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
6957640 159455 None 0 Rat Binding pIC50 = 9.3 9.3 - 0
In vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determinedIn vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determined
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
CHEMBL410035 159455 None 0 Rat Binding pIC50 = 9.3 9.3 - 0
In vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determinedIn vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determined
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
44396718 67420 None 0 Rat Binding pIC50 = 9.3 9.3 - 0
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 530 7 2 5 4.6 C[C@@H]1C(=O)N(Cc2ccccc2)C(=O)N2CCC[C@H](N[C@@H](Cc3c[nH]c4ccccc34)C(=O)OC(C)(C)C)C12 10.1021/jm0498755
CHEMBL188808 67420 None 0 Rat Binding pIC50 = 9.3 9.3 - 0
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 530 7 2 5 4.6 C[C@@H]1C(=O)N(Cc2ccccc2)C(=O)N2CCC[C@H](N[C@@H](Cc3c[nH]c4ccccc34)C(=O)OC(C)(C)C)C12 10.1021/jm0498755
44562311 188825 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL504707 188825 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 589 8 0 8 5.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3COC(C)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
155557064 174696 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1998 75 18 24 4.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4557012 174696 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1998 75 18 24 4.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
443375 210065 None 33 Human Binding pIC50 = 9.3 9.3 -2 5
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm701575k
CHEMBL9506 210065 None 33 Human Binding pIC50 = 9.3 9.3 -2 5
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm701575k
4627 822 None 42 Rat Binding pIC50 = 9.3 9.3 -1 5
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL None None None None 10.1021/jm00079a003
864 822 None 42 Rat Binding pIC50 = 9.3 9.3 -1 5
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL None None None None 10.1021/jm00079a003
9833444 822 None 42 Rat Binding pIC50 = 9.3 9.3 -1 5
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL None None None None 10.1021/jm00079a003
CHEMBL1121 822 None 42 Rat Binding pIC50 = 9.3 9.3 -1 5
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL None None None None 10.1021/jm00079a003
DB09142 822 None 42 Rat Binding pIC50 = 9.3 9.3 -1 5
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL None None None None 10.1021/jm00079a003
6918156 97341 None 4 Human Binding pIC50 = 9.3 9.3 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL269016 97341 None 4 Human Binding pIC50 = 9.3 9.3 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
6918156 97341 None 4 Guinea pig Binding pIC50 = 9.3 9.3 - 0
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL269016 97341 None 4 Guinea pig Binding pIC50 = 9.3 9.3 - 0
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
155530671 171665 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1627 65 14 19 4.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4464703 171665 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1627 65 14 19 4.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
155524770 171041 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1641 66 14 19 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4455361 171041 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1641 66 14 19 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)NC(=O)Cc1ccc(O)cc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44562309 171685 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 603 8 2 7 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL446502 171685 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 603 8 2 7 5.1 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@@H]3CNC(=O)NC)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
24785703 179458 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 534 6 0 5 6.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473664 179458 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 534 6 0 5 6.5 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2F)c1 10.1016/j.bmcl.2008.06.057
122077 2322 None 40 Human Binding pIC50 = 9.3 9.3 - 1
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10.1016/j.bmcl.2007.09.093
890 2322 None 40 Human Binding pIC50 = 9.3 9.3 - 1
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10.1016/j.bmcl.2007.09.093
CHEMBL249973 2322 None 40 Human Binding pIC50 = 9.3 9.3 - 1
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10.1016/j.bmcl.2007.09.093
DB04867 2322 None 40 Human Binding pIC50 = 9.3 9.3 - 1
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10.1016/j.bmcl.2007.09.093
44578727 189859 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL515887 189859 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
10008654 127683 None 0 Rat Binding pIC50 = 9.2 9.2 - 0
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127683 None 0 Rat Binding pIC50 = 9.2 9.2 - 0
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
10008654 127683 None 0 Rat Binding pIC50 = 9.2 9.2 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL366344 127683 None 0 Rat Binding pIC50 = 9.2 9.2 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL438773 216258 None 0 Rat Binding pIC50 = 9.2 9.2 - 0
Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00100a033
10482714 78462 None 0 Rat Binding pIC50 = 9.2 9.2 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 551 6 3 5 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(C3CCCCC3)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL2111545 78462 None 0 Rat Binding pIC50 = 9.2 9.2 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 551 6 3 5 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(C3CCCCC3)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL2370122 212246 None 0 Rat Binding pIC50 = 9.2 9.2 - 0
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL None None None CSCC[C@@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
44578686 179479 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473865 179479 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 521 6 0 6 5.6 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL267849 213193 None 0 Rat Binding pIC50 = 9.2 9.2 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
14208225 67775 None 0 Rat Binding pIC50 = 9.2 9.2 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 426 3 2 3 3.9 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL1907855 67775 None 0 Rat Binding pIC50 = 9.2 9.2 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 426 3 2 3 3.9 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
155535249 172106 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1808 68 16 23 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4471373 172106 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1808 68 16 23 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
4627 822 None 42 Human Binding pIC50 = 9.2 9.2 -2 5
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm9601664
864 822 None 42 Human Binding pIC50 = 9.2 9.2 -2 5
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm9601664
9833444 822 None 42 Human Binding pIC50 = 9.2 9.2 -2 5
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm9601664
CHEMBL1121 822 None 42 Human Binding pIC50 = 9.2 9.2 -2 5
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm9601664
DB09142 822 None 42 Human Binding pIC50 = 9.2 9.2 -2 5
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1021/jm9601664
4627 822 None 42 Human Binding pIC50 = 9.2 9.2 -2 5
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm950626d
864 822 None 42 Human Binding pIC50 = 9.2 9.2 -2 5
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm950626d
9833444 822 None 42 Human Binding pIC50 = 9.2 9.2 -2 5
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm950626d
CHEMBL1121 822 None 42 Human Binding pIC50 = 9.2 9.2 -2 5
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm950626d
DB09142 822 None 42 Human Binding pIC50 = 9.2 9.2 -2 5
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm950626d
15667014 107314 None 0 Guinea pig Binding pIC50 = 9.2 9.2 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 976 28 10 11 1.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL316944 107314 None 0 Guinea pig Binding pIC50 = 9.2 9.2 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 976 28 10 11 1.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
132916 3161 None 15 Rat Binding pIC50 = 9.2 9.2 - 0
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 438 3 2 3 3.8 O=C(c1cc2c([nH]1)cccc2)N[C@H]1N=C(c2ccccc2F)c2c3N(C1=O)CCc3ccc2 10.1016/S0960-894X(96)00609-9
874 3161 None 15 Rat Binding pIC50 = 9.2 9.2 - 0
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 438 3 2 3 3.8 O=C(c1cc2c([nH]1)cccc2)N[C@H]1N=C(c2ccccc2F)c2c3N(C1=O)CCc3ccc2 10.1016/S0960-894X(96)00609-9
CHEMBL300072 3161 None 15 Rat Binding pIC50 = 9.2 9.2 - 0
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 438 3 2 3 3.8 O=C(c1cc2c([nH]1)cccc2)N[C@H]1N=C(c2ccccc2F)c2c3N(C1=O)CCc3ccc2 10.1016/S0960-894X(96)00609-9
443375 210065 None 33 Rat Binding pIC50 = 9.2 9.2 -3 5
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/0960-894X(96)00160-6
CHEMBL9506 210065 None 33 Rat Binding pIC50 = 9.2 9.2 -3 5
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/0960-894X(96)00160-6
443375 210065 None 33 Rat Binding pIC50 = 9.2 9.2 -3 5
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm991078x
CHEMBL9506 210065 None 33 Rat Binding pIC50 = 9.2 9.2 -3 5
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm991078x
443375 210065 None 33 Rat Binding pIC50 = 9.2 9.2 -3 5
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm000959x
CHEMBL9506 210065 None 33 Rat Binding pIC50 = 9.2 9.2 -3 5
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm000959x
44562313 172561 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
CHEMBL448118 172561 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 624 9 1 8 4.7 CCOc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)C[C@H]3CNS(C)(=O)=O)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.07.083
14208303 207149 None 1 Rat Binding pIC50 = 9.1 9.1 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)C(NC(=O)c2cccc(I)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL73946 207149 None 1 Rat Binding pIC50 = 9.1 9.1 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)C(NC(=O)c2cccc(I)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208303 207149 None 1 Rat Binding pIC50 = 9.1 9.1 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 513 3 1 3 4.0 CN1C(=O)C(NC(=O)c2cccc(I)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL73946 207149 None 1 Rat Binding pIC50 = 9.1 9.1 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 513 3 1 3 4.0 CN1C(=O)C(NC(=O)c2cccc(I)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
15666988 107315 None 0 Guinea pig Binding pIC50 = 9.1 9.1 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 976 29 10 11 1.6 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL316949 107315 None 0 Guinea pig Binding pIC50 = 9.1 9.1 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 976 29 10 11 1.6 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
15666988 107315 None 0 Guinea pig Binding pIC50 = 9.1 9.1 - 0
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 976 29 10 11 1.6 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL316949 107315 None 0 Guinea pig Binding pIC50 = 9.1 9.1 - 0
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 976 29 10 11 1.6 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
3476 1400 None 2 Rat Binding pIC50 = 9.1 9.1 - 3
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00047a021
59751 1400 None 2 Rat Binding pIC50 = 9.1 9.1 - 3
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00047a021
878 1400 None 2 Rat Binding pIC50 = 9.1 9.1 - 3
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00047a021
CHEMBL39263 1400 None 2 Rat Binding pIC50 = 9.1 9.1 - 3
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00047a021
14208294 206693 None 1 Rat Binding pIC50 = 9.1 9.1 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 465 3 1 3 4.2 CN1C(=O)C(NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL70984 206693 None 1 Rat Binding pIC50 = 9.1 9.1 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 465 3 1 3 4.2 CN1C(=O)C(NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
14208296 207087 None 1 Rat Binding pIC50 = 9.1 9.1 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 513 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(I)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL73483 207087 None 1 Rat Binding pIC50 = 9.1 9.1 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 513 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(I)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
155532425 171851 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01558
CHEMBL4467338 171851 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1822 71 18 23 2.5 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01558
CHEMBL1172428 211045 None 0 Human Binding pIC50 = 9.1 9.1 - 3
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
4627 822 None 42 Rat Binding pIC50 = 9.1 9.1 -1 5
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00548-4
864 822 None 42 Rat Binding pIC50 = 9.1 9.1 -1 5
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00548-4
9833444 822 None 42 Rat Binding pIC50 = 9.1 9.1 -1 5
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00548-4
CHEMBL1121 822 None 42 Rat Binding pIC50 = 9.1 9.1 -1 5
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00548-4
DB09142 822 None 42 Rat Binding pIC50 = 9.1 9.1 -1 5
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(98)00548-4
3476 1400 None 2 Rat Binding pIC50 = 9.1 9.1 - 3
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00120a002
59751 1400 None 2 Rat Binding pIC50 = 9.1 9.1 - 3
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00120a002
878 1400 None 2 Rat Binding pIC50 = 9.1 9.1 - 3
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00120a002
CHEMBL39263 1400 None 2 Rat Binding pIC50 = 9.1 9.1 - 3
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00120a002
14208297 67767 None 0 Rat Binding pIC50 = 9.1 9.1 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(I)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907848 67767 None 0 Rat Binding pIC50 = 9.1 9.1 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(I)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208295 67770 None 0 Rat Binding pIC50 = 9.1 9.1 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 465 3 1 3 4.2 CN1C(=O)[C@@H](NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907850 67770 None 0 Rat Binding pIC50 = 9.1 9.1 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 465 3 1 3 4.2 CN1C(=O)[C@@H](NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
46235271 73674 None 2 Human Binding pIC50 = 9.1 9.1 2 2
Displacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73674 None 2 Human Binding pIC50 = 9.1 9.1 2 2
Displacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
14208268 206942 None 0 Rat Binding pIC50 = 9.1 9.1 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 418 3 2 4 3.5 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2N)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL72428 206942 None 0 Rat Binding pIC50 = 9.1 9.1 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 418 3 2 4 3.5 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2N)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
13822922 189189 None 0 Rat Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 436 3 2 5 4.2 O=C(NC1N=C(c2ccccc2F)c2ccccc2-n2cnnc21)c1cc2ccccc2[nH]1 10.1021/jm00396a028
CHEMBL50986 189189 None 0 Rat Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 436 3 2 5 4.2 O=C(NC1N=C(c2ccccc2F)c2ccccc2-n2cnnc21)c1cc2ccccc2[nH]1 10.1021/jm00396a028
11757476 2064 None 1 Rat Binding pIC50 = 9.0 9.0 - 0
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 558 7 4 4 3.7 O=C(NC(C)(C)C)N[C@H](C(=O)N[C@@H]1CCCN2[C@H]1CC(=O)N(C2=O)Cc1ccccc1)Cc1c[nH]c2c1cccc2 10.1021/jm991078x
876 2064 None 1 Rat Binding pIC50 = 9.0 9.0 - 0
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 558 7 4 4 3.7 O=C(NC(C)(C)C)N[C@H](C(=O)N[C@@H]1CCCN2[C@H]1CC(=O)N(C2=O)Cc1ccccc1)Cc1c[nH]c2c1cccc2 10.1021/jm991078x
CHEMBL2112828 2064 None 1 Rat Binding pIC50 = 9.0 9.0 - 0
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 558 7 4 4 3.7 O=C(NC(C)(C)C)N[C@H](C(=O)N[C@@H]1CCCN2[C@H]1CC(=O)N(C2=O)Cc1ccccc1)Cc1c[nH]c2c1cccc2 10.1021/jm991078x
CHEMBL384035 214776 None 3 Guinea pig Binding pIC50 = 9.0 9.0 -8 4
In vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL428666 214776 None 3 Guinea pig Binding pIC50 = 9.0 9.0 -8 4
In vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
155526914 171305 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1837 72 19 24 0.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4459331 171305 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1837 72 19 24 0.8 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
11017163 79576 None 0 Rat Binding pIC50 = 9.0 9.0 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1ccccc1N1C(=O)C[C@H]2[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1021/jm010813d
CHEMBL2114081 79576 None 0 Rat Binding pIC50 = 9.0 9.0 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1ccccc1N1C(=O)C[C@H]2[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1021/jm010813d
15667011 96710 None 1 Human Binding pIC50 = 9 9.0 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL263742 96710 None 1 Human Binding pIC50 = 9 9.0 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
15667011 96710 None 1 Guinea pig Binding pIC50 = 9 9.0 - 0
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL263742 96710 None 1 Guinea pig Binding pIC50 = 9 9.0 - 0
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 990 29 9 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
196641 206856 None 11 Rat Binding pIC50 = 9 9.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 447 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL71950 206856 None 11 Rat Binding pIC50 = 9 9.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 447 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
4627 822 None 42 Rat Binding pIC50 = 9 9.0 -1 5
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00198-0
864 822 None 42 Rat Binding pIC50 = 9 9.0 -1 5
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00198-0
9833444 822 None 42 Rat Binding pIC50 = 9 9.0 -1 5
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00198-0
CHEMBL1121 822 None 42 Rat Binding pIC50 = 9 9.0 -1 5
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00198-0
DB09142 822 None 42 Rat Binding pIC50 = 9 9.0 -1 5
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00198-0
44469677 15179 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]CCK-8 from human recombinant CCKA receptor expressed in CHO cellsDisplacement of [125I]CCK-8 from human recombinant CCKA receptor expressed in CHO cells
ChEMBL 336 4 1 4 5.4 C/C(=N\OC(=O)Nc1ccccc1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2010.06.050
CHEMBL1210154 15179 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]CCK-8 from human recombinant CCKA receptor expressed in CHO cellsDisplacement of [125I]CCK-8 from human recombinant CCKA receptor expressed in CHO cells
ChEMBL 336 4 1 4 5.4 C/C(=N\OC(=O)Nc1ccccc1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2010.06.050
196641 206856 None 11 Rat Binding pIC50 = 9 9.0 - 0
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 447 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL71950 206856 None 11 Rat Binding pIC50 = 9 9.0 - 0
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 447 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
16755782 179457 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473663 179457 None 0 Human Binding pIC50 = 9 9.0 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2F)c1 10.1016/j.bmcl.2008.06.057
44329487 108569 None 0 Guinea pig Binding pIC50 = 9 9.0 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 544 6 3 3 5.7 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)C[C@H](c3cccc(F)c3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL319986 108569 None 0 Guinea pig Binding pIC50 = 9 9.0 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 544 6 3 3 5.7 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)C[C@H](c3cccc(F)c3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
155564421 175372 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1770 69 16 21 3.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4572516 175372 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1770 69 16 21 3.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
4627 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL None None None None 10.1021/jm991078x
864 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL None None None None 10.1021/jm991078x
9833444 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL None None None None 10.1021/jm991078x
CHEMBL1121 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL None None None None 10.1021/jm991078x
DB09142 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL None None None None 10.1021/jm991078x
4627 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL None None None None 10.1021/jm0498755
864 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL None None None None 10.1021/jm0498755
9833444 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL None None None None 10.1021/jm0498755
CHEMBL1121 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL None None None None 10.1021/jm0498755
DB09142 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL None None None None 10.1021/jm0498755
4627 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm010898i
864 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm010898i
9833444 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm010898i
CHEMBL1121 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm010898i
DB09142 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm010898i
444998 211778 None 25 Rat Binding pIC50 = 9.0 9.0 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm010813d
CHEMBL216166 211778 None 25 Rat Binding pIC50 = 9.0 9.0 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm010813d
4627 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)
ChEMBL None None None None 10.1016/S0960-894X(97)00107-8
864 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)
ChEMBL None None None None 10.1016/S0960-894X(97)00107-8
9833444 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)
ChEMBL None None None None 10.1016/S0960-894X(97)00107-8
CHEMBL1121 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)
ChEMBL None None None None 10.1016/S0960-894X(97)00107-8
DB09142 822 None 42 Rat Binding pIC50 = 9.0 9.0 -1 5
Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane(CCK-A)
ChEMBL None None None None 10.1016/S0960-894X(97)00107-8
10033396 108645 None 0 Guinea pig Binding pIC50 = 9.0 9.0 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 824 20 8 7 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL320405 108645 None 0 Guinea pig Binding pIC50 = 9.0 9.0 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 824 20 8 7 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44329323 107399 None 0 Guinea pig Binding pIC50 = 9.0 9.0 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 574 7 3 3 6.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)Nc3ccccc3C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL317615 107399 None 0 Guinea pig Binding pIC50 = 9.0 9.0 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 574 7 3 3 6.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)Nc3ccccc3C)C2=O)c1 10.1016/S0960-894X(01)80832-5
44329331 108121 None 0 Guinea pig Binding pIC50 = 9.0 9.0 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1ccc([C@H]2C[C@@H](NC(=O)Nc3cccc(C)c3)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c3ccccc3)C2)cc1 10.1016/S0960-894X(01)80832-5
CHEMBL319504 108121 None 0 Guinea pig Binding pIC50 = 9.0 9.0 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1ccc([C@H]2C[C@@H](NC(=O)Nc3cccc(C)c3)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c3ccccc3)C2)cc1 10.1016/S0960-894X(01)80832-5
44329363 108760 None 0 Guinea pig Binding pIC50 = 9.0 9.0 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 594 7 3 3 7.2 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)Nc3ccccc3Cl)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL320821 108760 None 0 Guinea pig Binding pIC50 = 9.0 9.0 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 594 7 3 3 7.2 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)Nc3ccccc3Cl)C2=O)c1 10.1016/S0960-894X(01)80832-5
11027990 67553 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL189634 67553 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 545 6 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccccc3)C(=O)C[C@@H]12 10.1021/jm010813d
44269000 32924 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL 671 14 6 5 6.3 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/s0960-894x(00)00198-0
CHEMBL14153 32924 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL 671 14 6 5 6.3 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/s0960-894x(00)00198-0
44269000 32924 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Inhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptorInhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptor
ChEMBL 671 14 6 5 6.3 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/s0960-894x(01)00630-8
CHEMBL14153 32924 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Inhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptorInhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptor
ChEMBL 671 14 6 5 6.3 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/s0960-894x(01)00630-8
155533399 171948 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1838 72 19 24 1.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4468861 171948 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1838 72 19 24 1.4 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
4627 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(97)00062-0
864 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(97)00062-0
9833444 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(97)00062-0
CHEMBL1121 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(97)00062-0
DB09142 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL None None None None 10.1016/S0960-894X(97)00062-0
14208311 207122 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 437 3 1 3 4.3 CN1C(=O)C(NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL73699 207122 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 437 3 1 3 4.3 CN1C(=O)C(NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
14208227 102319 None 1 Rat Binding pIC50 = 8.9 8.9 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 440 3 1 4 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL303227 102319 None 1 Rat Binding pIC50 = 8.9 8.9 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 440 3 1 4 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208312 77851 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 437 3 1 3 4.3 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL2092865 77851 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 437 3 1 3 4.3 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
10373344 166729 None 0 Guinea pig Binding pIC50 = 8.9 8.9 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 844 21 8 7 3.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL428103 166729 None 0 Guinea pig Binding pIC50 = 8.9 8.9 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 844 21 8 7 3.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
10341724 78546 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 2 4 3.7 COc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL2111922 78546 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 2 4 3.7 COc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
24861174 174711 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL455742 174711 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 546 6 1 6 5.7 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44578424 183032 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL479256 183032 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44329286 107261 None 0 Guinea pig Binding pIC50 = 8.9 8.9 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3cccc(C)c3)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL316619 107261 None 0 Guinea pig Binding pIC50 = 8.9 8.9 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3cccc(C)c3)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
4627 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL None None None None 10.1021/jm960249k
864 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL None None None None 10.1021/jm960249k
9833444 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL None None None None 10.1021/jm960249k
CHEMBL1121 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL None None None None 10.1021/jm960249k
DB09142 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL None None None None 10.1021/jm960249k
4627 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL None None None None 10.1021/jm960205b
864 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL None None None None 10.1021/jm960205b
9833444 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL None None None None 10.1021/jm960205b
CHEMBL1121 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL None None None None 10.1021/jm960205b
DB09142 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL None None None None 10.1021/jm960205b
4627 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL None None None None 10.1021/jm970265x
864 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL None None None None 10.1021/jm970265x
9833444 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL None None None None 10.1021/jm970265x
CHEMBL1121 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL None None None None 10.1021/jm970265x
DB09142 822 None 42 Human Binding pIC50 = 8.9 8.9 -2 5
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL None None None None 10.1021/jm970265x
11082524 115517 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 591 7 3 5 5.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=S)N(Cc3ccccc3)C(=S)C[C@@H]12 10.1021/jm010898i
CHEMBL3350853 115517 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 591 7 3 5 5.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=S)N(Cc3ccccc3)C(=S)C[C@@H]12 10.1021/jm010898i
14208227 102319 None 1 Rat Binding pIC50 = 8.9 8.9 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 440 3 1 4 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL303227 102319 None 1 Rat Binding pIC50 = 8.9 8.9 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 440 3 1 4 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL411202 215333 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00100a033
54580295 61933 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774032 61933 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 519 5 0 6 5.5 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2F)cc1 10.1016/j.bmcl.2011.03.069
14208232 206597 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 452 5 3 4 3.2 O=C(O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL70456 206597 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 452 5 3 4 3.2 O=C(O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
14208231 206704 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 422 3 1 4 3.7 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL71079 206704 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 422 3 1 4 3.7 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
10093957 207092 None 1 Rat Binding pIC50 = 8.9 8.9 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 426 3 2 3 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL73522 207092 None 1 Rat Binding pIC50 = 8.9 8.9 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 426 3 2 3 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
10350551 108511 None 0 Guinea pig Binding pIC50 = 8.9 8.9 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 838 21 8 7 3.9 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL319913 108511 None 0 Guinea pig Binding pIC50 = 8.9 8.9 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 838 21 8 7 3.9 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
14208231 206704 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 422 3 1 4 3.7 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL71079 206704 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 422 3 1 4 3.7 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
14208231 206704 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 422 3 1 4 3.7 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL71079 206704 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 422 3 1 4 3.7 CN1C(=O)C(NC(=O)c2cc3ccccc3n2C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
10093957 207092 None 1 Rat Binding pIC50 = 8.9 8.9 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 426 3 2 3 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL73522 207092 None 1 Rat Binding pIC50 = 8.9 8.9 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 426 3 2 3 3.9 CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
46235271 73674 None 2 Human Binding pIC50 = 8.9 8.9 2 2
Displacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73674 None 2 Human Binding pIC50 = 8.9 8.9 2 2
Displacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
14208228 103162 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 470 5 3 4 3.3 O=C(O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL307661 103162 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 470 5 3 4 3.3 O=C(O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1172429 211046 None 0 Human Binding pIC50 = 8.8 8.8 26 4
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
5311188 9807 None 1 Rat Binding pIC50 = 8.8 8.8 -1 2
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
CHEMBL113718 9807 None 1 Rat Binding pIC50 = 8.8 8.8 -1 2
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
5311188 9807 None 1 Rat Binding pIC50 = 8.8 8.8 -1 2
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL113718 9807 None 1 Rat Binding pIC50 = 8.8 8.8 -1 2
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
44396619 166340 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 516 7 2 5 4.4 CC(C)(C)OC(=O)[C@H](Cc1c[nH]c2ccccc12)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)CC12 10.1021/jm0498755
CHEMBL426792 166340 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 516 7 2 5 4.4 CC(C)(C)OC(=O)[C@H](Cc1c[nH]c2ccccc12)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)CC12 10.1021/jm0498755
5311188 9807 None 1 Rat Binding pIC50 = 8.8 8.8 -1 2
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm010898i
CHEMBL113718 9807 None 1 Rat Binding pIC50 = 8.8 8.8 -1 2
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm010898i
5311188 9807 None 1 Rat Binding pIC50 = 8.8 8.8 -1 2
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL113718 9807 None 1 Rat Binding pIC50 = 8.8 8.8 -1 2
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL107694 210949 None 0 Guinea pig Binding pIC50 = 8.8 8.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44329330 107243 None 0 Guinea pig Binding pIC50 = 8.8 8.8 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)C[C@H](c3cccc(C)c3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL316504 107243 None 0 Guinea pig Binding pIC50 = 8.8 8.8 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 540 6 3 3 5.9 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)C[C@H](c3cccc(C)c3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
10076650 26240 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 566 8 4 5 3.5 O=C(N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1021/jm050689o
CHEMBL13577 26240 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 566 8 4 5 3.5 O=C(N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1021/jm050689o
10010723 4915 None 0 Guinea pig Binding pIC50 = 8.8 8.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 836 20 8 7 3.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(F)(F)F)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL104598 4915 None 0 Guinea pig Binding pIC50 = 8.8 8.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 836 20 8 7 3.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(F)(F)F)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
108187 926 None 30 Rat Binding pIC50 = 8.8 8.8 4 5
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00086a017
873 926 None 30 Rat Binding pIC50 = 8.8 8.8 4 5
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00086a017
CHEMBL2062154 926 None 30 Rat Binding pIC50 = 8.8 8.8 4 5
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00086a017
CHEMBL287735 926 None 30 Rat Binding pIC50 = 8.8 8.8 4 5
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00086a017
10076650 26240 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
Inhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptorInhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptor
ChEMBL 566 8 4 5 3.5 O=C(N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1016/s0960-894x(01)00630-8
CHEMBL13577 26240 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
Inhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptorInhibition of [3H]propionyl-CCK-8 specific binding to rat pancreatic Cholecystokinin type A receptor
ChEMBL 566 8 4 5 3.5 O=C(N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1016/s0960-894x(01)00630-8
10076650 26240 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 566 8 4 5 3.5 O=C(N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1021/jm000959x
CHEMBL13577 26240 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
ChEMBL 566 8 4 5 3.5 O=C(N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(=O)O)N2C1=O)OCc1ccccc1 10.1021/jm000959x
44329352 111500 None 0 Guinea pig Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 544 6 3 3 5.7 Cc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(F)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
CHEMBL327496 111500 None 0 Guinea pig Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 544 6 3 3 5.7 Cc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(F)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
44578647 179434 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2c(F)cccc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL473457 179434 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 538 6 0 5 6.3 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2c(F)cccc2F)c1 10.1016/j.bmcl.2008.06.057
24785178 181645 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476530 181645 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(F)cc2)c1 10.1016/j.bmcl.2008.06.057
44578423 189768 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL515161 189768 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
24785431 189919 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
CHEMBL516355 189919 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 520 6 0 5 6.2 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccccc2F)c1 10.1016/j.bmcl.2008.06.057
52949124 876 None 4 Human Binding pIC50 = 8.7 8.7 -2 2
Displacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 876 None 4 Human Binding pIC50 = 8.7 8.7 -2 2
Displacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 876 None 4 Human Binding pIC50 = 8.7 8.7 -2 2
Displacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 876 None 4 Human Binding pIC50 = 8.7 8.7 -2 2
Displacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
44365788 121758 None 0 Human Binding pIC50 = 8 8.0 - 0
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL 643 7 1 7 5.5 COC(=O)n1c(C(=O)NC2C(=O)N(CC(=O)N(c3ccccc3)C(C)C)c3ccccc3N(c3ccccc3)C2=O)cc2ccccc21 10.1021/jm9601664
CHEMBL358778 121758 None 0 Human Binding pIC50 = 8 8.0 - 0
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL 643 7 1 7 5.5 COC(=O)n1c(C(=O)NC2C(=O)N(CC(=O)N(c3ccccc3)C(C)C)c3ccccc3N(c3ccccc3)C2=O)cc2ccccc21 10.1021/jm9601664
46235271 73674 None 2 Human Binding pIC50 = 8 8.0 2 2
Displacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73674 None 2 Human Binding pIC50 = 8 8.0 2 2
Displacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL1172252 211043 None 0 Human Binding pIC50 = 8 8.0 -12 4
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
10046672 116146 None 3 Rat Binding pIC50 = 8 8.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 402 3 2 3 3.8 CN1C(=O)C(NC(=O)Nc2cccc(F)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL335666 116146 None 3 Rat Binding pIC50 = 8 8.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 402 3 2 3 3.8 CN1C(=O)C(NC(=O)Nc2cccc(F)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10364786 104927 None 0 Rat Binding pIC50 = 8 8.0 - 0
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 419 2 2 4 3.7 Cc1cccc(NC(=O)NC2N=C(N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
CHEMBL311061 104927 None 0 Rat Binding pIC50 = 8 8.0 - 0
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 419 2 2 4 3.7 Cc1cccc(NC(=O)NC2N=C(N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
44329383 108347 None 0 Guinea pig Binding pIC50 = 8 8.0 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 526 6 3 3 5.5 Cc1cccc(NC(=O)N[C@H]2C[C@H](c3ccccc3)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL319749 108347 None 0 Guinea pig Binding pIC50 = 8 8.0 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 526 6 3 3 5.5 Cc1cccc(NC(=O)N[C@H]2C[C@H](c3ccccc3)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
44336539 5146 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]CCK from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5146 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]CCK from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
10364786 104927 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 419 2 2 4 3.7 Cc1cccc(NC(=O)NC2N=C(N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL311061 104927 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 419 2 2 4 3.7 Cc1cccc(NC(=O)NC2N=C(N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
10627173 209000 None 0 Human Binding pIC50 = 8.0 8.0 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 586 8 1 4 6.5 COc1ccc(N(C(=O)CN2C(=O)C(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL88602 209000 None 0 Human Binding pIC50 = 8.0 8.0 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 586 8 1 4 6.5 COc1ccc(N(C(=O)CN2C(=O)C(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
44346576 10773 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 399 4 2 3 3.8 O=C(/C=C\c1ccccc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00047a021
CHEMBL117158 10773 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 399 4 2 3 3.8 O=C(/C=C\c1ccccc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00047a021
14208272 67760 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 455 3 1 3 4.4 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL1907841 67760 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 455 3 1 3 4.4 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
10627173 209000 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 586 8 1 4 6.5 COc1ccc(N(C(=O)CN2C(=O)C(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
CHEMBL88602 209000 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 586 8 1 4 6.5 COc1ccc(N(C(=O)CN2C(=O)C(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
14208230 103264 None 0 Rat Binding pIC50 = 7 7.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 446 3 3 3 4.5 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Cl)ccc2[nH]1 10.1021/jm00047a021
CHEMBL308414 103264 None 0 Rat Binding pIC50 = 7 7.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 446 3 3 3 4.5 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Cl)ccc2[nH]1 10.1021/jm00047a021
14208274 169395 None 0 Rat Binding pIC50 = 7 7.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 443 3 1 3 4.7 CN1C(=O)C(NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL441445 169395 None 0 Rat Binding pIC50 = 7 7.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 443 3 1 3 4.7 CN1C(=O)C(NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
15689736 106656 None 0 Guinea pig Binding pIC50 = 7 7.0 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 862 20 9 8 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC/N=C(\S)Nc1ccccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142702 106656 None 0 Guinea pig Binding pIC50 = 7 7.0 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 862 20 9 8 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC/N=C(\S)Nc1ccccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
11801335 119599 None 0 Human Binding pIC50 = 7 7.0 - 0
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 579 7 2 4 5.5 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(F)cc1 10.1021/jm950626d
CHEMBL345786 119599 None 0 Human Binding pIC50 = 7 7.0 - 0
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 579 7 2 4 5.5 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(F)cc1 10.1021/jm950626d
44306868 102138 None 0 Human Binding pIC50 = 7 7.0 - 1
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 836 18 9 7 3.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1ccc(NC(=O)Nc2ccccc2Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL302150 102138 None 0 Human Binding pIC50 = 7 7.0 - 1
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 836 18 9 7 3.7 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1ccc(NC(=O)Nc2ccccc2Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
44306888 102385 None 0 Human Binding pIC50 = 7 7.0 - 1
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1cccc(NC(=O)Nc2ccccc2C)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL303635 102385 None 0 Human Binding pIC50 = 7 7.0 - 1
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 816 18 9 7 3.4 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(Cc1cccc(NC(=O)Nc2ccccc2C)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
13953709 162432 None 0 Rat Binding pIC50 = 7 7.0 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 409 4 1 6 4.0 O=C(NC1N=C(c2ccccc2)c2ccccc2-n2cnnc21)OCc1ccccc1 10.1021/jm00396a028
CHEMBL416483 162432 None 0 Rat Binding pIC50 = 7 7.0 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 409 4 1 6 4.0 O=C(NC1N=C(c2ccccc2)c2ccccc2-n2cnnc21)OCc1ccccc1 10.1021/jm00396a028
14208274 169395 None 0 Rat Binding pIC50 = 7 7.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 443 3 1 3 4.7 CN1C(=O)C(NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL441445 169395 None 0 Rat Binding pIC50 = 7 7.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 443 3 1 3 4.7 CN1C(=O)C(NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
9988264 109779 None 0 Guinea pig Binding pIC50 = 7 7.0 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 888 22 9 8 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL322955 109779 None 0 Guinea pig Binding pIC50 = 7 7.0 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 888 22 9 8 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
10886229 78624 None 0 Rat Binding pIC50 = 7 7.0 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1cccc(N2C(=O)C[C@@H]3[C@@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)c1 10.1021/jm010813d
CHEMBL2112234 78624 None 0 Rat Binding pIC50 = 7 7.0 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1cccc(N2C(=O)C[C@@H]3[C@@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)c1 10.1021/jm010813d
44382057 120399 None 0 Rat Binding pIC50 = 6 6.0 - 0
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 420 4 2 3 3.1 Cc1cccc(NC(=O)N[C@H]2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL352939 120399 None 0 Rat Binding pIC50 = 6 6.0 - 0
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 420 4 2 3 3.1 Cc1cccc(NC(=O)N[C@H]2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
44301015 201517 None 0 Guinea pig Binding pIC50 = 6 6.0 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 609 7 5 7 3.7 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)Nc3nn[nH]n3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL58658 201517 None 0 Guinea pig Binding pIC50 = 6 6.0 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 609 7 5 7 3.7 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)Nc3nn[nH]n3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
10001488 165021 None 0 Rat Binding pIC50 = 6 6.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 4 3 3 3.6 O=C(Cc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00047a021
CHEMBL422411 165021 None 0 Rat Binding pIC50 = 6 6.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 408 4 3 3 3.6 O=C(Cc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00047a021
CHEMBL2112688 211707 None 0 Guinea pig Binding pIC50 = 6 6.0 - 0
Binding affinity towards Cholecystokinin type A receptor was determined in guinea pig pancreatic membranes using [125I]-BH-CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor was determined in guinea pig pancreatic membranes using [125I]-BH-CCK-8 as radioligand
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@@H](NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O)[C@H](C)c1c[nH]c2ccccc12 10.1021/jm960078j
52949124 876 None 4 Human Binding pIC50 = 6 6.0 -2 2
Displacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 876 None 4 Human Binding pIC50 = 6 6.0 -2 2
Displacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 876 None 4 Human Binding pIC50 = 6 6.0 -2 2
Displacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 876 None 4 Human Binding pIC50 = 6 6.0 -2 2
Displacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
46235271 73674 None 2 Human Binding pIC50 = 6 6.0 2 2
Displacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73674 None 2 Human Binding pIC50 = 6 6.0 2 2
Displacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
46235271 73674 None 2 Human Binding pIC50 = 6 6.0 2 2
Displacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73674 None 2 Human Binding pIC50 = 6 6.0 2 2
Displacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
10649606 49630 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]CCK from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49630 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of [125I]CCK from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
10001488 165021 None 0 Rat Binding pIC50 = 6 6.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 4 3 3 3.6 O=C(Cc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL422411 165021 None 0 Rat Binding pIC50 = 6 6.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 4 3 3 3.6 O=C(Cc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
14208202 207100 None 0 Rat Binding pIC50 = 6 6.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 443 4 2 4 4.5 O=C(Cc1cccc2sccc12)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL73563 207100 None 0 Rat Binding pIC50 = 6 6.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 443 4 2 4 4.5 O=C(Cc1cccc2sccc12)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
44362701 121198 None 0 Rat Binding pIC50 = 6 6.0 - 0
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
CHEMBL357576 121198 None 0 Rat Binding pIC50 = 6 6.0 - 0
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 580 9 4 5 3.9 O=C(O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
44370446 119665 None 0 Guinea pig Binding pIC50 = 6 6.0 - 0
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 467 15 2 4 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCC)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL346361 119665 None 0 Guinea pig Binding pIC50 = 6 6.0 - 0
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 467 15 2 4 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCC)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
20152922 119039 None 0 Rat Binding pIC50 = 6 6.0 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 440 5 2 3 4.3 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)Cc1c[nH]c2ccccc12 10.1021/jm00163a069
CHEMBL342415 119039 None 0 Rat Binding pIC50 = 6 6.0 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 440 5 2 3 4.3 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)Cc1c[nH]c2ccccc12 10.1021/jm00163a069
10414170 170721 None 0 Rat Binding pIC50 = 6 6.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00078a018
CHEMBL445095 170721 None 0 Rat Binding pIC50 = 6 6.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00078a018
15200522 120532 None 0 Rat Binding pIC50 = 6 6.0 - 0
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 422 4 2 3 3.7 CN1C(=O)C(NC(=O)Cc2c[nH]c3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL354126 120532 None 0 Rat Binding pIC50 = 6 6.0 - 0
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 422 4 2 3 3.7 CN1C(=O)C(NC(=O)Cc2c[nH]c3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL37983 214726 None 0 Rat Binding pIC50 = 5 5.0 - 0
Binding affinity towards Cholecystokinin type A receptor by displacement of [125I]BH-CCK-8 from rat pancreatic aciniBinding affinity towards Cholecystokinin type A receptor by displacement of [125I]BH-CCK-8 from rat pancreatic acini
ChEMBL None None None CS[C@H]1CCN(C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(C)=O)[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00001a019
656755 67731 None 24 Guinea pig Binding pIC50 = 5 5.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 397 3 1 2 4.7 CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
CHEMBL1907717 67731 None 24 Guinea pig Binding pIC50 = 5 5.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 397 3 1 2 4.7 CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
15167824 67740 None 0 Guinea pig Binding pIC50 = 5 5.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 379 3 1 2 4.6 CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
CHEMBL1907731 67740 None 0 Guinea pig Binding pIC50 = 5 5.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 379 3 1 2 4.6 CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
20190196 31796 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 388 4 1 4 3.3 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1cccnc1 10.1021/jm00163a069
CHEMBL140620 31796 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 388 4 1 4 3.3 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1cccnc1 10.1021/jm00163a069
15167799 119251 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 379 4 2 4 3.9 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)c1ccsc1 10.1021/jm00163a069
CHEMBL343158 119251 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 379 4 2 4 3.9 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)c1ccsc1 10.1021/jm00163a069
44381820 120688 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 689 18 7 8 2.8 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](C#N)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
CHEMBL354631 120688 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 689 18 7 8 2.8 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](C#N)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
44381821 120689 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 689 18 7 8 2.8 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@H](C#N)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
CHEMBL354632 120689 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 689 18 7 8 2.8 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@H](C#N)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
44348835 16828 None 0 Rat Binding pIC50 = 5 5.0 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 938 25 11 11 0.2 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL124719 16828 None 0 Rat Binding pIC50 = 5 5.0 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 938 25 11 11 0.2 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
14208262 206977 None 0 Rat Binding pIC50 = 4 4.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 431 4 2 3 4.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(-c2ccccc2)cc1 10.1021/jm00047a021
CHEMBL72670 206977 None 0 Rat Binding pIC50 = 4 4.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 431 4 2 3 4.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(-c2ccccc2)cc1 10.1021/jm00047a021
7216755 59559 None 3 Rat Binding pIC50 = 4 4.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 265 1 1 3 1.8 CN1C(=O)[C@@H](N)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL171651 59559 None 3 Rat Binding pIC50 = 4 4.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 265 1 1 3 1.8 CN1C(=O)[C@@H](N)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
44311988 103086 None 0 Rat Binding pIC50 = 4 4.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 412 5 2 4 2.5 CN1C(=O)[C@H](NC(=O)[C@H](N)Cc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL307034 103086 None 0 Rat Binding pIC50 = 4 4.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 412 5 2 4 2.5 CN1C(=O)[C@H](NC(=O)[C@H](N)Cc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
14208206 163564 None 0 Rat Binding pIC50 = 4 4.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 4 3 4 2.8 O=C1Nc2ccccc2C(c2ccccc2F)=NC1NC(=O)C(O)c1ccccc1 10.1021/jm00120a002
CHEMBL419997 163564 None 0 Rat Binding pIC50 = 4 4.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 4 3 4 2.8 O=C1Nc2ccccc2C(c2ccccc2F)=NC1NC(=O)C(O)c1ccccc1 10.1021/jm00120a002
14208262 206977 None 0 Rat Binding pIC50 = 4 4.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 431 4 2 3 4.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(-c2ccccc2)cc1 10.1021/jm00120a002
CHEMBL72670 206977 None 0 Rat Binding pIC50 = 4 4.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 431 4 2 3 4.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(-c2ccccc2)cc1 10.1021/jm00120a002
2794055 67729 None 1 Guinea pig Binding pIC50 = 4 4.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 360 3 1 2 4.7 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=N[C@@H]1Cc1ccccc1 10.1021/jm00390a019
CHEMBL1907712 67729 None 1 Guinea pig Binding pIC50 = 4 4.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 360 3 1 2 4.7 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=N[C@@H]1Cc1ccccc1 10.1021/jm00390a019
15167780 67734 None 0 Guinea pig Binding pIC50 = 4 4.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 415 3 2 3 4.6 O=C1Nc2ccccc2C1C[C@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=O 10.1021/jm00390a019
CHEMBL1907723 67734 None 0 Guinea pig Binding pIC50 = 4 4.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 415 3 2 3 4.6 O=C1Nc2ccccc2C1C[C@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=O 10.1021/jm00390a019
15614736 167404 None 0 Guinea pig Binding pIC50 = 4 4.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 410 3 1 2 5.9 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=NC1Cc1cccc2ccccc12 10.1021/jm00390a019
CHEMBL429391 167404 None 0 Guinea pig Binding pIC50 = 4 4.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 410 3 1 2 5.9 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=NC1Cc1cccc2ccccc12 10.1021/jm00390a019
44359880 32337 None 0 Rat Binding pIC50 = 4 4.0 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 428 7 2 5 2.4 CC(=O)NCSCC(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C 10.1021/jm00163a069
CHEMBL141048 32337 None 0 Rat Binding pIC50 = 4 4.0 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 428 7 2 5 2.4 CC(=O)NCSCC(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C 10.1021/jm00163a069
44359841 116693 None 0 Rat Binding pIC50 = 4 4.0 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 498 7 1 4 6.5 CCN(CC)c1ccc(NCC2CN=C(c3ccccc3F)c3ccccc3N2C)cc1C(F)(F)F 10.1021/jm00163a069
CHEMBL336881 116693 None 0 Rat Binding pIC50 = 4 4.0 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 498 7 1 4 6.5 CCN(CC)c1ccc(NCC2CN=C(c3ccccc3F)c3ccccc3N2C)cc1C(F)(F)F 10.1021/jm00163a069
7216755 59559 None 3 Rat Binding pIC50 = 4 4.0 - 0
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 265 1 1 3 1.8 CN1C(=O)[C@@H](N)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL171651 59559 None 3 Rat Binding pIC50 = 4 4.0 - 0
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 265 1 1 3 1.8 CN1C(=O)[C@@H](N)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
71450869 84418 None 0 Rat Binding pIC50 = 6 6.0 - 0
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 650 12 5 6 4.3 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCS(=O)(=O)O)c1ccccc1 10.1021/jm00092a007
CHEMBL2112338 84418 None 0 Rat Binding pIC50 = 6 6.0 - 0
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 650 12 5 6 4.3 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCS(=O)(=O)O)c1ccccc1 10.1021/jm00092a007
CHEMBL2219559 84418 None 0 Rat Binding pIC50 = 6 6.0 - 0
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 650 12 5 6 4.3 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCS(=O)(=O)O)c1ccccc1 10.1021/jm00092a007
10325770 130763 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 573 8 4 5 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)[C@@](Cc3ccccc3)(C(N)=O)C[C@H]12 10.1016/0960-894X(96)00160-6
CHEMBL368380 130763 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 573 8 4 5 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)[C@@](Cc3ccccc3)(C(N)=O)C[C@H]12 10.1016/0960-894X(96)00160-6
44349203 117118 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NN1CCC2(CCCCC2)C1 10.1021/jm00079a003
CHEMBL339134 117118 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NN1CCC2(CCCCC2)C1 10.1021/jm00079a003
45482109 200506 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)N[C@@H](Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL574062 200506 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)N[C@@H](Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
44408411 161404 None 0 Human Binding pIC50 = 6.0 6.0 -2089 4
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1242 31 11 15 4.4 CCCC[C@@H](C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O)N(C(=O)Nc1ccccc1Cl)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
CHEMBL412331 161404 None 0 Human Binding pIC50 = 6.0 6.0 -2089 4
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1242 31 11 15 4.4 CCCC[C@@H](C(=O)N[C@@H](Cc1cn(C(C)=O)c2ccccc12)C(=O)O)N(C(=O)Nc1ccccc1Cl)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)N(C)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
44408484 137595 None 0 Human Binding pIC50 = 5.0 5.0 -19498 4
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1033 30 13 12 1.4 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL375412 137595 None 0 Human Binding pIC50 = 5.0 5.0 -19498 4
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1033 30 13 12 1.4 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm050851n
44418924 156974 None 0 Human Binding pIC50 = 5.0 5.0 -19952 4
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@H](NC(=O)[C@H](N)Cc1cc2ccccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL407198 156974 None 0 Human Binding pIC50 = 5.0 5.0 -19952 4
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@H](NC(=O)[C@H](N)Cc1cc2ccccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL333299 213850 None 0 Guinea pig Binding pIC50 = 5.0 5.0 - 0
Compound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pigCompound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pig
ChEMBL None None None C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00105a068
10340882 26037 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3cccnc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL135498 26037 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3cccnc3N(C)C2=O)c1 10.1021/jm00078a018
46235271 73674 None 2 Human Binding pIC50 = 7.0 7.0 2 2
Displacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73674 None 2 Human Binding pIC50 = 7.0 7.0 2 2
Displacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R N2.61T mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
10256428 119752 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 529 9 4 4 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL347278 119752 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 529 9 4 4 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
108187 926 None 30 Human Binding pIC50 = 6.0 6.0 - 5
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00017a022
873 926 None 30 Human Binding pIC50 = 6.0 6.0 - 5
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00017a022
CHEMBL2062154 926 None 30 Human Binding pIC50 = 6.0 6.0 - 5
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00017a022
CHEMBL287735 926 None 30 Human Binding pIC50 = 6.0 6.0 - 5
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 614 12 5 5 4.9 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1021/jm00017a022
CHEMBL205965 211628 None 0 Human Binding pIC50 = 5.0 5.0 - 3
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
44369590 119613 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 458 7 3 6 3.5 Cc1cccc(NCNC2N=C(c3cc[nH]n3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL345880 119613 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 458 7 3 6 3.5 Cc1cccc(NCNC2N=C(c3cc[nH]n3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
51353551 18141 None 18 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL1269257 18141 None 18 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
44353183 116840 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 743-1710Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 743-1710
ChEMBL 555 8 3 4 5.2 O=C(OC1C2CC3CC(C2)CC1C3)N1CCCC1(Cc1c[nH]c2ccccc12)C(=O)NC(CO)Cc1ccccc1 10.1016/S0960-894X(00)80156-0
CHEMBL337692 116840 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 743-1710Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 743-1710
ChEMBL 555 8 3 4 5.2 O=C(OC1C2CC3CC(C2)CC1C3)N1CCCC1(Cc1c[nH]c2ccccc12)C(=O)NC(CO)Cc1ccccc1 10.1016/S0960-894X(00)80156-0
71456173 78515 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CC[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL2111826 78515 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CC[C@H](NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
10342469 201056 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)N[C@H](Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL578650 201056 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)N[C@H](Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
44283496 100228 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 527 9 2 3 6.1 CC(=O)N(CCc1ccccc1)CC(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL288037 100228 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 527 9 2 3 6.1 CC(=O)N(CCc1ccccc1)CC(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
10668688 209991 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 400 4 4 6 3.4 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(N)c2)c1 10.1021/jm970373j
CHEMBL9465 209991 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 400 4 4 6 3.4 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(N)c2)c1 10.1021/jm970373j
53465782 69431 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 455 9 4 3 4.6 O=C(Nc1ccccc1C(=O)NC(CCCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933101 69431 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 455 9 4 3 4.6 O=C(Nc1ccccc1C(=O)NC(CCCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
10793168 167996 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 570 7 1 3 6.9 CC(C)N(C(=O)CN1C(=O)C(C)(Cc2c[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
CHEMBL431212 167996 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 570 7 1 3 6.9 CC(C)N(C(=O)CN1C(=O)C(C)(Cc2c[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
9960964 86027 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A); value ranges from 1000 to 1100The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A); value ranges from 1000 to 1100
ChEMBL 638 12 5 7 4.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCc1nnn[nH]1)c1ccccc1 10.1016/S0960-894X(00)80652-6
CHEMBL2304152 86027 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A); value ranges from 1000 to 1100The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A); value ranges from 1000 to 1100
ChEMBL 638 12 5 7 4.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCc1nnn[nH]1)c1ccccc1 10.1016/S0960-894X(00)80652-6
10325426 107657 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 3 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1016/S0960-894X(01)80769-1
CHEMBL318963 107657 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 3 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1016/S0960-894X(01)80769-1
10165354 22153 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 770-2020Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 770-2020
ChEMBL 529 9 4 4 4.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC(CO)Cc1ccccc1 10.1016/S0960-894X(00)80156-0
CHEMBL132233 22153 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 770-2020Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 770-2020
ChEMBL 529 9 4 4 4.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC(CO)Cc1ccccc1 10.1016/S0960-894X(00)80156-0
44283132 120865 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 485 9 3 3 5.9 CC(CNCCc1ccccc1)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL35555 120865 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 485 9 3 3 5.9 CC(CNCCc1ccccc1)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
10624013 33546 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 464 6 3 4 4.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CCCC1 10.1021/jm970065l
CHEMBL142063 33546 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 464 6 3 4 4.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CCCC1 10.1021/jm970065l
14208240 102400 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 418 4 2 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc([N+](=O)[O-])cc1 10.1021/jm00047a021
CHEMBL303724 102400 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 418 4 2 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc([N+](=O)[O-])cc1 10.1021/jm00047a021
14208213 207066 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 362 3 3 3 2.7 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc[nH]1 10.1021/jm00047a021
CHEMBL73272 207066 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 362 3 3 3 2.7 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc[nH]1 10.1021/jm00047a021
9896825 103032 None 0 Mouse Binding pIC50 = 6.0 6.0 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 742 14 6 10 2.9 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL30656 103032 None 0 Mouse Binding pIC50 = 6.0 6.0 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 742 14 6 10 2.9 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
14208314 102978 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 495 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccccc2I)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL306166 102978 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 495 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccccc2I)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
14208199 103127 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 394 3 3 3 3.7 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1c[nH]c2ccccc12 10.1021/jm00047a021
CHEMBL307370 103127 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 394 3 3 3 3.7 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1c[nH]c2ccccc12 10.1021/jm00047a021
CHEMBL218327 211853 None 0 Human Binding pIC50 = 6.0 6.0 -2630 4
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
14208272 67760 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 455 3 1 3 4.4 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907841 67760 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 455 3 1 3 4.4 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208208 169582 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 399 4 2 3 3.8 O=C(/C=C/c1ccccc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL443009 169582 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 399 4 2 3 3.8 O=C(/C=C/c1ccccc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
10260206 167572 None 0 Guinea pig Binding pIC50 = 8.0 8.0 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 918 21 8 8 4.9 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL429932 167572 None 0 Guinea pig Binding pIC50 = 8.0 8.0 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 918 21 8 8 4.9 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL415706 215659 None 0 Guinea pig Binding pIC50 = 8.0 8.0 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CN(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44341426 110395 None 0 Guinea pig Binding pIC50 = 8.0 8.0 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 514 13 3 4 6.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccc(O)cc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL324022 110395 None 0 Guinea pig Binding pIC50 = 8.0 8.0 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 514 13 3 4 6.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccc(O)cc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
9934162 27739 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 464 5 3 4 4.3 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(Cc3c[nH]cn3)C2=O)c1 10.1021/jm00078a018
CHEMBL137043 27739 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 464 5 3 4 4.3 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(Cc3c[nH]cn3)C2=O)c1 10.1021/jm00078a018
10649606 49630 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49630 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
10432393 100400 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 422 3 3 3 4.4 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00121a004
CHEMBL289533 100400 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 422 3 3 3 4.4 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00121a004
14208242 156514 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 493 6 1 5 4.0 CCOC(=O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
CHEMBL40668 156514 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 493 6 1 5 4.0 CCOC(=O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
14208240 102400 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 418 4 2 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc([N+](=O)[O-])cc1 10.1021/jm00120a002
CHEMBL303724 102400 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 418 4 2 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc([N+](=O)[O-])cc1 10.1021/jm00120a002
14208242 156514 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 493 6 1 5 4.0 CCOC(=O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL40668 156514 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 493 6 1 5 4.0 CCOC(=O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208213 207066 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 362 3 3 3 2.7 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc[nH]1 10.1021/jm00120a002
CHEMBL73272 207066 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 362 3 3 3 2.7 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc[nH]1 10.1021/jm00120a002
5279169 26207 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 404 3 3 3 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00078a018
CHEMBL135715 26207 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 404 3 3 3 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00078a018
10070678 120819 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL355092 120819 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14208242 156514 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 493 6 1 5 4.0 CCOC(=O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00078a018
CHEMBL40668 156514 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 493 6 1 5 4.0 CCOC(=O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00078a018
90663976 106855 None 0 Guinea pig Binding pIC50 = 7.0 7.0 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 21 9 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccccc1O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144538 106855 None 0 Guinea pig Binding pIC50 = 7.0 7.0 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 21 9 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccccc1O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14991577 163339 None 0 Guinea pig Binding pIC50 = 7.0 7.0 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 870 20 9 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cc2cc(Cl)ccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL418500 163339 None 0 Guinea pig Binding pIC50 = 7.0 7.0 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 870 20 9 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cc2cc(Cl)ccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44381960 120343 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 474 3 3 4 4.6 CN1C(=O)[C@@H](NC(=O)Nc2cc3c4ccccc4nc-3c[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL352573 120343 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 474 3 3 4 4.6 CN1C(=O)[C@@H](NC(=O)Nc2cc3c4ccccc4nc-3c[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
44301037 100911 None 0 Guinea pig Binding pIC50 = 6.0 6.0 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 633 8 4 6 4.0 CCS(=O)(=O)NC(=O)c1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccc(C)cc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00327-P
CHEMBL293490 100911 None 0 Guinea pig Binding pIC50 = 6.0 6.0 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 633 8 4 6 4.0 CCS(=O)(=O)NC(=O)c1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccc(C)cc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00327-P
10319892 59108 None 1 Rat Binding pIC50 = 6.0 6.0 - 0
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
CHEMBL169661 59108 None 1 Rat Binding pIC50 = 6.0 6.0 - 0
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
14208199 103127 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 394 3 3 3 3.7 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1c[nH]c2ccccc12 10.1021/jm00120a002
CHEMBL307370 103127 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 394 3 3 3 3.7 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1c[nH]c2ccccc12 10.1021/jm00120a002
10182876 206580 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 457 7 1 3 5.1 CCCCCc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)cc1 10.1021/jm00120a002
CHEMBL70361 206580 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 457 7 1 3 5.1 CCCCCc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)cc1 10.1021/jm00120a002
14208280 67709 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 335 3 1 3 2.6 CC(C)C(=O)N[C@H]1N=C(c2ccccc2)c2ccccc2N(C)C1=O 10.1021/jm00120a002
CHEMBL1907665 67709 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 335 3 1 3 2.6 CC(C)C(=O)N[C@H]1N=C(c2ccccc2)c2ccccc2N(C)C1=O 10.1021/jm00120a002
14208315 67758 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 495 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccccc2I)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL1907839 67758 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 495 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccccc2I)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
14802528 118529 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 642 14 5 5 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CNC(=O)CCCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
CHEMBL341281 118529 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 642 14 5 5 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@H](CNC(=O)CCCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
15104622 10035 None 0 Guinea pig Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 476 13 3 2 6.4 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1cccc(C)c1 10.1021/jm00116a002
CHEMBL115093 10035 None 0 Guinea pig Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 476 13 3 2 6.4 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1cccc(C)c1 10.1021/jm00116a002
14720389 165178 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 373 10 3 3 2.8 CCCN(CCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
CHEMBL422701 165178 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 373 10 3 3 2.8 CCCN(CCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
10075297 115570 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 518 6 3 5 4.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)Nc3ccncc3)C2=O)c1 10.1021/jm00078a018
CHEMBL335239 115570 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 518 6 3 5 4.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)Nc3ccncc3)C2=O)c1 10.1021/jm00078a018
14991564 106859 None 0 Guinea pig Binding pIC50 = 6.0 6.0 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 827 21 9 9 2.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144541 106859 None 0 Guinea pig Binding pIC50 = 6.0 6.0 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 827 21 9 9 2.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44334338 108969 None 0 Guinea pig Binding pIC50 = 6.0 6.0 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 547 9 2 5 4.2 Cc1cccc(NC(=O)N[C@H](CS(=O)(=O)Cc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL321107 108969 None 0 Guinea pig Binding pIC50 = 6.0 6.0 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 547 9 2 5 4.2 Cc1cccc(NC(=O)N[C@H](CS(=O)(=O)Cc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
10319892 59108 None 1 Rat Binding pIC50 = 6.0 6.0 - 0
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL169661 59108 None 1 Rat Binding pIC50 = 6.0 6.0 - 0
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
14519983 120040 None 0 Guinea pig Binding pIC50 = 5.0 5.0 - 0
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ncccc2c1 10.1021/jm00124a003
CHEMBL349857 120040 None 0 Guinea pig Binding pIC50 = 5.0 5.0 - 0
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ncccc2c1 10.1021/jm00124a003
14519979 9532 None 0 Guinea pig Binding pIC50 = 5.0 5.0 - 0
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cccc2ccccc12 10.1021/jm00124a003
CHEMBL112215 9532 None 0 Guinea pig Binding pIC50 = 5.0 5.0 - 0
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in cortical cells.
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cccc2ccccc12 10.1021/jm00124a003
44349070 164586 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 421 7 3 4 3.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL421438 164586 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 421 7 3 4 3.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL103485 210916 None 0 Guinea pig Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
14208251 77856 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@H](NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL2092870 77856 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@H](NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
15167804 67732 None 0 Guinea pig Binding pIC50 = 5.0 5.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 455 6 2 3 4.6 O=C(O)CCN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
CHEMBL1907719 67732 None 0 Guinea pig Binding pIC50 = 5.0 5.0 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 455 6 2 3 4.6 O=C(O)CCN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
45482485 200467 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 486 8 3 6 3.8 Cn1c(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)cc2cc([N+](=O)[O-])ccc21 10.1016/j.bmc.2009.05.067
CHEMBL573793 200467 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 486 8 3 6 3.8 Cn1c(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)cc2cc([N+](=O)[O-])ccc21 10.1016/j.bmc.2009.05.067
21842317 121745 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 482 5 2 4 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL358646 121745 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 482 5 2 4 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
21842317 121745 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Compound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreas at dose of 0.03 umol/kgCompound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreas at dose of 0.03 umol/kg
ChEMBL 482 5 2 4 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00556-9
CHEMBL358646 121745 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Compound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreas at dose of 0.03 umol/kgCompound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreas at dose of 0.03 umol/kg
ChEMBL 482 5 2 4 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00556-9
10322988 10150 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 482 5 2 4 4.9 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
CHEMBL115772 10150 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 482 5 2 4 4.9 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
44349434 117079 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 396 11 3 3 3.6 CCC(C)(CC)CCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
CHEMBL338929 117079 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 396 11 3 3 3.6 CCC(C)(CC)CCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
5311201 209854 None 26 Mouse Binding pIC50 = 5.0 5.0 - 9
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
5311201 209854 None 26 Mouse Binding pIC50 = 5.0 5.0 - 9
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00249-1
CHEMBL9387 209854 None 26 Mouse Binding pIC50 = 5.0 5.0 - 9
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL9387 209854 None 26 Mouse Binding pIC50 = 5.0 5.0 - 9
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00249-1
10722103 111537 None 0 Human Binding pIC50 = 7.0 7.0 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 588 8 1 6 5.3 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ncccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL327656 111537 None 0 Human Binding pIC50 = 7.0 7.0 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 588 8 1 6 5.3 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ncccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
73349872 89235 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1016/0960-894X(96)00160-6
CHEMBL2367718 89235 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1016/0960-894X(96)00160-6
CHEMBL2367719 89235 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1016/0960-894X(96)00160-6
11442153 200654 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 444 7 3 4 4.6 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2s1 10.1016/j.bmc.2009.05.067
CHEMBL575161 200654 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 444 7 3 4 4.6 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2s1 10.1016/j.bmc.2009.05.067
10789434 209094 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 444 6 3 8 3.1 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccnc2)c1 10.1021/jm970373j
CHEMBL8921 209094 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 444 6 3 8 3.1 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccnc2)c1 10.1021/jm970373j
73349872 89235 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1021/jm0498755
CHEMBL2367718 89235 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1021/jm0498755
CHEMBL2367719 89235 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1021/jm0498755
10839478 110720 None 1 Rat Binding pIC50 = 7.0 7.0 - 0
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 512 6 2 6 4.1 CN(C)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
CHEMBL325863 110720 None 1 Rat Binding pIC50 = 7.0 7.0 - 0
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 512 6 2 6 4.1 CN(C)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
15104595 10094 None 0 Guinea pig Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL115456 10094 None 0 Guinea pig Binding pIC50 = 6.0 6.0 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
138106885 167007 None 49 Human Binding pIC50 = 4.9 4.9 -1 4
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
36314 167007 None 49 Human Binding pIC50 = 4.9 4.9 -1 4
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
CHEMBL428647 167007 None 49 Human Binding pIC50 = 4.9 4.9 -1 4
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
ChEMBL 853 10 4 14 3.7 CC(=O)O[C@H]1C(=O)[C@]2(C)[C@@H](O)C[C@H]3OC[C@@]3(OC(C)=O)[C@H]2[C@H](OC(=O)c2ccccc2)[C@]2(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)c3ccccc3)c3ccccc3)C(C)=C1C2(C)C nan
44592082 179249 None 0 Guinea pig Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 411 8 4 4 3.4 CSCC[C@@H](NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL472079 179249 None 0 Guinea pig Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 411 8 4 4 3.4 CSCC[C@@H](NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
10413579 117147 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 498 5 3 3 5.0 Cc1ccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)NC(C)(C)C)C2=O)cc1 10.1021/jm00048a015
CHEMBL339260 117147 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 498 5 3 3 5.0 Cc1ccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)NC(C)(C)C)C2=O)cc1 10.1021/jm00048a015
44283152 99908 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 501 10 4 4 4.8 O=C(NC(CNC(CO)Cc1ccccc1)Cc1c[nH]c2ccccc12)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL285762 99908 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 501 10 4 4 4.8 O=C(NC(CNC(CO)Cc1ccccc1)Cc1c[nH]c2ccccc12)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
44591978 184015 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 533 10 4 4 5.4 O=C(Nc1ccccc1C(=O)NC(Cc1ccc(OCc2ccccc2)cc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL481265 184015 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 533 10 4 4 5.4 O=C(Nc1ccccc1C(=O)NC(Cc1ccc(OCc2ccccc2)cc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
19766227 33211 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 469 6 3 4 3.6 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(N)Cc1c[nH]c2ccccc12 10.1021/jm00163a069
CHEMBL141786 33211 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 469 6 3 4 3.6 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(N)Cc1c[nH]c2ccccc12 10.1021/jm00163a069
132190 120401 None 12 Rat Binding pIC50 = 4.9 4.9 - 0
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 435 3 2 2 4.9 O=C1NN(C(=O)Nc2ccc(Br)cc2)C(c2ccccc2)C1c1ccccc1 10.1016/S0960-894X(00)80684-8
CHEMBL352949 120401 None 12 Rat Binding pIC50 = 4.9 4.9 - 0
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 435 3 2 2 4.9 O=C1NN(C(=O)Nc2ccc(Br)cc2)C(c2ccccc2)C1c1ccccc1 10.1016/S0960-894X(00)80684-8
10373378 49678 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 854 20 8 8 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)C 10.1021/jm00031a013
CHEMBL156642 49678 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 854 20 8 8 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)C 10.1021/jm00031a013
10530757 118627 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 553 10 3 7 3.6 COC(=O)CC(CC(=O)OC)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
CHEMBL341560 118627 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 553 10 3 7 3.6 COC(=O)CC(CC(=O)OC)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
44287092 100515 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 824 21 7 7 5.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL290702 100515 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 824 21 7 7 5.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
44368382 45353 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 511 9 4 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1Cl)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL152682 45353 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 511 9 4 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1Cl)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
44286961 162161 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 824 22 8 7 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL416064 162161 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 824 22 8 7 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
10478431 9901 None 8 Guinea pig Binding pIC50 = 7.9 7.9 - 0
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cell
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00124a003
CHEMBL114325 9901 None 8 Guinea pig Binding pIC50 = 7.9 7.9 - 0
Compound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against Cholecystokinin type A receptor in pancreatic acinar cell
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00124a003
127050962 140833 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 283 3 1 2 2.6 CC(C)CN1C(=O)C=C(Cl)C1(O)c1ccc(F)cc1 10.1039/C6MD00052E
CHEMBL3818164 140833 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 283 3 1 2 2.6 CC(C)CN1C(=O)C=C(Cl)C1(O)c1ccc(F)cc1 10.1039/C6MD00052E
10478431 9901 None 8 Guinea pig Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00116a002
CHEMBL114325 9901 None 8 Guinea pig Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00116a002
10919004 78463 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 590 7 3 7 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccc([N+](=O)[O-])cc3)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL2111547 78463 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 590 7 3 7 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3ccc([N+](=O)[O-])cc3)C(=O)C[C@@H]12 10.1021/jm010813d
10074366 120662 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3349028 120662 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3545866 120662 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
10032955 168138 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)NC(=O)CCC(=O)O 10.1021/jm00017a022
CHEMBL432256 168138 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)NC(=O)CCC(=O)O 10.1021/jm00017a022
52949124 876 None 4 Rat Binding pIC50 = 7.9 7.9 - 2
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
9055 876 None 4 Rat Binding pIC50 = 7.9 7.9 - 2
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
CHEMBL1269258 876 None 4 Rat Binding pIC50 = 7.9 7.9 - 2
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
DB12694 876 None 4 Rat Binding pIC50 = 7.9 7.9 - 2
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2010.08.115
13953715 194788 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 428 3 2 5 4.6 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2-n2cnnc21 10.1021/jm00396a028
CHEMBL53234 194788 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 428 3 2 5 4.6 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2-n2cnnc21 10.1021/jm00396a028
127050298 140927 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 265 1 1 2 2.6 CC(C)(C)N1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
CHEMBL3819315 140927 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 265 1 1 2 2.6 CC(C)(C)N1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
14208233 206975 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 490 3 3 3 4.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Br)ccc2[nH]1 10.1021/jm00120a002
CHEMBL72667 206975 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 490 3 3 3 4.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Br)ccc2[nH]1 10.1021/jm00120a002
44341429 110515 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2ccccc2n1 10.1021/jm00116a002
CHEMBL324652 110515 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2ccccc2n1 10.1021/jm00116a002
14888719 77265 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1041 29 11 14 -0.1 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(-c2nn[nH]n2)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL2079547 77265 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1041 29 11 14 -0.1 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(-c2nn[nH]n2)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
44370694 48024 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 488 15 2 4 4.8 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)N1CCCC1)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
CHEMBL155017 48024 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 488 15 2 4 4.8 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)N1CCCC1)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
10459108 28417 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 513 8 2 5 3.9 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(OC)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137516 28417 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 513 8 2 5 3.9 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(OC)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
9977368 116312 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 385 3 2 4 3.0 CN1C(=O)C(NC(=O)Nc2cccnc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL335865 116312 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 385 3 2 4 3.0 CN1C(=O)C(NC(=O)Nc2cccnc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
90663992 106877 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 866 22 8 9 3.3 CN(C)c1ccc(/C=C\C(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00089a010
CHEMBL3144561 106877 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 866 22 8 9 3.3 CN(C)c1ccc(/C=C\C(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00089a010
14991536 106883 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 841 22 9 9 2.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144567 106883 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 841 22 9 9 2.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44279861 103239 None 0 Mouse Binding pIC50 = 6.9 6.9 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 726 14 6 9 3.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL30821 103239 None 0 Mouse Binding pIC50 = 6.9 6.9 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 726 14 6 9 3.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
23844129 113563 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 497 6 3 5 4.7 CNc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
CHEMBL332024 113563 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 497 6 3 5 4.7 CNc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
14208233 206975 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 490 3 3 3 4.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Br)ccc2[nH]1 10.1021/jm00047a021
CHEMBL72667 206975 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 490 3 3 3 4.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Br)ccc2[nH]1 10.1021/jm00047a021
10721792 167889 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 571 7 1 4 6.3 CC(C)N(C(=O)CN1C(=O)C(C)(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
CHEMBL430451 167889 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 571 7 1 4 6.3 CC(C)N(C(=O)CN1C(=O)C(C)(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
10392653 119105 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 544 5 2 5 3.4 CN1CCN(C(=O)CN2C(=O)C(NC(=O)Nc3ccc(Cl)cc3)N=C(c3ccccc3)c3ccccc32)CC1 10.1016/S0960-894X(00)80683-6
CHEMBL342640 119105 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 544 5 2 5 3.4 CN1CCN(C(=O)CN2C(=O)C(NC(=O)Nc3ccc(Cl)cc3)N=C(c3ccccc3)c3ccccc32)CC1 10.1016/S0960-894X(00)80683-6
10456021 209967 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 442 4 2 5 3.4 COC(=O)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm970373j
CHEMBL9449 209967 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 442 4 2 5 3.4 COC(=O)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm970373j
21842327 46057 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Compound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 468 6 2 4 4.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)C)C2=O)c1 10.1016/0960-894X(95)00556-9
CHEMBL153308 46057 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Compound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]-L-364,718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 468 6 2 4 4.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)C)C2=O)c1 10.1016/0960-894X(95)00556-9
11316391 200334 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 431 7 4 3 3.6 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2c([nH]1)CCCC2 10.1016/j.bmc.2009.05.067
CHEMBL572650 200334 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 431 7 4 3 3.6 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2c([nH]1)CCCC2 10.1016/j.bmc.2009.05.067
44382698 59490 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 742 15 5 7 5.3 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccc(OS(=O)(=O)O)cc1)NCCc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL171375 59490 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 742 15 5 7 5.3 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccc(OS(=O)(=O)O)cc1)NCCc1ccccc1 10.1016/S0960-894X(00)80687-3
44370446 119665 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 467 15 2 4 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCC)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL346361 119665 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 467 15 2 4 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCC)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
10392653 119105 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 544 5 2 5 3.4 CN1CCN(C(=O)CN2C(=O)C(NC(=O)Nc3ccc(Cl)cc3)N=C(c3ccccc3)c3ccccc32)CC1 10.1021/jm00078a018
CHEMBL342640 119105 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 544 5 2 5 3.4 CN1CCN(C(=O)CN2C(=O)C(NC(=O)Nc3ccc(Cl)cc3)N=C(c3ccccc3)c3ccccc32)CC1 10.1021/jm00078a018
10070677 161818 None 15 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL41361 161818 None 15 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10456021 209967 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 442 4 2 5 3.4 COC(=O)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL9449 209967 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 442 4 2 5 3.4 COC(=O)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL338056 214063 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
15673180 86031 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 1100 to 1500The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 1100 to 1500
ChEMBL 681 13 6 8 3.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)Nc1nn[nH]n1)c1ccccc1 10.1016/S0960-894X(00)80652-6
CHEMBL2304157 86031 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 1100 to 1500The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 1100 to 1500
ChEMBL 681 13 6 8 3.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)Nc1nn[nH]n1)c1ccccc1 10.1016/S0960-894X(00)80652-6
CHEMBL3142686 213588 None 0 Guinea pig Binding pIC50 = 4.9 4.9 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44272230 67096 None 0 Mouse Binding pIC50 = 4.9 4.9 - 0
Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranesConcentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranes
ChEMBL 442 6 3 3 2.9 C[C@H](NC(=O)C1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1)C(=O)NCCc1ccccc1 10.1016/S0960-894X(00)80644-7
CHEMBL18727 67096 None 0 Mouse Binding pIC50 = 4.9 4.9 - 0
Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranesConcentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranes
ChEMBL 442 6 3 3 2.9 C[C@H](NC(=O)C1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1)C(=O)NCCc1ccccc1 10.1016/S0960-894X(00)80644-7
14208310 67762 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 439 7 1 3 5.0 CCCCCc1ccc(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00120a002
CHEMBL1907843 67762 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 439 7 1 3 5.0 CCCCCc1ccc(C(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00120a002
10454826 99393 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against Cholecystokinin type A receptor in rat pancreas using [125 I ]- CCK-8 as radioligand.Inhibitory activity against Cholecystokinin type A receptor in rat pancreas using [125 I ]- CCK-8 as radioligand.
ChEMBL 420 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2C[C@H](N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00234-K
CHEMBL282294 99393 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibitory activity against Cholecystokinin type A receptor in rat pancreas using [125 I ]- CCK-8 as radioligand.Inhibitory activity against Cholecystokinin type A receptor in rat pancreas using [125 I ]- CCK-8 as radioligand.
ChEMBL 420 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2C[C@H](N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00234-K
10838675 209671 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 487 8 3 8 4.1 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OCC)c2)c1 10.1021/jm970373j
CHEMBL9267 209671 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 487 8 3 8 4.1 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OCC)c2)c1 10.1021/jm970373j
10279334 125124 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 513 8 2 3 5.7 CN(CCc1ccccc1)C(=O)C(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL36443 125124 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 513 8 2 3 5.7 CN(CCc1ccccc1)C(=O)C(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
10253714 25502 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 460 4 2 3 5.3 CN1C(=O)C(NC(=O)Nc2cccc(-c3ccccc3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135060 25502 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 460 4 2 3 5.3 CN1C(=O)C(NC(=O)Nc2cccc(-c3ccccc3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
15177358 99125 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 515 9 4 4 4.6 O=C(NC(Cc1c[nH]c2ccccc12)NC(=O)C(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL280502 99125 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 515 9 4 4 4.6 O=C(NC(Cc1c[nH]c2ccccc12)NC(=O)C(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
71457981 78559 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 1147 14 6 10 9.0 CC(C)(C)OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12.CC(C)(C)OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm991078x
CHEMBL2111993 78559 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 1147 14 6 10 9.0 CC(C)(C)OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12.CC(C)(C)OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm991078x
10720403 119494 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 507 6 4 4 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H]1CCCCC[C@H]1O 10.1021/jm970065l
CHEMBL344882 119494 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 507 6 4 4 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H]1CCCCC[C@H]1O 10.1021/jm970065l
13605417 210027 None 3 Guinea pig Binding pIC50 = 4.9 4.9 - 1
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00124a003
CHEMBL9485 210027 None 3 Guinea pig Binding pIC50 = 4.9 4.9 - 1
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00124a003
44359338 168769 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 489 6 3 3 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CC2CCC1C2 10.1021/jm970065l
CHEMBL436411 168769 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 489 6 3 3 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CC2CCC1C2 10.1021/jm970065l
9960432 39435 None 7 Human Binding pIC50 = 6.9 6.9 -12 2
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm9601664
CHEMBL147186 39435 None 7 Human Binding pIC50 = 6.9 6.9 -12 2
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm9601664
CHEMBL1172246 211040 None 0 Human Binding pIC50 = 6.9 6.9 1 4
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc2ccccc2)C(N)=O)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC1=O 10.1016/j.bmcl.2010.05.078
10762723 97083 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 386 4 3 6 3.2 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccnc2)c1 10.1021/jm970373j
CHEMBL266819 97083 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 386 4 3 6 3.2 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccnc2)c1 10.1021/jm970373j
44349324 16680 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.4 O=C(O)CCC(NC(=O)c1cccc(C(F)(F)F)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL124261 16680 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.4 O=C(O)CCC(NC(=O)c1cccc(C(F)(F)F)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
44274261 98922 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 782 19 8 7 4.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL279005 98922 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 782 19 8 7 4.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
44283514 170720 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 585 12 3 4 6.0 CC(Cc1c[nH]c2ccccc12)(CN(CCc1ccccc1)C(=O)CCC(=O)O)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL445094 170720 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 585 12 3 4 6.0 CC(Cc1c[nH]c2ccccc12)(CN(CCc1ccccc1)C(=O)CCC(=O)O)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
11442807 77318 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 471 9 4 4 3.2 CC(=O)N/C(=C/c1ccccc1)C(=O)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1021/jm051050n
CHEMBL208171 77318 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 471 9 4 4 3.2 CC(=O)N/C(=C/c1ccccc1)C(=O)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1021/jm051050n
45481637 200798 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 471 10 4 4 3.2 O=C(CC(=O)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)N/C=C/c1ccccc1 10.1016/j.bmc.2009.05.067
CHEMBL576347 200798 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 471 10 4 4 3.2 O=C(CC(=O)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)N/C=C/c1ccccc1 10.1016/j.bmc.2009.05.067
51353551 18141 None 18 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]BDZ1 from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R (unknown origin) expressed in CHO cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL1269257 18141 None 18 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]BDZ1 from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R (unknown origin) expressed in CHO cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2015.03.051
10649606 49630 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]CCK from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49630 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]CCK from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
10817241 107178 None 0 Human Binding pIC50 = 6.9 6.9 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 591 8 1 5 5.6 COc1ccc(N(C(=O)CN2C(=O)C(Cc3[nH]nc4c3CCCC4)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL316077 107178 None 0 Human Binding pIC50 = 6.9 6.9 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 591 8 1 5 5.6 COc1ccc(N(C(=O)CN2C(=O)C(Cc3[nH]nc4c3CCCC4)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
44381758 11734 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 565 9 2 5 3.4 CN1CCN(CCNC(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL1181391 11734 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 565 9 2 5 3.4 CN1CCN(CCNC(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL169440 11734 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 565 9 2 5 3.4 CN1CCN(CCNC(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
44458096 85083 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 388 5 2 3 2.7 O=C(N[C@@H]1C(=O)N(Cc2ccccc2)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
CHEMBL22417 85083 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 388 5 2 3 2.7 O=C(N[C@@H]1C(=O)N(Cc2ccccc2)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
10009526 110566 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Compound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranesCompound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 655 6 3 7 4.6 O=C(Nc1cccc(-c2nn[nH]n2)c1)NC1N=C(c2ccccc2F)c2cccc(Cl)c2N(CC(=O)N2CC3CCC(CC3)C2)C1=O 10.1016/s0960-894x(98)00237-6
CHEMBL32492 110566 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Compound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranesCompound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 655 6 3 7 4.6 O=C(Nc1cccc(-c2nn[nH]n2)c1)NC1N=C(c2ccccc2F)c2cccc(Cl)c2N(CC(=O)N2CC3CCC(CC3)C2)C1=O 10.1016/s0960-894x(98)00237-6
54580296 61936 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774035 61936 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc5ccccc5cn4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
10418081 110428 None 0 Guinea pig Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 840 23 9 8 2.4 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL324219 110428 None 0 Guinea pig Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 840 23 9 8 2.4 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44293998 188531 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 609 6 2 5 5.3 CC(=O)c1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
CHEMBL50215 188531 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 609 6 2 5 5.3 CC(=O)c1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
90663995 106880 None 0 Guinea pig Binding pIC50 = 7.9 7.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 919 23 9 11 2.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144564 106880 None 0 Guinea pig Binding pIC50 = 7.9 7.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 919 23 9 11 2.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
10769902 209003 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity against human Cholecystokinin type A receptor by the displacement of [125I]Bolton-Hunter CCK-8Binding affinity against human Cholecystokinin type A receptor by the displacement of [125I]Bolton-Hunter CCK-8
ChEMBL 601 8 1 5 6.3 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
CHEMBL88629 209003 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity against human Cholecystokinin type A receptor by the displacement of [125I]Bolton-Hunter CCK-8Binding affinity against human Cholecystokinin type A receptor by the displacement of [125I]Bolton-Hunter CCK-8
ChEMBL 601 8 1 5 6.3 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
10769902 209003 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 601 8 1 5 6.3 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL88629 209003 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 601 8 1 5 6.3 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
10555804 111661 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 616 9 1 5 6.3 COc1ccc(N(C(=O)CN2C(=O)C(Cc3c[nH]c4ccccc34)(OC)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL328285 111661 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 616 9 1 5 6.3 COc1ccc(N(C(=O)CN2C(=O)C(Cc3c[nH]c4ccccc34)(OC)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
11114520 115515 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 7 3 5 4.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=S)C[C@H]12 10.1021/jm010898i
CHEMBL3350849 115515 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 7 3 5 4.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=S)C[C@H]12 10.1021/jm010898i
19766167 59253 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 420 4 2 3 3.1 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL170293 59253 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 420 4 2 3 3.1 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
44381577 96689 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 840 23 10 10 2.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)N[C@H](CNN[C@@H](Cc1ccccc1)C(N)=O)CC(=O)O 10.1016/S0960-894X(00)80680-0
CHEMBL263525 96689 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 840 23 10 10 2.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)N[C@H](CNN[C@@H](Cc1ccccc1)C(N)=O)CC(=O)O 10.1016/S0960-894X(00)80680-0
44330731 210703 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 946 25 9 11 0.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CN1CC[C@H](NC(=O)CCc2ccc(OS(=O)(=O)O)cc2)C1=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL98720 210703 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 946 25 9 11 0.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CN1CC[C@H](NC(=O)CCc2ccc(OS(=O)(=O)O)cc2)C1=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
10369805 100606 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
CHEMBL291458 100606 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
10073082 25145 None 3 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 462 3 2 3 4.4 CN1C(=O)C(NC(=O)Nc2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL134750 25145 None 3 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 462 3 2 3 4.4 CN1C(=O)C(NC(=O)Nc2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44578530 188793 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 556 5 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL504024 188793 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 556 5 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
90663980 106866 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 891 21 8 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(Cl)cc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144549 106866 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 891 21 8 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(Cl)cc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44301036 201160 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 695 8 4 6 5.4 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)c3ccccc3C)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL58154 201160 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 695 8 4 6 5.4 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)c3ccccc3C)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
44300864 204376 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 681 8 4 6 5.1 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)c3ccccc3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL60754 204376 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 681 8 4 6 5.1 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)c3ccccc3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
367892 9534 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
CHEMBL112222 9534 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
44349027 16833 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 438 7 3 5 2.9 O=C(O)CCC(NC(=O)c1cnc2ccccc2c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL124732 16833 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 438 7 3 5 2.9 O=C(O)CCC(NC(=O)c1cnc2ccccc2c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
44349083 118127 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL340463 118127 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
44336486 109415 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 669 8 2 6 6.5 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C3(C(F)(F)F)N=N3)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/s0960-894x(98)00548-4
CHEMBL321915 109415 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 669 8 2 6 6.5 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C3(C(F)(F)F)N=N3)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/s0960-894x(98)00548-4
73349789 106193 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 629 12 6 6 4.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)NO)c1ccccc1 10.1021/jm00092a007
CHEMBL313499 106193 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 629 12 6 6 4.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)NO)c1ccccc1 10.1021/jm00092a007
73346724 208546 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 681 13 5 9 5.0 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)NC1N=NN=N1)c1ccccc1 10.1021/jm00092a007
CHEMBL85607 208546 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 681 13 5 9 5.0 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCC(=O)NC1N=NN=N1)c1ccccc1 10.1021/jm00092a007
44311923 206959 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 421 4 2 3 4.0 O=C(Cc1ccc(Cl)cc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL72570 206959 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Half-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-8 binding to cholecystokinin receptor from rat pancreatic tissue
ChEMBL 421 4 2 3 4.0 O=C(Cc1ccc(Cl)cc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
14802536 157423 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 628 13 5 5 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NC[C@H](NC(=O)CCCC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL2112694 157423 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 628 13 5 5 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NC[C@H](NC(=O)CCCC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL407753 157423 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor
ChEMBL 628 13 5 5 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NC[C@H](NC(=O)CCCC(=O)O)c1ccccc1 10.1021/jm00105a062
44356799 26072 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 452 3 2 3 4.7 CN1C(=O)C(NC(=O)Nc2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135538 26072 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 452 3 2 3 4.7 CN1C(=O)C(NC(=O)Nc2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10392870 29108 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 552 7 2 5 5.4 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)OCc2ccccc2)C1=O 10.1021/jm00078a018
CHEMBL138122 29108 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 552 7 2 5 5.4 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)OCc2ccccc2)C1=O 10.1021/jm00078a018
44356710 116675 None 9 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 426 4 2 4 3.9 CC(=O)c1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL336765 116675 None 9 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 426 4 2 4 3.9 CC(=O)c1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL285995 99946 None 0 Mouse Binding pIC50 = 5.9 5.9 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 741 16 6 11 4.5 CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCCNCCSCc3csc(C=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
44280225 100017 None 0 Mouse Binding pIC50 = 5.9 5.9 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 743 15 4 7 5.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL286475 100017 None 0 Mouse Binding pIC50 = 5.9 5.9 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 743 15 4 7 5.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
44334278 4702 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 515 9 2 4 5.5 Cc1cccc(NC(=O)N[C@H](CSCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL103457 4702 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 515 9 2 4 5.5 Cc1cccc(NC(=O)N[C@H](CSCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44334224 5057 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 480 7 2 5 3.3 Cc1cccc(NC(=O)N[C@H](COC(=O)N(C)C)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL105303 5057 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 480 7 2 5 3.3 Cc1cccc(NC(=O)N[C@H](COC(=O)N(C)C)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44334176 5072 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 527 9 2 5 4.7 Cc1cccc(NC(=O)N[C@H](CC(=O)OCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL105404 5072 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 527 9 2 5 4.7 Cc1cccc(NC(=O)N[C@H](CC(=O)OCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44334438 109311 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 513 9 2 4 5.2 Cc1cccc(NC(=O)N[C@@H](C(=O)N2CCC(C(=O)c3ccccc3)CC2)[C@@H](C)OCc2ccccc2)c1 10.1016/0960-894X(95)00537-3
CHEMBL321800 109311 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 513 9 2 4 5.2 Cc1cccc(NC(=O)N[C@@H](C(=O)N2CCC(C(=O)c3ccccc3)CC2)[C@@H](C)OCc2ccccc2)c1 10.1016/0960-894X(95)00537-3
44334270 163582 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 437 8 2 4 3.5 CC(=O)C1CCN(C(=O)[C@@H](COCc2ccccc2)NC(=O)Nc2cccc(C)c2)CC1 10.1016/0960-894X(95)00537-3
CHEMBL420098 163582 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 437 8 2 4 3.5 CC(=O)C1CCN(C(=O)[C@@H](COCc2ccccc2)NC(=O)Nc2cccc(C)c2)CC1 10.1016/0960-894X(95)00537-3
44366601 42440 None 7 Rat Binding pIC50 = 4.9 4.9 - 0
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 11-16 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 11-16 uM
ChEMBL 323 4 0 3 3.5 O=C1CCN(C(=O)OCc2ccccc2)CC1Cc1ccccc1 10.1016/0960-894X(94)80030-8
CHEMBL149905 42440 None 7 Rat Binding pIC50 = 4.9 4.9 - 0
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 11-16 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 11-16 uM
ChEMBL 323 4 0 3 3.5 O=C1CCN(C(=O)OCc2ccccc2)CC1Cc1ccccc1 10.1016/0960-894X(94)80030-8
44382487 165731 None 0 Mouse Binding pIC50 = 4.9 4.9 - 0
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 518 10 4 4 2.7 CC(C)C[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
CHEMBL424370 165731 None 0 Mouse Binding pIC50 = 4.9 4.9 - 0
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 518 10 4 4 2.7 CC(C)C[C@H](NC(=O)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
44349023 16361 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 384 8 3 3 3.4 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00079a003
CHEMBL122922 16361 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 384 8 3 3 3.4 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00079a003
15167808 207007 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 4.1 CN(C(=O)c1cc2ccccc2[nH]1)C1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL72894 207007 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 408 3 2 3 4.1 CN(C(=O)c1cc2ccccc2[nH]1)C1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
19766230 30732 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 499 6 1 4 4.7 COC(C(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C)(c1ccccc1)C(F)(F)F 10.1021/jm00163a069
CHEMBL139520 30732 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 499 6 1 4 4.7 COC(C(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C)(c1ccccc1)C(F)(F)F 10.1021/jm00163a069
45481627 199152 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 419 7 4 4 2.7 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)C1=CC2CCCC2N1 10.1016/j.bmc.2009.05.067
CHEMBL564796 199152 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 419 7 4 4 2.7 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)C1=CC2CCCC2N1 10.1016/j.bmc.2009.05.067
51353551 18141 None 18 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
CHEMBL1269257 18141 None 18 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
16100406 83256 None 0 Human Binding pIC50 = 6.9 6.9 -33 4
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1132 28 13 13 1.7 CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL218600 83256 None 0 Human Binding pIC50 = 6.9 6.9 -33 4
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1132 28 13 13 1.7 CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
10531224 168104 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 575 7 2 4 5.7 CC(C)N(C(=O)CN1C(=O)C(C)(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
CHEMBL432015 168104 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 575 7 2 4 5.7 CC(C)N(C(=O)CN1C(=O)C(C)(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
10531224 168104 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assayDisplacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assay
ChEMBL 575 7 2 4 5.7 CC(C)N(C(=O)CN1C(=O)C(C)(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/acs.jmedchem.0c00829
CHEMBL432015 168104 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assayDisplacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assay
ChEMBL 575 7 2 4 5.7 CC(C)N(C(=O)CN1C(=O)C(C)(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/acs.jmedchem.0c00829
11775012 200568 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 439 7 3 4 3.9 O=C(NC(Cc1ccccc1)C(=O)O)c1ccccc1NC(=O)c1nccc2ccccc12 10.1016/j.bmc.2009.05.067
CHEMBL574530 200568 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 439 7 3 4 3.9 O=C(NC(Cc1ccccc1)C(=O)O)c1ccccc1NC(=O)c1nccc2ccccc12 10.1016/j.bmc.2009.05.067
44287088 100265 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 838 22 7 7 5.6 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL288373 100265 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 838 22 7 7 5.6 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
10649606 49630 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]BDZ2 from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49630 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]BDZ2 from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
44396785 67199 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 530 7 2 5 4.6 C[C@H]1C(=O)N(Cc2ccccc2)C(=O)N2CCC[C@@H](N[C@@H](Cc3c[nH]c4ccccc34)C(=O)OC(C)(C)C)C12 10.1021/jm0498755
CHEMBL187732 67199 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 530 7 2 5 4.6 C[C@H]1C(=O)N(Cc2ccccc2)C(=O)N2CCC[C@@H](N[C@@H](Cc3c[nH]c4ccccc34)C(=O)OC(C)(C)C)C12 10.1021/jm0498755
44303669 168392 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 573 10 4 5 3.9 O=C(O)CCC(=O)N[C@@H](CNC(=O)C1(NC(=O)OC2C3CC4CC(C3)CC2C4)Cc2ccccc2C1)c1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL434020 168392 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 573 10 4 5 3.9 O=C(O)CCC(=O)N[C@@H](CNC(=O)C1(NC(=O)OC2C3CC4CC(C3)CC2C4)Cc2ccccc2C1)c1ccccc1 10.1016/S0960-894X(97)00356-9
44349069 118123 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL340413 118123 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
65987 99631 None 12 Rat Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 440 6 2 3 4.1 O=C(O)CC[C@@H](NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL283820 99631 None 12 Rat Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 440 6 2 3 4.1 O=C(O)CC[C@@H](NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
65987 99631 None 12 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreas
ChEMBL 440 6 2 3 4.1 O=C(O)CC[C@@H](NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1021/jm950372w
CHEMBL283820 99631 None 12 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in rat pancreas
ChEMBL 440 6 2 3 4.1 O=C(O)CC[C@@H](NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1021/jm950372w
15281185 49468 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 484 5 2 6 3.7 Cc1cccc(NC(=O)NC2N=C(c3cnccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL156484 49468 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 484 5 2 6 3.7 Cc1cccc(NC(=O)NC2N=C(c3cnccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
10555164 112817 None 0 Human Binding pIC50 = 6.9 6.9 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 575 7 1 4 6.0 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(F)cc1 10.1021/jm970265x
CHEMBL330521 112817 None 0 Human Binding pIC50 = 6.9 6.9 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 575 7 1 4 6.0 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(F)cc1 10.1021/jm970265x
44359376 119423 None 1 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 493 6 4 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1O 10.1021/jm970065l
CHEMBL344380 119423 None 1 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 493 6 4 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1O 10.1021/jm970065l
10647112 163518 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 447 3 3 4 4.1 Cc1cccc(NC(=O)N[C@@H]2N=C([C@H]3CCC(C)(C)CCN3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
CHEMBL419663 163518 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 447 3 3 4 4.1 Cc1cccc(NC(=O)N[C@@H]2N=C([C@H]3CCC(C)(C)CCN3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
44211353 59070 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 552 9 2 5 3.5 O=C(CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1)NCCN1CCOCC1 10.1016/S0960-894X(00)80681-2
CHEMBL169453 59070 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 552 9 2 5 3.5 O=C(CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1)NCCN1CCOCC1 10.1016/S0960-894X(00)80681-2
10484212 99933 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Compound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranesCompound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 635 6 3 7 4.3 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/s0960-894x(98)00237-6
CHEMBL285921 99933 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Compound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranesCompound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 635 6 3 7 4.3 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/s0960-894x(98)00237-6
CHEMBL355608 214198 None 0 Mouse Binding pIC50 = 7.9 7.9 - 0
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N1CC(=O)N[C@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
CHEMBL3142924 213597 None 0 Guinea pig Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL None None None COc1ccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm960509y
10484212 99933 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 635 6 3 7 4.3 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
CHEMBL285921 99933 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 635 6 3 7 4.3 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
9823890 26942 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 428 4 3 4 3.3 CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL136412 26942 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 428 4 3 4 3.3 CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44578251 182538 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 486 5 0 5 5.5 COc1cccc(-n2cc(C(=O)N3CCN(c4cccc(Cl)c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL478604 182538 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 486 5 0 5 5.5 COc1cccc(-n2cc(C(=O)N3CCN(c4cccc(Cl)c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
14991568 100765 None 0 Guinea pig Binding pIC50 = 7.9 7.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 847 20 8 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL292519 100765 None 0 Guinea pig Binding pIC50 = 7.9 7.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 847 20 8 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14991575 100838 None 0 Guinea pig Binding pIC50 = 7.9 7.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 852 20 10 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cc2cc(O)ccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL293026 100838 None 0 Guinea pig Binding pIC50 = 7.9 7.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 852 20 10 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cc2cc(O)ccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL434674 216121 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CN[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
44336539 5146 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]BDZ2 from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5146 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]BDZ2 from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
10675328 111568 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 617 9 1 6 5.7 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ccccc34)(OC)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL327815 111568 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 617 9 1 6 5.7 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ccccc34)(OC)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
46235271 73674 None 2 Rat Binding pIC50 = 7.8 7.8 - 2
Displacement of [125I]-CCK-2 from rat CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from rat CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
CHEMBL2017835 73674 None 2 Rat Binding pIC50 = 7.8 7.8 - 2
Displacement of [125I]-CCK-2 from rat CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from rat CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
44210424 119282 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 423 4 2 4 3.8 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)OC(C)(C)C)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL34335 119282 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 423 4 2 4 3.8 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)OC(C)(C)C)C2=O)c1 10.1016/S0960-894X(00)80683-6
9868877 210125 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 460 8 2 4 3.8 COc1cccc(N(CC(=O)N(C)c2ccccc2)C(=O)CNC(=O)Nc2cccc(C)c2)c1 10.1021/jm970373j
CHEMBL9534 210125 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 460 8 2 4 3.8 COc1cccc(N(CC(=O)N(C)c2ccccc2)C(=O)CNC(=O)Nc2cccc(C)c2)c1 10.1021/jm970373j
10440992 161390 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 990 28 9 11 1.8 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL412238 161390 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 990 28 9 11 1.8 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
10440992 161390 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 990 28 9 11 1.8 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL412238 161390 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 990 28 9 11 1.8 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
44382735 120827 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 646 13 4 4 6.1 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL355275 120827 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 646 13 4 4 6.1 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL2079550 211652 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(C(F)(F)C(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
19910130 119855 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 439 14 3 3 4.9 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL348168 119855 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 439 14 3 3 4.9 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
44578562 181640 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc3c2OCCO3)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL476519 181640 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 4 0 6 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc3c2OCCO3)cc1 10.1016/j.bmcl.2008.06.057
14991540 106858 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 855 23 8 9 3.2 COc1ccc(CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00089a010
CHEMBL3144540 106858 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 855 23 8 9 3.2 COc1ccc(CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 10.1021/jm00089a010
90663993 106878 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 901 21 8 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(Br)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144562 106878 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 901 21 8 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(Br)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
9828961 168089 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 548 6 4 4 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)O)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
CHEMBL431919 168089 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 548 6 4 4 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)O)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
44382709 59235 None 0 Mouse Binding pIC50 = 5.9 5.9 - 0
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 504 10 4 4 2.9 CCCC[C@H](NC(=O)c1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
CHEMBL170207 59235 None 0 Mouse Binding pIC50 = 5.9 5.9 - 0
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 504 10 4 4 2.9 CCCC[C@H](NC(=O)c1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
44368454 121279 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Concentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissueConcentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 549 4 3 7 3.5 CC(C)C[C@]1(C)N[C@H]2N(C1=O)c1ccccc1[C@@]2(O)C[C@@H]1NC(=O)c2ccccc2-n2c1nc1ccccc1c2=O 10.1021/jm020424z
CHEMBL357749 121279 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Concentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissueConcentration required for 50% inhibition of Cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 549 4 3 7 3.5 CC(C)C[C@]1(C)N[C@H]2N(C1=O)c1ccccc1[C@@]2(O)C[C@@H]1NC(=O)c2ccccc2-n2c1nc1ccccc1c2=O 10.1021/jm020424z
14208264 102164 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 411 3 2 3 4.5 CC(C)(C)c1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL302282 102164 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 411 3 2 3 4.5 CC(C)(C)c1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
44382560 120381 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 660 14 4 4 6.5 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCCc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL352817 120381 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 660 14 4 4 6.5 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCCc1ccccc1 10.1016/S0960-894X(00)80687-3
44362745 33064 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 680 12 3 6 5.7 C[Si](C)(C)CCOC(=O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
CHEMBL141655 33064 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 680 12 3 6 5.7 C[Si](C)(C)CCOC(=O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
10030203 25898 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 540 6 2 6 2.8 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CCN(C)CC3)C2=O)c1 10.1021/jm00078a018
CHEMBL135371 25898 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 540 6 2 6 2.8 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CCN(C)CC3)C2=O)c1 10.1021/jm00078a018
44357031 28706 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 585 8 2 9 3.1 COC(=O)[C@H]1CCCN1OC(=O)CN1C(=O)C(NC(=O)Nc2cccc(OC)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137779 28706 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 585 8 2 9 3.1 COC(=O)[C@H]1CCCN1OC(=O)CN1C(=O)C(NC(=O)Nc2cccc(OC)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
3035433 99522 None 8 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of cholecystokinin A receptorInhibition of cholecystokinin A receptor
ChEMBL 535 4 3 7 3.1 CC(C)C[C@@H]1N[C@H]2N(C1=O)c1ccccc1[C@@]2(O)C[C@@H]1NC(=O)c2ccccc2-n2c1nc1ccccc1c2=O 10.1021/np9800102
CHEMBL283117 99522 None 8 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of cholecystokinin A receptorInhibition of cholecystokinin A receptor
ChEMBL 535 4 3 7 3.1 CC(C)C[C@@H]1N[C@H]2N(C1=O)c1ccccc1[C@@]2(O)C[C@@H]1NC(=O)c2ccccc2-n2c1nc1ccccc1c2=O 10.1021/np9800102
44334177 109823 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 508 7 3 3 5.3 Cc1cccc(NC(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL323127 109823 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 508 7 3 3 5.3 Cc1cccc(NC(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
9983680 163418 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 506 7 2 5 3.8 Cc1cccc(NC(=O)N[C@H](COC(=O)N2CCCC2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL418987 163418 None 0 Guinea pig Binding pIC50 = 5.9 5.9 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 506 7 2 5 3.8 Cc1cccc(NC(=O)N[C@H](COC(=O)N2CCCC2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44349185 16538 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 421 7 3 4 3.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCCC2)C1 10.1021/jm00079a003
CHEMBL123720 16538 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 421 7 3 4 3.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCCC2)C1 10.1021/jm00079a003
13953698 101964 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 464 5 1 5 5.1 CN(C)Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=N[C@@H]2Cc1c[nH]c2ccccc12 10.1021/jm00396a028
CHEMBL300926 101964 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 464 5 1 5 5.1 CN(C)Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=N[C@@H]2Cc1c[nH]c2ccccc12 10.1021/jm00396a028
15614752 118813 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 549 6 3 5 4.6 O=C1Nc2ccccc2C(c2ccccc2F)=NC1CNCC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00163a069
CHEMBL341815 118813 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 549 6 3 5 4.6 O=C1Nc2ccccc2C(c2ccccc2F)=NC1CNCC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00163a069
44286977 100192 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 782 18 7 7 4.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL287712 100192 None 0 Guinea pig Binding pIC50 = 6.9 6.9 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 782 18 7 7 4.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
14208264 102164 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 411 3 2 3 4.5 CC(C)(C)c1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
CHEMBL302282 102164 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 411 3 2 3 4.5 CC(C)(C)c1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
10625001 29186 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 493 7 4 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1(CO)CCCC1 10.1021/jm970065l
CHEMBL138190 29186 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 493 7 4 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1(CO)CCCC1 10.1021/jm970065l
73349872 89235 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1016/S0960-894X(97)00107-8
CHEMBL2367718 89235 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1016/S0960-894X(97)00107-8
CHEMBL2367719 89235 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 616 12 5 5 5.2 CC1(C)[C@H]2CC[C@@]1(C)[C@H](OC(=O)N[C@](C)(Cc1c[nH]c3ccccc13)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1)C2 10.1016/S0960-894X(97)00107-8
44376113 120025 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreatic tissue using [125]BH CCK-A as radioligandThe compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreatic tissue using [125]BH CCK-A as radioligand
ChEMBL 494 6 3 6 3.9 CC(C)CN1C(=O)[C@@H](NC(=O)Nc2ccc(-c3nn[nH]n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
CHEMBL349730 120025 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreatic tissue using [125]BH CCK-A as radioligandThe compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreatic tissue using [125]BH CCK-A as radioligand
ChEMBL 494 6 3 6 3.9 CC(C)CN1C(=O)[C@@H](NC(=O)Nc2ccc(-c3nn[nH]n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
10369803 16589 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 7 3 3 5.7 CCC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21 10.1021/jm00048a015
CHEMBL123951 16589 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 7 3 3 5.7 CCC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21 10.1021/jm00048a015
10481751 113154 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 518 5 3 3 5.3 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21 10.1021/jm00048a015
CHEMBL331315 113154 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 518 5 3 3 5.3 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21 10.1021/jm00048a015
11741648 26367 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccncc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL135909 26367 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccncc3N(C)C2=O)c1 10.1021/jm00078a018
3452843 119589 None 6 Rat Binding pIC50 = 6.8 6.8 - 10
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL345686 119589 None 6 Rat Binding pIC50 = 6.8 6.8 - 10
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 10.1016/0960-894X(95)00557-A
122130 4115 None 31 Rat Binding pIC50 = 6.8 6.8 - 1
Compound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 10.1016/0960-894X(95)00556-9
888 4115 None 31 Rat Binding pIC50 = 6.8 6.8 - 1
Compound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 10.1016/0960-894X(95)00556-9
CHEMBL115121 4115 None 31 Rat Binding pIC50 = 6.8 6.8 - 1
Compound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreasCompound was evaluated for its ability to displace [3H]L-364718 from Cholecystokinin type A receptor from rat pancreas
ChEMBL 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 10.1016/0960-894X(95)00556-9
122130 4115 None 31 Rat Binding pIC50 = 6.8 6.8 - 1
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 10.1021/jm960669+
888 4115 None 31 Rat Binding pIC50 = 6.8 6.8 - 1
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 10.1021/jm960669+
CHEMBL115121 4115 None 31 Rat Binding pIC50 = 6.8 6.8 - 1
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 10.1021/jm960669+
44283150 165340 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 529 9 3 4 4.7 CN(C(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(CO)Cc1ccccc1 10.1021/jm00086a017
CHEMBL422941 165340 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 529 9 3 4 4.7 CN(C(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(CO)Cc1ccccc1 10.1021/jm00086a017
15104604 109520 None 0 Guinea pig Binding pIC50 = 4.8 4.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 448 13 2 3 5.1 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccnc1 10.1021/jm00116a002
CHEMBL322031 109520 None 0 Guinea pig Binding pIC50 = 4.8 4.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 448 13 2 3 5.1 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccnc1 10.1021/jm00116a002
44359338 168769 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 489 6 3 3 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CC2CCC1C2 10.1021/jm970065l
CHEMBL436411 168769 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 489 6 3 3 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CC2CCC1C2 10.1021/jm970065l
11755707 57539 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 500 8 2 7 4.7 CCOC(=O)c1cccc(NC(=O)NCc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1016/S0960-894X(97)00108-X
CHEMBL166168 57539 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 500 8 2 7 4.7 CCOC(=O)c1cccc(NC(=O)NCc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1016/S0960-894X(97)00108-X
10345812 18657 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 498 5 3 3 5.0 Cc1ccccc1NC(=O)N[C@@H]1C[C@H](c2ccccc2)c2ccccc2N(CC(=O)NC(C)(C)C)C1=O 10.1021/jm00048a015
CHEMBL127687 18657 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 498 5 3 3 5.0 Cc1ccccc1NC(=O)N[C@@H]1C[C@H](c2ccccc2)c2ccccc2N(CC(=O)NC(C)(C)C)C1=O 10.1021/jm00048a015
42636923 178936 None 0 Guinea pig Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 393 7 4 3 3.6 CC(C)C[C@@H](NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL469341 178936 None 0 Guinea pig Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 393 7 4 3 3.6 CC(C)C[C@@H](NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
15689733 106670 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 870 21 9 10 3.0 COC(=O)c1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm960509y
CHEMBL3142905 106670 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 870 21 9 10 3.0 COC(=O)c1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm960509y
52943046 18145 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 557 8 0 6 5.8 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Oc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269262 18145 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 557 8 0 6 5.8 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Oc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
14208305 67765 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2cccc(I)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907846 67765 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 513 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2cccc(I)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208248 207099 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 441 3 2 3 4.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00120a002
CHEMBL73561 207099 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 441 3 2 3 4.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00120a002
10897104 78626 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 573 7 3 5 4.7 C[C@H](c1ccccc1)N1C(=O)C[C@H]2[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1021/jm010813d
CHEMBL2112237 78626 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 573 7 3 5 4.7 C[C@H](c1ccccc1)N1C(=O)C[C@H]2[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1021/jm010813d
14991582 203706 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 871 21 7 8 4.3 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1ccc(Cl)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL60385 203706 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 871 21 7 8 4.3 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1ccc(Cl)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14208248 207099 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 441 3 2 3 4.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00047a021
CHEMBL73561 207099 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 441 3 2 3 4.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00047a021
52949124 876 None 4 Human Binding pIC50 = 7.8 7.8 -2 2
Displacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 876 None 4 Human Binding pIC50 = 7.8 7.8 -2 2
Displacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 876 None 4 Human Binding pIC50 = 7.8 7.8 -2 2
Displacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 876 None 4 Human Binding pIC50 = 7.8 7.8 -2 2
Displacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
10008654 127683 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127683 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
71456294 79689 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL2115133 79689 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm010813d
136055866 56533 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 468 4 3 7 3.4 CN1C(=O)[C@H](NC(=O)Nc2ccc(-c3noc(O)n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
CHEMBL163610 56533 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 468 4 3 7 3.4 CN1C(=O)[C@H](NC(=O)Nc2ccc(-c3noc(O)n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
10509945 89418 None 0 Human Binding pIC50 = 7.8 7.8 - 2
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL2369816 89418 None 0 Human Binding pIC50 = 7.8 7.8 - 2
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 896 26 9 9 2.1 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44215880 69430 None 0 Rat Binding pIC50 = 7.8 7.8 - 2
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)NC(CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933100 69430 None 0 Rat Binding pIC50 = 7.8 7.8 - 2
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)NC(CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
10507561 121065 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL 585 7 2 4 5.4 CC(C)N(C(=O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm9601664
CHEMBL356408 121065 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptorCompound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
ChEMBL 585 7 2 4 5.4 CC(C)N(C(=O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm9601664
CHEMBL2372623 212736 None 0 Human Binding pIC50 = 7.8 7.8 -16 4
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1Cc2ccccc2CN1C(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
44310934 206862 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 575 7 3 6 4.1 COc1ccc(N2C(=O)CC3C(NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm010813d
CHEMBL71996 206862 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 575 7 3 6 4.1 COc1ccc(N2C(=O)CC3C(NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm010813d
10462874 98890 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL 766 16 6 5 7.1 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCCCNC(=O)Nc1ccccc1Cl 10.1016/s0960-894x(00)00198-0
CHEMBL278780 98890 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptorCompound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor
ChEMBL 766 16 6 5 7.1 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCCCNC(=O)Nc1ccccc1Cl 10.1016/s0960-894x(00)00198-0
15666987 210656 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 976 29 10 11 1.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL98446 210656 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 976 29 10 11 1.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](CCCC)NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
15667019 210688 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 905 26 9 10 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCCNC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL98631 210688 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 905 26 9 10 2.0 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCCNC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
14208217 206608 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 379 3 2 4 3.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccsc1 10.1021/jm00120a002
CHEMBL70550 206608 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 379 3 2 4 3.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccsc1 10.1021/jm00120a002
44381914 13008 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 522 14 1 4 4.7 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCN(C)CC1)NC(=O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80681-2
CHEMBL1189721 13008 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 522 14 1 4 4.7 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCN(C)CC1)NC(=O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80681-2
CHEMBL539320 13008 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 522 14 1 4 4.7 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCN(C)CC1)NC(=O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80681-2
73354295 106002 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 643 13 5 6 4.5 CONC(=O)CCC(=O)N[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1021/jm00092a007
CHEMBL312894 106002 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 643 13 5 6 4.5 CONC(=O)CCC(=O)N[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1021/jm00092a007
44311626 206602 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 455 4 2 4 4.8 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(SC(F)(F)F)cc1 10.1021/jm00120a002
CHEMBL70499 206602 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 455 4 2 4 4.8 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(SC(F)(F)F)cc1 10.1021/jm00120a002
15104623 10022 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 476 13 3 2 6.4 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1cccc(C)c1 10.1021/jm00116a002
CHEMBL114997 10022 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 476 13 3 2 6.4 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1cccc(C)c1 10.1021/jm00116a002
15104625 110585 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 651 16 2 6 8.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c(Sc2ccccc2[N+](=O)[O-])[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL325067 110585 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 651 16 2 6 8.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c(Sc2ccccc2[N+](=O)[O-])[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
44334225 4990 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 522 7 2 6 3.1 Cc1cccc(NC(=O)N[C@H](COC(=O)N2CCOCC2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL104958 4990 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 522 7 2 6 3.1 Cc1cccc(NC(=O)N[C@H](COC(=O)N2CCOCC2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
71452639 78482 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 542 9 2 5 4.0 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCN(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL2111654 78482 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 542 9 2 5 4.0 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCN(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
10673078 29095 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 502 6 3 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1C#N 10.1021/jm970065l
CHEMBL138112 29095 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 502 6 3 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1C#N 10.1021/jm970065l
CHEMBL406978 215091 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Compound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptorCompound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00378a012
CHEMBL2372073 212639 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@H]1CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2007.05.067
44359840 165543 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 395 4 2 5 3.5 O=C1Nc2ccccc2C(c2ccccc2F)=NC1CNc1cnc(Cl)cn1 10.1021/jm00163a069
CHEMBL423918 165543 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 395 4 2 5 3.5 O=C1Nc2ccccc2C(c2ccccc2F)=NC1CNc1cnc(Cl)cn1 10.1021/jm00163a069
44280373 99442 None 0 Mouse Binding pIC50 = 4.8 4.8 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 16 4 8 5.4 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL282646 99442 None 0 Mouse Binding pIC50 = 4.8 4.8 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 16 4 8 5.4 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
10839347 30269 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 507 7 4 4 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1(CO)CCCCC1 10.1021/jm970065l
CHEMBL139101 30269 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 507 7 4 4 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1(CO)CCCCC1 10.1021/jm970065l
45482481 200333 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)N[C@H](Cc1ccccc1)C(=O)O)c1cc2cc(F)ccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL572649 200333 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)N[C@H](Cc1ccccc1)C(=O)O)c1cc2cc(F)ccc2[nH]1 10.1016/j.bmc.2009.05.067
44336539 5146 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]CCK from CCK1R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5146 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]CCK from CCK1R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
10156187 103161 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 373 3 2 3 3.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1 10.1021/jm00120a002
CHEMBL307659 103161 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 373 3 2 3 3.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1 10.1021/jm00120a002
10156187 103161 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 373 3 2 3 3.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1 10.1021/jm00047a021
CHEMBL307659 103161 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 373 3 2 3 3.4 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1 10.1021/jm00047a021
10249484 22662 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 385 3 2 4 3.0 CN1C(=O)C(NC(=O)Nc2ccncc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL132699 22662 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 385 3 2 4 3.0 CN1C(=O)C(NC(=O)Nc2ccncc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10672231 208415 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 475 5 3 4 4.9 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
CHEMBL84433 208415 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 475 5 3 4 4.9 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
14208195 15265 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 455 4 2 4 4.8 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc(SC(F)(F)F)c1 10.1021/jm00047a021
CHEMBL121210 15265 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 455 4 2 4 4.8 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc(SC(F)(F)F)c1 10.1021/jm00047a021
10673570 30164 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 521 7 4 4 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1(C(=O)O)CCCCC1 10.1021/jm970065l
CHEMBL139001 30164 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 521 7 4 4 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1(C(=O)O)CCCCC1 10.1021/jm970065l
10719765 78392 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 487 6 4 7 3.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CNc3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm9506736
CHEMBL2110202 78392 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 487 6 4 7 3.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CNc3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm9506736
44336539 5146 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]CCK from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5146 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]CCK from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
44368562 122029 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 588 12 5 5 4.3 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CNC(=O)/C=C/C(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL359076 122029 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 588 12 5 5 4.3 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CNC(=O)/C=C/C(=O)O)Cc1ccccc1 10.1021/jm00057a005
10698109 107352 None 0 Human Binding pIC50 = 6.8 6.8 5 2
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 560 8 1 4 5.8 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
CHEMBL317181 107352 None 0 Human Binding pIC50 = 6.8 6.8 5 2
Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligandBinding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand
ChEMBL 560 8 1 4 5.8 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
10698109 107352 None 0 Human Binding pIC50 = 6.8 6.8 5 2
Displacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assayDisplacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assay
ChEMBL 560 8 1 4 5.8 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/acs.jmedchem.0c00829
CHEMBL317181 107352 None 0 Human Binding pIC50 = 6.8 6.8 5 2
Displacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assayDisplacement of [125I]Bolton-Hunter CCK8 from human Cholecystokinin A receptor expressed in CHO-K1 cells by competitive radioligand binding assay
ChEMBL 560 8 1 4 5.8 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/acs.jmedchem.0c00829
10790099 209732 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 459 7 3 7 4.3 COc1ccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)cc1 10.1021/jm970373j
CHEMBL9311 209732 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 459 7 3 7 4.3 COc1ccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)cc1 10.1021/jm970373j
44341327 163427 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 504 13 3 2 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc2cc(F)ccc2[nH]1 10.1021/jm00116a002
CHEMBL419031 163427 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 504 13 3 2 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc2cc(F)ccc2[nH]1 10.1021/jm00116a002
15637206 78932 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 428 4 3 4 3.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(C(=O)O)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
CHEMBL2112932 78932 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.The compound was tested for binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 428 4 3 4 3.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(C(=O)O)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
9866980 4658 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 423 3 2 4 4.6 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N3C[C@H](C)N=C23)c1 10.1016/0960-894X(95)00530-0
CHEMBL103119 4658 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 423 3 2 4 4.6 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N3C[C@H](C)N=C23)c1 10.1016/0960-894X(95)00530-0
10577834 116808 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 518 6 3 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CC2CCC(CC2)C1 10.1021/jm970065l
CHEMBL337529 116808 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 518 6 3 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CC2CCC(CC2)C1 10.1021/jm970065l
10768419 29116 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 525 10 5 5 3.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC(CC(=O)O)CC(=O)O 10.1021/jm970065l
CHEMBL138127 29116 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 525 10 5 5 3.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC(CC(=O)O)CC(=O)O 10.1021/jm970065l
15291593 112915 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 537 6 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N3CCCC3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
CHEMBL330933 112915 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 537 6 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N3CCCC3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
5311201 209854 None 26 Human Binding pIC50 = 6.8 6.8 -1174 9
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00001a027
CHEMBL9387 209854 None 26 Human Binding pIC50 = 6.8 6.8 -1174 9
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00001a027
14208215 103855 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc2ccccc12 10.1021/jm00047a021
CHEMBL309017 103855 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc2ccccc12 10.1021/jm00047a021
10531430 112410 None 0 Human Binding pIC50 = 5.8 5.8 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 587 8 1 5 5.9 COc1ccccc1N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)C(C)C 10.1021/jm970265x
CHEMBL329407 112410 None 0 Human Binding pIC50 = 5.8 5.8 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 587 8 1 5 5.9 COc1ccccc1N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)C(C)C 10.1021/jm970265x
10391834 38235 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL 516 11 3 4 4.5 CC(C)N(C(=O)CN(C(=O)[C@@H](CCC(=O)O)NC(=O)Nc1ccccc1)c1ccccc1)c1ccccc1 10.1016/S0960-894X(97)00062-0
CHEMBL146206 38235 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Tested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptorTested for the 50% displacement of [125I]CCK-8 from membrane preparation isolated from CHO-K1 cells stably transfected with the cDNA of human Cholecystokinin type A receptor
ChEMBL 516 11 3 4 4.5 CC(C)N(C(=O)CN(C(=O)[C@@H](CCC(=O)O)NC(=O)Nc1ccccc1)c1ccccc1)c1ccccc1 10.1016/S0960-894X(97)00062-0
45482491 200866 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cccc(F)c2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL576957 200866 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 445 7 4 3 4.0 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cccc(F)c2[nH]1 10.1016/j.bmc.2009.05.067
44283151 119231 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 531 9 4 4 5.6 O=C(NC(Cc1c[nH]c2ccccc12)/C(S)=N/C(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL34300 119231 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 531 9 4 4 5.6 O=C(NC(Cc1c[nH]c2ccccc12)/C(S)=N/C(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
15689739 106648 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 862 20 9 8 4.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142683 106648 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 862 20 9 8 4.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
15689738 106659 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 862 20 9 8 4.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142705 106659 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 862 20 9 8 4.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL98468 218417 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None Cc1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm00113a023
44286653 147674 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 794 17 7 7 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H]1CC(=O)N([C@@H](Cc2ccccc2)C(N)=O)C1 10.1021/jm00037a005
CHEMBL39310 147674 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 794 17 7 7 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H]1CC(=O)N([C@@H](Cc2ccccc2)C(N)=O)C1 10.1021/jm00037a005
CHEMBL98468 218417 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL None None None Cc1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm960509y
CHEMBL98468 218417 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm00173a006
44381479 59543 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 824 21 8 9 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)[C@@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
CHEMBL171593 59543 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 824 21 8 9 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)[C@@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
44458112 98761 None 0 Rat Binding pIC50 = 7.8 7.8 - 1
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 374 4 2 3 2.7 O=C(N[C@@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
CHEMBL277661 98761 None 0 Rat Binding pIC50 = 7.8 7.8 - 1
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 374 4 2 3 2.7 O=C(N[C@@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
CHEMBL2310857 211948 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL None None None CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N1CC(OS(=O)(=O)O)C[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
44578422 181668 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5n4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL476739 181668 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5n4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
90663974 106853 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 21 9 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144536 106853 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 21 9 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
155550911 174032 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1884 70 16 23 3.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4540877 174032 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1884 70 16 23 3.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL160753 211268 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CN[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
52949124 876 None 4 Human Binding pIC50 = 7.8 7.8 -2 2
Displacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 876 None 4 Human Binding pIC50 = 7.8 7.8 -2 2
Displacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 876 None 4 Human Binding pIC50 = 7.8 7.8 -2 2
Displacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 876 None 4 Human Binding pIC50 = 7.8 7.8 -2 2
Displacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
54586174 61935 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 514 5 0 5 6.2 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774034 61935 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 514 5 0 5 6.2 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
11801911 111578 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 613 8 1 5 6.4 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C2CCCC2)cc1 10.1021/jm970265x
CHEMBL327849 111578 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 613 8 1 5 6.4 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C2CCCC2)cc1 10.1021/jm970265x
15689728 106657 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1c(Cl)cccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142703 106657 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1c(Cl)cccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44336583 110100 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 665 9 2 5 6.6 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)c3ccccc3)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/s0960-894x(98)00548-4
CHEMBL323512 110100 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptorDisplacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor
ChEMBL 665 9 2 5 6.6 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)c3ccccc3)c2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1016/s0960-894x(98)00548-4
44293971 189141 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 611 6 3 5 4.8 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(C(=O)O)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
CHEMBL50926 189141 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 611 6 3 5 4.8 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(C(=O)O)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
9802550 119240 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 426 4 2 3 4.4 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1cc2ccccc2[nH]1 10.1021/jm00163a069
CHEMBL343066 119240 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 426 4 2 3 4.4 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1cc2ccccc2[nH]1 10.1021/jm00163a069
10047370 78848 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 413 4 3 4 3.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(CN)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2112754 78848 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 413 4 3 4 3.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(CN)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44578529 182880 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 7 0 5 6.8 CCCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL479030 182880 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 530 7 0 5 6.8 CCCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
14991544 106861 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 857 22 10 10 2.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(O)c(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144543 106861 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 857 22 10 10 2.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(O)c(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44381481 120698 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 841 22 9 9 3.9 Cc1ccccc1NC(=O)NCCCC[C@@H](CNN[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
CHEMBL354670 120698 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL 841 22 9 9 3.9 Cc1ccccc1NC(=O)NCCCC[C@@H](CNN[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
14208288 67704 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 349 2 1 3 3.0 CN1C(=O)[C@@H](NC(=O)C(C)(C)C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL1907660 67704 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 349 2 1 3 3.0 CN1C(=O)[C@@H](NC(=O)C(C)(C)C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
14208215 103855 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc2ccccc12 10.1021/jm00120a002
CHEMBL309017 103855 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc2ccccc12 10.1021/jm00120a002
10673039 58281 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 501 5 3 7 3.8 Cc1ccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)cc1N(C)c1nn[nH]n1 10.1021/jm9506736
CHEMBL168253 58281 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 501 5 3 7 3.8 Cc1ccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)cc1N(C)c1nn[nH]n1 10.1021/jm9506736
162672110 182966 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assayInhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assay
ChEMBL 848 22 9 9 2.0 CC(C)C[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00530
CHEMBL4791620 182966 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assayInhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assay
ChEMBL 848 22 9 9 2.0 CC(C)C[C@H](NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00530
132980 2240 None 13 Rat Binding pIC50 = 5.8 5.8 - 1
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1021/jm9608523
881 2240 None 13 Rat Binding pIC50 = 5.8 5.8 - 1
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1021/jm9608523
CHEMBL420783 2240 None 13 Rat Binding pIC50 = 5.8 5.8 - 1
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1021/jm9608523
44348850 17955 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 986 24 11 11 2.0 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL126008 17955 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 986 24 11 11 2.0 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
3040489 44575 None 1 Rat Binding pIC50 = 4.8 4.8 - 0
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 12-20 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 12-20 uM
ChEMBL 318 4 1 2 3.8 O=C1CCN(Cc2ccccc2)CC1Cc1c[nH]c2ccccc12 10.1016/0960-894X(94)80030-8
CHEMBL151990 44575 None 1 Rat Binding pIC50 = 4.8 4.8 - 0
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 12-20 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 12-20 uM
ChEMBL 318 4 1 2 3.8 O=C1CCN(Cc2ccccc2)CC1Cc1c[nH]c2ccccc12 10.1016/0960-894X(94)80030-8
15167783 67743 None 0 Guinea pig Binding pIC50 = 4.8 4.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 409 4 3 3 4.3 O=C(O)c1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc21 10.1021/jm00390a019
CHEMBL1907735 67743 None 0 Guinea pig Binding pIC50 = 4.8 4.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 409 4 3 3 4.3 O=C(O)c1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)C(=O)Nc2ccccc21 10.1021/jm00390a019
44370406 49901 None 0 Guinea pig Binding pIC50 = 4.8 4.8 - 0
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 529 16 2 4 6.6 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCc1ccccc1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL156814 49901 None 0 Guinea pig Binding pIC50 = 4.8 4.8 - 0
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 529 16 2 4 6.6 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCc1ccccc1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
132980 2240 None 13 Rat Binding pIC50 = 5.8 5.8 - 1
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1021/jm00032a002
881 2240 None 13 Rat Binding pIC50 = 5.8 5.8 - 1
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1021/jm00032a002
CHEMBL420783 2240 None 13 Rat Binding pIC50 = 5.8 5.8 - 1
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1021/jm00032a002
132980 2240 None 13 Rat Binding pIC50 = 5.8 5.8 - 1
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1016/0960-894X(95)00530-0
881 2240 None 13 Rat Binding pIC50 = 5.8 5.8 - 1
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1016/0960-894X(95)00530-0
CHEMBL420783 2240 None 13 Rat Binding pIC50 = 5.8 5.8 - 1
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 10.1016/0960-894X(95)00530-0
71456223 78797 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 1006 25 11 11 1.8 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C[C@@H]1CCCC[C@@H]1NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL2112635 78797 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 1006 25 11 11 1.8 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C[C@@H]1CCCC[C@@H]1NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
10530003 97056 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 520 7 2 5 5.3 CC(C)Oc1cccc(-n2c(CCNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL266598 97056 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 520 7 2 5 5.3 CC(C)Oc1cccc(-n2c(CCNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
44283031 100043 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 613 13 2 5 6.4 CCOC(=O)CCC(=O)N(CCc1ccccc1)CC(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL286664 100043 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 613 13 2 5 6.4 CCOC(=O)CCC(=O)N(CCc1ccccc1)CC(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
10530003 97056 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 520 7 2 5 5.3 CC(C)Oc1cccc(-n2c(CCNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
CHEMBL266598 97056 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 520 7 2 5 5.3 CC(C)Oc1cccc(-n2c(CCNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
136000594 61887 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 517 4 2 7 5.0 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc(O)c(O)c2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773890 61887 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 517 4 2 7 5.0 Cc1ccc(-c2nc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)ncc2-c2ccc(O)c(O)c2)cc1 10.1016/j.bmcl.2011.03.069
44379911 58890 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 442 6 2 5 4.8 Cc1cccc(NC(=O)NCc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1016/S0960-894X(97)00108-X
CHEMBL168875 58890 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasInhibition of specific binding of [125 I] Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 442 6 2 5 4.8 Cc1cccc(NC(=O)NCc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1016/S0960-894X(97)00108-X
136060576 87526 None 0 Guinea pig Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assay
ChEMBL 571 5 1 5 8.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(-c4ccccc4)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
CHEMBL233457 87526 None 0 Guinea pig Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from Guinea pig CCK1 after 30 mins by receptor binding assay
ChEMBL 571 5 1 5 8.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(-c4ccccc4)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
10071178 74521 None 3 Guinea pig Binding pIC50 = 4.8 4.8 - 2
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL202861 74521 None 3 Guinea pig Binding pIC50 = 4.8 4.8 - 2
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
54580265 61881 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccccc1-c1cnc(C(=O)N2CCN(c3cnc4ccccc4c3)CC2)nc1-c1ccc(C)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773884 61881 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccccc1-c1cnc(C(=O)N2CCN(c3cnc4ccccc4c3)CC2)nc1-c1ccc(C)cc1 10.1016/j.bmcl.2011.03.069
15104632 110603 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 520 9 3 5 4.5 CCOC(=O)[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1)c1ccccc1 10.1021/jm00116a002
CHEMBL325161 110603 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 520 9 3 5 4.5 CCOC(=O)[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1)c1ccccc1 10.1021/jm00116a002
11734332 78623 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 551 6 3 5 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(C3CCCCC3)C(=O)C[C@H]12 10.1021/jm010813d
CHEMBL2112233 78623 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 551 6 3 5 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(C3CCCCC3)C(=O)C[C@H]12 10.1021/jm010813d
10047411 28613 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 2 4 3.7 COc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00078a018
CHEMBL137684 28613 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 2 4 3.7 COc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00078a018
71459887 78513 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 1006 25 11 11 1.8 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C[C@H]1CCCC[C@@H]1NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL2111823 78513 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 1006 25 11 11 1.8 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C[C@H]1CCCC[C@@H]1NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
52949124 876 None 4 Human Binding pIC50 = 6.8 6.8 -2 2
Displacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 876 None 4 Human Binding pIC50 = 6.8 6.8 -2 2
Displacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 876 None 4 Human Binding pIC50 = 6.8 6.8 -2 2
Displacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 876 None 4 Human Binding pIC50 = 6.8 6.8 -2 2
Displacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R M3.32A mutant expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
155542545 173222 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1770 70 16 21 3.9 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4520699 173222 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1770 70 16 21 3.9 CCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44281204 99904 None 0 Mouse Binding pIC50 = 5.8 5.8 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 871 18 4 10 5.5 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL285719 99904 None 0 Mouse Binding pIC50 = 5.8 5.8 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 871 18 4 10 5.5 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
10649296 30784 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 507 6 4 4 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H]1CCCCC[C@@H]1O 10.1021/jm970065l
CHEMBL139601 30784 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 507 6 4 4 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H]1CCCCC[C@@H]1O 10.1021/jm970065l
10391769 17745 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 514 6 3 4 4.7 COc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1021/jm00048a015
CHEMBL125863 17745 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 514 6 3 4 4.7 COc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1021/jm00048a015
10601831 96557 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 511 6 3 7 5.0 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(Cl)c2Cl)c1 10.1021/jm970373j
CHEMBL262569 96557 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 511 6 3 7 5.0 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(Cl)c2Cl)c1 10.1021/jm970373j
44336539 5146 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]CCK from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5146 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]CCK from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
10047172 78846 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 410 4 2 3 4.3 C=Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL2112752 78846 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 410 4 2 3 4.3 C=Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
70689619 73664 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 592 6 1 5 6.5 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017825 73664 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 592 6 1 5 6.5 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
46235271 73674 None 2 Rat Binding pIC50 = 6.8 6.8 - 2
Displacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counterDisplacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
CHEMBL2017835 73674 None 2 Rat Binding pIC50 = 6.8 6.8 - 2
Displacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counterDisplacement of [125I]-BDZ-1 from wild-type rat CCK1R expressed in COS cells after 60 mins by scintillation counter
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1021/acs.jmedchem.5b01110
44592045 179011 None 0 Guinea pig Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 441 8 4 3 4.2 O=C(O)CC(Cc1ccccc1)NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL469979 179011 None 0 Guinea pig Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortexDisplacement of [125I]BH-CCK8 from CCK1 receptor in Hartley guinea pig cerebral cortex
ChEMBL 441 8 4 3 4.2 O=C(O)CC(Cc1ccccc1)NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
14208252 67774 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL1907854 67774 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
14208256 206987 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 433 5 2 5 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1OC 10.1021/jm00047a021
CHEMBL72727 206987 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 433 5 2 5 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1OC 10.1021/jm00047a021
10341247 120154 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 405 2 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(N3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL350853 120154 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 405 2 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(N3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
44286672 100429 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 836 18 6 7 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC[C@H]1CC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL289804 100429 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 836 18 6 7 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC[C@H]1CC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
52946666 18143 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 600 9 2 7 5.6 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269260 18143 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 600 9 2 7 5.6 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
10056643 109263 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 918 21 8 8 5.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL321653 109263 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 918 21 8 8 5.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44293810 101808 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 581 5 2 4 5.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
CHEMBL299800 101808 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 581 5 2 4 5.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
44578399 182060 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 492 5 1 6 4.7 COc1cccc(-n2cc(C(=O)N3CCN(c4nc5ccccc5[nH]4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL477996 182060 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 492 5 1 6 4.7 COc1cccc(-n2cc(C(=O)N3CCN(c4nc5ccccc5[nH]4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44382329 120690 None 1 Rat Binding pIC50 = 7.8 7.8 - 0
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 475 3 2 2 5.9 O=C1NN(C(=S)Nc2ccc(Cl)c(C(F)(F)F)c2)[C@H](c2ccccc2)[C@H]1c1ccccc1 10.1016/S0960-894X(00)80684-8
CHEMBL354633 120690 None 1 Rat Binding pIC50 = 7.8 7.8 - 0
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 475 3 2 2 5.9 O=C1NN(C(=S)Nc2ccc(Cl)c(C(F)(F)F)c2)[C@H](c2ccccc2)[C@H]1c1ccccc1 10.1016/S0960-894X(00)80684-8
10603713 111711 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 605 8 1 5 6.0 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4cccc(F)c34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL328586 111711 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 605 8 1 5 6.0 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4cccc(F)c34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
10770092 111593 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 614 8 0 5 6.9 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3cn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL327909 111593 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 614 8 0 5 6.9 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3cn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
54582287 61889 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 501 5 0 6 5.3 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773892 61889 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 501 5 0 6 5.3 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2)cc1 10.1016/j.bmcl.2011.03.069
15689725 106658 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142704 106658 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 880 20 9 8 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142689 213590 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None CC(C)(C)NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44458114 85432 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 393 4 2 4 2.2 O=C(N[C@@H]1C(=O)N(c2ccccc2F)C[C@@H]1C(=O)O)c1cnc2ccccc2c1 10.1016/S0960-894X(00)80224-3
CHEMBL22630 85432 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 393 4 2 4 2.2 O=C(N[C@@H]1C(=O)N(c2ccccc2F)C[C@@H]1C(=O)O)c1cnc2ccccc2c1 10.1016/S0960-894X(00)80224-3
3960 2345 None 18 Rat Binding pIC50 = 6.8 6.8 - 1
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1039/C6MD00052E
891 2345 None 18 Rat Binding pIC50 = 6.8 6.8 - 1
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1039/C6MD00052E
CHEMBL24938 2345 None 18 Rat Binding pIC50 = 6.8 6.8 - 1
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1039/C6MD00052E
10463229 119873 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 840 20 9 8 3.8 CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)Nc1ccccc1C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1021/jm00031a013
CHEMBL348346 119873 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
In vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [125I]Bolton-Hunter-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 840 20 9 8 3.8 CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)Nc1ccccc1C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1021/jm00031a013
14888714 77278 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1067 30 11 12 0.9 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(C(F)(F)C(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL2079602 77278 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1067 30 11 12 0.9 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(C(F)(F)C(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
44370461 119630 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 488 15 2 4 4.8 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)N1CCCC1)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
CHEMBL346070 119630 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 488 15 2 4 4.8 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)N1CCCC1)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
10075097 28652 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 511 6 2 5 3.6 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1021/jm00078a018
CHEMBL137726 28652 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 511 6 2 5 3.6 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1021/jm00078a018
19766160 58526 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 456 4 2 3 3.9 O=C(Nc1cccc2ccccc12)NC1CCc2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1016/S0960-894X(00)80683-6
CHEMBL168386 58526 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 456 4 2 3 3.9 O=C(Nc1cccc2ccccc12)NC1CCc2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1016/S0960-894X(00)80683-6
71449079 78658 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Evaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 639 11 5 7 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)Cc1cc(O)no1)c1ccccc1 10.1021/jm00092a007
CHEMBL2112334 78658 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Evaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of CCK-A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 639 11 5 7 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)Cc1cc(O)no1)c1ccccc1 10.1021/jm00092a007
73348230 208820 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 634 11 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CP(C)(=O)O)c1ccccc1 10.1021/jm00092a007
CHEMBL87470 208820 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 634 11 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CP(C)(=O)O)c1ccccc1 10.1021/jm00092a007
14208252 67774 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL1907854 67774 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@@H](NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
14208256 206987 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 433 5 2 5 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1OC 10.1021/jm00120a002
CHEMBL72727 206987 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 433 5 2 5 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1OC 10.1021/jm00120a002
15104631 112911 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 520 9 3 5 4.5 CCOC(=O)[C@@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1)c1ccccc1 10.1021/jm00116a002
CHEMBL330918 112911 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 520 9 3 5 4.5 CCOC(=O)[C@@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1)c1ccccc1 10.1021/jm00116a002
44280114 5112 None 0 Guinea pig Binding pIC50 = 5.8 5.8 1 2
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 567 7 2 4 6.1 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
CHEMBL105618 5112 None 0 Guinea pig Binding pIC50 = 5.8 5.8 1 2
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 567 7 2 4 6.1 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
14208197 207095 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 537 6 4 5 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL73535 207095 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 537 6 4 5 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
15614734 67738 None 1 Guinea pig Binding pIC50 = 4.8 4.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 411 3 0 3 4.7 CN1C(=O)[C@@H](Cc2cn(C)c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
CHEMBL1907729 67738 None 1 Guinea pig Binding pIC50 = 4.8 4.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 411 3 0 3 4.7 CN1C(=O)[C@@H](Cc2cn(C)c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
10031700 12194 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 486 7 2 4 3.7 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC[N+](C)(C)C)C2=O)c1 10.1021/jm00078a018
CHEMBL1184246 12194 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 486 7 2 4 3.7 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC[N+](C)(C)C)C2=O)c1 10.1021/jm00078a018
CHEMBL340975 12194 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 486 7 2 4 3.7 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC[N+](C)(C)C)C2=O)c1 10.1021/jm00078a018
10007047 16930 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 524 5 3 3 5.8 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](C2CCCCC2)c2ccccc21 10.1021/jm00048a015
CHEMBL125253 16930 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 524 5 3 3 5.8 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](C2CCCCC2)c2ccccc21 10.1021/jm00048a015
44381641 168744 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 723 20 7 8 3.2 CCCC[C@H](N[C@H](C#N)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
CHEMBL436253 168744 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 723 20 7 8 3.2 CCCC[C@H](N[C@H](C#N)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
10646538 97420 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 435 6 3 6 4.1 CC(C)Oc1cccc(-n2c(NNC(=O)NC3CCCCC3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL269606 97420 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 435 6 3 6 4.1 CC(C)Oc1cccc(-n2c(NNC(=O)NC3CCCCC3)nc3ccccc3c2=O)c1 10.1021/jm970373j
54586149 61891 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2cccc(C)c2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773894 61891 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2cccc(C)c2)cc1 10.1016/j.bmcl.2011.03.069
9853654 22797 None 34 Rat Binding pIC50 = 5.8 5.8 - 2
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 767 20 8 9 1.5 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00079a003
CHEMBL1328 22797 None 34 Rat Binding pIC50 = 5.8 5.8 - 2
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 767 20 8 9 1.5 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00079a003
44318235 12081 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 513 7 2 4 3.0 CCN(CC)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C(c2cccc[n+]2C)c2ccccc21 10.1021/jm9608523
CHEMBL1183721 12081 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 513 7 2 4 3.0 CCN(CC)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C(c2cccc[n+]2C)c2ccccc21 10.1021/jm9608523
CHEMBL314846 12081 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 513 7 2 4 3.0 CCN(CC)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C(c2cccc[n+]2C)c2ccccc21 10.1021/jm9608523
10369805 100606 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
CHEMBL291458 100606 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
In vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligandIn vitro binding affinity for the cholecystokinin type A receptor in guinea pig pancreas assayed using [125I]BH-CCK-8 as radioligand
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
14208266 104435 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 371 3 3 4 2.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(O)cc1 10.1021/jm00047a021
CHEMBL310250 104435 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 371 3 3 4 2.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(O)cc1 10.1021/jm00047a021
45482484 200436 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 455 9 4 3 4.2 O=C(CCc1c[nH]c2ccccc12)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1016/j.bmc.2009.05.067
CHEMBL573555 200436 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 455 9 4 3 4.2 O=C(CCc1c[nH]c2ccccc12)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1016/j.bmc.2009.05.067
9953071 201521 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL58699 201521 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
9953071 201521 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
In vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determinedIn vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determined
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
CHEMBL58699 201521 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
In vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determinedIn vitro test for inhibition of [125I]CCK binding to Cholecystokinin type A receptor from rat pancreatic tissues was determined
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
71460027 79746 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 541 9 4 4 5.3 O=C(O)C[C@H](Cc1ccccc1)NC(=O)C(=Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80273-5
CHEMBL2115544 79746 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.Compound measured for half-maximal inhibition of specific binding of [125I]-Bolton Hunter CCK-26-33 to CCK-A receptor in the rat pancreas.
ChEMBL 541 9 4 4 5.3 O=C(O)C[C@H](Cc1ccccc1)NC(=O)C(=Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80273-5
10009450 99920 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Compound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranesCompound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 649 7 3 7 4.5 CCc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/s0960-894x(98)00237-6
CHEMBL285850 99920 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Compound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranesCompound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 649 7 3 7 4.5 CCc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(-c3nn[nH]n3)c1)N=C2c1ccccc1F 10.1016/s0960-894x(98)00237-6
14208259 206615 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 545 4 1 4 5.9 O=C(NC1N=C(c2ccccc2F)c2ccccc2N(C(=O)c2ccc(Cl)cc2)C1=O)c1ccc(Cl)cc1 10.1021/jm00120a002
CHEMBL70593 206615 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 545 4 1 4 5.9 O=C(NC1N=C(c2ccccc2F)c2ccccc2N(C(=O)c2ccc(Cl)cc2)C1=O)c1ccc(Cl)cc1 10.1021/jm00120a002
10260012 109705 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 858 22 8 7 3.7 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL322391 109705 None 0 Guinea pig Binding pIC50 = 7.8 7.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 858 22 8 7 3.7 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
3960 2345 None 18 Rat Binding pIC50 = 7.8 7.8 - 1
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00164a020
891 2345 None 18 Rat Binding pIC50 = 7.8 7.8 - 1
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00164a020
CHEMBL24938 2345 None 18 Rat Binding pIC50 = 7.8 7.8 - 1
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00164a020
10074366 120662 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3349028 120662 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3545866 120662 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
44359879 33031 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 445 7 1 5 4.4 COC(=O)CC(NCC1CN=C(c2ccccc2F)c2ccccc2N1C)c1ccccc1 10.1021/jm00163a069
CHEMBL141629 33031 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 445 7 1 5 4.4 COC(=O)CC(NCC1CN=C(c2ccccc2F)c2ccccc2N1C)c1ccccc1 10.1021/jm00163a069
44458049 99151 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 363 4 3 3 2.0 O=C(N[C@@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1cc2ccccc2[nH]1 10.1016/S0960-894X(00)80224-3
CHEMBL280733 99151 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 363 4 3 3 2.0 O=C(N[C@@H]1C(=O)N(c2ccccc2)C[C@@H]1C(=O)O)c1cc2ccccc2[nH]1 10.1016/S0960-894X(00)80224-3
44372113 10272 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
In vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 1105 30 11 13 2.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)NC 10.1021/jm00031a013
CHEMBL1161390 10272 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
In vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreasIn vitro ability to inhibit [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 1105 30 11 13 2.4 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)OC(C)(C)C)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)NC 10.1021/jm00031a013
10369805 100606 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL291458 100606 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 532 5 3 3 5.6 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
15104630 9567 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 462 7 3 3 4.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1)c1ccccc1 10.1021/jm00116a002
CHEMBL112387 9567 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 462 7 3 3 4.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1)c1ccccc1 10.1021/jm00116a002
44362746 119055 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 680 12 3 6 5.7 C[Si](C)(C)CCOC(=O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
CHEMBL342520 119055 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 680 12 3 6 5.7 C[Si](C)(C)CCOC(=O)C[C@@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
10252412 25780 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 435 3 2 4 4.2 CN1C(=O)C(NC(=O)Nc2ccc3ccccc3n2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135289 25780 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 435 3 2 4 4.2 CN1C(=O)C(NC(=O)Nc2ccc3ccccc3n2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14991537 106852 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 921 24 9 11 2.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1cccc(OS(=O)(=O)O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144535 106852 None 0 Guinea pig Binding pIC50 = 6.8 6.8 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 921 24 9 11 2.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1cccc(OS(=O)(=O)O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3143668 213638 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/0960-894X(96)00160-6
CHEMBL64605 218346 None 5 Guinea pig Binding pIC50 = 5.8 5.8 -1288 3
Compound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pigCompound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pig
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00105a068
44381749 12903 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 540 14 1 4 4.9 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCN(C)CC1)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(00)80681-2
CHEMBL1188959 12903 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 540 14 1 4 4.9 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCN(C)CC1)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(00)80681-2
CHEMBL537834 12903 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 540 14 1 4 4.9 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCN(C)CC1)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(00)80681-2
CHEMBL64605 218346 None 5 Guinea pig Binding pIC50 = 5.8 5.8 -1288 3
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
CHEMBL64605 218346 None 5 Guinea pig Binding pIC50 = 5.8 5.8 -1288 3
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptorDisplacement of [125I]Bolton-Hunter-CCK-8 from guinea pig pancreas Cholecystokinin type A receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
CHEMBL64605 218346 None 5 Rat Binding pIC50 = 5.8 5.8 - 3
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050689o
14208266 104435 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 371 3 3 4 2.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(O)cc1 10.1021/jm00120a002
CHEMBL310250 104435 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 371 3 3 4 2.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(O)cc1 10.1021/jm00120a002
CHEMBL64605 218346 None 5 Guinea pig Binding pIC50 = 5.8 5.8 -1288 3
Inhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assayInhibition of [125]BH-CCK8 binding to guinea pig pancreas CCKAR by radioligand binding assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00530
9953071 201521 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
CHEMBL58699 201521 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 404 3 2 3 4.5 Cc1cccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
CHEMBL64605 218346 None 5 Guinea pig Binding pIC50 = 5.8 5.8 -1288 3
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44334258 4466 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 451 8 3 4 3.5 Cc1cccc(NC(=O)N[C@H](CCC(=O)O)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL101752 4466 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 451 8 3 4 3.5 Cc1cccc(NC(=O)N[C@H](CCC(=O)O)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44334452 4561 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 497 9 2 3 5.6 Cc1cccc(NC(=O)N[C@H](CCCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL102461 4561 None 0 Guinea pig Binding pIC50 = 5.8 5.8 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 497 9 2 3 5.6 Cc1cccc(NC(=O)N[C@H](CCCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL64605 218346 None 5 Guinea pig Binding pIC50 = 5.8 5.8 -1288 3
Tested for the inhibition of specific [3H]propionyl-CCK-8 binding to guinea pig cortical Cholecystokinin type A receptorTested for the inhibition of specific [3H]propionyl-CCK-8 binding to guinea pig cortical Cholecystokinin type A receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(97)00107-8
15673181 86030 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 900 to 1900The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 900 to 1900
ChEMBL 629 12 6 6 4.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)NO)c1ccccc1 10.1016/S0960-894X(00)80652-6
CHEMBL2304156 86030 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 900 to 1900The concentration (nM) producing half-maximal inhibition of specific binding of [1251] Bolton Hunter CCK-8 to CCK receptors in the rat pancreas (CCK-A);value ranges from 900 to 1900
ChEMBL 629 12 6 6 4.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)NO)c1ccccc1 10.1016/S0960-894X(00)80652-6
44354125 23159 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 628 13 5 5 5.2 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL133101 23159 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 628 13 5 5 5.2 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
14802539 76580 None 1 Rat Binding pIC50 = 4.8 4.8 - 1
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 614 12 5 5 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL2062144 76580 None 1 Rat Binding pIC50 = 4.8 4.8 - 1
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 614 12 5 5 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(00)80685-X
44286962 100532 None 0 Guinea pig Binding pIC50 = 5.7 5.7 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 810 21 8 7 4.9 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL290896 100532 None 0 Guinea pig Binding pIC50 = 5.7 5.7 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 810 21 8 7 4.9 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
44368521 46308 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 576 12 5 5 4.6 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00057a005
CHEMBL153557 46308 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 576 12 5 5 4.6 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00057a005
23844130 10116 None 18 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 484 5 3 6 3.6 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm960669+
CHEMBL115612 10116 None 18 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 484 5 3 6 3.6 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm960669+
45482479 200300 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 461 7 4 3 4.5 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cc(Cl)ccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL572412 200300 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 461 7 4 3 4.5 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cc(Cl)ccc2[nH]1 10.1016/j.bmc.2009.05.067
71719689 86023 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 500 8 3 4 4.8 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccn1 10.1016/S0960-894X(01)80769-1
CHEMBL2304063 86023 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 500 8 3 4 4.8 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccn1 10.1016/S0960-894X(01)80769-1
44381925 12856 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 538 11 2 4 4.5 CCN(CC)CCNC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL1188615 12856 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 538 11 2 4 4.5 CCN(CC)CCNC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL536938 12856 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Displacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic aciniDisplacement of [125I](BH)-CCK-8 to Cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 538 11 2 4 4.5 CCN(CC)CCNC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
5311347 107412 None 1 Rat Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL317675 107412 None 1 Rat Binding pIC50 = 6.7 6.7 - 0
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1016/S0960-894X(01)80769-1
5311347 33034 None 1 Rat Binding pIC50 = 6.7 6.7 - 1
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL141630 33034 None 1 Rat Binding pIC50 = 6.7 6.7 - 1
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
5311347 107412 None 1 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL317675 107412 None 1 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1021/jm00057a005
5311347 33034 None 1 Rat Binding pIC50 = 6.7 6.7 - 1
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1021/jm970065l
CHEMBL141630 33034 None 1 Rat Binding pIC50 = 6.7 6.7 - 1
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1021/jm970065l
45482097 200818 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(NC(Cc1ccccc1)C(=O)O)c1ccccc1NC(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2009.05.067
CHEMBL576584 200818 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(NC(Cc1ccccc1)C(=O)O)c1ccccc1NC(=O)c1c[nH]c2ccccc12 10.1016/j.bmc.2009.05.067
10649606 49630 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]CCK from CCK2R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
CHEMBL156605 49630 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]CCK from CCK2R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cells
ChEMBL 519 6 3 4 4.5 O=C(CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)Nc1ccccc1 10.1016/j.bmcl.2015.03.051
44349024 17138 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 402 8 3 3 3.5 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00079a003
CHEMBL125551 17138 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 402 8 3 3 3.5 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00079a003
44381851 120442 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 723 20 7 8 3.2 CCCC[C@H](N[C@H](C#N)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(=O)O 10.1016/S0960-894X(97)00107-8
CHEMBL353305 120442 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptorInhibition of specific [3H]propionyl-CCK-8 binding to rat pancreas membrane Cholecystokinin type A receptor
ChEMBL 723 20 7 8 3.2 CCCC[C@H](N[C@H](C#N)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(=O)O 10.1016/S0960-894X(97)00107-8
44283500 139350 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 516 9 3 5 4.8 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)OC(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL37903 139350 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 516 9 3 5 4.8 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)OC(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
11753772 25999 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 455 6 2 4 3.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCN(C)C)C2=O)c1 10.1021/jm00078a018
CHEMBL135447 25999 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 455 6 2 4 3.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCN(C)C)C2=O)c1 10.1021/jm00078a018
15689734 106665 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 854 21 9 9 3.5 CC(=O)c1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm00113a023
CHEMBL3142899 106665 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 854 21 9 9 3.5 CC(=O)c1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm00113a023
367892 9534 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Compound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cell
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
CHEMBL112222 9534 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Compound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cell
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
44287094 100355 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 824 20 6 7 5.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL289209 100355 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 824 20 6 7 5.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
15689734 106665 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 854 21 9 9 3.5 CC(=O)c1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm960509y
CHEMBL3142899 106665 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 854 21 9 9 3.5 CC(=O)c1cccc(NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1021/jm960509y
54584255 61937 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ncccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774036 61937 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4ccc5ncccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
14208275 67768 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 443 3 1 3 4.7 CN1C(=O)[C@@H](NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907849 67768 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 443 3 1 3 4.7 CN1C(=O)[C@@H](NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208226 77857 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 426 3 2 3 3.9 CN1C(=O)[C@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL2092871 77857 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 426 3 2 3 3.9 CN1C(=O)[C@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
10011017 108788 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 916 22 8 7 5.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL320854 108788 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 916 22 8 7 5.1 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
367892 9534 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00116a002
CHEMBL112222 9534 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00116a002
14991579 101044 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 862 21 9 8 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C/c1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL294304 101044 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 862 21 9 8 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C/c1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14208275 67768 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 443 3 1 3 4.7 CN1C(=O)[C@@H](NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL1907849 67768 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 443 3 1 3 4.7 CN1C(=O)[C@@H](NC(=O)c2ccc(C(C)(C)C)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
155531277 171734 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1821 72 18 23 2.1 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4465747 171734 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1821 72 18 23 2.1 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
52944224 18142 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 586 8 2 7 5.6 CC(C)N(C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
CHEMBL1269259 18142 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 586 8 2 7 5.6 CC(C)N(C(=O)CN1C(=O)C(Nc2cccc(C(=O)O)c2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
10478703 119976 None 1 Rat Binding pIC50 = 7.7 7.7 - 1
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 445 2 2 4 4.0 Cc1cccc(NC(=O)NC2N=C(N3CC4CCC(CC4)C3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL349291 119976 None 1 Rat Binding pIC50 = 7.7 7.7 - 1
Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.Binding activity against Cholecystokinin type A receptor from rat pancreas using [125]BH CCK-8s as radioligand.
ChEMBL 445 2 2 4 4.0 Cc1cccc(NC(=O)NC2N=C(N3CC4CCC(CC4)C3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
14208271 102950 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 455 3 1 3 4.4 CN1C(=O)C(NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL305951 102950 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 455 3 1 3 4.4 CN1C(=O)C(NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
14208214 165343 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc2ccccc2c1 10.1021/jm00047a021
CHEMBL422951 165343 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc2ccccc2c1 10.1021/jm00047a021
44306744 102721 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 782 20 9 7 2.5 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL304524 102721 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptorDisplacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor
ChEMBL 782 20 9 7 2.5 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL1172253 211044 None 0 Human Binding pIC50 = 7.7 7.7 -138 4
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in human HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2010.05.078
CHEMBL319438 213676 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00017a022
44304324 203159 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Concentration required for 50% inhibition of cholecystokinin A(CCK A)Concentration required for 50% inhibition of cholecystokinin A(CCK A)
ChEMBL 515 13 2 2 7.0 CCCCCN(CCCCC)C(=O)C(Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(97)00353-3
CHEMBL59993 203159 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Concentration required for 50% inhibition of cholecystokinin A(CCK A)Concentration required for 50% inhibition of cholecystokinin A(CCK A)
ChEMBL 515 13 2 2 7.0 CCCCCN(CCCCC)C(=O)C(Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(97)00353-3
444998 211778 None 25 Guinea pig Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
CHEMBL216166 211778 None 25 Guinea pig Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
44382563 120816 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 742 15 5 7 5.3 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCc1ccc(OS(=O)(=O)O)cc1 10.1016/S0960-894X(00)80687-3
CHEMBL355052 120816 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 742 15 5 7 5.3 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCc1ccc(OS(=O)(=O)O)cc1 10.1016/S0960-894X(00)80687-3
15104599 10017 None 0 Guinea pig Binding pIC50 = 6.7 6.7 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 515 13 2 2 7.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00116a002
CHEMBL114980 10017 None 0 Guinea pig Binding pIC50 = 6.7 6.7 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 515 13 2 2 7.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00116a002
11757086 25684 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 541 10 2 6 4.2 CCN(CC)CC(=O)OCCN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135218 25684 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 541 10 2 6 4.2 CCN(CC)CC(=O)OCCN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44578456 189705 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5cnccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL514716 189705 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 503 5 0 6 5.4 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5cnccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
44279811 96978 None 0 Mouse Binding pIC50 = 6.7 6.7 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 743 15 4 7 5.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL265987 96978 None 0 Mouse Binding pIC50 = 6.7 6.7 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 743 15 4 7 5.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44280028 99231 None 0 Mouse Binding pIC50 = 6.7 6.7 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 768 17 6 9 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL281318 99231 None 0 Mouse Binding pIC50 = 6.7 6.7 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 768 17 6 9 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44333341 107842 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 448 4 2 5 2.9 CCCN1C(=O)[C@@H](NC(=O)Nc2cccc(C)c2)N=C(N2CCN(C)CC2)c2ccccc21 10.1016/0960-894X(95)00530-0
CHEMBL319180 107842 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreasDisplacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
ChEMBL 448 4 2 5 2.9 CCCN1C(=O)[C@@H](NC(=O)Nc2cccc(C)c2)N=C(N2CCN(C)CC2)c2ccccc21 10.1016/0960-894X(95)00530-0
13809514 206561 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 412 5 2 4 2.5 CN1C(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL70259 206561 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 412 5 2 4 2.5 CN1C(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
121964 207 None 26 Human Binding pIC50 = 5.7 5.7 - 2
Inhibitory activity against cholecystokinin type A receptor from bovine striatal binding assayInhibitory activity against cholecystokinin type A receptor from bovine striatal binding assay
ChEMBL None None None None 10.1021/jm00100a033
858 207 None 26 Human Binding pIC50 = 5.7 5.7 - 2
Inhibitory activity against cholecystokinin type A receptor from bovine striatal binding assayInhibitory activity against cholecystokinin type A receptor from bovine striatal binding assay
ChEMBL None None None None 10.1021/jm00100a033
CHEMBL323521 207 None 26 Human Binding pIC50 = 5.7 5.7 - 2
Inhibitory activity against cholecystokinin type A receptor from bovine striatal binding assayInhibitory activity against cholecystokinin type A receptor from bovine striatal binding assay
ChEMBL None None None None 10.1021/jm00100a033
44334345 163949 None 0 Guinea pig Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 504 8 2 4 4.0 Cc1cccc(NC(=O)N[C@H](CCC(=O)N2CCCC2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL420658 163949 None 0 Guinea pig Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 504 8 2 4 4.0 Cc1cccc(NC(=O)N[C@H](CCC(=O)N2CCCC2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
367893 51635 None 0 Guinea pig Binding pIC50 = 4.7 4.7 - 0
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
CHEMBL158362 51635 None 0 Guinea pig Binding pIC50 = 4.7 4.7 - 0
Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.Compound was evaluated for the binding affinity against CCK A receptor in cortical cells.
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
44408526 137032 None 0 Human Binding pIC50 = 5.7 5.7 -2344 4
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1148 30 11 15 3.0 CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
CHEMBL374325 137032 None 0 Human Binding pIC50 = 5.7 5.7 -2344 4
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1148 30 11 15 3.0 CCCC[C@@H](C(=O)N[C@H](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O)N(C)C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NN[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O 10.1021/jm050851n
16100409 83266 None 0 Human Binding pIC50 = 5.7 5.7 -870 3
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
CHEMBL218651 83266 None 0 Human Binding pIC50 = 5.7 5.7 -870 3
Displacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8-SO3 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1031 27 13 12 0.2 CCCC[C@@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1cc2ccccc2[nH]1)C(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm061268p
44303251 102289 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 618 12 5 5 4.6 O=C(O)CCC(=O)N[C@@H](CNC(=O)C(Cc1c[nH]c2ccc(F)cc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL303020 102289 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 618 12 5 5 4.6 O=C(O)CCC(=O)N[C@@H](CNC(=O)C(Cc1c[nH]c2ccc(F)cc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1016/S0960-894X(97)00356-9
44349325 168651 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 465 7 3 4 3.1 O=C(O)CCC(NC(=O)c1cccc(Br)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL435587 168651 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 465 7 3 4 3.1 O=C(O)CCC(NC(=O)c1cccc(Br)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
9827037 78860 None 9 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 493 6 4 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H]1CCCC[C@@H]1O 10.1021/jm970065l
CHEMBL2112795 78860 None 9 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 493 6 4 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H]1CCCC[C@@H]1O 10.1021/jm970065l
CHEMBL379405 214725 None 0 Human Binding pIC50 = 5.7 5.7 -11 4
Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm050921q
1614 2349 None 53 Human Binding pIC50 = 6.7 6.7 - 1
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 10.1021/jm051050n
60182 2349 None 53 Human Binding pIC50 = 6.7 6.7 - 1
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 10.1021/jm051050n
892 2349 None 53 Human Binding pIC50 = 6.7 6.7 - 1
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 10.1021/jm051050n
CHEMBL206025 2349 None 53 Human Binding pIC50 = 6.7 6.7 - 1
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 10.1021/jm051050n
44368368 121141 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 481 8 3 3 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1Cl)C(=O)NCCc1ccccc1 10.1021/jm00057a005
CHEMBL357027 121141 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 481 8 3 3 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1Cl)C(=O)NCCc1ccccc1 10.1021/jm00057a005
10071178 74521 None 3 Human Binding pIC50 = 6.7 6.7 501 2
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm051050n
CHEMBL202861 74521 None 3 Human Binding pIC50 = 6.7 6.7 501 2
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor in A431 cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm051050n
136060576 87526 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assay
ChEMBL 571 5 1 5 8.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(-c4ccccc4)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
CHEMBL233457 87526 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assayDisplacement of [125I](BH)CCK8 from rat CCK1 after 30 mins by receptor binding assay
ChEMBL 571 5 1 5 8.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(-c4ccccc4)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
10071178 74521 None 3 Rat Binding pIC50 = 6.7 6.7 - 2
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL202861 74521 None 3 Rat Binding pIC50 = 6.7 6.7 - 2
Displacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-countingDisplacement of [125I]-BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acini after 120 hrs by gamma-counting
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
10071178 74521 None 3 Rat Binding pIC50 = 6.7 6.7 - 2
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL202861 74521 None 3 Rat Binding pIC50 = 6.7 6.7 - 2
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
10071178 74521 None 3 Rat Binding pIC50 = 6.7 6.7 - 2
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL202861 74521 None 3 Rat Binding pIC50 = 6.7 6.7 - 2
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
44283081 99925 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 500 9 3 3 6.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(O)CCCc1ccccc1 10.1021/jm00086a017
CHEMBL2112071 99925 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 500 9 3 3 6.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(O)CCCc1ccccc1 10.1021/jm00086a017
CHEMBL285880 99925 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 500 9 3 3 6.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(O)CCCc1ccccc1 10.1021/jm00086a017
44327456 210301 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 585 11 2 5 5.7 COC(=O)CCN(CCc1ccccc1)C(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1016/S0960-894X(01)80769-1
CHEMBL96401 210301 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 585 11 2 5 5.7 COC(=O)CCN(CCc1ccccc1)C(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1016/S0960-894X(01)80769-1
44303652 203146 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 570 8 2 3 7.2 CC(Cc1ccc2c(c1)C(C)(C)CCC2(C)C)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL59985 203146 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 570 8 2 3 7.2 CC(Cc1ccc2c(c1)C(C)(C)CCC2(C)C)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
10530400 119399 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 535 7 3 5 5.0 COC(=O)C1(NC(=O)[C@@](C)(Cc2c[nH]c3ccccc23)NC(=O)OC2C3CC4CC(C3)CC2C4)CCCCC1 10.1021/jm970065l
CHEMBL344220 119399 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 535 7 3 5 5.0 COC(=O)C1(NC(=O)[C@@](C)(Cc2c[nH]c3ccccc23)NC(=O)OC2C3CC4CC(C3)CC2C4)CCCCC1 10.1021/jm970065l
14208235 103195 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 442 4 3 4 3.9 COc1ccc2[nH]c(C(=O)NC3N=C(c4ccccc4F)c4ccccc4NC3=O)cc2c1 10.1021/jm00047a021
CHEMBL307878 103195 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 442 4 3 4 3.9 COc1ccc2[nH]c(C(=O)NC3N=C(c4ccccc4F)c4ccccc4NC3=O)cc2c1 10.1021/jm00047a021
10746778 47574 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 646 8 2 6 5.2 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(N2CCOCC2)cc1 10.1021/jm950626d
CHEMBL154615 47574 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cellsConcentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
ChEMBL 646 8 2 6 5.2 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(N2CCOCC2)cc1 10.1021/jm950626d
14208201 207039 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 436 6 3 3 4.4 O=C(CCCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00047a021
CHEMBL73110 207039 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 436 6 3 3 4.4 O=C(CCCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00047a021
52942901 18144 None 0 Rat Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269261 18144 None 0 Rat Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
54583298 61943 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 558 6 1 6 5.9 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774042 61943 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 558 6 1 6 5.9 COc1ccc(-c2cnc(C(=O)N3CCN(c4cc(C(=O)O)c5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
10079035 163956 None 0 Guinea pig Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 796 21 8 7 2.9 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL420667 163956 None 0 Guinea pig Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 796 21 8 7 2.9 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
5311201 209854 None 26 Guinea pig Binding pIC50 = 8.7 8.7 -2570 9
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00164a020
CHEMBL9387 209854 None 26 Guinea pig Binding pIC50 = 8.7 8.7 -2570 9
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00164a020
10476766 103055 None 0 Rat Binding pIC50 = 8.7 8.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 412 3 3 3 3.9 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00047a021
CHEMBL306806 103055 None 0 Rat Binding pIC50 = 8.7 8.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 412 3 3 3 3.9 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00047a021
15667016 86152 None 0 Guinea pig Binding pIC50 = 8.7 8.7 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 960 25 9 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL2310856 86152 None 0 Guinea pig Binding pIC50 = 8.7 8.7 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 960 25 9 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
10476766 103055 None 0 Rat Binding pIC50 = 8.7 8.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 412 3 3 3 3.9 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00120a002
CHEMBL306806 103055 None 0 Rat Binding pIC50 = 8.7 8.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 412 3 3 3 3.9 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00120a002
10008654 127683 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptorInhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptor
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL366344 127683 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Inhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptorInhibition of CCK binding to Cos-7 cells expressing human cholecystokinin 1 receptor
ChEMBL 595 6 3 5 5.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(c3cccc4ccccc34)C(=O)C[C@@H]12 10.1021/jm0501127
44348650 113169 None 0 Rat Binding pIC50 = 8.7 8.7 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 986 24 11 11 2.0 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL331408 113169 None 0 Rat Binding pIC50 = 8.7 8.7 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 986 24 11 11 2.0 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
10011110 161423 None 0 Guinea pig Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 948 24 8 7 5.7 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL412544 161423 None 0 Guinea pig Binding pIC50 = 8.7 8.7 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL 948 24 8 7 5.7 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44329343 112393 None 0 Guinea pig Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 556 7 3 4 5.6 COc1ccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)cc1 10.1016/S0960-894X(01)80832-5
CHEMBL329286 112393 None 0 Guinea pig Binding pIC50 = 8.7 8.7 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 556 7 3 4 5.6 COc1ccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)cc1 10.1016/S0960-894X(01)80832-5
155546692 173746 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1861 72 19 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4534236 173746 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1861 72 19 23 3.2 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.8b01558
10454890 155232 None 1 Rat Binding pIC50 = 8.6 8.6 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL40211 155232 None 1 Rat Binding pIC50 = 8.6 8.6 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
10454890 155232 None 1 Rat Binding pIC50 = 8.6 8.6 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 421 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL40211 155232 None 1 Rat Binding pIC50 = 8.6 8.6 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 421 3 1 3 4.0 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL106722 210931 None 0 Guinea pig Binding pIC50 = 8.6 8.6 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreasInhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
24784941 189827 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 516 6 0 5 6.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL515616 189827 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 516 6 0 5 6.4 CCOc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL263155 213019 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.Concentration inhibiting [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor of rat pancreatic membranes.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00100a033
54587150 61884 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773887 61884 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 515 5 0 6 5.6 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
54580266 61885 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 529 6 0 6 6.0 CCOc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773888 61885 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 529 6 0 6 6.0 CCOc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
14208241 67772 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907852 67772 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
24784940 182893 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
CHEMBL479046 182893 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 502 5 0 5 6.0 COc1cccc(-n2cc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2008.06.057
14208269 77855 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 447 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL2092869 77855 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 447 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL2079549 211651 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(CC(=O)O)cc1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
155551968 174121 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1793 69 16 20 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4542927 174121 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1793 69 16 20 4.5 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N(C)[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44348901 141915 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 1000 24 11 11 2.3 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)c1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL386376 141915 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 1000 24 11 11 2.3 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)c1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
44344743 163668 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 555 11 4 3 5.3 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)CC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1021/jm000937a
CHEMBL420320 163668 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 555 11 4 3 5.3 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)CC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccccc1 10.1021/jm000937a
904 3026 None 12 Rat Binding pIC50 = 8.6 8.6 - 1
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
9915756 3026 None 12 Rat Binding pIC50 = 8.6 8.6 - 1
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL2111204 3026 None 12 Rat Binding pIC50 = 8.6 8.6 - 1
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL356898 3026 None 12 Rat Binding pIC50 = 8.6 8.6 - 1
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
904 3026 None 12 Rat Binding pIC50 = 8.6 8.6 - 1
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/s0960-894x(98)00677-5
9915756 3026 None 12 Rat Binding pIC50 = 8.6 8.6 - 1
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/s0960-894x(98)00677-5
CHEMBL2111204 3026 None 12 Rat Binding pIC50 = 8.6 8.6 - 1
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/s0960-894x(98)00677-5
CHEMBL356898 3026 None 12 Rat Binding pIC50 = 8.6 8.6 - 1
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/s0960-894x(98)00677-5
44329486 112662 None 0 Guinea pig Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 544 6 3 3 5.7 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)C[C@H](c3ccc(F)cc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL330197 112662 None 0 Guinea pig Binding pIC50 = 8.6 8.6 - 0
Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.Inhibitory activity against cholecystokinin-A (CCK-A) receptor in pancreas of guinea pig.
ChEMBL 544 6 3 3 5.7 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)C[C@H](c3ccc(F)cc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
904 3026 None 12 Rat Binding pIC50 = 8.6 8.6 - 1
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
9915756 3026 None 12 Rat Binding pIC50 = 8.6 8.6 - 1
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
CHEMBL2111204 3026 None 12 Rat Binding pIC50 = 8.6 8.6 - 1
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
CHEMBL356898 3026 None 12 Rat Binding pIC50 = 8.6 8.6 - 1
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
44398261 124453 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
CHEMBL363916 124453 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptorInhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
ChEMBL 577 7 4 6 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(S)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm0501127
11103804 115518 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 7 3 5 4.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=S)C[C@@H]12 10.1021/jm010898i
CHEMBL3350855 115518 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 575 7 3 5 4.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=S)C[C@@H]12 10.1021/jm010898i
14208241 67772 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL1907852 67772 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
10320031 77854 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
CHEMBL2092868 77854 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 421 3 1 3 4.0 CN1C(=O)[C@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
14208269 77855 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 447 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL2092869 77855 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 447 3 1 3 4.0 CN1C(=O)[C@@H](NC(=O)c2ccc(Br)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
10973734 78465 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1ccc(N2C(=O)C[C@H]3[C@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm010813d
CHEMBL2111549 78465 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1ccc(N2C(=O)C[C@H]3[C@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm010813d
14991570 205273 None 0 Guinea pig Binding pIC50 = 8.5 8.5 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 943 22 9 11 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccc2cc(OS(=O)(=O)O)ccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL62345 205273 None 0 Guinea pig Binding pIC50 = 8.5 8.5 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 943 22 9 11 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccc2cc(OS(=O)(=O)O)ccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44382008 59067 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80684-8
CHEMBL169438 59067 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 403 3 1 3 3.9 CN1C(=O)[C@H](NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80684-8
13503154 100321 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Compound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptorCompound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptor
ChEMBL 363 9 4 6 0.1 CSCC[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00378a012
CHEMBL288892 100321 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Compound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptorCompound was tested for in vitro inhibition of the binding of [125I](Nle11)-HG-13 to Histamine H2 receptor
ChEMBL 363 9 4 6 0.1 CSCC[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00378a012
72707158 140839 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 265 3 1 2 2.5 CC(C)CN1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
CHEMBL3818215 140839 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 265 3 1 2 2.5 CC(C)CN1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
14208271 102950 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 455 3 1 3 4.4 CN1C(=O)C(NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL305951 102950 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 455 3 1 3 4.4 CN1C(=O)C(NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208214 165343 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc2ccccc2c1 10.1021/jm00120a002
CHEMBL422951 165343 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 405 3 2 3 4.4 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc2ccccc2c1 10.1021/jm00120a002
10074366 120662 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3349028 120662 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3545866 120662 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 491 9 4 4 4.5 C[C@H]1CCCC[C@@H]1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
46235271 73674 None 2 Human Binding pIC50 = 7.7 7.7 2 2
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
CHEMBL2017835 73674 None 2 Human Binding pIC50 = 7.7 7.7 2 2
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 649 7 1 6 6.7 Cc1cc(C)cc(C[C@H]2CCCCN2C(=O)CN2C(=O)[C@@H](Cc3n[nH]c4ccccc34)c3nnc(-c4ccccc4)n3-c3ccccc32)c1 10.1016/j.bmcl.2012.02.049
14208249 207090 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 387 3 2 3 3.7 Cc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
CHEMBL73510 207090 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 387 3 2 3 3.7 Cc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
10603714 156609 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 605 8 1 5 6.0 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4c(F)cccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL406790 156609 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 605 8 1 5 6.0 COc1ccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4c(F)cccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
367893 51635 None 0 Guinea pig Binding pIC50 = 6.7 6.7 - 0
Compound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cell
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
CHEMBL158362 51635 None 0 Guinea pig Binding pIC50 = 6.7 6.7 - 0
Compound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cellCompound was evaluated for the binding affinity against CCK A receptor in pancreatic acinar cell
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00124a003
13953692 101776 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 407 3 1 4 5.0 Fc1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)c2nncn2-c2ccccc21 10.1021/jm00396a028
CHEMBL299538 101776 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 407 3 1 4 5.0 Fc1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)c2nncn2-c2ccccc21 10.1021/jm00396a028
89913094 140868 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 251 2 1 2 2.2 CC(C)N1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
CHEMBL3818578 140868 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 251 2 1 2 2.2 CC(C)N1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
14208235 103195 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 442 4 3 4 3.9 COc1ccc2[nH]c(C(=O)NC3N=C(c4ccccc4F)c4ccccc4NC3=O)cc2c1 10.1021/jm00120a002
CHEMBL307878 103195 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 442 4 3 4 3.9 COc1ccc2[nH]c(C(=O)NC3N=C(c4ccccc4F)c4ccccc4NC3=O)cc2c1 10.1021/jm00120a002
11798691 58288 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 473 5 4 7 3.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(Nc3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm9506736
CHEMBL168263 58288 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissueInhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
ChEMBL 473 5 4 7 3.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(Nc3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm9506736
10962743 78628 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1ccc(N2C(=O)C[C@@H]3[C@@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm010813d
CHEMBL2112239 78628 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 6 3 5 4.4 Cc1ccc(N2C(=O)C[C@@H]3[C@@H](NC(=O)[C@H](Cc4c[nH]c5ccccc45)NC(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm010813d
44370505 51295 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 543 10 2 4 6.3 O=C(CC[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N(C1CCCCC1)C1CCCCC1)OCc1ccccc1 10.1021/jm00164a020
CHEMBL158078 51295 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 543 10 2 4 6.3 O=C(CC[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N(C1CCCCC1)C1CCCCC1)OCc1ccccc1 10.1021/jm00164a020
10029582 27173 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 517 7 2 4 4.5 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL136608 27173 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 517 7 2 4 4.5 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44356717 116844 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 513 5 3 5 4.7 CN1C(=O)C(NC(=O)Nc2cccc(CNC(=O)OC(C)(C)C)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL337722 116844 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 513 5 3 5 4.7 CN1C(=O)C(NC(=O)Nc2cccc(CNC(=O)OC(C)(C)C)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44578531 172665 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 570 6 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OCC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL448597 172665 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 570 6 0 5 6.9 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(OCC(F)(F)F)c2)cc1 10.1016/j.bmcl.2008.06.057
44334332 108942 None 0 Guinea pig Binding pIC50 = 6.7 6.7 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 574 10 3 4 5.6 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC(Cc2ccccc2)CC1 10.1016/0960-894X(95)00537-3
CHEMBL321072 108942 None 0 Guinea pig Binding pIC50 = 6.7 6.7 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 574 10 3 4 5.6 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC(Cc2ccccc2)CC1 10.1016/0960-894X(95)00537-3
44349028 117286 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 437 7 3 4 3.5 O=C(O)CCC(NC(=O)c1ccc2ccccc2c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL339453 117286 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 437 7 3 4 3.5 O=C(O)CCC(NC(=O)c1ccc2ccccc2c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
89913112 140889 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 257 1 1 2 2.1 CN1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
CHEMBL3818822 140889 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma countingDisplacement of [125]I-CCK-8 from CCK-A receptor in rat pancreatic membrane after 2 hrs by gamma counting
ChEMBL 257 1 1 2 2.1 CN1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
44280215 99884 None 0 Mouse Binding pIC50 = 5.7 5.7 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 756 15 6 10 3.3 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL285586 99884 None 0 Mouse Binding pIC50 = 5.7 5.7 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 756 15 6 10 3.3 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
44334379 108829 None 0 Guinea pig Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 435 7 2 3 4.7 Cc1cccc(NC(=O)N[C@H](CC(C)C)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL320901 108829 None 0 Guinea pig Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 435 7 2 3 4.7 Cc1cccc(NC(=O)N[C@H](CC(C)C)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
19766161 59201 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 403 4 3 3 3.4 O=C(O)CN1C(=O)C(NC(=O)Nc2cccc3ccccc23)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
CHEMBL170068 59201 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 403 4 3 3 3.4 O=C(O)CN1C(=O)C(NC(=O)Nc2cccc3ccccc23)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
14208201 207039 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 436 6 3 3 4.4 O=C(CCCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL73110 207039 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 436 6 3 3 4.4 O=C(CCCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
44356972 27664 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 555 7 3 7 3.3 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)ON3CCC[C@@H]3C(=O)O)C2=O)c1 10.1021/jm00078a018
CHEMBL136990 27664 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 555 7 3 7 3.3 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)ON3CCC[C@@H]3C(=O)O)C2=O)c1 10.1021/jm00078a018
52945789 18291 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 541 7 0 5 6.0 CC(C)N(C(=O)CN1C(=O)C(Cc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
CHEMBL1270487 18291 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 541 7 0 5 6.0 CC(C)N(C(=O)CN1C(=O)C(Cc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21)c1ccccc1 10.1016/j.bmcl.2010.08.115
2802894 2403 None 25 Rat Binding pIC50 = 4.7 4.7 - 0
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@H]([C@@H]1c1ccccc1)c1ccccc1 10.1021/jm000937a
3509 2403 None 25 Rat Binding pIC50 = 4.7 4.7 - 0
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@H]([C@@H]1c1ccccc1)c1ccccc1 10.1021/jm000937a
CHEMBL333081 2403 None 25 Rat Binding pIC50 = 4.7 4.7 - 0
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@H]([C@@H]1c1ccccc1)c1ccccc1 10.1021/jm000937a
2802894 2403 None 25 Rat Binding pIC50 = 4.7 4.7 - 0
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@H]([C@@H]1c1ccccc1)c1ccccc1 10.1016/S0960-894X(00)80684-8
3509 2403 None 25 Rat Binding pIC50 = 4.7 4.7 - 0
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@H]([C@@H]1c1ccccc1)c1ccccc1 10.1016/S0960-894X(00)80684-8
CHEMBL333081 2403 None 25 Rat Binding pIC50 = 4.7 4.7 - 0
The compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreasThe compound was tested for its activity to inhibit the binding of [3H]-L-364,718 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@H]([C@@H]1c1ccccc1)c1ccccc1 10.1016/S0960-894X(00)80684-8
45482487 201057 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 441 7 4 3 4.2 Cc1c(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)[nH]c2ccccc12 10.1016/j.bmc.2009.05.067
CHEMBL578652 201057 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 441 7 4 3 4.2 Cc1c(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)[nH]c2ccccc12 10.1016/j.bmc.2009.05.067
10768071 9836 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 512 6 3 5 4.3 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
CHEMBL113988 9836 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreasInhibitory concentration against radioligand [3 H]L-364,718 binding to gastrin/Cholecystokinin type A receptor from rat pancreas
ChEMBL 512 6 3 5 4.3 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C(=O)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
44591977 179165 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 443 7 5 4 3.6 O=C(Nc1ccccc1C(=O)NC(Cc1ccc(O)cc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL471464 179165 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cellsDisplacement of [125I]BH-CCK8 from CCK1 receptor in Sprague-Dawley rat pancreatic acinar cells
ChEMBL 443 7 5 4 3.6 O=C(Nc1ccccc1C(=O)NC(Cc1ccc(O)cc1)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
44349336 164609 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1cccc(Cl)c1Cl)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL421474 164609 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 455 7 3 4 3.6 O=C(O)CCC(NC(=O)c1cccc(Cl)c1Cl)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
10813333 105409 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 447 5 2 4 4.2 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCCCN2C)c2ccccc21 10.1021/jm9608523
CHEMBL311638 105409 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.Inhibition of ligand binding to Cholecystokinin type A receptor from rat pancreatic tissue.
ChEMBL 447 5 2 4 4.2 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCCCN2C)c2ccccc21 10.1021/jm9608523
CHEMBL3142682 213586 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)NC1CCCCC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
52940616 18146 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 581 7 1 6 5.7 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(c2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269263 18146 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
ChEMBL 581 7 1 6 5.7 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(c2n[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
14208249 207090 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 387 3 2 3 3.7 Cc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL73510 207090 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 387 3 2 3 3.7 Cc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
9914964 9633 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 530 13 4 5 5.7 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc(O)c2cccc(O)c2n1 10.1021/jm00116a002
CHEMBL112682 9633 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 530 13 4 5 5.7 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc(O)c2cccc(O)c2n1 10.1021/jm00116a002
44293892 161781 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 613 6 2 5 5.8 CSc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
CHEMBL413267 161781 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 613 6 2 5 5.8 CSc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
14888709 77279 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1031 30 11 12 0.3 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(CC(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL2079603 77279 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1031 30 11 12 0.3 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(CC(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
71449099 78845 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 3 4 3.0 CN1C(=O)[C@H](NC(=O)NCc2cccc(O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2112751 78845 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 414 4 3 4 3.0 CN1C(=O)[C@H](NC(=O)NCc2cccc(O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14991578 161809 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 824 21 8 9 2.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C/c1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL413548 161809 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 824 21 8 9 2.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C/c1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14208203 114526 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 425 3 2 3 4.3 CC1C(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)=Cc2ccccc21 10.1021/jm00047a021
CHEMBL333459 114526 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 425 3 2 3 4.3 CC1C(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)=Cc2ccccc21 10.1021/jm00047a021
14888706 77280 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1017 29 11 12 0.4 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(C(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL2079604 77280 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL 1017 29 11 12 0.4 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(C(=O)O)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
10455302 28007 None 3 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 429 4 2 5 3.6 CN1C(=O)C(NC(=O)Nc2ccc([N+](=O)[O-])cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137240 28007 None 3 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 429 4 2 5 3.6 CN1C(=O)C(NC(=O)Nc2ccc([N+](=O)[O-])cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
19766170 59175 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 383 5 3 4 2.2 COc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)O)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL169931 59175 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas.
ChEMBL 383 5 3 4 2.2 COc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)O)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL2370879 212400 None 0 Guinea pig Binding pIC50 = 5.7 5.7 - 0
Compound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pigCompound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pig
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00105a068
44356697 25630 None 1 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 456 5 2 5 3.4 COC(=O)Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL135166 25630 None 1 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 456 5 2 5 3.4 COC(=O)Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
9870046 26356 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 486 5 3 6 3.4 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(Cc2nn[nH]n2)C1=O 10.1021/jm00078a018
CHEMBL135901 26356 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 486 5 3 6 3.4 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(Cc2nn[nH]n2)C1=O 10.1021/jm00078a018
10005779 116728 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 489 6 3 4 3.8 CCNC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL337065 116728 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 489 6 3 4 3.8 CCNC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44280214 107358 None 0 Mouse Binding pIC50 = 5.7 5.7 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 770 16 6 10 3.6 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL31726 107358 None 0 Mouse Binding pIC50 = 5.7 5.7 - 1
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 770 16 6 10 3.6 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL292097 213344 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Compound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranesCompound was tested for its binding affinity towards Cholecystokinin type A receptor in pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CN)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(01)81005-2
5279366 104216 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 401 4 2 4 4.0 CSc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
CHEMBL309575 104216 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 401 4 2 4 4.0 CSc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
155564367 175260 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 72 18 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
CHEMBL4570130 175260 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assayDisplacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay
ChEMBL 1836 72 18 23 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@H](NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.8b01558
44303527 96542 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 632 12 5 5 5.0 CC(Cc1c[nH]c2ccc(F)cc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL262456 96542 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreasInhibition of binding of [125I]- Bolton-Hunter labeled CCK-8 to CCK-A receptor in the rat pancreas
ChEMBL 632 12 5 5 5.0 CC(Cc1c[nH]c2ccc(F)cc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(97)00356-9
136794946 106668 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1[N+](=O)[O-])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
15689731 106668 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1[N+](=O)[O-])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142903 106668 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1[N+](=O)[O-])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
136794946 106668 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1[N+](=O)[O-])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
15689731 106668 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1[N+](=O)[O-])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
CHEMBL3142903 106668 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 857 21 9 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1[N+](=O)[O-])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
3960 2345 None 18 Rat Binding pIC50 = 7.7 7.7 - 1
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1016/S0960-894X(00)80224-3
891 2345 None 18 Rat Binding pIC50 = 7.7 7.7 - 1
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1016/S0960-894X(00)80224-3
CHEMBL24938 2345 None 18 Rat Binding pIC50 = 7.7 7.7 - 1
Displacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assayDisplacement of [125I]CCK-OP radioligand from Cholecystokinin type A receptor in rat pancreatic acinar membrane binding assay
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1016/S0960-894X(00)80224-3
44311642 206607 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 425 3 2 3 4.0 CC1(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)C=Cc2ccccc21 10.1021/jm00120a002
CHEMBL70549 206607 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 425 3 2 3 4.0 CC1(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)C=Cc2ccccc21 10.1021/jm00120a002
24784942 181449 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 488 4 1 5 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(O)c2)cc1 10.1016/j.bmcl.2008.06.057
CHEMBL476297 181449 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of human CCK1 receptorInhibition of human CCK1 receptor
ChEMBL 488 4 1 5 5.7 Cc1ccc(-c2nc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)cn2-c2cccc(O)c2)cc1 10.1016/j.bmcl.2008.06.057
90663975 106854 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 21 9 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1cccc(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144537 106854 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 839 21 9 9 3.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1cccc(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44303224 142022 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 933 23 8 11 2.8 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL387073 142022 None 0 Guinea pig Binding pIC50 = 7.7 7.7 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 933 23 8 11 2.8 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44348637 164605 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 966 27 11 11 1.0 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCCNC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL421471 164605 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 966 27 11 11 1.0 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCCNC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
52949124 876 None 4 Human Binding pIC50 = 7.7 7.7 -2 2
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
9055 876 None 4 Human Binding pIC50 = 7.7 7.7 -2 2
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
CHEMBL1269258 876 None 4 Human Binding pIC50 = 7.7 7.7 -2 2
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
DB12694 876 None 4 Human Binding pIC50 = 7.7 7.7 -2 2
Displacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counter
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1021/acs.jmedchem.5b01110
10507071 113674 None 0 Rat Binding pIC50 = 7.6 7.6 - 1
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
CHEMBL332261 113674 None 0 Rat Binding pIC50 = 7.6 7.6 - 1
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
44396744 124113 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 516 7 2 5 4.4 CC(C)(C)OC(=O)[C@H](Cc1c[nH]c2ccccc12)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)CC12 10.1021/jm0498755
CHEMBL363106 124113 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenatesInhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates
ChEMBL 516 7 2 5 4.4 CC(C)(C)OC(=O)[C@H](Cc1c[nH]c2ccccc12)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)CC12 10.1021/jm0498755
10626665 10263 None 0 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm010898i
CHEMBL116127 10263 None 0 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm010898i
10626665 10263 None 0 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm010813d
CHEMBL116127 10263 None 0 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreasInhibition of [3H]pCCK-8 specific binding to cholecystokinin type A receptor in rat pancreas
ChEMBL 559 7 3 5 4.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm010813d
5311148 1896 None 8 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 10.1021/jm960249k
865 1896 None 8 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 10.1021/jm960249k
CHEMBL293226 1896 None 8 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
ChEMBL 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 10.1021/jm960249k
5311148 1896 None 8 Human Binding pIC50 = 7.6 7.6 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 10.1021/jm970265x
865 1896 None 8 Human Binding pIC50 = 7.6 7.6 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 10.1021/jm970265x
CHEMBL293226 1896 None 8 Human Binding pIC50 = 7.6 7.6 - 0
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 587 8 1 5 5.9 COc1ccc(cc1)N(C(=O)CN1C(=O)C(Cc2[nH]nc3c2cccc3)C(=O)N(c2c1cccc2)c1ccccc1)C(C)C 10.1021/jm970265x
44300891 202010 None 0 Guinea pig Binding pIC50 = 6.7 6.7 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 586 7 4 6 5.1 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2CC1CCCCC1 10.1016/0960-894X(95)00327-P
CHEMBL59234 202010 None 0 Guinea pig Binding pIC50 = 6.7 6.7 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 586 7 4 6 5.1 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2CC1CCCCC1 10.1016/0960-894X(95)00327-P
CHEMBL3142698 213593 None 0 Guinea pig Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity towards cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None Cc1ccccc1/N=C(/S)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
10075014 163076 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 508 6 2 5 4.4 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
CHEMBL417521 163076 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreasDisplacement of [125 I] CCK-8 from Cholecystokinin type A receptor of rat pancreas
ChEMBL 508 6 2 5 4.4 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00121a004
13822924 101999 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 427 4 1 6 4.2 O=C(NC1N=C(c2ccccc2F)c2ccccc2-n2cnnc21)OCc1ccccc1 10.1021/jm00396a028
CHEMBL301172 101999 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 427 4 1 6 4.2 O=C(NC1N=C(c2ccccc2F)c2ccccc2-n2cnnc21)OCc1ccccc1 10.1021/jm00396a028
5279366 104216 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 401 4 2 4 4.0 CSc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL309575 104216 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 401 4 2 4 4.0 CSc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
10078285 121571 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 680 12 3 6 5.7 C[Si](C)(C)CCOC(=O)C[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
CHEMBL358334 121571 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptorInhibition of [3H]propionyl-CCK-8 binding to rat pancreas cholecystokinin-A (CCK-A) receptor
ChEMBL 680 12 3 6 5.7 C[Si](C)(C)CCOC(=O)C[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(98)00677-5
10075014 163076 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 508 6 2 5 4.4 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00078a018
CHEMBL417521 163076 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 508 6 2 5 4.4 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00078a018
90663983 106869 None 0 Guinea pig Binding pIC50 = 6.7 6.7 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 891 21 8 8 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144552 106869 None 0 Guinea pig Binding pIC50 = 6.7 6.7 - 0
Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.Inhibition of specific binding of [125I]BH-CCK-8 in guinea pig pancreas.
ChEMBL 891 21 8 8 4.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(C(F)(F)F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
3960 2345 None 18 Guinea pig Binding pIC50 = 5.7 5.7 - 1
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00164a020
891 2345 None 18 Guinea pig Binding pIC50 = 5.7 5.7 - 1
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00164a020
CHEMBL24938 2345 None 18 Guinea pig Binding pIC50 = 5.7 5.7 - 1
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00164a020
19766234 32344 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 427 4 1 3 5.6 CN1c2ccccc2C(c2ccccc2F)=NCC1CNc1cccc(C(F)(F)F)c1 10.1021/jm00163a069
CHEMBL141051 32344 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 427 4 1 3 5.6 CN1c2ccccc2C(c2ccccc2F)=NCC1CNc1cccc(C(F)(F)F)c1 10.1021/jm00163a069
10319892 59108 None 1 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL169661 59108 None 1 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 418 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44334250 4598 None 0 Guinea pig Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 514 9 3 4 4.6 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCCC(C(=O)Nc3ccccc3)C2)c1 10.1016/0960-894X(95)00537-3
CHEMBL102703 4598 None 0 Guinea pig Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 514 9 3 4 4.6 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCCC(C(=O)Nc3ccccc3)C2)c1 10.1016/0960-894X(95)00537-3
44334434 5093 None 0 Guinea pig Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 483 8 2 3 5.2 Cc1cccc(NC(=O)N[C@H](CCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL105527 5093 None 0 Guinea pig Binding pIC50 = 5.7 5.7 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 483 8 2 3 5.2 Cc1cccc(NC(=O)N[C@H](CCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
13953696 102017 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 483 4 1 4 6.7 Fc1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1021/jm00396a028
CHEMBL301331 102017 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 483 4 1 4 6.7 Fc1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1021/jm00396a028
15104615 172852 None 0 Guinea pig Binding pIC50 = 4.7 4.7 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 545 13 2 4 6.1 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)S(=O)(=O)c1ccc(Cl)cc1 10.1021/jm00116a002
CHEMBL450883 172852 None 0 Guinea pig Binding pIC50 = 4.7 4.7 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 545 13 2 4 6.1 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)S(=O)(=O)c1ccc(Cl)cc1 10.1021/jm00116a002
15614749 32253 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 393 4 2 4 3.5 O=C(NCC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccsc1 10.1021/jm00163a069
CHEMBL140984 32253 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 393 4 2 4 3.5 O=C(NCC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccsc1 10.1021/jm00163a069
20063245 115406 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 417 5 2 4 3.9 O=C(NCC1N=C(c2ccccc2F)c2ccccc2NC1=O)OCc1ccccc1 10.1021/jm00163a069
CHEMBL334933 115406 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 417 5 2 4 3.9 O=C(NCC1N=C(c2ccccc2F)c2ccccc2NC1=O)OCc1ccccc1 10.1021/jm00163a069
44349011 116924 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 373 8 4 3 2.7 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00079a003
CHEMBL338134 116924 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 373 8 4 3 2.7 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00079a003
10555387 30102 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 589 10 3 3 7.0 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC(Cc1ccccc1)Cc1ccccc1 10.1021/jm970065l
CHEMBL138952 30102 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 589 10 3 3 7.0 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC(Cc1ccccc1)Cc1ccccc1 10.1021/jm970065l
10720107 209141 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 497 6 3 6 5.3 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C(F)(F)F)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL8954 209141 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 497 6 3 6 5.3 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C(F)(F)F)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
44361556 116785 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 571 4 2 5 4.3 CC(C)(C)OC(=O)N1Cc2[nH]c3ccccc3c2CC1C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm991078x
CHEMBL337362 116785 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreasBinding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas
ChEMBL 571 4 2 5 4.3 CC(C)(C)OC(=O)N1Cc2[nH]c3ccccc3c2CC1C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm991078x
10032956 168139 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@H](CNC(=O)[C@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)NC(=O)CCC(=O)O 10.1021/jm00017a022
CHEMBL432258 168139 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cellsIn vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells
ChEMBL 742 17 7 6 5.8 Cc1ccccc1NC(=O)NCCCC[C@H](CNC(=O)[C@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)NC(=O)CCC(=O)O 10.1021/jm00017a022
15689730 106652 None 0 Guinea pig Binding pIC50 = 7.6 7.6 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 854 21 9 8 4.4 CC(C)c1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142694 106652 None 0 Guinea pig Binding pIC50 = 7.6 7.6 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL 854 21 9 8 4.4 CC(C)c1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL100609 210911 None 0 Guinea pig Binding pIC50 = 7.6 7.6 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None COc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL100609 210911 None 0 Guinea pig Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreasDisplacement of [125I]- BH-CCK-8 from Cholecystokinin type A receptor of guinea pig pancreas
ChEMBL None None None COc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
CHEMBL100609 210911 None 0 Guinea pig Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreasDisplacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas
ChEMBL None None None COc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
15667017 210635 None 0 Guinea pig Binding pIC50 = 7.6 7.6 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 974 28 10 11 1.7 CCCC[C@H](NC(=O)/C=C/c1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL98332 210635 None 0 Guinea pig Binding pIC50 = 7.6 7.6 - 0
Evaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreasEvaluated in vitro for its binding affinity towards cholecystokinin type A receptor of guinea pig pancreas
ChEMBL 974 28 10 11 1.7 CCCC[C@H](NC(=O)/C=C/c1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
15104594 10125 None 0 Guinea pig Binding pIC50 = 7.6 7.6 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL115656 10125 None 0 Guinea pig Binding pIC50 = 7.6 7.6 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL2370119 212244 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranesInhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
ChEMBL None None None CSCC[C@H](NC(=O)C(Cc1cccc(CC(=O)O)c1)NC(C)=O)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
52949124 876 None 4 Human Binding pIC50 = 7.6 7.6 -2 2
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
9055 876 None 4 Human Binding pIC50 = 7.6 7.6 -2 2
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
CHEMBL1269258 876 None 4 Human Binding pIC50 = 7.6 7.6 -2 2
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
DB12694 876 None 4 Human Binding pIC50 = 7.6 7.6 -2 2
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 594 8 1 5 6.5 CC(N(C(=O)CN1c2ccccc2n2c([C@@H](C1=O)Cc1c[nH]c3c1cccc3)nnc2c1ccccc1)Cc1ccccc1)C 10.1016/j.bmcl.2012.02.049
CHEMBL3142687 213589 None 0 Guinea pig Binding pIC50 = 6.6 6.6 - 0
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligandBinding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)NCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
5311201 209854 None 26 Rat Binding pIC50 = 6.6 6.6 26 9
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00092a007
CHEMBL9387 209854 None 26 Rat Binding pIC50 = 6.6 6.6 26 9
Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreasEvaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00092a007
5311201 209854 None 26 Rat Binding pIC50 = 6.6 6.6 26 9
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00105a062
CHEMBL9387 209854 None 26 Rat Binding pIC50 = 6.6 6.6 26 9
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptorHalf-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00105a062
44382244 59213 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 618 11 4 4 6.4 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)Nc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL170129 59213 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Inhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]- Bolton-Hunter CCK-26-33 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 618 11 4 4 6.4 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)Nc1ccccc1 10.1016/S0960-894X(00)80687-3
367893 51635 None 0 Guinea pig Binding pIC50 = 6.6 6.6 - 0
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
CHEMBL158362 51635 None 0 Guinea pig Binding pIC50 = 6.6 6.6 - 0
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
5311201 209854 None 26 Rat Binding pIC50 = 6.6 6.6 26 9
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00057a005
CHEMBL9387 209854 None 26 Rat Binding pIC50 = 6.6 6.6 26 9
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00057a005
9828961 168089 None 0 Guinea pig Binding pIC50 = 5.6 5.6 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 548 6 4 4 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)O)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
CHEMBL431919 168089 None 0 Guinea pig Binding pIC50 = 5.6 5.6 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 548 6 4 4 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)O)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
10046475 115571 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3cccnc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL335241 115571 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3cccnc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
44349087 118513 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 420 7 3 3 3.8 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCC2CCCCC2C1 10.1021/jm00079a003
CHEMBL341143 118513 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic aciniConcentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini
ChEMBL 420 7 3 3 3.8 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCC2CCCCC2C1 10.1021/jm00079a003
15167776 67737 None 0 Guinea pig Binding pIC50 = 4.6 4.6 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 441 5 2 3 4.2 O=C(O)CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
CHEMBL1907728 67737 None 0 Guinea pig Binding pIC50 = 4.6 4.6 - 0
Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor
ChEMBL 441 5 2 3 4.2 O=C(O)CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
15282007 168411 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 472 5 3 5 3.7 Cc1cccc(NC(=O)NC2N=C(c3c[nH]cn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL434126 168411 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligandBinding affinity towards Cholecystokinin type A receptor from rat pancreas using [I125]-L-364,718 as the radioligand
ChEMBL 472 5 3 5 3.7 Cc1cccc(NC(=O)NC2N=C(c3c[nH]cn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
44336539 5146 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]BDZ1 from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5146 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]BDZ1 from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
10838217 209793 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 473 7 3 8 3.7 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC)c2)c1 10.1021/jm970373j
CHEMBL9354 209793 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 473 7 3 8 3.7 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC)c2)c1 10.1021/jm970373j
44327420 111649 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 571 10 2 5 5.3 COC(=O)CN(CCc1ccccc1)C(=O)[C@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1016/S0960-894X(01)80769-1
CHEMBL328213 111649 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 571 10 2 5 5.3 COC(=O)CN(CCc1ccccc1)C(=O)[C@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1016/S0960-894X(01)80769-1
10438352 9801 None 0 Rat Binding pIC50 = 5.6 5.6 - 1
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 588 8 3 6 3.9 COC(=O)[C@@]1(Cc2ccccc2)C[C@@H]2[C@@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1016/0960-894X(96)00160-6
CHEMBL113699 9801 None 0 Rat Binding pIC50 = 5.6 5.6 - 1
Binding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreasBinding of [3H]propionyl-CCK-8 to Cholecystokinin type A receptor from rat pancreas
ChEMBL 588 8 3 6 3.9 COC(=O)[C@@]1(Cc2ccccc2)C[C@@H]2[C@@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C1=O 10.1016/0960-894X(96)00160-6
44286821 167955 None 0 Guinea pig Binding pIC50 = 6.6 6.6 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 822 18 7 7 5.0 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC[C@H]1CC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL430937 167955 None 0 Guinea pig Binding pIC50 = 6.6 6.6 - 0
Concentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreasConcentration that inhibited 50% of specific binding of [125I]Bolton-Hunter CCK-8 binding in guinea pig pancreas
ChEMBL 822 18 7 7 5.0 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC[C@H]1CC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
15104608 108883 None 0 Guinea pig Binding pIC50 = 6.6 6.6 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2ncccc2c1 10.1021/jm00116a002
CHEMBL320976 108883 None 0 Guinea pig Binding pIC50 = 6.6 6.6 - 0
Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.Inhibition of [125I]Bolton-Hunter CCK-8 binding to cholecystokinin type A receptor in guinea pig pancreatic membranes.
ChEMBL 498 13 2 3 6.3 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2ncccc2c1 10.1021/jm00116a002
14208260 102174 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 423 3 2 3 4.3 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00047a021
CHEMBL302359 102174 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 423 3 2 3 4.3 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00047a021
19754257 120441 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 340 3 3 2 4.3 O=C(Cc1c[nH]c2ccccc12)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
CHEMBL353304 120441 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreasTested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 340 3 3 2 4.3 O=C(Cc1c[nH]c2ccccc12)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
52942901 18144 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269261 18144 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 556 8 1 6 5.9 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)C(Nc2ccccc2)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
44336539 5146 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
CHEMBL105775 5146 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cellsDisplacement of [125I]CCK from CCK2R TM7 (unknown origin) containing L7.39H chimeric mutant expressed in CHO cells
ChEMBL 563 7 2 5 4.6 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/j.bmcl.2015.03.051
14208260 102174 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 423 3 2 3 4.3 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00120a002
CHEMBL302359 102174 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 423 3 2 3 4.3 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(C(F)(F)F)cc1 10.1021/jm00120a002
10453004 26133 None 10 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 390 3 2 3 3.5 CN1C(=O)C(NC(=O)NC2CCCCC2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135618 26133 None 10 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 390 3 2 3 3.5 CN1C(=O)C(NC(=O)NC2CCCCC2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10482726 26149 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 551 7 3 4 5.0 O=C(CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21)NCc1ccccc1 10.1021/jm00078a018
CHEMBL135638 26149 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissueInhibition of binding of [125I]CCK-8 to cholecystokinin type A receptor in rat pancreatic tissue
ChEMBL 551 7 3 4 5.0 O=C(CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21)NCc1ccccc1 10.1021/jm00078a018
44334704 4620 None 0 Guinea pig Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 499 9 2 4 4.8 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL102862 4620 None 0 Guinea pig Binding pIC50 = 5.6 5.6 - 0
Inhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissueInhibitory activity towards binding of [125I]Bolton-Hunter-CCK-8 to CCKA receptor in guinea pig pancreatic tissue
ChEMBL 499 9 2 4 4.8 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
10552615 29321 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 477 6 3 3 5.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1 10.1021/jm970065l
CHEMBL138311 29321 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 477 6 3 3 5.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1 10.1021/jm970065l
44382805 59230 None 0 Mouse Binding pIC50 = 4.6 4.6 - 0
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 536 9 3 5 3.4 CC(C)C[C@H](NC(=O)C(NC(=O)OC(C)(C)C)c1ccccc1)C(=O)N1CC(=O)N[C@@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
CHEMBL170197 59230 None 0 Mouse Binding pIC50 = 4.6 4.6 - 0
Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)Concentration producing half-maximal inhibition of specific binding of [125I]- CCK-8 to CCK receptors on mouse pancreatic membranes (CCK-A)
ChEMBL 536 9 3 5 3.4 CC(C)C[C@H](NC(=O)C(NC(=O)OC(C)(C)C)c1ccccc1)C(=O)N1CC(=O)N[C@@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
44359866 116602 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 557 9 3 7 3.3 CC(=O)NCSCC(NC(=O)OC(C)(C)C)C(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C 10.1021/jm00163a069
CHEMBL336256 116602 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
Inhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreasInhibition of binding of [125I]CCK-8 to Cholecystokinin type A receptor in rat pancreas
ChEMBL 557 9 3 7 3.3 CC(=O)NCSCC(NC(=O)OC(C)(C)C)C(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C 10.1021/jm00163a069
10837829 98617 None 1 Rat Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 463 6 3 6 5.0 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(Cl)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL276627 98617 None 1 Rat Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligandBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor from rat pancreas using [125I]bolton Hunter CCK-8 as radioligand
ChEMBL 463 6 3 6 5.0 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(Cl)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
52946667 18147 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 580 7 1 5 6.3 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)[C@H](c2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
CHEMBL1269264 18147 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
ChEMBL 580 7 1 5 6.3 CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)[C@H](c2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21 10.1016/j.bmcl.2010.08.115
613843 207037 None 26 Rat Binding pIC50 = 4.6 4.6 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 250 1 0 2 2.5 CN1C(=O)CN=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL73096 207037 None 26 Rat Binding pIC50 = 4.6 4.6 - 0
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissueHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue
ChEMBL 250 1 0 2 2.5 CN1C(=O)CN=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL2372077 212642 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Displacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cellsDisplacement of [111In]DTPA-Glu-Gly-[Tyr27(SO3H)]-CCK8 from human CCK1 receptor expressed in A431 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@H]1CNC(=O)CNC(=O)[C@H](CCCCNCc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1016/j.bmc.2007.05.067
70685411 73663 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 606 6 1 5 6.8 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
CHEMBL2017824 73663 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation countingDisplacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
ChEMBL 606 6 1 5 6.8 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1c1ccccc1 10.1016/j.bmcl.2012.02.049
54581261 61883 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 529 6 0 6 6.0 CCOc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773886 61883 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation countingDisplacement of [I125]-CCK8 from human CCK1 receptor expressed in CHO Flip cells after 2 hrs by scintillation counting
ChEMBL 529 6 0 6 6.0 CCOc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
44348922 16248 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 992 25 11 11 1.4 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC1CCC[C@H]1NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL122438 16248 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranesThe compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
ChEMBL 992 25 11 11 1.4 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC1CCC[C@H]1NC(=O)[C@H](Cc1ccc(S(=O)(=O)O)cc1)NC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
903 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm000937a
9850711 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm000937a
CHEMBL138534 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm000937a
CHEMBL2111312 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasHalf maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm000937a
904 3026 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(01)80769-1
9915756 3026 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL2111204 3026 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL356898 3026 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.In vitro inhibition of [125I]- Bolton Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@H](NC(=O)[C@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(01)80769-1
903 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
9850711 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL138534 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL2111312 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreasInhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
903 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
9850711 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
CHEMBL138534 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
CHEMBL2111312 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm00057a005
903 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm970065l
9850711 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm970065l
CHEMBL138534 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm970065l
CHEMBL2111312 3024 None 12 Rat Binding pIC50 = 7.6 7.6 - 1
Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreasInhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas
ChEMBL 557 10 4 4 5.2 OC(=O)C[C@@H](NC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)Cc1ccccc1 10.1021/jm970065l
11714635 72491 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 717 10 6 6 3.7 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(N)=O)N2C1=O 10.1021/jm050689o
CHEMBL198902 72491 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]propionylCCK8 from rat pancreatic CCK1Displacement of [3H]propionylCCK8 from rat pancreatic CCK1
ChEMBL 717 10 6 6 3.7 CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1C[C@H]2c3[nH]c4ccccc4c3C[C@H](C(=O)N[C@@H](Cc3ccccc3)C(N)=O)N2C1=O 10.1021/jm050689o
44300889 100815 None 0 Guinea pig Binding pIC50 = 6.6 6.6 - 0
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 532 6 4 6 3.8 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2C(C)C 10.1016/0960-894X(95)00327-P
CHEMBL292856 100815 None 0 Guinea pig Binding pIC50 = 6.6</