Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
51353551 17935 10 None 1 3 Human 11.0 pEC50 = 11 Functional
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 17935 10 None 1 3 Human 11.0 pEC50 = 11 Functional
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 17935 10 None 1 3 Human 10.9 pEC50 = 10.9 Functional
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 17935 10 None 1 3 Human 10.9 pEC50 = 10.9 Functional
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 49334 0 None 4 2 Human 10.9 pEC50 = 10.9 Functional
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 49334 0 None 4 2 Human 10.9 pEC50 = 10.9 Functional
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 49334 0 None 4 2 Human 10.7 pEC50 = 10.7 Functional
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 49334 0 None 4 2 Human 10.7 pEC50 = 10.7 Functional
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 5060 0 None 1 3 Human 10.7 pEC50 = 10.7 Functional
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 5060 0 None 1 3 Human 10.7 pEC50 = 10.7 Functional
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 164879 0 None 218776 2 Human 10.6 pEC50 = 10.6 Functional
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 164879 0 None 218776 2 Human 10.6 pEC50 = 10.6 Functional
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 188109 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
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 188109 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
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 187598 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
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 187598 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
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 188094 0 None -1 2 Mouse 10.5 pEC50 = 10.5 Functional
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 188094 0 None -1 2 Mouse 10.5 pEC50 = 10.5 Functional
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 49334 0 None 4 2 Human 10.4 pEC50 = 10.4 Functional
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 49334 0 None 4 2 Human 10.4 pEC50 = 10.4 Functional
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 188028 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
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 188028 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
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 807 44 None -1 6 Human 10.4 pEC50 = 10.4 Functional
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
864 807 44 None -1 6 Human 10.4 pEC50 = 10.4 Functional
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 807 44 None -1 6 Human 10.4 pEC50 = 10.4 Functional
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 807 44 None -1 6 Human 10.4 pEC50 = 10.4 Functional
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 807 44 None -1 6 Human 10.4 pEC50 = 10.4 Functional
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 187597 0 None 24 2 Human 10.3 pEC50 = 10.3 Functional
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 187597 0 None 24 2 Human 10.3 pEC50 = 10.3 Functional
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 187597 0 None 24 2 Human 10.3 pEC50 = 10.3 Functional
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 5060 0 None 1 3 Human 10.3 pEC50 = 10.3 Functional
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 5060 0 None 1 3 Human 10.3 pEC50 = 10.3 Functional
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 188540 3 None - 1 Human 10.3 pEC50 = 10.3 Functional
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 188540 3 None - 1 Human 10.3 pEC50 = 10.3 Functional
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 188454 0 None 3 2 Human 10.3 pEC50 = 10.3 Functional
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 188454 0 None 3 2 Human 10.3 pEC50 = 10.3 Functional
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 188131 0 None 5 3 Human 10.3 pEC50 = 10.3 Functional
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 188131 0 None 5 3 Human 10.3 pEC50 = 10.3 Functional
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 188131 0 None 5 3 Human 10.3 pEC50 = 10.3 Functional
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 188131 0 None 5 3 Human 10.3 pEC50 = 10.3 Functional
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 188131 0 None 5 3 Human 10.3 pEC50 = 10.3 Functional
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 188131 0 None 5 3 Human 10.3 pEC50 = 10.3 Functional
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 170986 0 None 47863 2 Human 10.2 pEC50 = 10.2 Functional
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 170986 0 None 47863 2 Human 10.2 pEC50 = 10.2 Functional
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 61580 0 None 5 3 Human 10.2 pEC50 = 10.2 Functional
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 61580 0 None 5 3 Human 10.2 pEC50 = 10.2 Functional
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 178132 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
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 178132 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
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 61512 0 None 2 3 Human 10.2 pEC50 = 10.2 Functional
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 61512 0 None 2 3 Human 10.2 pEC50 = 10.2 Functional
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 170276 0 None 4 2 Human 10.2 pEC50 = 10.2 Functional
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 170276 0 None 4 2 Human 10.2 pEC50 = 10.2 Functional
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 188094 0 None 1 2 Human 10.2 pEC50 = 10.2 Functional
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 188094 0 None 1 2 Human 10.2 pEC50 = 10.2 Functional
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 188278 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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 188278 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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 188458 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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 188458 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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 171894 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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 171894 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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 188042 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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 188042 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
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 172110 0 None 2 2 Human 10.1 pEC50 = 10.1 Functional
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 172110 0 None 2 2 Human 10.1 pEC50 = 10.1 Functional
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 188155 0 None 2 2 Human 10.0 pEC50 = 10.0 Functional
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 188155 0 None 2 2 Human 10.0 pEC50 = 10.0 Functional
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 188155 0 None 2 2 Human 10.0 pEC50 = 10.0 Functional
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 188189 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
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 188189 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
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 188189 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
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 188189 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
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 188189 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
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 188189 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
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 188189 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
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 188189 10 None 9 3 Human 10.0 pEC50 = 10.0 Functional
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 170875 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
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 170875 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
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 188050 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
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 188050 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
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 188332 0 None 8 2 Human 10.0 pEC50 = 10.0 Functional
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 188332 0 None 8 2 Human 10.0 pEC50 = 10.0 Functional
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 188406 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
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 188406 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
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 172127 0 None - 1 Human 10.0 pEC50 = 10 Functional
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 172127 0 None - 1 Human 10.0 pEC50 = 10 Functional
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 172209 0 None - 1 Human 10.0 pEC50 = 10 Functional
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 172209 0 None - 1 Human 10.0 pEC50 = 10 Functional
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 210630 0 None 60 2 Guinea pig 10.0 pEC50 = 10 Functional
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 171438 0 None 323 2 Human 10.0 pEC50 = 10.0 Functional
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 171438 0 None 323 2 Human 10.0 pEC50 = 10.0 Functional
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 171742 0 None 46773 2 Human 10.0 pEC50 = 10.0 Functional
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 171742 0 None 46773 2 Human 10.0 pEC50 = 10.0 Functional
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 171172 0 None 3 2 Human 10.0 pEC50 = 10.0 Functional
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 171172 0 None 3 2 Human 10.0 pEC50 = 10.0 Functional
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 172110 0 None -2 2 Mouse 10.0 pEC50 = 10.0 Functional
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 172110 0 None -2 2 Mouse 10.0 pEC50 = 10.0 Functional
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 188454 0 None -3 2 Mouse 10.0 pEC50 = 10.0 Functional
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 188454 0 None -3 2 Mouse 10.0 pEC50 = 10.0 Functional
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 173790 0 None 3 2 Human 9.9 pEC50 = 9.9 Functional
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 173790 0 None 3 2 Human 9.9 pEC50 = 9.9 Functional
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 174010 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 174010 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 5060 0 None 1 3 Human 9.9 pEC50 = 9.9 Functional
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 5060 0 None 1 3 Human 9.9 pEC50 = 9.9 Functional
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 189029 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 189029 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 61512 0 None -2 3 Mouse 9.9 pEC50 = 9.9 Functional
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 61512 0 None -2 3 Mouse 9.9 pEC50 = 9.9 Functional
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 73286 2 None 3 3 Human 9.9 pEC50 = 9.9 Functional
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 73286 2 None 3 3 Human 9.9 pEC50 = 9.9 Functional
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 169511 0 None 1 2 Human 9.9 pEC50 = 9.9 Functional
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 169511 0 None 1 2 Human 9.9 pEC50 = 9.9 Functional
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 174354 0 None 1 2 Human 9.9 pEC50 = 9.9 Functional
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 174354 0 None 1 2 Human 9.9 pEC50 = 9.9 Functional
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 178868 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 178868 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 188272 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 188272 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 188109 0 None -2 2 Mouse 9.9 pEC50 = 9.9 Functional
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 188109 0 None -2 2 Mouse 9.9 pEC50 = 9.9 Functional
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 171596 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 171596 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 172339 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 172339 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 188166 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 188166 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
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 174686 0 None 12302 2 Human 9.8 pEC50 = 9.8 Functional
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 174686 0 None 12302 2 Human 9.8 pEC50 = 9.8 Functional
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 170361 0 None 12882 2 Human 9.8 pEC50 = 9.8 Functional
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 170361 0 None 12882 2 Human 9.8 pEC50 = 9.8 Functional
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 171006 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
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 171006 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
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 170626 0 None 2 2 Human 9.8 pEC50 = 9.8 Functional
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 170626 0 None 2 2 Human 9.8 pEC50 = 9.8 Functional
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 174282 0 None 1 2 Human 9.8 pEC50 = 9.8 Functional
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 174282 0 None 1 2 Human 9.8 pEC50 = 9.8 Functional
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 171269 0 None -2 2 Human 9.8 pEC50 = 9.8 Functional
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 171269 0 None -2 2 Human 9.8 pEC50 = 9.8 Functional
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 171427 0 None 2754 2 Human 9.8 pEC50 = 9.8 Functional
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 171427 0 None 2754 2 Human 9.8 pEC50 = 9.8 Functional
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 171474 0 None 158 2 Human 9.8 pEC50 = 9.8 Functional
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 171474 0 None 158 2 Human 9.8 pEC50 = 9.8 Functional
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 172074 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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 172074 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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 173486 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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 173486 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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 17935 10 None 1 3 Human 9.7 pEC50 = 9.7 Functional
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 17935 10 None 1 3 Human 9.7 pEC50 = 9.7 Functional
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 172553 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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 172553 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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 61579 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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 61579 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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 172077 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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 172077 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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 169292 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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 169292 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
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 169287 0 None 1096 2 Human 9.7 pEC50 = 9.7 Functional
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 169287 0 None 1096 2 Human 9.7 pEC50 = 9.7 Functional
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 173435 0 None 9772 2 Human 9.7 pEC50 = 9.7 Functional
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 173435 0 None 9772 2 Human 9.7 pEC50 = 9.7 Functional
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 61570 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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 61570 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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 171930 0 None 3388 2 Human 9.6 pEC50 = 9.6 Functional
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 171930 0 None 3388 2 Human 9.6 pEC50 = 9.6 Functional
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 178783 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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 178783 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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 188025 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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 188025 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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 169292 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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 169292 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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 180220 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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 180220 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
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 73286 2 None 3 3 Human 9.5 pEC50 = 9.5 Functional
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 73286 2 None 3 3 Human 9.5 pEC50 = 9.5 Functional
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 172254 0 None 3235 2 Human 9.5 pEC50 = 9.5 Functional
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 172254 0 None 3235 2 Human 9.5 pEC50 = 9.5 Functional
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 172705 0 None 8709 2 Human 9.5 pEC50 = 9.5 Functional
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 172705 0 None 8709 2 Human 9.5 pEC50 = 9.5 Functional
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 188131 0 None -5 3 Mouse 9.5 pEC50 = 9.5 Functional
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 188131 0 None -5 3 Mouse 9.5 pEC50 = 9.5 Functional
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 188131 0 None -5 3 Mouse 9.5 pEC50 = 9.5 Functional
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 169579 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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 169579 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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 173094 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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 173094 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
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 173060 0 None -3 2 Human 9.5 pEC50 = 9.5 Functional
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 173060 0 None -3 2 Human 9.5 pEC50 = 9.5 Functional
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 73286 2 None 3 3 Human 9.5 pEC50 = 9.5 Functional
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 73286 2 None 3 3 Human 9.5 pEC50 = 9.5 Functional
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 169371 0 None 1819 2 Human 9.4 pEC50 = 9.4 Functional
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 169371 0 None 1819 2 Human 9.4 pEC50 = 9.4 Functional
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 175157 0 None 4677 2 Human 9.4 pEC50 = 9.4 Functional
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 175157 0 None 4677 2 Human 9.4 pEC50 = 9.4 Functional
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 172741 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 172741 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 173150 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 173150 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 174025 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 174025 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
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 175258 0 None 4168 2 Human 9.4 pEC50 = 9.4 Functional
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 175258 0 None 4168 2 Human 9.4 pEC50 = 9.4 Functional
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 173752 0 None 4168 2 Human 9.4 pEC50 = 9.4 Functional
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 173752 0 None 4168 2 Human 9.4 pEC50 = 9.4 Functional
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 171881 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
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 171881 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
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 73286 2 None 3 3 Human 9.3 pEC50 = 9.3 Functional
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 73286 2 None 3 3 Human 9.3 pEC50 = 9.3 Functional
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 188332 0 None -8 2 Mouse 9.3 pEC50 = 9.3 Functional
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 188332 0 None -8 2 Mouse 9.3 pEC50 = 9.3 Functional
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 169645 0 None 416 2 Human 9.3 pEC50 = 9.3 Functional
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 169645 0 None 416 2 Human 9.3 pEC50 = 9.3 Functional
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 174510 0 None 72 2 Human 9.3 pEC50 = 9.3 Functional
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 174510 0 None 72 2 Human 9.3 pEC50 = 9.3 Functional
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 175494 0 None 36 2 Human 9.3 pEC50 = 9.3 Functional
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 175494 0 None 36 2 Human 9.3 pEC50 = 9.3 Functional
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 861 2 None 2 3 Human 9.3 pEC50 = 9.3 Functional
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 861 2 None 2 3 Human 9.3 pEC50 = 9.3 Functional
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 861 2 None 2 3 Human 9.3 pEC50 = 9.3 Functional
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 861 2 None 2 3 Human 9.3 pEC50 = 9.3 Functional
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 189148 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
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 189148 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
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 61580 0 None -5 3 Mouse 9.2 pEC50 = 9.2 Functional
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 61580 0 None -5 3 Mouse 9.2 pEC50 = 9.2 Functional
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 61569 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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 61569 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
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 171179 0 None 27542 2 Human 9.1 pEC50 = 9.1 Functional
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 171179 0 None 27542 2 Human 9.1 pEC50 = 9.1 Functional
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 172934 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
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 172934 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
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 172934 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
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 172934 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
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 172934 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
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 172934 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
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 61524 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 61524 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 188122 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 188122 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
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 17935 10 None 1 3 Human 9.1 pEC50 = 9.1 Functional
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 17935 10 None 1 3 Human 9.1 pEC50 = 9.1 Functional
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 190105 0 None -12 2 Human 9.1 pEC50 = 9.1 Functional
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 190105 0 None -12 2 Human 9.1 pEC50 = 9.1 Functional
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 190310 0 None -10 2 Human 9.0 pEC50 = 9.0 Functional
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 190310 0 None -10 2 Human 9.0 pEC50 = 9.0 Functional
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 172631 0 None -14 2 Human 9.0 pEC50 = 9.0 Functional
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 172631 0 None -14 2 Human 9.0 pEC50 = 9.0 Functional
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 181694 0 None - 1 Human 9.0 pEC50 = 9 Functional
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 181694 0 None - 1 Human 9.0 pEC50 = 9 Functional
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 190137 0 None -3 2 Human 9.0 pEC50 = 9.0 Functional
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 190137 0 None -3 2 Human 9.0 pEC50 = 9.0 Functional
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 178761 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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 178761 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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 182334 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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 182334 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
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 172357 0 None 58 2 Human 9.0 pEC50 = 9.0 Functional
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 172357 0 None 58 2 Human 9.0 pEC50 = 9.0 Functional
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 190094 0 None -7 2 Human 8.9 pEC50 = 8.9 Functional
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 190094 0 None -7 2 Human 8.9 pEC50 = 8.9 Functional
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 190104 0 None -2 2 Human 8.9 pEC50 = 8.9 Functional
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 190104 0 None -2 2 Human 8.9 pEC50 = 8.9 Functional
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 211010 1 None 11 2 Guinea pig 8.9 pEC50 = 8.9 Functional
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 190032 0 None -9 2 Human 8.9 pEC50 = 8.9 Functional
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 190032 0 None -9 2 Human 8.9 pEC50 = 8.9 Functional
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 61520 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 61520 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
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 188189 10 None -12 3 Mouse 8.9 pEC50 = 8.9 Functional
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 188189 10 None -12 3 Mouse 8.9 pEC50 = 8.9 Functional
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 188189 10 None -12 3 Mouse 8.9 pEC50 = 8.9 Functional
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 188189 10 None -12 3 Mouse 8.9 pEC50 = 8.9 Functional
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 861 2 None 2 3 Human 8.9 pEC50 = 8.9 Functional
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 861 2 None 2 3 Human 8.9 pEC50 = 8.9 Functional
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 861 2 None 2 3 Human 8.9 pEC50 = 8.9 Functional
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 861 2 None 2 3 Human 8.9 pEC50 = 8.9 Functional
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 211387 0 None 8 2 Guinea pig 8.9 pEC50 = 8.9 Functional
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 861 2 None 2 3 Human 8.8 pEC50 = 8.8 Functional
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 861 2 None 2 3 Human 8.8 pEC50 = 8.8 Functional
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 861 2 None 2 3 Human 8.8 pEC50 = 8.8 Functional
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 861 2 None 2 3 Human 8.8 pEC50 = 8.8 Functional
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 173854 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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 173854 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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 173346 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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 173346 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
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 61529 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 61529 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 861 2 None 2 3 Human 8.7 pEC50 = 8.7 Functional
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 861 2 None 2 3 Human 8.7 pEC50 = 8.7 Functional
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 861 2 None 2 3 Human 8.7 pEC50 = 8.7 Functional
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 861 2 None 2 3 Human 8.7 pEC50 = 8.7 Functional
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 178762 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 178762 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
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 61574 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 61574 0 None - 1 Human 8.0 pEC50 = 8 Functional
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 189056 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 189056 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 188995 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 188995 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 171055 0 None 2 2 Human 7.9 pEC50 = 7.9 Functional
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 171055 0 None 2 2 Human 7.9 pEC50 = 7.9 Functional
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 173593 0 None -26 2 Human 7.9 pEC50 = 7.9 Functional
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 173593 0 None -26 2 Human 7.9 pEC50 = 7.9 Functional
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 174574 0 None -457 2 Human 6.9 pEC50 = 6.9 Functional
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 174574 0 None -457 2 Human 6.9 pEC50 = 6.9 Functional
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 73284 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 73284 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
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 861 2 None 2 3 Human 6.9 pEC50 = 6.9 Functional
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 861 2 None 2 3 Human 6.9 pEC50 = 6.9 Functional
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 861 2 None 2 3 Human 6.9 pEC50 = 6.9 Functional
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 861 2 None 2 3 Human 6.9 pEC50 = 6.9 Functional
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 108727 0 None -51 4 Guinea pig 5.9 pEC50 = 5.9 Functional
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 108727 0 None -51 4 Guinea pig 5.9 pEC50 = 5.9 Functional
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 73234 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 73234 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 171984 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 171984 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 140041 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
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 140041 0 None - 1 Rat 6.8 pEC50 = 6.8 Functional
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 17936 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 17936 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 73275 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 73275 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 61572 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 61572 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 180969 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 180969 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 18085 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 18085 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 61527 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 61527 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 207617 0 None 4 2 Guinea pig 8.7 pEC50 = 8.7 Functional
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 73283 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 73283 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
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 180947 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 180947 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 189179 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 189179 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 208949 0 None 7 2 Guinea pig 7.7 pEC50 = 7.7 Functional
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 61521 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 61521 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 73276 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 73276 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 173936 0 None -295 2 Human 6.6 pEC50 = 6.6 Functional
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 173936 0 None -295 2 Human 6.6 pEC50 = 6.6 Functional
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 173545 0 None 53 2 Human 6.6 pEC50 = 6.6 Functional
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 173545 0 None 53 2 Human 6.6 pEC50 = 6.6 Functional
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 180578 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 180578 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 73286 2 None 3 3 Human 7.6 pEC50 = 7.6 Functional
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 73286 2 None 3 3 Human 7.6 pEC50 = 7.6 Functional
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 207445 0 None -30 5 Human 5.6 pEC50 = 5.6 Functional
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 207445 0 None -30 5 Human 5.6 pEC50 = 5.6 Functional
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 73279 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 73279 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 61522 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 61522 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 1364 29 None -354 2 Human 6.6 pEC50 = 6.6 Functional
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 1364 29 None -354 2 Human 6.6 pEC50 = 6.6 Functional
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 1364 29 None -354 2 Human 6.6 pEC50 = 6.6 Functional
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 1364 29 None -354 2 Human 6.6 pEC50 = 6.6 Functional
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 61571 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 61571 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 210461 4 None -1 2 Human 7.6 pEC50 = 7.6 Functional
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 807 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
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
864 807 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
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 807 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
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 807 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
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 807 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
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 807 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
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
864 807 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
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 807 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
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 807 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
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 807 44 None -1 6 Human 7.6 pEC50 = 7.6 Functional
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 17935 10 None 1 3 Human 6.6 pEC50 = 6.6 Functional
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 17935 10 None 1 3 Human 6.6 pEC50 = 6.6 Functional
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 61517 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 61517 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 17938 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
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 17938 0 None 1 2 Rat 6.5 pEC50 = 6.5 Functional
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 210536 0 None -331 5 Human 6.5 pEC50 = 6.5 Functional
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 207624 0 None 6 2 Guinea pig 8.5 pEC50 = 8.5 Functional
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 73286 2 None 3 3 Human 8.5 pEC50 = 8.5 Functional
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 73286 2 None 3 3 Human 8.5 pEC50 = 8.5 Functional
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 172539 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 172539 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
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 210536 0 None -331 5 Human 6.5 pEC50 = 6.5 Functional
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 182204 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 182204 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 73280 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 73280 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 861 2 None 2 3 Human 6.5 pEC50 = 6.5 Functional
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 861 2 None 2 3 Human 6.5 pEC50 = 6.5 Functional
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 861 2 None 2 3 Human 6.5 pEC50 = 6.5 Functional
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 861 2 None 2 3 Human 6.5 pEC50 = 6.5 Functional
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 188091 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 188091 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 61519 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 61519 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 61526 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 61526 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 61513 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 61513 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 73282 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 73282 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 39172 6 None -3 3 Guinea pig 7.4 pEC50 = 7.4 Functional
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 39172 6 None -3 3 Guinea pig 7.4 pEC50 = 7.4 Functional
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 106799 0 None -2 3 Guinea pig 6.4 pEC50 = 6.4 Functional
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 106799 0 None -2 3 Guinea pig 6.4 pEC50 = 6.4 Functional
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 178738 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 178738 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 73233 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 73233 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 61575 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 61575 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 861 2 None 2 3 Human 7.4 pEC50 = 7.4 Functional
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 861 2 None 2 3 Human 7.4 pEC50 = 7.4 Functional
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 861 2 None 2 3 Human 7.4 pEC50 = 7.4 Functional
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 861 2 None 2 3 Human 7.4 pEC50 = 7.4 Functional
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 61518 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 61518 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 73281 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 73281 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 17937 0 None 2 2 Rat 6.4 pEC50 = 6.4 Functional
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 17937 0 None 2 2 Rat 6.4 pEC50 = 6.4 Functional
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 180970 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 180970 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
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 861 2 None -2 3 Rat 6.4 pEC50 = 6.4 Functional
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 861 2 None -2 3 Rat 6.4 pEC50 = 6.4 Functional
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 861 2 None -2 3 Rat 6.4 pEC50 = 6.4 Functional
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 861 2 None -2 3 Rat 6.4 pEC50 = 6.4 Functional
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 180942 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 180942 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 17940 0 None 1 2 Rat 6.3 pEC50 = 6.3 Functional
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 17940 0 None 1 2 Rat 6.3 pEC50 = 6.3 Functional
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 73277 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 73277 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 73286 2 None 3 3 Human 8.3 pEC50 = 8.3 Functional
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 73286 2 None 3 3 Human 8.3 pEC50 = 8.3 Functional
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 180948 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 180948 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
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 61576 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 61576 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 73232 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 73232 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 17940 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
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 17940 0 None -1 2 Human 6.3 pEC50 = 6.3 Functional
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 181692 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 181692 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 209025 0 None 5 2 Guinea pig 7.3 pEC50 = 7.3 Functional
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 181192 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 181192 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 73274 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 73274 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 61577 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 61577 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 61525 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 61525 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 189208 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 189208 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 189116 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 189116 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
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 208059 0 None -1 2 Guinea pig 7.2 pEC50 = 7.2 Functional
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 172360 0 None -1584 2 Human 6.2 pEC50 = 6.2 Functional
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 172360 0 None -1584 2 Human 6.2 pEC50 = 6.2 Functional
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 61528 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 61528 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 17939 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 17939 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 17935 10 None -18 3 Rat 7.2 pEC50 = 7.2 Functional
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 17935 10 None -18 3 Rat 7.2 pEC50 = 7.2 Functional
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 17937 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
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 17937 0 None -2 2 Human 6.2 pEC50 = 6.2 Functional
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 180971 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 180971 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 73285 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 73285 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 73286 2 None 3 3 Human 7.2 pEC50 = 7.2 Functional
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 73286 2 None 3 3 Human 7.2 pEC50 = 7.2 Functional
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 180944 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 180944 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 61573 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 61573 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 181840 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 181840 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 189057 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 189057 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 171252 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 171252 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
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 180751 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 180751 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 73278 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 73278 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 61523 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 61523 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 181362 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 181362 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 88940 0 None 63 2 Human 8.0 pEC50 = 8.0 Functional
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 88940 0 None 63 2 Human 8.0 pEC50 = 8.0 Functional
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 181863 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 181863 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 182195 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 182195 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 61578 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 61578 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
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 5060 0 None 1 3 Human 7.1 pEC50 = 7.1 Functional
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 5060 0 None 1 3 Human 7.1 pEC50 = 7.1 Functional
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 17938 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
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 17938 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
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 169633 0 None -457 2 Human 6.0 pEC50 = 6.0 Functional
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 169633 0 None -457 2 Human 6.0 pEC50 = 6.0 Functional
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 182182 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 182182 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 205862 40 None 2 6 Human 10.1 pIC50 = 10.1 Functional
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 205862 40 None 2 6 Human 10.1 pIC50 = 10.1 Functional
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 123854 0 None -91 2 Human 7.9 pIC50 = 7.9 Functional
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 123854 0 None -91 2 Human 7.9 pIC50 = 7.9 Functional
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 67177 0 None -100 2 Human 6.0 pIC50 = 6.0 Functional
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 67177 0 None -100 2 Human 6.0 pIC50 = 6.0 Functional
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 123854 0 None -91 2 Human 6.9 pIC50 = 6.9 Functional
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 123854 0 None -91 2 Human 6.9 pIC50 = 6.9 Functional
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 98996 12 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 98996 12 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 123854 0 None -91 2 Human 6.7 pIC50 = 6.7 Functional
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 123854 0 None -91 2 Human 6.7 pIC50 = 6.7 Functional
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 123854 0 None -91 2 Human 5.7 pIC50 = 5.7 Functional
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 123854 0 None -91 2 Human 5.7 pIC50 = 5.7 Functional
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 113098 0 None -524 4 Human 4.7 pIC50 = 4.7 Functional
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 113098 0 None -524 4 Human 4.7 pIC50 = 4.7 Functional
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 127081 0 None -7 2 Human 6.6 pIC50 = 6.6 Functional
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 127081 0 None -7 2 Human 6.6 pIC50 = 6.6 Functional
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 67177 0 None -100 2 Human 5.6 pIC50 = 5.6 Functional
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 67177 0 None -100 2 Human 5.6 pIC50 = 5.6 Functional
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 67177 0 None -100 2 Human 7.6 pIC50 = 7.6 Functional
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 67177 0 None -100 2 Human 7.6 pIC50 = 7.6 Functional
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 67177 0 None -100 2 Human 7.6 pIC50 = 7.6 Functional
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 67177 0 None -100 2 Human 7.6 pIC50 = 7.6 Functional
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 127081 0 None -7 2 Human 7.6 pIC50 = 7.6 Functional
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 127081 0 None -7 2 Human 7.6 pIC50 = 7.6 Functional
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 127081 0 None -7 2 Human 7.6 pIC50 = 7.6 Functional
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 127081 0 None -7 2 Human 7.6 pIC50 = 7.6 Functional
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 123854 0 None -91 2 Human 7.6 pIC50 = 7.6 Functional
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 123854 0 None -91 2 Human 7.6 pIC50 = 7.6 Functional
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 210461 4 None -1 2 Human 7.6 pIC50 = 7.6 Functional
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 123854 0 None -91 2 Human 7.6 pIC50 = 7.6 Functional
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 123854 0 None -91 2 Human 7.6 pIC50 = 7.6 Functional
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 861 2 None 2 3 Human 8.5 pIC50 = 8.5 Functional
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 861 2 None 2 3 Human 8.5 pIC50 = 8.5 Functional
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 861 2 None 2 3 Human 8.5 pIC50 = 8.5 Functional
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 861 2 None 2 3 Human 8.5 pIC50 = 8.5 Functional
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 127081 0 None -7 2 Human 8.4 pIC50 = 8.4 Functional
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 127081 0 None -7 2 Human 8.4 pIC50 = 8.4 Functional
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 123854 0 None -91 2 Human 7.5 pIC50 = 7.5 Functional
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 123854 0 None -91 2 Human 7.5 pIC50 = 7.5 Functional
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 67177 0 None -100 2 Human 7.5 pIC50 = 7.5 Functional
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 67177 0 None -100 2 Human 7.5 pIC50 = 7.5 Functional
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 67177 0 None -100 2 Human 7.5 pIC50 = 7.5 Functional
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 67177 0 None -100 2 Human 7.5 pIC50 = 7.5 Functional
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 67177 0 None -100 2 Human 7.5 pIC50 = 7.5 Functional
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 67177 0 None -100 2 Human 7.5 pIC50 = 7.5 Functional
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 67177 0 None -100 2 Human 7.4 pIC50 = 7.4 Functional
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 67177 0 None -100 2 Human 7.4 pIC50 = 7.4 Functional
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 67177 0 None -100 2 Human 5.3 pIC50 = 5.3 Functional
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 67177 0 None -100 2 Human 5.3 pIC50 = 5.3 Functional
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 127081 0 None -7 2 Human 8.3 pIC50 = 8.3 Functional
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 127081 0 None -7 2 Human 8.3 pIC50 = 8.3 Functional
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 123854 0 None -91 2 Human 8.2 pIC50 = 8.2 Functional
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 123854 0 None -91 2 Human 8.2 pIC50 = 8.2 Functional
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 123854 0 None -91 2 Human 8.2 pIC50 = 8.2 Functional
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 123854 0 None -91 2 Human 8.2 pIC50 = 8.2 Functional
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 67177 0 None -100 2 Human 6.3 pIC50 = 6.3 Functional
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 67177 0 None -100 2 Human 6.3 pIC50 = 6.3 Functional
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 127081 0 None -7 2 Human 6.2 pIC50 = 6.2 Functional
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 127081 0 None -7 2 Human 6.2 pIC50 = 6.2 Functional
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 123854 0 None -91 2 Human 8.1 pIC50 = 8.1 Functional
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 123854 0 None -91 2 Human 8.1 pIC50 = 8.1 Functional
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 127081 0 None -7 2 Human 8.1 pIC50 = 8.1 Functional
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 127081 0 None -7 2 Human 8.1 pIC50 = 8.1 Functional
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 67177 0 None -100 2 Human 7.1 pIC50 = 7.1 Functional
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 67177 0 None -100 2 Human 7.1 pIC50 = 7.1 Functional
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 127081 0 None -7 2 Human 8.1 pIC50 = 8.1 Functional
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 127081 0 None -7 2 Human 8.1 pIC50 = 8.1 Functional
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 127081 0 None -7 2 Human 8.1 pIC50 = 8.1 Functional
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 127081 0 None -7 2 Human 8.1 pIC50 = 8.1 Functional
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 127081 0 None -7 2 Human 6.1 pIC50 = 6.1 Functional
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 127081 0 None -7 2 Human 6.1 pIC50 = 6.1 Functional
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 123854 0 None -91 2 Human 6.1 pIC50 = 6.1 Functional
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 123854 0 None -91 2 Human 6.1 pIC50 = 6.1 Functional
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 127081 0 None -7 2 Human 8.0 pIC50 = 8.0 Functional
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 127081 0 None -7 2 Human 8.0 pIC50 = 8.0 Functional
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 101578 0 None - 2 Guinea pig 7.4 pKd = 7.4 Functional
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 101578 0 None - 2 Guinea pig 7.4 pKd = 7.4 Functional
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 157321 0 None - 2 Guinea pig 7.4 pKd = 7.4 Functional
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 157321 0 None - 2 Guinea pig 7.4 pKd = 7.4 Functional
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 98241 0 None - 1 Guinea pig 8.2 pKd = 8.2 Functional
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 98241 0 None - 1 Guinea pig 8.2 pKd = 8.2 Functional
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 101847 0 None - 2 Guinea pig 7.2 pKd = 7.2 Functional
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 101847 0 None - 2 Guinea pig 7.2 pKd = 7.2 Functional
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 101600 0 None - 2 Guinea pig 7.1 pKd = 7.1 Functional
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 101600 0 None - 2 Guinea pig 7.1 pKd = 7.1 Functional
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 3233 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 None
5042 3233 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 None
871 3233 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 None
CHEMBL1697771 3233 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 None
DB11656 3233 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 None
1614 2307 60 None -1 2 Rat 8.2 pIC50 = 8.2 Functional
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 2307 60 None -1 2 Rat 8.2 pIC50 = 8.2 Functional
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 2307 60 None -1 2 Rat 8.2 pIC50 = 8.2 Functional
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 2307 60 None -1 2 Rat 8.2 pIC50 = 8.2 Functional
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 1371 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 1371 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 1371 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 1371 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 1371 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
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 804 0 None -158 2 Rat 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
861 804 0 None -158 2 Rat 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
16168172 1732 0 None -158 2 Rat 6.1 pIC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
3559 1732 0 None -158 2 Rat 6.1 pIC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
444007 2982 0 None -794 2 Rat 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
870 2982 0 None -794 2 Rat 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
DB00183 2982 0 None -794 2 Rat 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
3960 2303 20 None 53 4 Rat 7.5 pIC50 = 7.5 Functional
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 2303 20 None 53 4 Rat 7.5 pIC50 = 7.5 Functional
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 2303 20 None 53 4 Rat 7.5 pIC50 = 7.5 Functional
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 2303 20 None 53 4 Rat 7.5 pIC50 = 7.5 Functional
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 2303 20 None 53 4 Rat 7.5 pIC50 = 7.5 Functional
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 2303 20 None 53 4 Rat 7.5 pIC50 = 7.5 Functional
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 861 2 None 2 3 Human 7.5 pIC50 = 7.5 Functional
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 861 2 None 2 3 Human 7.5 pIC50 = 7.5 Functional
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 861 2 None 2 3 Human 7.5 pIC50 = 7.5 Functional
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 861 2 None 2 3 Human 7.5 pIC50 = 7.5 Functional
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 1857 5 None 41 2 Human 7.6 pIC50 = 7.6 Functional
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 1857 5 None 41 2 Human 7.6 pIC50 = 7.6 Functional
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 1857 5 None 41 2 Human 7.6 pIC50 = 7.6 Functional
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 2082 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7654246
5311196 2082 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7654246
122077 2281 45 None -8 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10988332
890 2281 45 None -8 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10988332
CHEMBL249973 2281 45 None -8 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10988332
DB04867 2281 45 None -8 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 10988332
121964 205 28 None 4265 2 Rat 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1636779
858 205 28 None 4265 2 Rat 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1636779
CHEMBL323521 205 28 None 4265 2 Rat 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1636779
904 2965 7 None 3 3 Rat 8.6 pIC50 = 8.6 Functional
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 2965 7 None 3 3 Rat 8.6 pIC50 = 8.6 Functional
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 2965 7 None 3 3 Rat 8.6 pIC50 = 8.6 Functional
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 2965 7 None 3 3 Rat 8.6 pIC50 = 8.6 Functional
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
862 805 0 None -1 2 Mouse 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12370550
127948 3649 0 None 79432 2 Rat 9.6 pIC50 = 9.6 Functional
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 3649 0 None 79432 2 Rat 9.6 pIC50 = 9.6 Functional
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 1368 8 None 870 2 Rat 9.7 pIC50 = 9.7 Functional
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 1368 8 None 870 2 Rat 9.7 pIC50 = 9.7 Functional
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 1368 8 None 870 2 Rat 9.7 pIC50 = 9.7 Functional
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 1368 8 None 870 2 Rat 9.7 pIC50 = 9.7 Functional
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 807 44 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
864 807 44 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
9833444 807 44 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
CHEMBL1121 807 44 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
DB09142 807 44 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
2281 3114 76 None -2454 2 Rat 2.2 pIC50 None 2.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 3440035
4922 3114 76 None -2454 2 Rat 2.2 pIC50 None 2.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 3440035
893 3114 76 None -2454 2 Rat 2.2 pIC50 None 2.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 3440035
CHEMBL316561 3114 76 None -2454 2 Rat 2.2 pIC50 None 2.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 3440035
DB13431 3114 76 None -2454 2 Rat 2.2 pIC50 None 2.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 334 10 2 3 2.3 CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC 3440035
2360 3233 0 None - 1 Rat 4.4 pIC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 15556137
5042 3233 0 None - 1 Rat 4.4 pIC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 15556137
871 3233 0 None - 1 Rat 4.4 pIC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 15556137
CHEMBL1697771 3233 0 None - 1 Rat 4.4 pIC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 15556137
DB11656 3233 0 None - 1 Rat 4.4 pIC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 370 5 3 3 2.6 Clc1ccc(cc1)C(=O)NC(C(=O)O)Cc1cc(=O)[nH]c2c1cccc2 15556137
108187 911 30 None -794 5 Rat 5.6 pIC50 None 5.6 Functional
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
873 911 30 None -794 5 Rat 5.6 pIC50 None 5.6 Functional
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 911 30 None -794 5 Rat 5.6 pIC50 None 5.6 Functional
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 911 30 None -794 5 Rat 5.6 pIC50 None 5.6 Functional
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 2962 0 None -1000 2 Rat 5.9 pIC50 None 5.9 Functional
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 2962 0 None -1000 2 Rat 5.9 pIC50 None 5.9 Functional
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 2199 3 None -7413 2 Rat 6.4 pIC50 None 6.4 Functional
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 2199 3 None -7413 2 Rat 6.4 pIC50 None 6.4 Functional
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 2199 3 None -7413 2 Rat 6.4 pIC50 None 6.4 Functional
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 2307 60 None -1 2 Rat 6.5 pIC50 None 6.5 Functional
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 2307 60 None -1 2 Rat 6.5 pIC50 None 6.5 Functional
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 2307 60 None -1 2 Rat 6.5 pIC50 None 6.5 Functional
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 2307 60 None -1 2 Rat 6.5 pIC50 None 6.5 Functional
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 2180 8 None -12 3 Rat 6.6 pIC50 None 6.6 Functional
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 2180 8 None -12 3 Rat 6.6 pIC50 None 6.6 Functional
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 2180 8 None -12 3 Rat 6.6 pIC50 None 6.6 Functional
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 2180 8 None -12 3 Rat 6.6 pIC50 None 6.6 Functional
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 3924 0 None - 1 Rat 6.7 pIC50 None 6.7 Functional
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 3924 0 None - 1 Rat 6.7 pIC50 None 6.7 Functional
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 3924 0 None - 1 Rat 6.7 pIC50 None 6.7 Functional
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 4035 24 None -2511 3 Rat 6.9 pIC50 None 6.9 Functional
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 4035 24 None -2511 3 Rat 6.9 pIC50 None 6.9 Functional
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 4035 24 None -2511 3 Rat 6.9 pIC50 None 6.9 Functional
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 4035 24 None -2511 3 Rat 6.9 pIC50 None 6.9 Functional
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 807 44 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
864 807 44 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
9833444 807 44 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
CHEMBL1121 807 44 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
DB09142 807 44 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
10348659 1766 0 None 3 2 Human 7.2 pIC50 None 7.2 Functional
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 1766 0 None 3 2 Human 7.2 pIC50 None 7.2 Functional
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 1766 0 None 3 2 Human 7.2 pIC50 None 7.2 Functional
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 3471 0 None - 1 Rat 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 363 4 3 3 2.0 OC(=O)C1CN(C(=O)C1NC(=O)c1c[nH]c2c1cccc2)c1ccccc1 None
883 3471 0 None - 1 Rat 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 363 4 3 3 2.0 OC(=O)C1CN(C(=O)C1NC(=O)c1c[nH]c2c1cccc2)c1ccccc1 None
11757476 2025 1 None - 1 Rat 9.0 pIC50 None 9 Functional
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 2025 1 None - 1 Rat 9.0 pIC50 None 9 Functional
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 2025 1 None - 1 Rat 9.0 pIC50 None 9 Functional
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 3597 0 None - 1 Human 9.3 pIC50 None 9.3 Functional
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 3597 0 None - 1 Human 9.3 pIC50 None 9.3 Functional
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 3597 0 None - 1 Human 9.3 pIC50 None 9.3 Functional
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 3100 11 None 602 2 Rat 9.4 pIC50 None 9.4 Functional
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 3100 11 None 602 2 Rat 9.4 pIC50 None 9.4 Functional
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 3100 11 None 602 2 Rat 9.4 pIC50 None 9.4 Functional
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 2281 45 None 8 2 Rat 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 7681406
890 2281 45 None 8 2 Rat 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 7681406
CHEMBL249973 2281 45 None 8 2 Rat 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 411 5 2 5 4.8 OC(=O)Cn1c(cc2c1cccc2)C(=O)Nc1scc(n1)c1ccccc1Cl 7681406
DB04867 2281 45 None 8 2 Rat 9.7 pIC50 None 9.7 Functional
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 Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
4627 807 44 None -2 5 Human 10.0 pEC50 = 10 Binding
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
864 807 44 None -2 5 Human 10.0 pEC50 = 10 Binding
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 807 44 None -2 5 Human 10.0 pEC50 = 10 Binding
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 807 44 None -2 5 Human 10.0 pEC50 = 10 Binding
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 807 44 None -2 5 Human 10.0 pEC50 = 10 Binding
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 167461 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
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 167461 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
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 209461 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
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 188094 0 None - 0 Human 11.0 pIC50 = 11 Binding
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 188094 0 None - 0 Human 11.0 pIC50 = 11 Binding
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 188454 0 None - 0 Human 10.8 pIC50 = 10.8 Binding
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 188454 0 None - 0 Human 10.8 pIC50 = 10.8 Binding
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 172110 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
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 172110 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
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 188155 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
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 188155 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
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 188155 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
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 188458 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
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 188458 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
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 61512 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
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 61512 0 None - 0 Human 10.5 pIC50 = 10.5 Binding
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 188332 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
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 188332 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
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 188131 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
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 188131 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
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 188131 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
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 172741 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
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 172741 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
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 187598 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
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 187598 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
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 175258 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
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 175258 0 None - 0 Human 10.4 pIC50 = 10.4 Binding
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 164879 0 None - 2 Human 10.4 pIC50 = 10.4 Binding
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 164879 0 None - 2 Human 10.4 pIC50 = 10.4 Binding
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 211105 0 None - 0 Rat 10.3 pIC50 = 10.3 Binding
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 205 28 None 831 2 Rat 10.3 pIC50 = 10.3 Binding
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
858 205 28 None 831 2 Rat 10.3 pIC50 = 10.3 Binding
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 205 28 None 831 2 Rat 10.3 pIC50 = 10.3 Binding
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 172705 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
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 172705 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
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 178132 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
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 178132 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
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 169292 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
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 169292 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
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 188109 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
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 188109 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
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 188131 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
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 188131 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
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 188131 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
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 172254 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
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 172254 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
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 169287 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
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 169287 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
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 171930 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
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 171930 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
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 172209 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
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 172209 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
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 188540 3 None - 0 Human 10.2 pIC50 = 10.2 Binding
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 188540 3 None - 0 Human 10.2 pIC50 = 10.2 Binding
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 169371 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 169371 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 175157 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 175157 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 174282 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 174282 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 173094 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 173094 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 174510 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 174510 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -2 5 Human 10.1 pIC50 = 10.1 Binding
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 205862 40 None -2 5 Human 10.1 pIC50 = 10.1 Binding
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 187597 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 187597 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 187597 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 188028 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 188028 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 188272 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 188272 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 205862 40 None -3 5 Rat 10.1 pIC50 = 10.1 Binding
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 171596 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 171596 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 173790 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 173790 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 171474 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 171474 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
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 123854 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
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 123854 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
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 114944 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
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 114944 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
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 188278 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
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 188278 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
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 173752 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
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 173752 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
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 209023 0 None - 0 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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
864 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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
864 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 205862 40 None -3 5 Rat 10.0 pIC50 = 10 Binding
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 205862 40 None -3 5 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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
864 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 205862 40 None -3 5 Rat 10.0 pIC50 = 10 Binding
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 205862 40 None -3 5 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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
864 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 807 44 None -1 5 Rat 10.0 pIC50 = 10 Binding
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 205862 40 None -3 5 Rat 10.0 pIC50 = 10 Binding
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 205862 40 None -3 5 Rat 10.0 pIC50 = 10 Binding
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 171179 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
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 171179 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
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 169579 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
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 169579 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
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 188042 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
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 188042 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
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 807 44 None -2 5 Human 10.0 pIC50 = 10.0 Binding
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
864 807 44 None -2 5 Human 10.0 pIC50 = 10.0 Binding
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 807 44 None -2 5 Human 10.0 pIC50 = 10.0 Binding
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 807 44 None -2 5 Human 10.0 pIC50 = 10.0 Binding
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 807 44 None -2 5 Human 10.0 pIC50 = 10.0 Binding
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 169645 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 169645 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 161007 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 161007 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 170875 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 170875 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 180220 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 180220 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 188189 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 188189 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 188189 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 188189 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 188189 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 188189 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 188189 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 188189 10 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 807 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
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
864 807 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
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 807 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
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 807 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
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 807 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
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 807 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
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
864 807 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
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 807 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
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 807 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
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 807 44 None -2 5 Human 9.9 pIC50 = 9.9 Binding
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 171894 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 171894 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 172339 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 172339 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 188406 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 188406 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
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 173486 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
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 173486 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
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 61524 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
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 61524 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
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 172553 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
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 172553 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
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 211321 0 None - 2 Rat 9.7 pIC50 = 9.7 Binding
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 193138 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
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 193138 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
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 189029 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
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 189029 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
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 172074 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
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 172074 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
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 61580 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
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 61580 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
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 178868 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 178868 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 188025 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 188025 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 188166 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 188166 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 169511 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 169511 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 170276 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 170276 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 167272 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
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 167272 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
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 172127 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 172127 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 61570 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 61570 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 78089 1 None - 0 Rat 9.6 pIC50 = 9.6 Binding
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 78089 1 None - 0 Rat 9.6 pIC50 = 9.6 Binding
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 175494 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 175494 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 174354 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 174354 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
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 807 44 None -1 5 Guinea pig 9.6 pIC50 = 9.6 Binding
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
864 807 44 None -1 5 Guinea pig 9.6 pIC50 = 9.6 Binding
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 807 44 None -1 5 Guinea pig 9.6 pIC50 = 9.6 Binding
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 807 44 None -1 5 Guinea pig 9.6 pIC50 = 9.6 Binding
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 807 44 None -1 5 Guinea pig 9.6 pIC50 = 9.6 Binding
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 67327 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
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 67327 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
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 171742 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
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 171742 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
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 171438 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
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 171438 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
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 807 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
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
864 807 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
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 807 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
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 807 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
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 807 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
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 807 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
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
864 807 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
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 807 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
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 807 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
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 807 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
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 67394 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
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 67394 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
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 188050 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
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 188050 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
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 58545 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
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 58545 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
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 807 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
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
864 807 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
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 807 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
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 807 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
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 807 44 None -2 5 Human 9.4 pIC50 = 9.4 Binding
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 807 44 None -1 5 Guinea pig 9.4 pIC50 = 9.4 Binding
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
864 807 44 None -1 5 Guinea pig 9.4 pIC50 = 9.4 Binding
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 807 44 None -1 5 Guinea pig 9.4 pIC50 = 9.4 Binding
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 807 44 None -1 5 Guinea pig 9.4 pIC50 = 9.4 Binding
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 807 44 None -1 5 Guinea pig 9.4 pIC50 = 9.4 Binding
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 181694 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
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 181694 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
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 172077 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
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 172077 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
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 172934 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
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 172934 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
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 172934 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
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 172934 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
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 172934 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
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 172934 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
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 158802 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
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 158802 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
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 67047 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
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 67047 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
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 188122 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
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 188122 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
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 174010 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
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 174010 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
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 205862 40 None -2 5 Human 9.3 pIC50 = 9.3 Binding
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 205862 40 None -2 5 Human 9.3 pIC50 = 9.3 Binding
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 807 44 None -1 5 Rat 9.3 pIC50 = 9.3 Binding
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
864 807 44 None -1 5 Rat 9.3 pIC50 = 9.3 Binding
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 807 44 None -1 5 Rat 9.3 pIC50 = 9.3 Binding
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 807 44 None -1 5 Rat 9.3 pIC50 = 9.3 Binding
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 807 44 None -1 5 Rat 9.3 pIC50 = 9.3 Binding
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 96826 2 None - 0 Human 9.3 pIC50 = 9.3 Binding
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 96826 2 None - 0 Human 9.3 pIC50 = 9.3 Binding
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 96826 2 None - 0 Guinea pig 9.3 pIC50 = 9.3 Binding
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 96826 2 None - 0 Guinea pig 9.3 pIC50 = 9.3 Binding
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 170986 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
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 170986 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
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 170361 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
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 170361 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
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 171006 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
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 171006 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
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 178762 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
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 178762 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
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 2281 45 None - 1 Human 9.3 pIC50 = 9.3 Binding
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 2281 45 None - 1 Human 9.3 pIC50 = 9.3 Binding
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 2281 45 None - 1 Human 9.3 pIC50 = 9.3 Binding
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 2281 45 None - 1 Human 9.3 pIC50 = 9.3 Binding
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 189148 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
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 189148 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
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 127081 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
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 127081 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
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 127081 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
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 127081 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
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 212039 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
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 78007 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
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 78007 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
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 208032 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
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 178783 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
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 178783 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
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 208979 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
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 67397 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
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 67397 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
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 171427 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
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 171427 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
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 807 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
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
864 807 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
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 807 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
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 807 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
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 807 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
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 807 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
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
864 807 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
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 807 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
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 807 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
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 807 44 None -2 5 Human 9.2 pIC50 = 9.2 Binding
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 106761 0 None - 0 Guinea pig 9.2 pIC50 = 9.2 Binding
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 106761 0 None - 0 Guinea pig 9.2 pIC50 = 9.2 Binding
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 3100 11 None - 0 Rat 9.2 pIC50 = 9.2 Binding
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 3100 11 None - 0 Rat 9.2 pIC50 = 9.2 Binding
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 3100 11 None - 0 Rat 9.2 pIC50 = 9.2 Binding
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 205862 40 None -3 5 Rat 9.2 pIC50 = 9.2 Binding
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 205862 40 None -3 5 Rat 9.2 pIC50 = 9.2 Binding
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 205862 40 None -3 5 Rat 9.2 pIC50 = 9.2 Binding
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 205862 40 None -3 5 Rat 9.2 pIC50 = 9.2 Binding
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 205862 40 None -3 5 Rat 9.2 pIC50 = 9.2 Binding
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 205862 40 None -3 5 Rat 9.2 pIC50 = 9.2 Binding
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 171881 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
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 171881 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
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 202975 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 202975 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 202975 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 202975 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 106762 0 None - 0 Guinea pig 9.1 pIC50 = 9.1 Binding
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 106762 0 None - 0 Guinea pig 9.1 pIC50 = 9.1 Binding
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 106762 0 None - 0 Guinea pig 9.1 pIC50 = 9.1 Binding
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 106762 0 None - 0 Guinea pig 9.1 pIC50 = 9.1 Binding
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 1368 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
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 1368 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
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 1368 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
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 1368 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
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 202525 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 202525 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 202913 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 202913 1 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 171172 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
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 171172 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
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 206834 0 None - 3 Human 9.1 pIC50 = 9.1 Binding
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 807 44 None -1 5 Rat 9.1 pIC50 = 9.1 Binding
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
864 807 44 None -1 5 Rat 9.1 pIC50 = 9.1 Binding
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 807 44 None -1 5 Rat 9.1 pIC50 = 9.1 Binding
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 807 44 None -1 5 Rat 9.1 pIC50 = 9.1 Binding
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 807 44 None -1 5 Rat 9.1 pIC50 = 9.1 Binding
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 1368 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
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 1368 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
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 1368 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
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 1368 8 None - 3 Rat 9.1 pIC50 = 9.1 Binding
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 67389 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 67389 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 67392 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 67392 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 73286 2 None 2 2 Human 9.1 pIC50 = 9.1 Binding
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 73286 2 None 2 2 Human 9.1 pIC50 = 9.1 Binding
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 202769 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 202769 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 188482 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 188482 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
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 2025 1 None - 0 Rat 9.0 pIC50 = 9.0 Binding
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 2025 1 None - 0 Rat 9.0 pIC50 = 9.0 Binding
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 2025 1 None - 0 Rat 9.0 pIC50 = 9.0 Binding
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 210559 1 None -8 4 Guinea pig 9.0 pIC50 = 9.0 Binding
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 210559 1 None -8 4 Guinea pig 9.0 pIC50 = 9.0 Binding
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 170626 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
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 170626 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
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 79120 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
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 79120 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
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 96196 0 None - 0 Human 9.0 pIC50 = 9 Binding
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 96196 0 None - 0 Human 9.0 pIC50 = 9 Binding
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 96196 0 None - 0 Guinea pig 9.0 pIC50 = 9 Binding
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 96196 0 None - 0 Guinea pig 9.0 pIC50 = 9 Binding
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 202683 7 None - 0 Rat 9.0 pIC50 = 9 Binding
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 202683 7 None - 0 Rat 9.0 pIC50 = 9 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9 Binding
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
864 807 44 None -1 5 Rat 9.0 pIC50 = 9 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9 Binding
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 14989 0 None - 0 Human 9.0 pIC50 = 9 Binding
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 14989 0 None - 0 Human 9.0 pIC50 = 9 Binding
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 202683 7 None - 0 Rat 9.0 pIC50 = 9 Binding
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 202683 7 None - 0 Rat 9.0 pIC50 = 9 Binding
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 178761 0 None - 0 Human 9.0 pIC50 = 9 Binding
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 178761 0 None - 0 Human 9.0 pIC50 = 9 Binding
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 108014 0 None - 0 Guinea pig 9.0 pIC50 = 9 Binding
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 108014 0 None - 0 Guinea pig 9.0 pIC50 = 9 Binding
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 174686 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
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 174686 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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
864 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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
864 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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
864 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 207564 26 None - 0 Rat 9.0 pIC50 = 9.0 Binding
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 207564 26 None - 0 Rat 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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
864 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 807 44 None -1 5 Rat 9.0 pIC50 = 9.0 Binding
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 108089 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
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 108089 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
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 106846 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
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 106846 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
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 107566 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
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 107566 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
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 108204 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
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 108204 0 None - 0 Guinea pig 9.0 pIC50 = 9.0 Binding
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 67177 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 67177 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 32682 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 32682 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 32682 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 32682 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 171269 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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 171269 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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
864 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 202948 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 202948 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 101781 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 101781 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 77454 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 77454 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 166070 0 None - 0 Guinea pig 8.9 pIC50 = 8.9 Binding
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 166070 0 None - 0 Guinea pig 8.9 pIC50 = 8.9 Binding
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 78091 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 78091 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 174025 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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 174025 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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 182334 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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 182334 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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 106708 0 None - 0 Guinea pig 8.9 pIC50 = 8.9 Binding
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 106708 0 None - 0 Guinea pig 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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
864 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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
864 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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
864 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 807 44 None -2 5 Human 8.9 pIC50 = 8.9 Binding
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 114941 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 114941 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 101781 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 101781 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 211116 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 61569 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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 61569 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
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 202429 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 202429 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 202535 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 202535 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 202918 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 202918 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 107956 0 None - 0 Guinea pig 8.9 pIC50 = 8.9 Binding
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 107956 0 None - 0 Guinea pig 8.9 pIC50 = 8.9 Binding
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 202535 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 202535 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 202535 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 202535 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 202918 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 202918 1 None - 0 Rat 8.9 pIC50 = 8.9 Binding
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 73286 2 None 2 2 Human 8.9 pIC50 = 8.9 Binding
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 73286 2 None 2 2 Human 8.9 pIC50 = 8.9 Binding
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 102620 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
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 102620 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
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 206835 0 None 26 4 Human 8.8 pIC50 = 8.8 Binding
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 9697 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
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 9697 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
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 9697 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
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 9697 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
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 165681 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
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 165681 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
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 9697 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
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 9697 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
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 9697 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
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 9697 2 None -1 2 Rat 8.8 pIC50 = 8.8 Binding
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 206738 0 None - 0 Guinea pig 8.8 pIC50 = 8.8 Binding
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 106690 0 None - 0 Guinea pig 8.8 pIC50 = 8.8 Binding
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 106690 0 None - 0 Guinea pig 8.8 pIC50 = 8.8 Binding
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 26012 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
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 26012 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
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 4829 0 None - 0 Guinea pig 8.8 pIC50 = 8.8 Binding
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 4829 0 None - 0 Guinea pig 8.8 pIC50 = 8.8 Binding
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 911 30 None 4 5 Rat 8.8 pIC50 = 8.8 Binding
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
873 911 30 None 4 5 Rat 8.8 pIC50 = 8.8 Binding
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 911 30 None 4 5 Rat 8.8 pIC50 = 8.8 Binding
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 911 30 None 4 5 Rat 8.8 pIC50 = 8.8 Binding
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 26012 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
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 26012 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
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 26012 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
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 26012 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
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 110936 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
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 110936 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
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 178738 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 178738 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 180947 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 180947 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 189057 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 189057 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 189208 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 189208 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 861 2 None -2 2 Human 8.7 pIC50 = 8.7 Binding
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 861 2 None -2 2 Human 8.7 pIC50 = 8.7 Binding
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 861 2 None -2 2 Human 8.7 pIC50 = 8.7 Binding
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 861 2 None -2 2 Human 8.7 pIC50 = 8.7 Binding
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 121166 0 None - 0 Human 8.0 pIC50 = 8 Binding
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 121166 0 None - 0 Human 8.0 pIC50 = 8 Binding
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 73286 2 None 2 2 Human 8.0 pIC50 = 8 Binding
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 73286 2 None 2 2 Human 8.0 pIC50 = 8 Binding
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 206832 0 None -12 4 Human 8.0 pIC50 = 8 Binding
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 115569 1 None - 0 Rat 8.0 pIC50 = 8 Binding
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 115569 1 None - 0 Rat 8.0 pIC50 = 8 Binding
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 104379 0 None - 0 Rat 8.0 pIC50 = 8 Binding
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 104379 0 None - 0 Rat 8.0 pIC50 = 8 Binding
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 107792 0 None - 0 Guinea pig 8.0 pIC50 = 8 Binding
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 107792 0 None - 0 Guinea pig 8.0 pIC50 = 8 Binding
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 5060 0 None - 0 Human 8.0 pIC50 = 8 Binding
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 5060 0 None - 0 Human 8.0 pIC50 = 8 Binding
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 104379 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
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 104379 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
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 204806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 204806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 10654 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
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 10654 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
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 67382 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
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 67382 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
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 204806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 204806 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 102721 0 None - 0 Rat 7.0 pIC50 = 7 Binding
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 102721 0 None - 0 Rat 7.0 pIC50 = 7 Binding
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 168715 0 None - 0 Rat 7.0 pIC50 = 7 Binding
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 168715 0 None - 0 Rat 7.0 pIC50 = 7 Binding
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 106105 0 None - 0 Guinea pig 7.0 pIC50 = 7 Binding
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 106105 0 None - 0 Guinea pig 7.0 pIC50 = 7 Binding
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 119017 0 None - 0 Human 7.0 pIC50 = 7 Binding
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 119017 0 None - 0 Human 7.0 pIC50 = 7 Binding
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 101600 0 None - 1 Human 7.0 pIC50 = 7 Binding
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 101600 0 None - 1 Human 7.0 pIC50 = 7 Binding
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 101847 0 None - 1 Human 7.0 pIC50 = 7 Binding
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 101847 0 None - 1 Human 7.0 pIC50 = 7 Binding
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 161776 0 None - 0 Rat 7.0 pIC50 = 7 Binding
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 161776 0 None - 0 Rat 7.0 pIC50 = 7 Binding
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 168715 0 None - 0 Rat 7.0 pIC50 = 7 Binding
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 168715 0 None - 0 Rat 7.0 pIC50 = 7 Binding
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 109222 0 None - 0 Guinea pig 7.0 pIC50 = 7 Binding
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 109222 0 None - 0 Guinea pig 7.0 pIC50 = 7 Binding
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 78168 0 None - 0 Rat 7.0 pIC50 = 7 Binding
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 78168 0 None - 0 Rat 7.0 pIC50 = 7 Binding
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 119816 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 119816 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 197373 0 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
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 197373 0 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
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 164363 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 164363 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 207494 0 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
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 861 2 None -2 2 Human 6.0 pIC50 = 6 Binding
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 861 2 None -2 2 Human 6.0 pIC50 = 6 Binding
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 861 2 None -2 2 Human 6.0 pIC50 = 6 Binding
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 861 2 None -2 2 Human 6.0 pIC50 = 6 Binding
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 73286 2 None 2 2 Human 6.0 pIC50 = 6 Binding
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 73286 2 None 2 2 Human 6.0 pIC50 = 6 Binding
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 73286 2 None 2 2 Human 6.0 pIC50 = 6 Binding
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 73286 2 None 2 2 Human 6.0 pIC50 = 6 Binding
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 49334 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 49334 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 164363 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 164363 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 202926 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 202926 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 120608 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 120608 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 119083 0 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
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 119083 0 None - 0 Guinea pig 6.0 pIC50 = 6 Binding
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 118457 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 118457 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 170041 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 170041 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 119949 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 119949 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 210509 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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 67353 28 None - 0 Guinea pig 5.0 pIC50 = 5 Binding
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 67353 28 None - 0 Guinea pig 5.0 pIC50 = 5 Binding
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 67362 0 None - 0 Guinea pig 5.0 pIC50 = 5 Binding
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 67362 0 None - 0 Guinea pig 5.0 pIC50 = 5 Binding
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 31557 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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 31557 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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 118669 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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 118669 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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 120099 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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 120099 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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 120100 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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 120100 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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 16627 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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 16627 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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 202804 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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 202804 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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 59213 7 None - 0 Rat 4.0 pIC50 = 4 Binding
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 59213 7 None - 0 Rat 4.0 pIC50 = 4 Binding
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 102544 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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 102544 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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 162905 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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 162905 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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 202804 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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 202804 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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 67351 3 None - 0 Guinea pig 4.0 pIC50 = 4 Binding
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 67351 3 None - 0 Guinea pig 4.0 pIC50 = 4 Binding
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 67356 0 None - 0 Guinea pig 4.0 pIC50 = 4 Binding
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 67356 0 None - 0 Guinea pig 4.0 pIC50 = 4 Binding
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 166743 0 None - 0 Guinea pig 4.0 pIC50 = 4 Binding
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 166743 0 None - 0 Guinea pig 4.0 pIC50 = 4 Binding
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 32098 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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 32098 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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 116116 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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 116116 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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 59213 7 None - 0 Rat 4.0 pIC50 = 4 Binding
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 59213 7 None - 0 Rat 4.0 pIC50 = 4 Binding
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 83950 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 83950 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 83950 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 130160 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 130160 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 116540 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 116540 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 196363 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 196363 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 160751 0 None -2089 4 Human 6.0 pIC50 = 6.0 Binding
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 160751 0 None -2089 4 Human 6.0 pIC50 = 6.0 Binding
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 136970 0 None -19498 4 Human 5.0 pIC50 = 5.0 Binding
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 136970 0 None -19498 4 Human 5.0 pIC50 = 5.0 Binding
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 156328 0 None -19952 4 Human 5.0 pIC50 = 5.0 Binding
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 156328 0 None -19952 4 Human 5.0 pIC50 = 5.0 Binding
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 209635 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
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 25809 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 25809 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 73286 2 None 2 2 Human 7.0 pIC50 = 7.0 Binding
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 73286 2 None 2 2 Human 7.0 pIC50 = 7.0 Binding
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 119170 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 119170 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 911 30 None - 5 Human 6.0 pIC50 = 6.0 Binding
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
873 911 30 None - 5 Human 6.0 pIC50 = 6.0 Binding
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 911 30 None - 5 Human 6.0 pIC50 = 6.0 Binding
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 911 30 None - 5 Human 6.0 pIC50 = 6.0 Binding
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 207415 0 None - 3 Human 5.0 pIC50 = 5.0 Binding
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 119031 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 119031 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 17935 10 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 17935 10 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 116263 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 116263 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 78060 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 78060 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 196913 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 196913 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 99698 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 99698 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 205789 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 205789 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 69051 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 69051 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 167319 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 167319 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 85552 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 85552 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 107102 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 107102 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 21931 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 21931 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 120275 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 120275 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 33304 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 33304 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 101862 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 101862 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 202892 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 202892 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 102491 0 None - 1 Mouse 6.0 pIC50 = 6.0 Binding
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 102491 0 None - 1 Mouse 6.0 pIC50 = 6.0 Binding
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 102437 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 102437 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 102585 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 102585 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 207639 0 None -2630 4 Human 6.0 pIC50 = 6.0 Binding
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 67382 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
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 67382 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
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 168901 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
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 168901 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
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 166902 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
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 166902 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
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 211441 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
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 109837 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
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 109837 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
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 27508 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
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 27508 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
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 49334 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 49334 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 99869 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 99869 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 155870 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 155870 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 101862 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 101862 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 155870 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 155870 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 202892 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 202892 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 25979 1 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 25979 1 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 120229 1 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 120229 1 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 155870 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 155870 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 106303 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
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 106303 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
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 162681 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
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 162681 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
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 119760 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 119760 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 100377 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 100377 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 58767 2 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 58767 2 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 102585 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 102585 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 202413 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 202413 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 67331 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 67331 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 67380 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 67380 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 117948 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 117948 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 9923 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 9923 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 164520 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 164520 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 114994 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 114994 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 106307 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 106307 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 108413 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 108413 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 58767 2 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 58767 2 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 119458 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
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 119458 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
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 9424 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
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 9424 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
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 163928 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 163928 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 206705 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
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 77459 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 77459 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 67354 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
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 67354 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
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 196324 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 196324 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 121153 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 121153 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 121153 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 121153 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 10038 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 10038 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 116501 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 116501 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 205653 30 None - 6 Mouse 5.0 pIC50 = 5.0 Binding
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 205653 30 None - 6 Mouse 5.0 pIC50 = 5.0 Binding
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 205653 30 None - 6 Mouse 5.0 pIC50 = 5.0 Binding
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 205653 30 None - 6 Mouse 5.0 pIC50 = 5.0 Binding
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 110973 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 110973 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 88757 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 88757 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 88757 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 196511 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 196511 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 204900 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 204900 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 88757 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 88757 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 88757 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 110155 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 110155 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 9982 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 9982 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 166347 71 None -1 4 Human 4.9 pIC50 = 4.9 Binding
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 166347 71 None -1 4 Human 4.9 pIC50 = 4.9 Binding
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 166347 71 None -1 4 Human 4.9 pIC50 = 4.9 Binding
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 178554 0 None - 0 Guinea pig 4.9 pIC50 = 4.9 Binding
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 178554 0 None - 0 Guinea pig 4.9 pIC50 = 4.9 Binding
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 116569 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 116569 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 99379 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 99379 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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
14208313 67383 0 None - 0 Rat 3.9 pIC50 = 3.9 Binding
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
CHEMBL1907842 67383 0 None - 0 Rat 3.9 pIC50 = 3.9 Binding
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
44591978 183317 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 183317 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 32969 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 32969 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 119818 16 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 119818 16 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 49381 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 49381 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 118045 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 118045 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 99982 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 99982 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 45069 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 45069 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 161506 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 161506 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 9791 7 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
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 9791 7 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
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 140202 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 140202 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 9791 7 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
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 9791 7 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
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 78008 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 78008 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 120074 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 120074 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 120074 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 167461 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 167461 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 861 2 None - 2 Rat 7.9 pIC50 = 7.9 Binding
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 861 2 None - 2 Rat 7.9 pIC50 = 7.9 Binding
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 861 2 None - 2 Rat 7.9 pIC50 = 7.9 Binding
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 861 2 None - 2 Rat 7.9 pIC50 = 7.9 Binding
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 193000 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 193000 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 140296 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 140296 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 202802 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 202802 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 109950 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 109950 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 76868 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 76868 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 47731 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 47731 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 28182 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 28182 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 115735 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 115735 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 106325 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 106325 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 106331 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 106331 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 102696 0 None - 1 Mouse 6.9 pIC50 = 6.9 Binding
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 102696 0 None - 1 Mouse 6.9 pIC50 = 6.9 Binding
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 112987 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 112987 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 202802 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 202802 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 167212 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 167212 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 118523 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 118523 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 205765 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 205765 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 45768 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 45768 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 196191 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 196191 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 59145 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 59145 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 119083 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 119083 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 118523 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 118523 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 161163 13 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 161163 13 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 205765 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 205765 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 209848 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 85556 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 85556 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 209373 0 None - 0 Guinea pig 4.9 pIC50 = 4.9 Binding
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 66725 0 None - 0 Mouse 4.9 pIC50 = 4.9 Binding
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 66725 0 None - 0 Mouse 4.9 pIC50 = 4.9 Binding
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 67384 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 67384 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 98867 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 98867 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 205474 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 205474 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 124524 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 124524 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 25275 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 25275 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 98601 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 98601 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 78104 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 78104 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 118912 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 118912 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 205824 3 None - 1 Guinea pig 4.9 pIC50 = 4.9 Binding
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 205824 3 None - 1 Guinea pig 4.9 pIC50 = 4.9 Binding
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 168090 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 168090 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 39172 6 None -12 2 Human 6.9 pIC50 = 6.9 Binding
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 39172 6 None -12 2 Human 6.9 pIC50 = 6.9 Binding
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 206829 0 None 1 4 Human 6.9 pIC50 = 6.9 Binding
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 96569 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 96569 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 16479 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 16479 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 98399 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 98399 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 170040 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 170040 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 76921 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
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 76921 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
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 196655 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 196655 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 17935 10 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 17935 10 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 49334 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 49334 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 106625 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 106625 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 11610 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 11610 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 11610 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 84611 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 84611 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 110001 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 110001 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 61572 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 61572 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 109870 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
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 109870 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
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 187830 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 187830 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 106328 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
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 106328 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
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 204809 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 204809 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 204809 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 204809 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 111095 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 111095 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 114939 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 114939 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 58908 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 58908 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 96175 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 96175 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 206493 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 206493 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 100073 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 100073 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 24918 1 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 24918 1 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 188091 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 188091 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 106314 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 106314 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 197017 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 197017 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 200225 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 200225 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 9426 1 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 9426 1 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 16632 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 16632 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 117547 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 117547 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 108858 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 108858 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 105644 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 105644 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 204358 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 204358 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 202786 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 202786 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 156777 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 156777 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 156777 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 25844 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 25844 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 28872 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 28872 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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
14208312 77454 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 437 3 1 3 4.3 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2092865 77454 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 437 3 1 3 4.3 CN1C(=O)[C@@H](NC(=O)c2ccc(C(F)(F)F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44356710 116098 6 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 116098 6 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 99417 0 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
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 99488 0 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
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 99488 0 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
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 4617 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 4617 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 4971 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 4971 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 4986 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 4986 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 108755 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 108755 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 162923 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 162923 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 42166 9 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 42166 9 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 165073 0 None - 0 Mouse 4.9 pIC50 = 4.9 Binding
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 165073 0 None - 0 Mouse 4.9 pIC50 = 4.9 Binding
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 16163 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 16163 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 202834 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 202834 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 30493 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 30493 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 195011 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 195011 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 17935 10 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 17935 10 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 82797 0 None -33 4 Human 6.9 pIC50 = 6.9 Binding
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 82797 0 None -33 4 Human 6.9 pIC50 = 6.9 Binding
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 167427 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 167427 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 167427 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 167427 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 196425 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 196425 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 99735 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 99735 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 49334 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 49334 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 66827 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 66827 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 167715 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 167715 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 117543 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 117543 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 99103 9 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 99103 9 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 99103 9 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 99103 9 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 49174 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 49174 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 112244 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 112244 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 118841 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 118841 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 162859 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 162859 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 58729 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 58729 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 99404 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 99404 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 209982 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
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 209382 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
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 99404 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 99404 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 26713 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 26713 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 181840 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 181840 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 100231 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
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 100231 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
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 100304 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
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 100304 0 None - 0 Guinea pig 7.9 pIC50 = 7.9 Binding
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 211902 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 5060 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 5060 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 111004 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 111004 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 73286 2 None - 2 Rat 7.8 pIC50 = 7.8 Binding
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 73286 2 None - 2 Rat 7.8 pIC50 = 7.8 Binding
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 118700 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 118700 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 205922 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 205922 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 160737 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 160737 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 160737 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 160737 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 120237 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 120237 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 207439 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 119273 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 119273 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 180942 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 180942 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 106306 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 106306 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 106326 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 106326 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 167412 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 167412 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 58890 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
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 58890 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
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 120689 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 120689 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 101626 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 101626 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 119798 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 119798 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 32822 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 32822 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 25671 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 25671 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 28471 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 28471 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 98996 12 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 98996 12 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 109266 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 109266 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 162760 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 162760 0 None - 0 Guinea pig 5.9 pIC50 = 5.9 Binding
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 16339 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 16339 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 101426 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 101426 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 118231 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 118231 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 99663 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 99663 0 None - 0 Guinea pig 6.9 pIC50 = 6.9 Binding
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 101626 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 101626 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 28950 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 28950 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 88757 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 88757 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 88757 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 119443 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 119443 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 16390 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 16390 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 112579 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 112579 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 26139 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 26139 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 119007 13 None - 10 Rat 6.8 pIC50 = 6.8 Binding
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 119007 13 None - 10 Rat 6.8 pIC50 = 6.8 Binding
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 4039 33 None - 1 Rat 6.8 pIC50 = 6.8 Binding
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 4039 33 None - 1 Rat 6.8 pIC50 = 6.8 Binding
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 4039 33 None - 1 Rat 6.8 pIC50 = 6.8 Binding
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 4039 33 None - 1 Rat 6.8 pIC50 = 6.8 Binding
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 4039 33 None - 1 Rat 6.8 pIC50 = 6.8 Binding
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 4039 33 None - 1 Rat 6.8 pIC50 = 6.8 Binding
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 164682 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 164682 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 108963 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
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 108963 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
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 168090 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 168090 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 57203 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 57203 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 18448 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 18448 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 178243 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
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 178243 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
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 106119 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 106119 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 17939 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 17939 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 67387 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 67387 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 202925 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 202925 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 78170 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 78170 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 199554 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 199554 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 202925 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 202925 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 861 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
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 861 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
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 861 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
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 861 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
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 127081 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 127081 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 79233 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 79233 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 56208 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 56208 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 88940 0 None - 2 Human 7.8 pIC50 = 7.8 Binding
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 88940 0 None - 2 Human 7.8 pIC50 = 7.8 Binding
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 69050 0 None - 2 Rat 7.8 pIC50 = 7.8 Binding
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 69050 0 None - 2 Rat 7.8 pIC50 = 7.8 Binding
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 120475 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 120475 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 208522 0 None -16 4 Human 7.8 pIC50 = 7.8 Binding
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 202689 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 202689 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 98367 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 98367 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 206446 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 206446 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 206478 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 206478 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 202440 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 202440 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 12878 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 12878 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 12878 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 105453 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 105453 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 202434 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 202434 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 9910 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 9910 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 110020 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 110020 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 4904 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 4904 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 78027 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 78027 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 28859 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 28859 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 210874 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 208425 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
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 164885 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 164885 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 98916 0 None - 1 Mouse 4.8 pIC50 = 4.8 Binding
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 98916 0 None - 1 Mouse 4.8 pIC50 = 4.8 Binding
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 30032 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 30032 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 196190 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 196190 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 5060 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 5060 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 102619 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 102619 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 102619 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 102619 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 22438 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 22438 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 204231 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 204231 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 15075 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 15075 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 29927 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 29927 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 77943 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 77943 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 5060 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 5060 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 121436 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 121436 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 106799 0 None 5 2 Human 6.8 pIC50 = 6.8 Binding
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 106799 0 None 5 2 Human 6.8 pIC50 = 6.8 Binding
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 106799 0 None 5 2 Human 6.8 pIC50 = 6.8 Binding
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 106799 0 None 5 2 Human 6.8 pIC50 = 6.8 Binding
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 205533 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 205533 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 162768 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 162768 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 78476 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 78476 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 4573 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 4573 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 116231 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 116231 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 28880 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 28880 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 112341 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 112341 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 205653 30 None -1174 6 Human 6.8 pIC50 = 6.8 Binding
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 205653 30 None -1174 6 Human 6.8 pIC50 = 6.8 Binding
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 103310 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 103310 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 111842 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 111842 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 37975 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 37975 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 196723 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 196723 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 118649 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 118649 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 106097 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 106097 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 106108 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 106108 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 214140 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 147041 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 147041 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 214140 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 214140 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 59197 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 59197 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 98241 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
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 98241 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
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 207734 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 180970 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 180970 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 106301 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 106301 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 173346 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 173346 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 207056 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 861 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
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 861 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
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 861 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
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 861 2 None -2 2 Human 7.8 pIC50 = 7.8 Binding
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 61571 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 61571 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 111014 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 111014 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 106106 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 106106 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 109542 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 109542 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 188436 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 188436 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 118658 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 118658 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 78392 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 78392 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 182182 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 182182 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 106309 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 106309 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 120109 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 120109 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 67326 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 67326 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 103310 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 103310 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 57941 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 57941 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 182268 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 182268 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 2200 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
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 2200 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
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 2200 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
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 17751 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 17751 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 44295 1 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 44295 1 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 67365 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
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 67365 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
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 49602 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
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 49602 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
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 2200 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
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 2200 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
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 2200 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
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 2200 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
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 2200 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
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 2200 8 None - 1 Rat 5.8 pIC50 = 5.8 Binding
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 78341 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 78341 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 96542 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 96542 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 99514 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 99514 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 96542 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 96542 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 61523 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 61523 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 58550 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 58550 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 87050 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
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 87050 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
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 74131 1 None - 2 Guinea pig 4.8 pIC50 = 4.8 Binding
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 74131 1 None - 2 Guinea pig 4.8 pIC50 = 4.8 Binding
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 61517 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 61517 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 110038 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 110038 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 78167 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 78167 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 28378 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 28378 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 78058 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 78058 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 861 2 None -2 2 Human 6.8 pIC50 = 6.8 Binding
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 861 2 None -2 2 Human 6.8 pIC50 = 6.8 Binding
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 861 2 None -2 2 Human 6.8 pIC50 = 6.8 Binding
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 861 2 None -2 2 Human 6.8 pIC50 = 6.8 Binding
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 172539 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 172539 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 99375 0 None - 1 Mouse 5.8 pIC50 = 5.8 Binding
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 99375 0 None - 1 Mouse 5.8 pIC50 = 5.8 Binding
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 30545 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 30545 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 17541 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 17541 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 96044 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 96044 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 5060 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 5060 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 78390 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 78390 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 73276 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 73276 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 73286 2 None - 2 Rat 6.8 pIC50 = 6.8 Binding
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 73286 2 None - 2 Rat 6.8 pIC50 = 6.8 Binding
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 178317 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
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 178317 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
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 67396 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 67396 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 202814 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 202814 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 119572 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 119572 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 99897 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 99897 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 17937 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 17937 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 108707 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 108707 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 101270 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 101270 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 181362 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 181362 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 120101 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 120101 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 111144 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 111144 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 111029 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 111029 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 61525 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 61525 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 106107 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 106107 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 209375 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 84960 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 84960 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 2303 20 None - 1 Rat 6.8 pIC50 = 6.8 Binding
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 2303 20 None - 1 Rat 6.8 pIC50 = 6.8 Binding
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 2303 20 None - 1 Rat 6.8 pIC50 = 6.8 Binding
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 119291 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 119291 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 76881 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 76881 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 119048 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 119048 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 28417 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 28417 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 58186 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 58186 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 78202 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 78202 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 204629 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 204629 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 67396 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 67396 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 202814 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 202814 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 112337 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 112337 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 5026 0 None 1 2 Guinea pig 5.8 pIC50 = 5.8 Binding
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 5026 0 None 1 2 Guinea pig 5.8 pIC50 = 5.8 Binding
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 202921 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 202921 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 67360 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
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 67360 0 None - 0 Guinea pig 4.8 pIC50 = 4.8 Binding
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 12069 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 12069 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 12069 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 16727 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 16727 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 168065 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 168065 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 96905 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 96905 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 61527 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 61527 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 22573 37 None - 2 Rat 5.8 pIC50 = 5.8 Binding
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 22573 37 None - 2 Rat 5.8 pIC50 = 5.8 Binding
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 11956 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 11956 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 11956 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 100073 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 100073 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 103888 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 103888 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 196293 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 196293 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 197377 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 197377 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 197377 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 197377 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 79290 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 79290 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 99391 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 99391 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 202447 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 202447 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 109148 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 109148 0 None - 0 Guinea pig 7.8 pIC50 = 7.8 Binding
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 2303 20 None - 1 Rat 7.8 pIC50 = 7.8 Binding
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 2303 20 None - 1 Rat 7.8 pIC50 = 7.8 Binding
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 2303 20 None - 1 Rat 7.8 pIC50 = 7.8 Binding
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 120074 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 120074 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 120074 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 32789 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 32789 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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 98627 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 98627 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 10158 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 10158 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 100073 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 100073 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 9459 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 9459 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 118473 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 118473 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 25553 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 25553 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 106300 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 106300 0 None - 0 Guinea pig 6.8 pIC50 = 6.8 Binding
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 209423 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 214069 6 None -1288 3 Guinea pig 5.8 pIC50 = 5.8 Binding
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 12774 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 12774 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 12774 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 214069 6 None -1288 3 Guinea pig 5.8 pIC50 = 5.8 Binding
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 214069 6 None -1288 3 Guinea pig 5.8 pIC50 = 5.8 Binding
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 214069 6 None - 3 Rat 5.8 pIC50 = 5.8 Binding
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 103888 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 103888 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 214069 6 None -1288 3 Guinea pig 5.8 pIC50 = 5.8 Binding
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 197377 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 197377 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 214069 6 None -1288 3 Guinea pig 5.8 pIC50 = 5.8 Binding
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 4383 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 4383 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 4476 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 4476 0 None - 0 Guinea pig 5.8 pIC50 = 5.8 Binding
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 214069 6 None -1288 3 Guinea pig 5.8 pIC50 = 5.8 Binding
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 85555 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 85555 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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 22934 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 22934 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 76184 1 None - 1 Rat 4.8 pIC50 = 4.8 Binding
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 76184 1 None - 1 Rat 4.8 pIC50 = 4.8 Binding
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 99999 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
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 99999 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
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 46018 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 46018 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 10004 12 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 10004 12 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 196157 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 196157 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 85548 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 85548 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 12728 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 12728 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 12728 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 106859 3 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 106859 3 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 32792 3 None - 1 Rat 6.7 pIC50 = 6.7 Binding
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 32792 3 None - 1 Rat 6.7 pIC50 = 6.7 Binding
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 106859 3 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 106859 3 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 32792 3 None - 1 Rat 6.7 pIC50 = 6.7 Binding
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 32792 3 None - 1 Rat 6.7 pIC50 = 6.7 Binding
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 196675 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 196675 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 49334 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 49334 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 16935 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 16935 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 119859 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 119859 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 138720 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 138720 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 25771 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 25771 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 106114 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 106114 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 9426 1 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 9426 1 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 99824 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 99824 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 106114 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 106114 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 61573 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 61573 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 67390 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 67390 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 77460 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 77460 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 108232 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 108232 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 9426 1 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 9426 1 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 100508 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 100508 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 67390 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 67390 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 171055 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 171055 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 17936 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 17936 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 119394 1 None - 1 Rat 7.7 pIC50 = 7.7 Binding
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 119394 1 None - 1 Rat 7.7 pIC50 = 7.7 Binding
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 102409 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 102409 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 164685 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 164685 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 102180 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 102180 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 206833 0 None -138 4 Human 7.7 pIC50 = 7.7 Binding
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 209461 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 199009 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 199009 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 207564 26 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
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 207564 26 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
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 120226 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 120226 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 9905 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
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 9905 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
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 25457 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 25457 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 188995 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 188995 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 96464 0 None - 1 Mouse 6.7 pIC50 = 6.7 Binding
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 96464 0 None - 1 Mouse 6.7 pIC50 = 6.7 Binding
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 98707 0 None - 1 Mouse 6.7 pIC50 = 6.7 Binding
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 98707 0 None - 1 Mouse 6.7 pIC50 = 6.7 Binding
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 107287 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 107287 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 202395 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 202395 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 205 28 None - 2 Human 5.7 pIC50 = 5.7 Binding
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
858 205 28 None - 2 Human 5.7 pIC50 = 5.7 Binding
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 205 28 None - 2 Human 5.7 pIC50 = 5.7 Binding
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 163291 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
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 163291 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
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 51329 1 None - 0 Guinea pig 4.7 pIC50 = 4.7 Binding
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 51329 1 None - 0 Guinea pig 4.7 pIC50 = 4.7 Binding
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 136409 0 None -2344 4 Human 5.7 pIC50 = 5.7 Binding
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 136409 0 None -2344 4 Human 5.7 pIC50 = 5.7 Binding
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 82807 0 None -870 3 Human 5.7 pIC50 = 5.7 Binding
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 82807 0 None -870 3 Human 5.7 pIC50 = 5.7 Binding
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 101751 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 101751 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 167972 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 167972 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 78404 6 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 78404 6 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 210508 0 None -11 4 Human 5.7 pIC50 = 5.7 Binding
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 2307 60 None - 1 Human 6.7 pIC50 = 6.7 Binding
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 2307 60 None - 1 Human 6.7 pIC50 = 6.7 Binding
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 2307 60 None - 1 Human 6.7 pIC50 = 6.7 Binding
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 2307 60 None - 1 Human 6.7 pIC50 = 6.7 Binding
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 120551 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 120551 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 74131 1 None 501 2 Human 6.7 pIC50 = 6.7 Binding
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 74131 1 None 501 2 Human 6.7 pIC50 = 6.7 Binding
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 87050 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 87050 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 74131 1 None - 2 Rat 6.7 pIC50 = 6.7 Binding
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 74131 1 None - 2 Rat 6.7 pIC50 = 6.7 Binding
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 74131 1 None - 2 Rat 6.7 pIC50 = 6.7 Binding
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 74131 1 None - 2 Rat 6.7 pIC50 = 6.7 Binding
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 74131 1 None - 2 Rat 6.7 pIC50 = 6.7 Binding
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 74131 1 None - 2 Rat 6.7 pIC50 = 6.7 Binding
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 99396 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 99396 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 99396 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 206097 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 206097 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 198996 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 198996 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 118817 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 118817 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 102652 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 102652 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 47281 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 47281 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 202865 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 202865 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 17938 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
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 17938 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
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 61579 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 61579 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 163298 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
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 163298 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
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 205653 30 None -2570 6 Guinea pig 8.7 pIC50 = 8.7 Binding
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 205653 30 None -2570 6 Guinea pig 8.7 pIC50 = 8.7 Binding
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 102513 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
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 102513 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
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 85677 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
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 85677 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
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 102513 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
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 102513 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
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 127081 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 127081 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 112594 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
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 112594 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
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 160770 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
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 160770 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
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 111825 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
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 111825 0 None - 0 Guinea pig 8.7 pIC50 = 8.7 Binding
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 173060 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 173060 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
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 154591 1 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 154591 1 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 154591 1 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 154591 1 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 206720 0 None - 0 Guinea pig 8.6 pIC50 = 8.6 Binding
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 189116 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 189116 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 208805 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 61520 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 61520 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 61521 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 61521 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 67394 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 67394 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 182195 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 182195 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 77458 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 77458 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 207438 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 173435 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 173435 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
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 141284 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 141284 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 163009 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 163009 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 2965 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
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 2965 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
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 2965 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
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 2965 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
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 2965 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
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 2965 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
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 2965 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
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 2965 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
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 112089 0 None - 0 Guinea pig 8.6 pIC50 = 8.6 Binding
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 112089 0 None - 0 Guinea pig 8.6 pIC50 = 8.6 Binding
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 2965 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
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 2965 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
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 2965 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
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 2965 7 None - 1 Rat 8.6 pIC50 = 8.6 Binding
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 123854 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 123854 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 114942 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 114942 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
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 67394 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 67394 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 77457 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 77457 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 77458 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 77458 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 78010 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 78010 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 201118 0 None - 0 Guinea pig 8.5 pIC50 = 8.5 Binding
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 201118 0 None - 0 Guinea pig 8.5 pIC50 = 8.5 Binding
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 58726 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 58726 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 99790 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 99790 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 140208 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 140208 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 102409 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 102409 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 164685 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 164685 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 120074 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 120074 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 120074 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 73286 2 None 2 2 Human 7.7 pIC50 = 7.7 Binding
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 73286 2 None 2 2 Human 7.7 pIC50 = 7.7 Binding
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 202916 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 202916 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 155965 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 155965 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 51329 1 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
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 51329 1 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
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 101238 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 101238 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 140237 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 140237 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 102652 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 102652 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 57948 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 57948 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 78172 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 78172 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 50990 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 50990 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 26943 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 26943 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 116267 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 116267 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 171984 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 171984 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 108386 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
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 108386 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
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 116706 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 116706 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 140258 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 140258 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 99356 0 None - 1 Mouse 5.7 pIC50 = 5.7 Binding
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 99356 0 None - 1 Mouse 5.7 pIC50 = 5.7 Binding
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 108273 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
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 108273 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
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 58856 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 58856 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 202865 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 202865 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 27434 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 27434 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 18085 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 18085 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 2361 30 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 2361 30 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 2361 30 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 2361 30 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 2361 30 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 2361 30 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 196914 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 196914 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 9726 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 9726 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 178471 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 178471 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 163951 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 163951 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 104861 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 104861 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 209371 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 17940 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 17940 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 202916 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 202916 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 9525 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 9525 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 161126 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 161126 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 76882 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 76882 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 78389 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 78389 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 161154 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 161154 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 113951 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 113951 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 76883 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 76883 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 27775 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 27775 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 58830 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 58830 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 208186 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
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 25403 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 25403 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 26128 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 26128 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 116151 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 116151 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 106805 0 None - 1 Mouse 5.7 pIC50 = 5.7 Binding
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 106805 0 None - 1 Mouse 5.7 pIC50 = 5.7 Binding
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 209130 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 103671 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 103671 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 174574 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 174574 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 96029 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 96029 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 106117 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 106117 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 106117 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 106117 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 106117 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 106117 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 2303 20 None - 1 Rat 7.7 pIC50 = 7.7 Binding
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 2303 20 None - 1 Rat 7.7 pIC50 = 7.7 Binding
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 2303 20 None - 1 Rat 7.7 pIC50 = 7.7 Binding
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 202439 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 202439 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 180751 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 180751 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 106302 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 106302 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 141391 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 141391 0 None - 0 Guinea pig 7.7 pIC50 = 7.7 Binding
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 163947 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 163947 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 861 2 None -2 2 Human 7.7 pIC50 = 7.7 Binding
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 861 2 None -2 2 Human 7.7 pIC50 = 7.7 Binding
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 861 2 None -2 2 Human 7.7 pIC50 = 7.7 Binding
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 861 2 None -2 2 Human 7.7 pIC50 = 7.7 Binding
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 113098 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 113098 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 123515 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 123515 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 10149 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 10149 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 10149 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 10149 0 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 1857 5 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 1857 5 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 1857 5 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 1857 5 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 1857 5 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 1857 5 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 197863 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
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 197863 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
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 209378 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
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 162419 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 162419 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 101461 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 101461 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 103671 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 103671 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 120980 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 120980 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 162419 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 162419 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 106317 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
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 106317 0 None - 0 Guinea pig 6.7 pIC50 = 6.7 Binding
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 2303 20 None - 1 Guinea pig 5.7 pIC50 = 5.7 Binding
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 2303 20 None - 1 Guinea pig 5.7 pIC50 = 5.7 Binding
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 2303 20 None - 1 Guinea pig 5.7 pIC50 = 5.7 Binding
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 32105 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 32105 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 58767 2 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 58767 2 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 4513 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
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 4513 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
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 5007 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
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 5007 0 None - 0 Guinea pig 5.7 pIC50 = 5.7 Binding
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 101479 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 101479 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 172170 0 None - 0 Guinea pig 4.7 pIC50 = 4.7 Binding
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 172170 0 None - 0 Guinea pig 4.7 pIC50 = 4.7 Binding
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 32014 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 32014 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 114830 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 114830 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 116347 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 116347 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 29865 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 29865 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 204946 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 204946 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 116208 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 116208 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 167462 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 167462 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 106101 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 106101 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 206700 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 206700 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 206700 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 206425 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 206425 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 10013 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 10013 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 208030 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 861 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
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 861 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
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 861 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
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 861 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
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 209374 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
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 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
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 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
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 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
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 58868 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 58868 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 51329 1 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 51329 1 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
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 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
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 167412 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
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 167412 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
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 114995 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 114995 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 117932 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 117932 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 67359 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
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 67359 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
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 167734 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 167734 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 5060 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 5060 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 205593 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 205593 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 111084 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 111084 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 9691 0 None - 1 Rat 5.6 pIC50 = 5.6 Binding
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 9691 0 None - 1 Rat 5.6 pIC50 = 5.6 Binding
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 167278 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 167278 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 108327 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 108327 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 101636 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 101636 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 119858 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 119858 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 17938 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 17938 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 5060 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 5060 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 101636 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 101636 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 25905 6 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 25905 6 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 25921 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 25921 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 4535 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
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 4535 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
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 29085 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 29085 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 58885 0 None - 0 Mouse 4.6 pIC50 = 4.6 Binding
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 58885 0 None - 0 Mouse 4.6 pIC50 = 4.6 Binding
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 116025 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 116025 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 98099 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 98099 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 17941 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 17941 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 202863 28 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 202863 28 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 208428 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
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 73275 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 73275 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 61519 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 61519 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 16050 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 16050 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2965 7 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2965 7 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2965 7 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2965 7 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 2963 6 None - 1 Rat 7.6 pIC50 = 7.6 Binding
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 72107 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 72107 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 100281 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 100281 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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
10507109 108727 0 None - 2 Rat 6.6 pIC50 = 6.6 Binding
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 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/s0960-894x(98)00548-4
CHEMBL321761 108727 0 None - 2 Rat 6.6 pIC50 = 6.6 Binding
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 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/s0960-894x(98)00548-4
44381593 119953 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 854 23 9 10 3.3 CN(C(=O)[C@H](CC(=O)O)NNC[C@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
CHEMBL354171 119953 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 854 23 9 10 3.3 CN(C(=O)[C@H](CC(=O)O)NNC[C@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
14208309 67330 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
CHEMBL1907664 67330 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
44370393 119126 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 492 14 2 3 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCCC1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL346784 119126 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 492 14 2 3 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCCC1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
14991541 106312 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 843 22 8 8 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144546 106312 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 843 22 8 8 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
10369442 108047 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 521 7 3 5 3.6 Cc1cccc(NC(=O)N[C@H](COC(=O)N2CCCC2)C(=O)N2CCC(C(=O)Nc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL320154 108047 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 521 7 3 5 3.6 Cc1cccc(NC(=O)N[C@H](COC(=O)N2CCCC2)C(=O)N2CCC(C(=O)Nc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44367000 119178 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 494 6 2 4 5.1 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
CHEMBL347329 119178 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 494 6 2 4 5.1 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
89913427 140180 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 311 2 1 2 3.4 O=C1C=C(Cl)C(O)(c2ccc(Cl)cc2)N1C1CCCC1 10.1039/C6MD00052E
CHEMBL3817873 140180 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 311 2 1 2 3.4 O=C1C=C(Cl)C(O)(c2ccc(Cl)cc2)N1C1CCCC1 10.1039/C6MD00052E
89913617 140203 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 223 1 1 2 1.4 CN1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
CHEMBL3818165 140203 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 223 1 1 2 1.4 CN1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
71458029 78365 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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)NCC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL2112692 78365 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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)NCC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
15104620 110859 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
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)Nc1ccc(C)cc1 10.1021/jm00116a002
CHEMBL326979 110859 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
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)Nc1ccc(C)cc1 10.1021/jm00116a002
14802537 58759 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
CHEMBL169615 58759 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
10052234 67405 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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)N[C@H]1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00078a018
CHEMBL1907927 67405 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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)N[C@H]1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00078a018
44280115 106730 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 658 11 3 6 5.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL31671 106730 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 658 11 3 6 5.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44329519 107788 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
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 6 3 3 6.6 Cc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(C(F)(F)F)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
CHEMBL319748 107788 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
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 6 3 3 6.6 Cc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(C(F)(F)F)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
44334259 4390 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
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 8 2 3 4.8 CCCC[C@@H](NC(=O)Nc1cccc(C)c1)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
CHEMBL101803 4390 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
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 8 2 3 4.8 CCCC[C@@H](NC(=O)Nc1cccc(C)c1)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
13953694 188769 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 523 3 1 4 6.8 Fc1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)c2nnc(C(Cl)(Cl)Cl)n2-c2ccccc21 10.1021/jm00396a028
CHEMBL51280 188769 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 523 3 1 4 6.8 Fc1ccccc1C1=N[C@H](Cc2c[nH]c3ccccc23)c2nnc(C(Cl)(Cl)Cl)n2-c2ccccc21 10.1021/jm00396a028
44368567 168159 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 495 9 4 4 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1F)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL437039 168159 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 495 9 4 4 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1F)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
44365359 120762 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 546 12 3 5 4.5 COc1ccc(N(C(=O)CN(C(=O)[C@@H](CCC(=O)O)NC(=O)Nc2ccccc2)c2ccccc2)C(C)C)cc1 10.1016/S0960-894X(97)00062-0
CHEMBL357983 120762 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 546 12 3 5 4.5 COc1ccc(N(C(=O)CN(C(=O)[C@@H](CCC(=O)O)NC(=O)Nc2ccccc2)c2ccccc2)C(C)C)cc1 10.1016/S0960-894X(97)00062-0
44283246 99487 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 8 2 4 6.8 O=C(NC(Cc1c[nH]c2ccccc12)C1CN=C(CCc2ccccc2)S1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL286442 99487 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 8 2 4 6.8 O=C(NC(Cc1c[nH]c2ccccc12)C1CN=C(CCc2ccccc2)S1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
10722372 119063 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(C(=O)O)cc1 10.1021/jm950626d
CHEMBL346179 119063 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 605 8 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(C(=O)O)cc1 10.1021/jm950626d
CHEMBL1172251 206831 0 None -229 4 Human 5.6 pIC50 = 5.6 Binding
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](Cc1ccccc1)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
44327698 205730 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 572 10 2 6 4.7 COC(=O)CN(CCc1ccccn1)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
CHEMBL94298 205730 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 572 10 2 6 4.7 COC(=O)CN(CCc1ccccn1)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
44348869 16215 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 407 7 3 4 2.6 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCC2)C1 10.1021/jm00079a003
CHEMBL123089 16215 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 407 7 3 4 2.6 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCC2)C1 10.1021/jm00079a003
9850184 110369 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 538 6 2 6 4.6 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N3CCCC3)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm960669+
CHEMBL326102 110369 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 538 6 2 6 4.6 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N3CCCC3)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm960669+
11154528 196249 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 426 7 3 3 3.7 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)C1=Cc2ccccc2C1 10.1016/j.bmc.2009.05.067
CHEMBL573136 196249 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 426 7 3 3 3.7 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)C1=Cc2ccccc2C1 10.1016/j.bmc.2009.05.067
44349391 116536 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 422 9 3 3 4.2 CCC1(CC)CCC(NC(=O)C(CCC(=O)O)NC(=O)c2cccc(Cl)c2)CC1 10.1021/jm00079a003
CHEMBL339115 116536 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 422 9 3 3 4.2 CCC1(CC)CCC(NC(=O)C(CCC(=O)O)NC(=O)c2cccc(Cl)c2)CC1 10.1021/jm00079a003
10814373 205364 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 474 7 3 8 4.2 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc([N+](=O)[O-])c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL9203 205364 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 474 7 3 8 4.2 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc([N+](=O)[O-])c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
11234811 196696 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 394 7 3 4 3.4 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cccs1 10.1016/j.bmc.2009.05.067
CHEMBL576731 196696 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 394 7 3 4 3.4 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cccs1 10.1016/j.bmc.2009.05.067
10005159 114896 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 475 5 3 4 5.4 CN1C(=O)C(NC(=O)Nc2cccc(Nc3ccccc3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL335017 114896 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 475 5 3 4 5.4 CN1C(=O)C(NC(=O)Nc2cccc(Nc3ccccc3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10550527 205635 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 429 6 3 6 4.2 CCOc1cccc(-n2c(NNC(=O)Nc3cccc(C)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL9377 205635 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 429 6 3 6 4.2 CCOc1cccc(-n2c(NNC(=O)Nc3cccc(C)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
155517868 169633 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 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 169633 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 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
10027443 116019 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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(Cc3ncc[nH]3)C2=O)c1 10.1021/jm00078a018
CHEMBL336221 116019 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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(Cc3ncc[nH]3)C2=O)c1 10.1021/jm00078a018
44283246 99487 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 8 2 4 6.8 O=C(NC(Cc1c[nH]c2ccccc12)C1CN=C(CCc2ccccc2)S1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL286442 99487 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 8 2 4 6.8 O=C(NC(Cc1c[nH]c2ccccc12)C1CN=C(CCc2ccccc2)S1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
10649606 49334 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]BDZ1 from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 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 49334 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]BDZ1 from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 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
15689733 106119 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 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/jm00113a023
CHEMBL3142905 106119 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 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/jm00113a023
CHEMBL319814 209467 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 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
44373740 119374 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 569 8 3 5 5.2 COC(=O)[C@@]1(NC(=O)[C@@](C)(Cc2c[nH]c3ccccc23)NC(=O)OC2C3CC4CC(C3)CC2C4)C[C@H]1c1ccccc1 10.1016/S0960-894X(01)81250-6
CHEMBL349079 119374 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 569 8 3 5 5.2 COC(=O)[C@@]1(NC(=O)[C@@](C)(Cc2c[nH]c3ccccc23)NC(=O)OC2C3CC4CC(C3)CC2C4)C[C@H]1c1ccccc1 10.1016/S0960-894X(01)81250-6
10070678 120229 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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
CHEMBL355092 120229 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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
CHEMBL319814 209467 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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(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/jm00173a006
14888736 97622 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 974 29 10 11 1.2 CSCC[C@H](NC(=O)CCc1ccc(CC(=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
CHEMBL273344 97622 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 974 29 10 11 1.2 CSCC[C@H](NC(=O)CCc1ccc(CC(=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
10479056 25966 11 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 5.0 CN1C(=O)C(NC(=O)Nc2ccc(Cl)c(Cl)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135702 25966 11 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 5.0 CN1C(=O)C(NC(=O)Nc2ccc(Cl)c(Cl)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10070678 120229 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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
CHEMBL355092 120229 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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
44336539 5060 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 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 5060 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 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
52949124 861 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
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 861 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
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 861 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
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 861 2 None -2 2 Human 7.6 pIC50 = 7.6 Binding
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
14519977 119431 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00124a003
CHEMBL349640 119431 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00124a003
44310001 202180 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 415 4 1 3 4.5 Cc1ccc(C(=O)NC[C@H]2CN=C(c3ccc(F)cc3)c3ccc(C)cc3N2C)cc1 10.1021/jm00163a069
CHEMBL68870 202180 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 415 4 1 3 4.5 Cc1ccc(C(=O)NC[C@H]2CN=C(c3ccc(F)cc3)c3ccc(C)cc3N2C)cc1 10.1021/jm00163a069
21842325 119604 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 495 6 2 5 4.5 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL351144 119604 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 495 6 2 5 4.5 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00557-A
135837528 119718 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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(c3ncc[nH]3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL352217 119718 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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(c3ncc[nH]3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL2372075 208426 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
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](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
10349938 162357 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 722 14 4 6 6.7 CC(Cc1c[nH]c2ccc(F)cc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)OCc1ccccc1)c1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL417412 162357 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 722 14 4 6 6.7 CC(Cc1c[nH]c2ccc(F)cc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)OCc1ccccc1)c1ccccc1 10.1016/S0960-894X(97)00356-9
44287086 100010 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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)N(C)CC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL290975 100010 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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)N(C)CC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
44368382 45069 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 45069 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
10719721 205687 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 486 7 3 8 3.8 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(N(C)C)c2)c1 10.1021/jm970373j
CHEMBL9406 205687 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 486 7 3 8 3.8 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(N(C)C)c2)c1 10.1021/jm970373j
44368567 168159 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 495 9 4 4 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1F)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL437039 168159 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 495 9 4 4 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1F)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL2372076 208427 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
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)CCNC(=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
14208255 202952 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 416 4 2 4 3.4 CN(C)c1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
CHEMBL73745 202952 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 416 4 2 4 3.4 CN(C)c1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
52949124 861 2 None -2 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R W6.48A 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 861 2 None -2 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R W6.48A 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 861 2 None -2 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R W6.48A 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 861 2 None -2 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R W6.48A 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
44286816 160215 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 20 7 7 4.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL41142 160215 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 20 7 7 4.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
44286695 160407 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 796 19 7 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL41157 160407 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 796 19 7 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
44592082 178554 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 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 178554 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 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
44300551 195709 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 390 3 2 3 4.1 Cc1cccc(NC(=O)NC2N=C(C3CCCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
CHEMBL56944 195709 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 390 3 2 3 4.1 Cc1cccc(NC(=O)NC2N=C(C3CCCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
46235271 73286 2 None 2 2 Human 7.6 pIC50 = 7.6 Binding
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 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 73286 2 None 2 2 Human 7.6 pIC50 = 7.6 Binding
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 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
15689737 106104 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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)Nc1ccc(Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142701 106104 0 None - 0 Guinea pig 6.6 pIC50 = 6.6 Binding
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)Nc1ccc(Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL354363 209974 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
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)OC(C)(C)C)C(=O)N1CC(=O)N[C@@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
14208255 202952 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 416 4 2 4 3.4 CN(C)c1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL73745 202952 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 416 4 2 4 3.4 CN(C)c1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
443375 205862 40 None - 5 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00164a020
CHEMBL9506 205862 40 None - 5 Guinea pig 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00164a020
9845465 118341 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 5 3 4 3.3 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCO)C2=O)c1 10.1021/jm00078a018
CHEMBL342201 118341 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 5 3 4 3.3 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCO)C2=O)c1 10.1021/jm00078a018
44303664 100229 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 661 16 7 7 0.3 CCCC1C[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)N(C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)CN)C1 10.1016/S0960-894X(01)81005-2
CHEMBL292493 100229 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 661 16 7 7 0.3 CCCC1C[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)N(C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)CN)C1 10.1016/S0960-894X(01)81005-2
CHEMBL3143186 209383 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
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 CCC[C@@H]1CCN(C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)[C@@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00105a068
73354293 106061 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 6 5 4.6 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCP(=O)(O)O)c1ccccc1 10.1021/jm00092a007
CHEMBL314178 106061 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 6 5 4.6 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCP(=O)(O)O)c1ccccc1 10.1021/jm00092a007
44312041 103209 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 498 6 3 5 4.1 CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL308769 103209 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 498 6 3 5 4.1 CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
44382243 59195 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 632 12 4 4 6.1 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL171562 59195 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 632 12 4 4 6.1 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCc1ccccc1 10.1016/S0960-894X(00)80687-3
162666759 181728 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
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 846 23 9 9 2.9 CC(C)C[C@@H](/C=C/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)NC(=O)OC(C)(C)C 10.1021/acs.jmedchem.0c00530
CHEMBL4784305 181728 0 None - 0 Guinea pig 5.6 pIC50 = 5.6 Binding
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 846 23 9 9 2.9 CC(C)C[C@@H](/C=C/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)NC(=O)OC(C)(C)C 10.1021/acs.jmedchem.0c00530
15673154 85554 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 2300 to 3500The 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 2300 to 3500
ChEMBL 650 12 6 5 4.6 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCP(=O)(O)O)c1ccccc1 10.1016/S0960-894X(00)80652-6
CHEMBL2304155 85554 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 2300 to 3500The 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 2300 to 3500
ChEMBL 650 12 6 5 4.6 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCP(=O)(O)O)c1ccccc1 10.1016/S0960-894X(00)80652-6
14208263 202999 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 7 2 3 5.0 CCCCCc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL74170 202999 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 7 2 3 5.0 CCCCCc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
14720389 164520 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
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 164520 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 373 10 3 3 2.8 CCCN(CCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
44381609 128577 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 610 15 6 7 2.5 N#C[C@H](N[C@H](CC(=O)NC(Cc1ccccc1)C(N)=O)C(=O)O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
CHEMBL367057 128577 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 610 15 6 7 2.5 N#C[C@H](N[C@H](CC(=O)NC(Cc1ccccc1)C(N)=O)C(=O)O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
44349298 16435 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 429 8 3 4 3.5 CC(C)c1ccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)cc1 10.1021/jm00079a003
CHEMBL124155 16435 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 429 8 3 4 3.5 CC(C)c1ccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)cc1 10.1021/jm00079a003
44349101 16650 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 468 7 3 3 5.0 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NC1CCC2(CCCCC2)CC1 10.1021/jm00079a003
CHEMBL124805 16650 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 468 7 3 3 5.0 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NC1CCC2(CCCCC2)CC1 10.1021/jm00079a003
44592485 187233 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
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 379 6 4 3 3.3 CC(C)C(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL496066 187233 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
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 379 6 4 3 3.3 CC(C)C(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
42636922 178524 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 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
CHEMBL471870 178524 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 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
11799462 161455 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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)Nc3ccc(C(F)(F)F)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL415965 161455 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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)Nc3ccc(C(F)(F)F)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
10553146 116200 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 491 6 3 3 5.7 CC1CCCCC1NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
CHEMBL337310 116200 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 491 6 3 3 5.7 CC1CCCCC1NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
9821357 17082 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 382 9 3 3 3.2 CC(C)(C)CCCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
CHEMBL125703 17082 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 382 9 3 3 3.2 CC(C)(C)CCCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
45482486 196617 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 Cc1ccc2[nH]c(C(=O)Nc3ccccc3C(=O)NC(Cc3ccccc3)C(=O)O)cc2c1 10.1016/j.bmc.2009.05.067
CHEMBL576020 196617 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 Cc1ccc2[nH]c(C(=O)Nc3ccccc3C(=O)NC(Cc3ccccc3)C(=O)O)cc2c1 10.1016/j.bmc.2009.05.067
44382371 119982 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 436 5 2 4 2.8 COc1cccc(NC(=O)N[C@@H]2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL354442 119982 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 436 5 2 4 2.8 COc1cccc(NC(=O)N[C@@H]2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
14208216 102217 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 393 3 1 4 3.5 CN1C(=O)C(NC(=O)c2ccsc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL304768 102217 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
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 393 3 1 4 3.5 CN1C(=O)C(NC(=O)c2ccsc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
44286378 167541 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
In vitro binding for half maximal inhibition of [125I]- Bolton-Hunter-CCK-8 in guinea pig pancreasIn vitro binding for half maximal inhibition of [125I]- Bolton-Hunter-CCK-8 in guinea pig pancreas
ChEMBL 838 21 7 9 3.0 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1cccnc1)NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00037a006
CHEMBL432864 167541 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
In vitro binding for half maximal inhibition of [125I]- Bolton-Hunter-CCK-8 in guinea pig pancreasIn vitro binding for half maximal inhibition of [125I]- Bolton-Hunter-CCK-8 in guinea pig pancreas
ChEMBL 838 21 7 9 3.0 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1cccnc1)NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00037a006
14991586 100159 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 838 21 7 9 3.0 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1cccnc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL292071 100159 0 None - 0 Guinea pig 7.6 pIC50 = 7.6 Binding
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 838 21 7 9 3.0 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1cccnc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
5279119 203035 1 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 423 3 2 3 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00047a021
CHEMBL74515 203035 1 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 423 3 2 3 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00047a021
5311201 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm020424z
CHEMBL9387 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm020424z
5311201 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00121a004
CHEMBL9387 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00121a004
5311201 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm000937a
CHEMBL9387 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm000937a
5311201 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranes
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)00609-9
CHEMBL9387 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranes
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)00609-9
5311201 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to 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/jm00164a020
CHEMBL9387 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to 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/jm00164a020
5311201 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(00)80684-8
CHEMBL9387 205653 30 None 26 6 Rat 6.6 pIC50 = 6.6 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(00)80684-8
CHEMBL172135 207097 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
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)OC(C)(C)C)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
44409521 139627 4 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 351 5 4 3 2.6 CC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1021/jm051050n
CHEMBL380355 139627 4 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 351 5 4 3 2.6 CC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1021/jm051050n
70697534 77479 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
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 367 3 2 3 4.4 O=C1Nc2ccccc2C(c2ccccc2)=NC1C[C@H]1CNc2ccccc21 10.1021/jm00390a019
CHEMBL2092989 77479 0 None - 0 Guinea pig 4.6 pIC50 = 4.6 Binding
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 367 3 2 3 4.4 O=C1Nc2ccccc2C(c2ccccc2)=NC1C[C@H]1CNc2ccccc21 10.1021/jm00390a019
15167797 31426 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 403 5 2 4 4.4 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)OCc1ccccc1 10.1021/jm00163a069
CHEMBL140495 31426 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 403 5 2 4 4.4 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)OCc1ccccc1 10.1021/jm00163a069
44303233 100175 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 C[C@](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
CHEMBL292194 100175 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 C[C@](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
9985099 116762 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 552 5 3 3 6.0 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2cc(Cl)ccc21 10.1021/jm00048a015
CHEMBL339515 116762 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 552 5 3 3 6.0 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2cc(Cl)ccc21 10.1021/jm00048a015
44592485 187233 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 379 6 4 3 3.3 CC(C)C(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL496066 187233 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 379 6 4 3 3.3 CC(C)C(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
10255357 18317 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1021/jm00048a015
CHEMBL127397 18317 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)NC(C)(C)C)C2=O)c1 10.1021/jm00048a015
10074366 120074 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 120074 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 120074 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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
44368567 168159 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 495 9 4 4 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1F)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL437039 168159 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 495 9 4 4 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1F)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
44349393 16640 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 422 7 3 3 4.3 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCCCCCCCC1 10.1021/jm00079a003
CHEMBL124764 16640 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 422 7 3 3 4.3 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCCCCCCCC1 10.1021/jm00079a003
44381550 164670 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 842 23 11 10 3.0 Cc1ccccc1NC(=O)NCCCC[C@@H](CNN[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)NNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
CHEMBL422919 164670 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 842 23 11 10 3.0 Cc1ccccc1NC(=O)NCCCC[C@@H](CNN[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)NNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
5279119 203035 1 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00120a002
CHEMBL74515 203035 1 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00120a002
15104606 9351 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 497 13 2 2 6.9 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2ccccc2c1 10.1021/jm00116a002
CHEMBL111837 9351 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 497 13 2 2 6.9 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2ccccc2c1 10.1021/jm00116a002
44309988 102182 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 415 4 1 3 4.5 Cc1ccc(C(=O)NC[C@@H]2CN=C(c3ccc(F)cc3)c3ccc(C)cc3N2C)cc1 10.1021/jm00163a069
CHEMBL304546 102182 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 415 4 1 3 4.5 Cc1ccc(C(=O)NC[C@@H]2CN=C(c3ccc(F)cc3)c3ccc(C)cc3N2C)cc1 10.1021/jm00163a069
10698905 205135 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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]c4cc(F)ccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL90697 205135 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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]c4cc(F)ccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
10077842 108587 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 637 8 2 5 5.8 CN(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
CHEMBL321321 108587 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 637 8 2 5 5.8 CN(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
44458068 85321 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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
CHEMBL22918 85321 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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
10047669 78093 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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)Nc2cccc(Cl)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2111924 78093 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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)Nc2cccc(Cl)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14991543 106310 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 22 8 8 3.5 Cc1ccc(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
CHEMBL3144544 106310 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 22 8 8 3.5 Cc1ccc(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
44334248 4597 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 528 8 3 5 4.9 Cc1cccc(NC(=O)N[C@H](COC(=O)Nc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL103312 4597 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 528 8 3 5 4.9 Cc1cccc(NC(=O)N[C@H](COC(=O)Nc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
20190195 30557 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 405 4 1 3 4.1 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1ccccc1F 10.1021/jm00163a069
CHEMBL139615 30557 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 405 4 1 3 4.1 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1ccccc1F 10.1021/jm00163a069
44356619 118278 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 415 4 2 5 3.1 COc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cn1 10.1021/jm00078a018
CHEMBL342142 118278 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 415 4 2 5 3.1 COc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cn1 10.1021/jm00078a018
11799359 28823 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
CHEMBL138084 28823 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
54580264 61514 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 COc1cccc(-c2ncc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773880 61514 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 COc1cccc(-c2ncc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
21842340 43825 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 508 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C3(C)CCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
CHEMBL151483 43825 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 508 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)C3(C)CCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
45482489 196740 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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)c1cc2ccc(F)cc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL577161 196740 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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)c1cc2ccc(F)cc2[nH]1 10.1016/j.bmc.2009.05.067
135703408 142292 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
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 511 4 2 6 6.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(O)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
CHEMBL389311 142292 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
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 511 4 2 6 6.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(O)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
9936789 204853 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 529 7 3 8 5.3 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C(=O)OC(C)(C)C)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL8890 204853 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 529 7 3 8 5.3 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C(=O)OC(C)(C)C)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
9887120 202417 3 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00121a004
CHEMBL70380 202417 3 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00121a004
9887120 202417 3 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm000937a
CHEMBL70380 202417 3 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm000937a
14208237 202503 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 498 6 2 5 3.8 CCOC(=O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL70883 202503 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 498 6 2 5 3.8 CCOC(=O)CN1C(=O)C(NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
10079315 167294 0 None - 0 Guinea pig 8.5 pIC50 = 8.5 Binding
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 859 21 9 7 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL431065 167294 0 None - 0 Guinea pig 8.5 pIC50 = 8.5 Binding
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 859 21 9 7 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL156559 207052 0 None - 0 Guinea pig 8.5 pIC50 = 8.5 Binding
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)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
14888718 76884 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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](Cc1ccc(-c2nn[nH]n2)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
CHEMBL2079606 76884 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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](Cc1ccc(-c2nn[nH]n2)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
10253366 115832 11 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 5.0 CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL335951 115832 11 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 5.0 CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10094138 167756 6 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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)Nc2ccccc2[N+](=O)[O-])N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL434255 167756 6 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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)Nc2ccccc2[N+](=O)[O-])N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
9887120 202417 3 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(00)80684-8
CHEMBL70380 202417 3 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(00)80684-8
155540394 172357 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
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 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 172357 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
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 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
24785179 180944 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human CCK1 receptorInhibition of 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 180944 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human CCK1 receptorInhibition of 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
14991585 100544 0 None - 0 Guinea pig 8.5 pIC50 = 8.5 Binding
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 21 7 10 4.3 CC(=O)Oc1ccc2cc(C(=O)NCCCC[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc3ccccc3)C(N)=O)ccc2c1 10.1021/jm00089a010
CHEMBL294542 100544 0 None - 0 Guinea pig 8.5 pIC50 = 8.5 Binding
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 21 7 10 4.3 CC(=O)Oc1ccc2cc(C(=O)NCCCC[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc3ccccc3)C(N)=O)ccc2c1 10.1021/jm00089a010
14208292 203004 1 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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)c2cccc(Br)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL74228 203004 1 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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)c2cccc(Br)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
14208293 67393 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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)c2cccc(Br)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907851 67393 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
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)c2cccc(Br)c2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
15689729 106102 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 890 20 9 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1Br)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142695 106102 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 890 20 9 8 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1Br)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44386048 61173 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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(=C/c1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80273-5
CHEMBL177081 61173 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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(=C/c1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80273-5
CHEMBL156559 207052 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
44381480 59128 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 825 20 7 8 4.6 Cc1ccccc1NC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
CHEMBL171227 59128 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 825 20 7 8 4.6 Cc1ccccc1NC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
CHEMBL156559 207052 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL156559 207052 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL319340 209460 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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)Nc1ccccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL320868 209473 0 None - 2 Guinea pig 8.4 pIC50 = 8.4 Binding
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 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(N)=O 10.1021/jm00113a023
CHEMBL320868 209473 0 None - 2 Guinea pig 8.4 pIC50 = 8.4 Binding
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 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(N)=O 10.1021/jm960509y
CHEMBL319340 209460 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
CHEMBL320868 209473 0 None - 2 Guinea pig 8.4 pIC50 = 8.4 Binding
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 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(N)=O 10.1021/jm00173a006
44381695 120312 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 811 20 8 8 4.3 Cc1ccccc1NC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
CHEMBL355836 120312 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 811 20 8 8 4.3 Cc1ccccc1NC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(00)80680-0
CHEMBL320868 209473 0 None - 2 Guinea pig 8.4 pIC50 = 8.4 Binding
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 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(N)=O 10.1021/jm00031a013
44398261 123854 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 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 123854 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 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
CHEMBL319340 209460 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80687-3
14991584 161181 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 877 20 8 9 4.1 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)c1ccc2cc(O)ccc2c1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL413768 161181 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 877 20 8 9 4.1 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)c1ccc2cc(O)ccc2c1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
71452818 79289 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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
CHEMBL2115543 79289 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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
CHEMBL317477 209447 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 COC(=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
10074366 120074 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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 120074 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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 120074 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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
11146119 78011 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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
CHEMBL2111550 78011 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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
44382038 119941 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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
CHEMBL354040 119941 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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
903 2963 6 None - 1 Rat 7.5 pIC50 = 7.5 Binding
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 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)80273-5
9850711 2963 6 None - 1 Rat 7.5 pIC50 = 7.5 Binding
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 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)80273-5
CHEMBL138534 2963 6 None - 1 Rat 7.5 pIC50 = 7.5 Binding
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 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)80273-5
CHEMBL2111312 2963 6 None - 1 Rat 7.5 pIC50 = 7.5 Binding
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 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)80273-5
178143 16658 2 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00079a003
CHEMBL124832 16658 2 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 440 14 2 3 5.0 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1021/jm00079a003
44381915 58732 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 454 15 2 3 5.4 CCCCCN(CCCCC)C(=O)[C@@H](CCCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80681-2
CHEMBL169466 58732 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 454 15 2 3 5.4 CCCCCN(CCCCC)C(=O)[C@@H](CCCC(=O)O)NC(=O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80681-2
CHEMBL2079548 207437 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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(=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
24785430 181692 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human CCK1 receptorInhibition of 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 181692 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human CCK1 receptorInhibition of 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
14991581 101951 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 22 8 9 3.2 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)CCc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL303994 101951 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 22 8 9 3.2 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)CCc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
90663985 106319 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 853 22 8 9 3.3 COc1ccc(/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
CHEMBL3144554 106319 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 853 22 8 9 3.3 COc1ccc(/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
44349268 16592 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 399 9 3 4 3.1 CC(C)(C)CCCNC(=O)C(CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00079a003
CHEMBL124509 16592 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 399 9 3 4 3.1 CC(C)(C)CCCNC(=O)C(CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00079a003
44381482 58749 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 827 22 10 9 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@H](CNN[C@@H](Cc1ccccc1)C(N)=O)CC(=O)O 10.1016/S0960-894X(00)80680-0
CHEMBL169567 58749 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 827 22 10 9 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@H](CNN[C@@H](Cc1ccccc1)C(N)=O)CC(=O)O 10.1016/S0960-894X(00)80680-0
13822916 189124 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 421 3 1 4 5.3 Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=N[C@@H]2Cc1c[nH]c2ccccc12 10.1021/jm00396a028
CHEMBL51569 189124 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 421 3 1 4 5.3 Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=N[C@@H]2Cc1c[nH]c2ccccc12 10.1021/jm00396a028
89913710 140277 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 285 2 1 2 2.9 CC(C)N1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
CHEMBL3819054 140277 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 285 2 1 2 2.9 CC(C)N1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
73349790 105682 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 725 14 5 6 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCNS(=O)(=O)c1ccccc1)c1ccccc1 10.1021/jm00092a007
CHEMBL313756 105682 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 725 14 5 6 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCNS(=O)(=O)c1ccccc1)c1ccccc1 10.1021/jm00092a007
14208205 202508 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ncc2ccccc2n1 10.1021/jm00120a002
CHEMBL70896 202508 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ncc2ccccc2n1 10.1021/jm00120a002
14208238 202423 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 5 3 3 4.1 O=C1Nc2ccccc2C(c2ccccc2)=NC1NCCc1c[nH]c2ccccc12 10.1021/jm00120a002
CHEMBL70405 202423 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 5 3 3 4.1 O=C1Nc2ccccc2C(c2ccccc2)=NC1NCCc1c[nH]c2ccccc12 10.1021/jm00120a002
10648445 58590 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 481 6 4 7 2.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(CNc3nn[nH]n3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
CHEMBL168903 58590 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 481 6 4 7 2.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(CNc3nn[nH]n3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
10695559 58713 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 467 5 4 7 2.9 CN1C(=O)[C@H](NC(=O)Nc2cccc(Nc3nn[nH]n3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
CHEMBL169362 58713 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 467 5 4 7 2.9 CN1C(=O)[C@H](NC(=O)Nc2cccc(Nc3nn[nH]n3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
10576729 58903 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 481 5 4 7 3.2 Cc1ccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1Nc1nn[nH]n1 10.1021/jm9506736
CHEMBL170275 58903 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 481 5 4 7 3.2 Cc1ccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1Nc1nn[nH]n1 10.1021/jm9506736
10814625 83040 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 481 5 3 7 2.9 CN1C(=O)[C@H](NC(=O)Nc2cccc(N(C)c3nn[nH]n3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
CHEMBL22003 83040 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 481 5 3 7 2.9 CN1C(=O)[C@H](NC(=O)Nc2cccc(N(C)c3nn[nH]n3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
10815094 119880 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 495 5 3 7 3.2 Cc1ccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1N(C)c1nn[nH]n1 10.1021/jm9506736
CHEMBL353509 119880 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 495 5 3 7 3.2 Cc1ccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1N(C)c1nn[nH]n1 10.1021/jm9506736
44356620 28434 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 400 3 3 5 2.6 CN1C(=O)C(NC(=O)Nc2ccc(N)nc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137748 28434 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 400 3 3 5 2.6 CN1C(=O)C(NC(=O)Nc2ccc(N)nc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10765241 103490 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 433 5 3 4 3.8 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCCCN2)c2ccccc21 10.1021/jm9608523
CHEMBL309299 103490 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 433 5 3 4 3.8 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCCCN2)c2ccccc21 10.1021/jm9608523
10717652 105664 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 433 5 3 4 3.8 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@@H]2CCCCN2)c2ccccc21 10.1021/jm9608523
CHEMBL313653 105664 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 433 5 3 4 3.8 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@@H]2CCCCN2)c2ccccc21 10.1021/jm9608523
CHEMBL44345 212164 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00378a012
15167802 67355 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
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 436 5 1 3 5.0 N#CCCN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
CHEMBL1907720 67355 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
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 436 5 1 3 5.0 N#CCCN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
15614820 67367 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
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 437 5 1 2 5.5 O=C1[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc2N1CC1CC1 10.1021/jm00390a019
CHEMBL1907737 67367 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
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 437 5 1 2 5.5 O=C1[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc2N1CC1CC1 10.1021/jm00390a019
15614818 67371 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
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 4 1 2 5.1 CCN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
CHEMBL1907742 67371 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
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 4 1 2 5.1 CCN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
44370505 50990 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
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 50990 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
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
24039375 9779 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 540 8 2 6 4.9 CCN(CC)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
CHEMBL114277 9779 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 540 8 2 6 4.9 CCN(CC)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
10575687 205500 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 453 4 3 5 5.2 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(Cl)c2Cl)c1 10.1021/jm970373j
CHEMBL9287 205500 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 453 4 3 5 5.2 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(Cl)c2Cl)c1 10.1021/jm970373j
45482483 196510 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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
CHEMBL575160 196510 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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
14208205 202508 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 425 3 2 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ncc2ccccc2n1 10.1021/jm00047a021
CHEMBL70896 202508 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 425 3 2 5 3.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ncc2ccccc2n1 10.1021/jm00047a021
10649606 49334 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 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 49334 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 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
9805700 118637 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 492 6 3 4 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CCCCCC1 10.1021/jm970065l
CHEMBL342932 118637 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 492 6 3 4 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CCCCCC1 10.1021/jm970065l
44381319 120200 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 495 11 4 5 3.6 N#C[C@H](N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
CHEMBL354817 120200 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 495 11 4 5 3.6 N#C[C@H](N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
10556460 205002 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 677 10 0 6 7.4 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(Cc4ccccc4)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
CHEMBL89953 205002 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 677 10 0 6 7.4 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(Cc4ccccc4)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
10556460 205002 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 677 10 0 6 7.4 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(Cc4ccccc4)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL89953 205002 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 677 10 0 6 7.4 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(Cc4ccccc4)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
10344702 28403 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 471 7 2 5 3.6 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCN(C)C)C2=O)c1 10.1021/jm00078a018
CHEMBL137714 28403 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 471 7 2 5 3.6 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCN(C)C)C2=O)c1 10.1021/jm00078a018
10837729 105951 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 461 5 3 4 4.5 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
CHEMBL313983 105951 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 461 5 3 4 4.5 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
14519983 119458 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ncccc2c1 10.1021/jm00124a003
CHEMBL349857 119458 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ncccc2c1 10.1021/jm00124a003
44306360 157321 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
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(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 157321 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
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(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
CHEMBL1172249 206830 0 None -5 4 Human 7.5 pIC50 = 7.5 Binding
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
52949124 861 2 None -2 2 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human 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 861 2 None -2 2 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human 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 861 2 None -2 2 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human 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 861 2 None -2 2 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human 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
44301034 101103 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 556 6 3 5 4.8 COC(=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
CHEMBL298627 101103 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 556 6 3 5 4.8 COC(=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
44336585 110180 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 641 7 2 6 5.7 CN(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
CHEMBL325987 110180 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 641 7 2 6 5.7 CN(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
10252890 25404 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 444 5 2 5 3.7 COc1cc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc(OC)c1 10.1021/jm00078a018
CHEMBL135167 25404 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 444 5 2 5 3.7 COc1cc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc(OC)c1 10.1021/jm00078a018
44356868 25756 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 412 3 2 3 4.3 Cc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1C 10.1021/jm00078a018
CHEMBL135433 25756 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 412 3 2 3 4.3 Cc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1C 10.1021/jm00078a018
10071645 27770 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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)Nc2ccc3ncccc3c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137238 27770 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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)Nc2ccc3ncccc3c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14991534 106296 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 825 22 8 8 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144531 106296 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 825 22 8 8 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14991566 167659 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 831 22 8 8 3.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCC1CCCCC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL433636 167659 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 831 22 8 8 3.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCC1CCCCC1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44280741 156009 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 759 15 4 8 5.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL406844 156009 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 759 15 4 8 5.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
44312020 102719 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 398 5 3 4 2.5 N[C@H](Cc1ccccc1)C(=O)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL308404 102719 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 398 5 3 4 2.5 N[C@H](Cc1ccccc1)C(=O)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
71452652 78080 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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)NCC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL2111884 78080 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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)NCC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
14802539 76184 1 None - 1 Rat 5.5 pIC50 = 5.5 Binding
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 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(01)80769-1
CHEMBL2062144 76184 1 None - 1 Rat 5.5 pIC50 = 5.5 Binding
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 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(01)80769-1
44382561 167732 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 662 13 5 5 5.8 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCc1ccc(O)cc1 10.1016/S0960-894X(00)80687-3
CHEMBL434113 167732 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 662 13 5 5 5.8 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)NCCc1ccc(O)cc1 10.1016/S0960-894X(00)80687-3
14802538 96228 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
CHEMBL263969 96228 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
19756868 28190 1 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 409 3 2 4 3.5 CN1C(=O)C(NC(=O)Nc2cccc(C#N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137520 28190 1 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 409 3 2 4 3.5 CN1C(=O)C(NC(=O)Nc2cccc(C#N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10475990 115485 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 398 3 2 3 4.0 Cc1ccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00078a018
CHEMBL33554 115485 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 398 3 2 3 4.0 Cc1ccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00078a018
44379627 57809 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 4.9 CC(C)Oc1cccc(-n2c(CNC(=O)NCc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
CHEMBL167758 57809 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 4.9 CC(C)Oc1cccc(-n2c(CNC(=O)NCc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
CHEMBL432671 167521 0 None - 1 Mouse 5.5 pIC50 = 5.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 784 15 7 12 3.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCNC(=O)CC(=O)NCCSCc3csc(C=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
14802538 96228 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 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 10.1021/jm970065l
CHEMBL263969 96228 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 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 10.1021/jm970065l
53465843 69052 0 None - 2 Rat 6.5 pIC50 = 6.5 Binding
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)N[C@@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933103 69052 0 None - 2 Rat 6.5 pIC50 = 6.5 Binding
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)N[C@@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
11178152 196660 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cnc2ccccc2c1 10.1016/j.bmc.2009.05.067
CHEMBL576380 196660 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cnc2ccccc2c1 10.1016/j.bmc.2009.05.067
44349152 18360 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 354 10 3 3 2.6 CCCCCNC(=O)C(CCC(=O)O)NC(=O)c1ccc(Cl)cc1 10.1021/jm00079a003
CHEMBL127604 18360 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 354 10 3 3 2.6 CCCCCNC(=O)C(CCC(=O)O)NC(=O)c1ccc(Cl)cc1 10.1021/jm00079a003
44381892 12155 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 510 9 2 4 3.7 CN(C)CCNC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL1184772 12155 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 510 9 2 4 3.7 CN(C)CCNC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL368133 12155 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 510 9 2 4 3.7 CN(C)CCNC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL385727 210604 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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
10049168 196189 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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)c1cc2cc(F)ccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL572648 196189 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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)c1cc2cc(F)ccc2[nH]1 10.1016/j.bmc.2009.05.067
44592009 178316 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 397 6 3 2 4.8 CC(Cc1ccccc1)NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL469974 178316 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 397 6 3 2 4.8 CC(Cc1ccccc1)NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL206974 207428 0 None -72 5 Human 6.5 pIC50 = 6.5 Binding
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](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
10649606 49334 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 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 49334 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 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
10744012 96917 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 501 8 3 8 4.5 CCOC(=O)c1ccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)cc1 10.1021/jm970373j
CHEMBL269662 96917 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 501 8 3 8 4.5 CCOC(=O)c1ccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)cc1 10.1021/jm970373j
CHEMBL407057 210878 0 None -1513 4 Human 5.5 pIC50 = 5.5 Binding
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](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O 10.1021/jm050921q
44365304 164189 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 444 8 2 3 4.3 CC(C)N(C(=O)CN(C(=O)CNC(=O)Nc1ccccc1)c1ccccc1)c1ccccc1 10.1016/S0960-894X(97)00062-0
CHEMBL421778 164189 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 444 8 2 3 4.3 CC(C)N(C(=O)CN(C(=O)CNC(=O)Nc1ccccc1)c1ccccc1)c1ccccc1 10.1016/S0960-894X(97)00062-0
53465781 69048 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 413 6 4 3 4.0 O=C(Nc1ccccc1C(=O)NC(C(=O)O)c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933099 69048 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 413 6 4 3 4.0 O=C(Nc1ccccc1C(=O)NC(C(=O)O)c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm200438b
10030027 17749 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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)[C@@H](c1ccccc1)C[C@@H](NC(=O)Nc1cccc(Cl)c1)C(=O)N2CC(=O)NC(C)(C)C 10.1021/jm00048a015
CHEMBL126002 17749 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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)[C@@H](c1ccccc1)C[C@@H](NC(=O)Nc1cccc(Cl)c1)C(=O)N2CC(=O)NC(C)(C)C 10.1021/jm00048a015
CHEMBL2372072 208424 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CN)NC(=O)[C@H](CCSC)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](CCC(=O)O)N(CCN(CCC(=O)O)CCC(=O)O)CCN(CCC(=O)O)CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmc.2007.05.067
14208247 202935 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 5 2 4 3.5 O=C(O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL73621 202935 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 5 2 4 3.5 O=C(O)CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
10323690 100019 0 None - 2 Rat 7.5 pIC50 = 7.5 Binding
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 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00086a017
CHEMBL2114401 100019 0 None - 2 Rat 7.5 pIC50 = 7.5 Binding
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 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00086a017
CHEMBL291033 100019 0 None - 2 Rat 7.5 pIC50 = 7.5 Binding
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 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00086a017
10674587 78416 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 570 8 3 6 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)[C@@H](C#N)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
CHEMBL2112825 78416 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 570 8 3 6 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)[C@@H](C#N)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
44301016 157421 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 673 7 4 6 4.5 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)C(F)(F)F)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL408490 157421 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 673 7 4 6 4.5 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)C(F)(F)F)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
14519979 9424 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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)c1cccc2ccccc12 10.1021/jm00124a003
CHEMBL112215 9424 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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)c1cccc2ccccc12 10.1021/jm00124a003
10099144 114030 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 552 5 3 3 6.0 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccc(Cl)cc21 10.1021/jm00048a015
CHEMBL333671 114030 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 552 5 3 3 6.0 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccc(Cl)cc21 10.1021/jm00048a015
14519979 9424 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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)c1cccc2ccccc12 10.1021/jm00116a002
CHEMBL112215 9424 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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)c1cccc2ccccc12 10.1021/jm00116a002
21467078 4344 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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(NC(=O)Nc2cccc(C)c2)N=C(N2CCN(C)CC2)c2ccccc21 10.1016/0960-894X(95)00530-0
CHEMBL101528 4344 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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(NC(=O)Nc2cccc(C)c2)N=C(N2CCN(C)CC2)c2ccccc21 10.1016/0960-894X(95)00530-0
44210428 58787 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 485 4 2 4 3.1 CN1CCN(C(=O)CN2C(=O)C(NC(=O)Nc3cccc4ccccc34)CCc3ccccc32)CC1 10.1016/S0960-894X(00)80683-6
CHEMBL169794 58787 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 485 4 2 4 3.1 CN1CCN(C(=O)CN2C(=O)C(NC(=O)Nc3cccc4ccccc34)CCc3ccccc32)CC1 10.1016/S0960-894X(00)80683-6
14519977 119431 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
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 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00124a003
CHEMBL349640 119431 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
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 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00124a003
10601173 30963 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 491 6 3 3 5.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCCC1 10.1021/jm970065l
CHEMBL140073 30963 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 491 6 3 3 5.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCCC1 10.1021/jm970065l
10372508 98096 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 694 13 6 6 4.9 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(01)00630-8
CHEMBL276613 98096 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 694 13 6 6 4.9 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1016/s0960-894x(01)00630-8
44409521 139627 4 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 351 5 4 3 2.6 CC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL380355 139627 4 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 351 5 4 3 2.6 CC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
44349383 16573 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 480 9 3 3 4.7 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NCCC12CC3CC(CC(C3)C1)C2 10.1021/jm00079a003
CHEMBL124396 16573 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 480 9 3 3 4.7 O=C(O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)NCCC12CC3CC(CC(C3)C1)C2 10.1021/jm00079a003
54587149 61516 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 COc1cccc(-c2cnc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773883 61516 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 COc1cccc(-c2cnc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
90663982 106316 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 21 10 10 2.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(O)c(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144551 106316 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 21 10 10 2.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(O)c(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14991572 162618 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 848 20 8 9 3.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cnc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL418123 162618 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 848 20 8 9 3.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cnc2ccccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
10649606 49334 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]BDZ2 from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y 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 49334 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]BDZ2 from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y 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
57393204 67332 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 431 5 1 4 3.3 COc1cccc(CC(=O)N[C@H]2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)c1 10.1021/jm00120a002
CHEMBL1907666 67332 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 431 5 1 4 3.3 COc1cccc(CC(=O)N[C@H]2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)c1 10.1021/jm00120a002
44280029 95981 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 740 15 6 9 3.5 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL262125 95981 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 740 15 6 9 3.5 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44279810 103354 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 757 16 4 7 5.7 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL30917 103354 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 757 16 4 7 5.7 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44209154 58770 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 315 4 2 2 4.2 O=C(CCc1ccccc1)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
CHEMBL169675 58770 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 315 4 2 2 4.2 O=C(CCc1ccccc1)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
15167795 73715 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
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 344 2 0 3 4.6 CN1C(=O)/C(=C\c2ccsc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
CHEMBL20223 73715 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
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 344 2 0 3 4.6 CN1C(=O)/C(=C\c2ccsc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
44336539 5060 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 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 5060 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 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
44349082 17578 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 446 9 3 3 4.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NCCC12CC3CC(CC(C3)C1)C2 10.1021/jm00079a003
CHEMBL125874 17578 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 446 9 3 3 4.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NCCC12CC3CC(CC(C3)C1)C2 10.1021/jm00079a003
44359614 31637 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 491 8 3 4 5.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)CNC1CCCCC1 10.1021/jm970065l
CHEMBL140701 31637 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 491 8 3 4 5.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)CNC1CCCCC1 10.1021/jm970065l
44382327 59030 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 436 5 2 4 2.8 COc1cccc(NC(=O)N[C@H]2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL170777 59030 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 436 5 2 4 2.8 COc1cccc(NC(=O)N[C@H]2CCc3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
44327450 167627 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 558 10 3 5 4.6 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccn1)CC(=O)O 10.1016/S0960-894X(01)80769-1
CHEMBL433384 167627 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 558 10 3 5 4.6 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccn1)CC(=O)O 10.1016/S0960-894X(01)80769-1
14208250 167476 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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(NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL432334 167476 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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(NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
11327818 196417 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 428 7 4 4 3.2 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1nc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL574488 196417 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 428 7 4 4 3.2 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1nc2ccccc2[nH]1 10.1016/j.bmc.2009.05.067
44300890 101407 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 580 7 4 6 4.3 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
CHEMBL300776 101407 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 580 7 4 6 4.3 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
15689732 106120 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 870 21 9 10 3.0 COC(=O)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
CHEMBL3142906 106120 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 870 21 9 10 3.0 COC(=O)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
15689732 106120 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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)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/jm960509y
CHEMBL3142906 106120 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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)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/jm960509y
44349572 114548 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 533 5 2 4 6.0 Cc1ccc2c(c1)N(CC(=O)OC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
CHEMBL334305 114548 0 None - 0 Guinea pig 7.5 pIC50 = 7.5 Binding
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 533 5 2 4 6.0 Cc1ccc2c(c1)N(CC(=O)OC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
10455303 114708 6 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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)Nc2cccc([N+](=O)[O-])c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL334592 114708 6 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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)Nc2cccc([N+](=O)[O-])c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10604135 78414 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 637 8 3 5 5.1 O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12)OC1C2CC3CC(C2)CC1C3 10.1021/jm991078x
CHEMBL2112823 78414 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 637 8 3 5 5.1 O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12)OC1C2CC3CC(C2)CC1C3 10.1021/jm991078x
70693814 73281 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 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 73281 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 621 7 1 6 6.1 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccncc1 10.1016/j.bmcl.2012.02.049
44311939 202780 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 530 6 2 5 4.2 CN1C(=O)C(NC(=O)[C@H](Cc2ccccc2)NC(=O)OC(C)(C)C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL72526 202780 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 530 6 2 5 4.2 CN1C(=O)C(NC(=O)[C@H](Cc2ccccc2)NC(=O)OC(C)(C)C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
44396765 67023 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 594 8 2 5 5.4 O=C(OC1C2CC3CC(C2)CC1C3)[C@H](Cc1c[nH]c2ccccc12)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)CC12 10.1021/jm0498755
CHEMBL188667 67023 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 594 8 2 5 5.4 O=C(OC1C2CC3CC(C2)CC1C3)[C@H](Cc1c[nH]c2ccccc12)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)CC12 10.1021/jm0498755
10074702 27392 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 500 8 2 6 4.0 CCOC(=O)CCN1C(=O)C(NC(=O)Nc2cccc(OC)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL136966 27392 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 500 8 2 6 4.0 CCOC(=O)CCN1C(=O)C(NC(=O)Nc2cccc(OC)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44279809 98497 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 785 18 4 7 6.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL279778 98497 0 None - 1 Mouse 6.5 pIC50 = 6.5 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 785 18 4 7 6.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
14208317 67333 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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)c2ccccc2Cl)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907667 67333 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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)c2ccccc2Cl)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208250 167476 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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(NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL432334 167476 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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(NC(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
9865694 202466 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin receptor
ChEMBL 399 3 2 2 5.2 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=N[C@@H]1Cc1c[nH]c2ccccc12 10.1021/jm00120a002
CHEMBL70728 202466 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to cholecystokinin receptor
ChEMBL 399 3 2 2 5.2 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=N[C@@H]1Cc1c[nH]c2ccccc12 10.1021/jm00120a002
44280122 99026 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 640 10 3 4 5.7 CN(C(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1)[C@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm950372w
CHEMBL283276 99026 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 640 10 3 4 5.7 CN(C(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1)[C@H](Cc1c[nH]c2ccccc12)C(=O)O 10.1021/jm950372w
44370497 164630 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 453 8 3 3 4.6 O=C(O)CC[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N(C1CCCCC1)C1CCCCC1 10.1021/jm00164a020
CHEMBL422873 164630 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 453 8 3 3 4.6 O=C(O)CC[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N(C1CCCCC1)C1CCCCC1 10.1021/jm00164a020
44334325 167400 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
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 485 9 2 3 5.2 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCC(Cc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL431812 167400 0 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
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 485 9 2 3 5.2 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCC(Cc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
1043 1545 13 None - 29 Mouse 4.5 pIC50 = 4.5 Binding
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 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/S0960-894X(00)80644-7
149 1545 13 None - 29 Mouse 4.5 pIC50 = 4.5 Binding
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 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/S0960-894X(00)80644-7
8223 1545 13 None - 29 Mouse 4.5 pIC50 = 4.5 Binding
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 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/S0960-894X(00)80644-7
CHEMBL442 1545 13 None - 29 Mouse 4.5 pIC50 = 4.5 Binding
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 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/S0960-894X(00)80644-7
DB00696 1545 13 None - 29 Mouse 4.5 pIC50 = 4.5 Binding
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 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/S0960-894X(00)80644-7
15167794 98429 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
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 344 2 0 3 4.6 CN1C(=O)/C(=C/c2ccsc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
CHEMBL279237 98429 0 None - 0 Guinea pig 4.5 pIC50 = 4.5 Binding
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 344 2 0 3 4.6 CN1C(=O)/C(=C/c2ccsc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
10649303 205713 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 507 6 3 6 5.1 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL9422 205713 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 507 6 3 6 5.1 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
10625474 28998 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 508 8 3 5 4.2 COC[C@H]1CCCN1NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
CHEMBL138233 28998 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 508 8 3 5 4.2 COC[C@H]1CCCN1NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
44381610 119970 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 610 15 6 7 2.5 N#C[C@@H](N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
CHEMBL354359 119970 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 610 15 6 7 2.5 N#C[C@@H](N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
10791546 205344 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 501 8 3 8 4.5 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1021/jm970373j
CHEMBL9188 205344 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 501 8 3 8 4.5 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1021/jm970373j
46235271 73286 2 None 2 2 Human 7.5 pIC50 = 7.5 Binding
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 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 73286 2 None 2 2 Human 7.5 pIC50 = 7.5 Binding
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 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
54581260 61515 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 513 5 0 4 6.8 COc1cccc(-c2ccc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773882 61515 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 513 5 0 4 6.8 COc1cccc(-c2ccc(C(=O)N3CCN(c4ccc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
54586147 61518 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 COc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
CHEMBL1773885 61518 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 COc1cccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccc(C)cc2)c1 10.1016/j.bmcl.2011.03.069
54580267 61528 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 535 5 0 6 6.0 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2Cl)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773895 61528 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 535 5 0 6 6.0 COc1ccc(-c2cnc(C(=O)N3CCN(c4cnc5ccccc5c4)CC3)nc2-c2ccccc2Cl)cc1 10.1016/j.bmcl.2011.03.069
14888738 97889 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 984 28 10 13 0.8 CSCC[C@H](NC(=O)CCc1ccc(-c2nn[nH]n2)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
CHEMBL275167 97889 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 984 28 10 13 0.8 CSCC[C@H](NC(=O)CCc1ccc(-c2nn[nH]n2)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
44578611 189056 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human CCK1 receptorInhibition of 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 189056 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human CCK1 receptorInhibition of 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
19766169 165003 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 443 4 2 4 4.2 CC(C)(C)OC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
CHEMBL424211 165003 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 443 4 2 4 4.2 CC(C)(C)OC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
44336509 106856 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 667 9 2 6 5.8 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/s0960-894x(98)00548-4
CHEMBL317668 106856 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 667 9 2 6 5.8 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/s0960-894x(98)00548-4
9980735 177861 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 3 4 3.9 Cn1c(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)cc2ccccc21 10.1016/j.bmc.2009.05.067
CHEMBL466135 177861 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 3 4 3.9 Cn1c(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)cc2ccccc21 10.1016/j.bmc.2009.05.067
15104626 110115 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 7 3 3 4.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL325662 110115 0 None - 0 Guinea pig 6.5 pIC50 = 6.5 Binding
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 7 3 3 4.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccccc1)c1cnc2ccccc2c1 10.1021/jm00116a002
3081191 9442 9 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
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 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00124a003
CHEMBL112307 9442 9 None - 0 Guinea pig 5.5 pIC50 = 5.5 Binding
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 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00124a003
44272229 98278 0 None - 1 Mouse 5.5 pIC50 = 5.5 Binding
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 635 15 6 6 3.5 CC(C)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)NCCc1ccccc1 10.1016/S0960-894X(00)80644-7
CHEMBL278032 98278 0 None - 1 Mouse 5.5 pIC50 = 5.5 Binding
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 635 15 6 6 3.5 CC(C)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)NCCc1ccccc1 10.1016/S0960-894X(00)80644-7
44272229 98278 0 None - 1 Mouse 5.5 pIC50 = 5.5 Binding
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 635 15 6 6 3.5 CC(C)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)NCCc1ccccc1 10.1016/S0960-894X(01)80253-5
CHEMBL278032 98278 0 None - 1 Mouse 5.5 pIC50 = 5.5 Binding
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 635 15 6 6 3.5 CC(C)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)NCCc1ccccc1 10.1016/S0960-894X(01)80253-5
19754254 119831 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 321 2 2 2 4.6 O=C(Nc1cc2c3ccccc3nc-2c[nH]1)c1ccc(Cl)cc1 10.1016/S0960-894X(00)80682-4
CHEMBL353088 119831 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 321 2 2 2 4.6 O=C(Nc1cc2c3ccccc3nc-2c[nH]1)c1ccc(Cl)cc1 10.1016/S0960-894X(00)80682-4
44349102 167755 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 434 7 3 3 4.3 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCC2(CCCCC2)CC1 10.1021/jm00079a003
CHEMBL434250 167755 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 434 7 3 3 4.3 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCC2(CCCCC2)CC1 10.1021/jm00079a003
10817407 106634 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 601 7 1 6 5.6 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccc2c(c1)OCO2 10.1021/jm970265x
CHEMBL316106 106634 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 601 7 1 6 5.6 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccc2c(c1)OCO2 10.1021/jm970265x
10767360 204120 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 489 5 2 4 5.2 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCC(C)(C)CCN2C)c2ccccc21 10.1021/jm9608523
CHEMBL83591 204120 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 489 5 2 4 5.2 CCCN1C(=O)[C@H](NC(=O)Nc2cccc(C)c2)N=C([C@H]2CCC(C)(C)CCN2C)c2ccccc21 10.1021/jm9608523
44408590 161165 0 None - 2 Human 4.5 pIC50 = 4.5 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1134 30 12 15 2.6 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](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL413644 161165 0 None - 2 Human 4.5 pIC50 = 4.5 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1134 30 12 15 2.6 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](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
44418923 161224 0 None - 2 Human 4.5 pIC50 = 4.5 Binding
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](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)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
CHEMBL414087 161224 0 None - 2 Human 4.5 pIC50 = 4.5 Binding
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](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)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
45482480 196188 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 472 8 4 5 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cc([N+](=O)[O-])ccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL572647 196188 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 472 8 4 5 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cc([N+](=O)[O-])ccc2[nH]1 10.1016/j.bmc.2009.05.067
45482477 196392 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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)c1cc2cccc(F)c2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL574292 196392 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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)c1cc2cccc(F)c2[nH]1 10.1016/j.bmc.2009.05.067
44211352 13857 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 6 1 4 3.8 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL1196916 13857 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 6 1 4 3.8 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL558614 13857 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 6 1 4 3.8 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
10671800 205006 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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)Nc3ccc(Cl)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL8997 205006 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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)Nc3ccc(Cl)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
70691750 73284 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 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 73284 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 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
44336539 5060 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]BDZ2 from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 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 5060 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]BDZ2 from CCK2R TM6 (unknown origin) containing 16.51V, F6.52Y chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ2 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
10555363 96027 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 588 9 1 4 6.6 CCC1(CC(=O)Nc2ccccc2)C(=O)N(CC(=O)N(c2ccccc2)C(C)C)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm960205b
CHEMBL262444 96027 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 588 9 1 4 6.6 CCC1(CC(=O)Nc2ccccc2)C(=O)N(CC(=O)N(c2ccccc2)C(C)C)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm960205b
155553502 173593 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 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 173593 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 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
44303511 159201 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 750 18 4 10 5.7 CCCC[C@@H](C(=O)N[C@@H](CC(=O)OCc1ccccc1)[C@@H](Cc1ccccc1)C(N)=O)n1nnnc1[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(01)81005-2
CHEMBL410511 159201 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 750 18 4 10 5.7 CCCC[C@@H](C(=O)N[C@@H](CC(=O)OCc1ccccc1)[C@@H](Cc1ccccc1)C(N)=O)n1nnnc1[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1016/S0960-894X(01)81005-2
70695922 73233 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 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 73233 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 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
44458101 167572 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
CHEMBL433032 167572 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
72947518 140253 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 277 2 1 2 2.7 O=C1C=C(Cl)C(O)(c2ccccc2)N1C1CCCC1 10.1039/C6MD00052E
CHEMBL3818781 140253 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 277 2 1 2 2.7 O=C1C=C(Cl)C(O)(c2ccccc2)N1C1CCCC1 10.1039/C6MD00052E
44348764 168056 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 980 28 11 11 1.4 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCCCNC(=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
CHEMBL436199 168056 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 980 28 11 11 1.4 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCCCNC(=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
CHEMBL435339 211907 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
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)OC(C)(C)C)C(=O)N1C[C@@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
89913059 140179 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 327 6 1 2 4.0 CCCCCCN1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
CHEMBL3817870 140179 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 327 6 1 2 4.0 CCCCCCN1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
14208261 103199 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 397 5 2 3 4.2 CCCc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL308756 103199 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 397 5 2 3 4.2 CCCc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
44280371 102541 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 815 19 4 8 6.6 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL30701 102541 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 815 19 4 8 6.6 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
44281020 116131 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 16 4 8 6.2 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL33698 116131 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 16 4 8 6.2 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
13822910 67407 0 None - 0 Guinea pig 4.4 pIC50 = 4.4 Binding
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 383 3 2 2 4.7 O=C1Nc2ccccc2C(c2ccccc2F)=N[C@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
CHEMBL1907930 67407 0 None - 0 Guinea pig 4.4 pIC50 = 4.4 Binding
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 383 3 2 2 4.7 O=C1Nc2ccccc2C(c2ccccc2F)=N[C@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
44303488 100577 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 501 8 2 6 4.1 CC(Cn1nnc2ccccc21)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL294735 100577 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 501 8 2 6 4.1 CC(Cn1nnc2ccccc21)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
10369806 116307 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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
CHEMBL337937 116307 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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
CHEMBL218763 207644 0 None -3630 4 Human 5.4 pIC50 = 5.4 Binding
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
44303722 100369 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 807 20 5 11 4.8 CCCC[C@@H](C(=O)N[C@@H](CC(=O)OCc1ccccc1)[C@@H](Cc1ccccc1)C(N)=O)n1nnnc1[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)OC(C)(C)C 10.1016/S0960-894X(01)81005-2
CHEMBL293456 100369 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 807 20 5 11 4.8 CCCC[C@@H](C(=O)N[C@@H](CC(=O)OCc1ccccc1)[C@@H](Cc1ccccc1)C(N)=O)n1nnnc1[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)OC(C)(C)C 10.1016/S0960-894X(01)81005-2
11756709 22659 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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 528 9 3 6 3.7 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)CCC(=O)O)C2=O)c1 10.1021/jm00078a018
CHEMBL132875 22659 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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 528 9 3 6 3.7 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)CCC(=O)O)C2=O)c1 10.1021/jm00078a018
52949124 861 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R T3.28V, T3.29S 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 861 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R T3.28V, T3.29S 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 861 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R T3.28V, T3.29S 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 861 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R T3.28V, T3.29S 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
10435698 140864 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 490 6 2 5 4.2 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80683-6
CHEMBL38404 140864 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 490 6 2 5 4.2 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80683-6
44300745 196664 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 562 6 3 5 5.3 COC(=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
CHEMBL57643 196664 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 562 6 3 5 5.3 COC(=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
10435698 140864 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 490 6 2 5 4.2 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
CHEMBL38404 140864 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 490 6 2 5 4.2 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
15104597 110048 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 481 13 2 2 6.4 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)cc1 10.1021/jm00116a002
CHEMBL325220 110048 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 481 13 2 2 6.4 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)cc1 10.1021/jm00116a002
11028229 114943 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 8 3 5 4.6 CO[C@@H]1C[C@H]2[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C(=O)N1Cc1ccccc1 10.1021/jm010898i
CHEMBL3350856 114943 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 8 3 5 4.6 CO[C@@H]1C[C@H]2[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)CCCN2C(=O)N1Cc1ccccc1 10.1021/jm010898i
10435698 140864 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 490 6 2 5 4.2 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL38404 140864 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 490 6 2 5 4.2 CCOC(=O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14720390 49110 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
CHEMBL156415 49110 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
70695933 73274 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 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 73274 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 607 7 1 6 5.7 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCC1Cc1ccccn1 10.1016/j.bmcl.2012.02.049
10413618 201094 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
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 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL62205 201094 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
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 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(01)80769-1
10323690 100019 0 None - 2 Rat 6.4 pIC50 = 6.4 Binding
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 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00057a005
CHEMBL2114401 100019 0 None - 2 Rat 6.4 pIC50 = 6.4 Binding
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 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00057a005
CHEMBL291033 100019 0 None - 2 Rat 6.4 pIC50 = 6.4 Binding
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 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00057a005
11224455 196586 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 440 7 3 3 4.1 CC1=C(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)Cc2ccccc21 10.1016/j.bmc.2009.05.067
CHEMBL575814 196586 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 440 7 3 3 4.1 CC1=C(C(=O)Nc2ccccc2C(=O)NC(Cc2ccccc2)C(=O)O)Cc2ccccc21 10.1016/j.bmc.2009.05.067
44376132 119728 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 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
CHEMBL352264 119728 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 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
90663978 106308 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
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 883 23 8 10 3.3 COc1ccc(/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)c(OC)c1 10.1021/jm00089a010
CHEMBL3144542 106308 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
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 883 23 8 10 3.3 COc1ccc(/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)c(OC)c1 10.1021/jm00089a010
70695934 73282 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 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 73282 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 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
44283029 99579 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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 627 11 3 7 5.2 COC(=O)/C=C/C(=O)N[C@H](COC(=O)C(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)c1ccccc1 10.1021/jm00086a017
CHEMBL287079 99579 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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 627 11 3 7 5.2 COC(=O)/C=C/C(=O)N[C@H](COC(=O)C(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)c1ccccc1 10.1021/jm00086a017
10793883 106633 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 615 8 0 6 6.3 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3nn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL316104 106633 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 615 8 0 6 6.3 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3nn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
10323690 100019 0 None - 2 Rat 6.4 pIC50 = 6.4 Binding
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 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
CHEMBL2114401 100019 0 None - 2 Rat 6.4 pIC50 = 6.4 Binding
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 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
CHEMBL291033 100019 0 None - 2 Rat 6.4 pIC50 = 6.4 Binding
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 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
14888722 76880 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 1055 30 11 14 -0.2 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(Cc2nnn[nH]2)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
CHEMBL2079601 76880 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 1055 30 11 14 -0.2 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCSC)NC(=O)[C@@H](Cc1ccc(Cc2nnn[nH]2)cc1)NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00107a037
44280495 98656 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 641 10 5 8 3.7 CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL280980 98656 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 641 10 5 8 3.7 CN1C(=O)[C@H](NC(=O)Nc2cccc(C(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
10413618 201094 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
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 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1021/jm970065l
CHEMBL62205 201094 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
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 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1021/jm970065l
44349074 116522 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 426 7 4 4 2.8 O=C(O)CCC(NC(=O)c1cc2ccccc2[nH]1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL339041 116522 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 426 7 4 4 2.8 O=C(O)CCC(NC(=O)c1cc2ccccc2[nH]1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
44333305 4967 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 502 4 2 5 3.6 CCCN1C(=O)C(NC(=O)Nc2cccc(C(F)(F)F)c2)N=C(N2CCN(C)CC2)c2ccccc21 10.1016/0960-894X(95)00530-0
CHEMBL105273 4967 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 502 4 2 5 3.6 CCCN1C(=O)C(NC(=O)Nc2cccc(C(F)(F)F)c2)N=C(N2CCN(C)CC2)c2ccccc21 10.1016/0960-894X(95)00530-0
10430103 78090 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 384 3 3 3 3.9 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3NC2=O)c1 10.1021/jm00078a018
CHEMBL2111921 78090 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 384 3 3 3 3.9 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3NC2=O)c1 10.1021/jm00078a018
44281004 99604 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 15 4 8 6.4 Cc1cccc(NC(=O)N[C@@H]2N=C(c3cccc(OC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00249-1
CHEMBL287295 99604 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 15 4 8 6.4 Cc1cccc(NC(=O)N[C@@H]2N=C(c3cccc(OC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00249-1
10838382 118813 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 478 6 3 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CCCCC1 10.1021/jm970065l
CHEMBL344211 118813 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 478 6 3 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NN1CCCCC1 10.1021/jm970065l
71449051 78061 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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)c1cc(Cl)cc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL2111827 78061 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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)c1cc(Cl)cc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
44381819 58292 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
CHEMBL168435 58292 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
10322621 57239 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 473 7 2 7 4.4 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc([N+](=O)[O-])cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
CHEMBL166443 57239 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 473 7 2 7 4.4 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc([N+](=O)[O-])cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
15514018 78171 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 546 6 3 6 3.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(c3ccncc3)C(=O)C[C@H]12 10.1021/jm010813d
CHEMBL2112238 78171 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 546 6 3 6 3.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CCCN2C(=O)N(c3ccncc3)C(=O)C[C@H]12 10.1021/jm010813d
10580108 5027 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 650 10 1 4 7.4 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)(Cc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
CHEMBL105619 5027 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 650 10 1 4 7.4 CC(C)N(C(=O)CN1C(=O)C(CC(=O)Nc2ccccc2)(Cc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
14991574 100223 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
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 836 20 9 8 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL292471 100223 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
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 836 20 9 8 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
90663996 106329 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
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\c1cccc(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
CHEMBL3144565 106329 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
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\c1cccc(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
10415786 169140 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 577 7 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(O)cc1 10.1021/jm950626d
CHEMBL443825 169140 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 577 7 3 5 5.0 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(O)cc1 10.1021/jm950626d
44336539 5060 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 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/s0960-894x(98)00548-4
CHEMBL105775 5060 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 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/s0960-894x(98)00548-4
15104612 109283 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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]c2ccccc12)NC(=O)c1ccc2cccc(O)c2n1 10.1021/jm00116a002
CHEMBL323249 109283 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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]c2ccccc12)NC(=O)c1ccc2cccc(O)c2n1 10.1021/jm00116a002
CHEMBL2370120 208031 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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(CCC(=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
10318742 24788 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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(c3ccncc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL134657 24788 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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(c3ccncc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
14991542 106311 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 893 22 8 8 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(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
CHEMBL3144545 106311 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 893 22 8 8 4.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(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
44280714 99558 0 None - 1 Mouse 6.4 pIC50 = 6.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 726 14 6 9 3.2 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL286908 99558 0 None - 1 Mouse 6.4 pIC50 = 6.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 726 14 6 9 3.2 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
5556 201560 26 None - 1 Rat 4.4 pIC50 = 4.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 342 1 0 4 4.2 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1Cl)=NC2 10.1021/jm00396a028
CHEMBL646 201560 26 None - 1 Rat 4.4 pIC50 = 4.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 342 1 0 4 4.2 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1Cl)=NC2 10.1021/jm00396a028
13822916 189124 0 None - 0 Guinea pig 4.4 pIC50 = 4.4 Binding
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 421 3 1 4 5.3 Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=N[C@@H]2Cc1c[nH]c2ccccc12 10.1021/jm00390a019
CHEMBL51569 189124 0 None - 0 Guinea pig 4.4 pIC50 = 4.4 Binding
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 421 3 1 4 5.3 Cc1nnc2n1-c1ccccc1C(c1ccccc1F)=N[C@@H]2Cc1c[nH]c2ccccc12 10.1021/jm00390a019
44368541 168040 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 590 13 5 5 4.5 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL436065 168040 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 590 13 5 5 4.5 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00057a005
44286815 162705 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 20 7 7 4.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL418622 162705 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 20 7 7 4.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
155558199 174187 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 1894 75 19 24 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)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
CHEMBL4561184 174187 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 1894 75 19 24 2.9 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)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
10346551 114125 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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)Nc2ccc(Cl)cc2)C[C@H](c2ccccc2)c2ccccc21 10.1021/jm00048a015
CHEMBL333813 114125 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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)Nc2ccc(Cl)cc2)C[C@H](c2ccccc2)c2ccccc21 10.1021/jm00048a015
10485763 109175 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 860 21 8 8 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Oc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL322635 109175 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 860 21 8 8 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)Oc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44381815 58683 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 838 21 7 9 4.0 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
CHEMBL169126 58683 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 838 21 7 9 4.0 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C\c1ccc(O)cc1)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
15667003 96877 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 1016 27 8 11 2.3 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC(CCC)[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL269355 96877 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 1016 27 8 11 2.3 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC(CCC)[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
10346998 17911 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 2 3 5.7 CN(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21)C(C)(C)C 10.1021/jm00048a015
CHEMBL126865 17911 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 2 3 5.7 CN(C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21)C(C)(C)C 10.1021/jm00048a015
9962694 167660 3 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 853 21 8 9 3.3 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL433640 167660 3 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 853 21 8 9 3.3 CN(C(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCNC(=O)/C=C/c1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
46234969 73279 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 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 73279 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 626 7 1 5 7.4 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1CC1CCCCC1 10.1016/j.bmcl.2012.02.049
155548381 173150 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 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 173150 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
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 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
CHEMBL156559 207052 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
44396672 67161 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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 545 7 2 6 4.5 CN(C)c1ccc(N2C(=O)CC3[C@@H](N[C@@H](Cc4c[nH]c5ccccc45)C(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm0498755
CHEMBL189549 67161 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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 545 7 2 6 4.5 CN(C)c1ccc(N2C(=O)CC3[C@@H](N[C@@H](Cc4c[nH]c5ccccc45)C(=O)OC(C)(C)C)CCCN3C2=O)cc1 10.1021/jm0498755
10918992 79118 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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 588 7 3 6 4.2 CN(C)c1ccc(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
CHEMBL2114079 79118 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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 588 7 3 6 4.2 CN(C)c1ccc(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
13822921 101144 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 431 3 1 5 4.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2-n2cnnc21)c1ccc(Cl)cc1 10.1021/jm00396a028
CHEMBL298948 101144 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 431 3 1 5 4.3 O=C(NC1N=C(c2ccccc2F)c2ccccc2-n2cnnc21)c1ccc(Cl)cc1 10.1021/jm00396a028
10389657 24439 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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)Nc2cccc(Br)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL134340 24439 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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)Nc2cccc(Br)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44329150 111895 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 580 7 3 3 6.8 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC3(C)CCCCC3)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL329735 111895 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 580 7 3 3 6.8 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC3(C)CCCCC3)C2=O)c1 10.1016/S0960-894X(01)80832-5
10053472 78419 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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 557 8 3 4 4.1 CC(C)(C)CC(=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
CHEMBL2112829 78419 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
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 557 8 3 4 4.1 CC(C)(C)CC(=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
52949124 861 2 None -2 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S 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 861 2 None -2 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S 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 861 2 None -2 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S 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 861 2 None -2 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S 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
15689726 106099 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 880 20 9 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1cccc(Cl)c1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142691 106099 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 880 20 9 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1cccc(Cl)c1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44370451 50503 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
CHEMBL157658 50503 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
14991569 98330 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 863 20 9 9 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccc2cc(O)ccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL278447 98330 0 None - 0 Guinea pig 8.4 pIC50 = 8.4 Binding
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 863 20 9 9 3.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1ccc2cc(O)ccc2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14208192 102509 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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)c1cc2ccccc2[nH]1 10.1021/jm00047a021
CHEMBL306760 102509 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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)c1cc2ccccc2[nH]1 10.1021/jm00047a021
14208236 202965 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 426 3 2 4 3.9 Cn1c(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc2ccccc21 10.1021/jm00047a021
CHEMBL73885 202965 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 426 3 2 4 3.9 Cn1c(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc2ccccc21 10.1021/jm00047a021
10030842 98128 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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
CHEMBL276837 98128 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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
54581302 61578 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 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 61578 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 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
15667012 168473 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
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)CCc1ccc(OS(=O)(=O)O)cc1)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/jm00094a001
CHEMBL439591 168473 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
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)CCc1ccc(OS(=O)(=O)O)cc1)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/jm00094a001
14208192 102509 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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)c1cc2ccccc2[nH]1 10.1021/jm00120a002
CHEMBL306760 102509 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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)c1cc2ccccc2[nH]1 10.1021/jm00120a002
14208236 202965 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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 4 3.9 Cn1c(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc2ccccc21 10.1021/jm00120a002
CHEMBL73885 202965 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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 4 3.9 Cn1c(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc2ccccc21 10.1021/jm00120a002
15667012 168473 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
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 28 10 11 1.5 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](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL439591 168473 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
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 28 10 11 1.5 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](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
10030842 98128 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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
CHEMBL276837 98128 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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
10030842 98128 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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
CHEMBL276837 98128 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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
9887120 202417 3 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL70380 202417 3 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL319438 209461 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
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 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/jm00028a015
44348651 167663 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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 952 26 11 11 0.6 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCNC(=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
CHEMBL433647 167663 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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 952 26 11 11 0.6 CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCNC(=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
44381578 119989 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
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)CNN[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
CHEMBL354512 119989 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
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)CNN[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80680-0
90663979 106313 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
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 883 23 8 10 3.3 COc1ccc(/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)cc1OC 10.1021/jm00089a010
CHEMBL3144548 106313 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
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 883 23 8 10 3.3 COc1ccc(/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)cc1OC 10.1021/jm00089a010
44209151 59107 1 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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 301 3 2 2 3.8 O=C(Cc1ccccc1)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
CHEMBL171108 59107 1 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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 301 3 2 2 3.8 O=C(Cc1ccccc1)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
44336539 5060 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 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 5060 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 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
14208245 203041 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00047a021
CHEMBL74580 203041 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00047a021
155553269 173545 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 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 173545 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 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
44348870 114317 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 452 7 3 5 3.3 O=C(O)CCC(NC(=O)c1cnc2ccccc2c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
CHEMBL334171 114317 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 452 7 3 5 3.3 O=C(O)CCC(NC(=O)c1cnc2ccccc2c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
44348887 117573 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 469 7 3 4 4.0 O=C(O)CCC(NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
CHEMBL340630 117573 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 469 7 3 4 4.0 O=C(O)CCC(NC(=O)c1ccc(Cl)c(Cl)c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
880 2199 3 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 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 10.1021/jm9506736
9935175 2199 3 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 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 10.1021/jm9506736
CHEMBL2093059 2199 3 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 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 10.1021/jm9506736
15104628 9895 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 534 10 2 5 4.6 CCOC(=O)CN(Cc1ccccc1)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL114926 9895 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 534 10 2 5 4.6 CCOC(=O)CN(Cc1ccccc1)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
10369336 116242 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL337574 116242 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14991535 106299 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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)CCc1cccc(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144534 106299 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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)CCc1cccc(O)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44366563 119152 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.5-4.6 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.5-4.6 uM
ChEMBL 447 6 2 2 5.8 O=C1C(Cc2c[nH]c3ccccc23)CN(Cc2ccccc2)C[C@@H]1Cc1c[nH]c2ccccc12 10.1016/0960-894X(94)80030-8
CHEMBL347058 119152 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.5-4.6 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.5-4.6 uM
ChEMBL 447 6 2 2 5.8 O=C1C(Cc2c[nH]c3ccccc23)CN(Cc2ccccc2)C[C@@H]1Cc1c[nH]c2ccccc12 10.1016/0960-894X(94)80030-8
CHEMBL169054 207082 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
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 CCCC[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
11200806 137824 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 414 8 3 3 3.8 O=C(/C=C/c1ccccc1)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1021/jm051050n
CHEMBL377157 137824 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 414 8 3 3 3.8 O=C(/C=C/c1ccccc1)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1021/jm051050n
89913436 140244 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 2 1 2 2.6 O=C1C=C(Cl)C(O)(c2ccc(Cl)cc2)N1C1CC1 10.1039/C6MD00052E
CHEMBL3818705 140244 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 2 1 2 2.6 O=C1C=C(Cl)C(O)(c2ccc(Cl)cc2)N1C1CC1 10.1039/C6MD00052E
15167800 32485 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 412 4 3 3 4.4 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)c1cc2ccccc2[nH]1 10.1021/jm00163a069
CHEMBL141365 32485 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 412 4 3 3 4.4 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)c1cc2ccccc2[nH]1 10.1021/jm00163a069
10369346 24749 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 Cc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)Nc3ccncc3)C2=O)cc1 10.1021/jm00078a018
CHEMBL134618 24749 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 Cc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)Nc3ccncc3)C2=O)cc1 10.1021/jm00078a018
CHEMBL169054 207082 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
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 CCCC[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
14208211 202699 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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 311 2 2 3 2.1 CC(=O)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL72057 202699 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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 311 2 2 3 2.1 CC(=O)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00120a002
11200806 137824 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 414 8 3 3 3.8 O=C(/C=C/c1ccccc1)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1016/j.bmc.2009.05.067
CHEMBL377157 137824 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 414 8 3 3 3.8 O=C(/C=C/c1ccccc1)Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O 10.1016/j.bmc.2009.05.067
44300550 100416 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 376 3 2 3 3.7 Cc1cccc(NC(=O)NC2N=C(C3CCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
CHEMBL293786 100416 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 376 3 2 3 3.7 Cc1cccc(NC(=O)NC2N=C(C3CCC3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
44356801 164948 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 408 3 2 3 3.6 C#Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL424076 164948 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 408 3 2 3 3.6 C#Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
10696336 203614 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 487 5 3 4 4.6 CCCN1C(=O)[C@H](NC(=O)Nc2ccc3c(c2)CCC3)N=C([C@H]2CC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
CHEMBL79565 203614 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 487 5 3 4 4.6 CCCN1C(=O)[C@H](NC(=O)Nc2ccc3c(c2)CCC3)N=C([C@H]2CC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
71461592 78062 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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)CC[C@H](NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
CHEMBL2111828 78062 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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)CC[C@H](NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCC2)CC1 10.1021/jm00079a003
44357068 164319 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 3 4 3.6 CN1C(=O)C(NC(=O)NCc2cccc(C(C)(C)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL422102 164319 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 3 4 3.6 CN1C(=O)C(NC(=O)NCc2cccc(C(C)(C)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44408524 155152 0 None -169 4 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1134 30 12 15 2.6 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](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL405192 155152 0 None -169 4 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1134 30 12 15 2.6 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](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
10323431 57432 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 493 4 3 7 2.9 CN1C(=O)[C@H](NC(=O)Nc2ccc3c(c2)N(c2nn[nH]n2)CC3)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
CHEMBL166941 57432 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 493 4 3 7 2.9 CN1C(=O)[C@H](NC(=O)Nc2ccc3c(c2)N(c2nn[nH]n2)CC3)N=C(c2ccccc2)c2ccccc21 10.1021/jm9506736
10056421 106132 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
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)Nc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
CHEMBL3143025 106132 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
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)Nc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
14208245 203041 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00120a002
CHEMBL74580 203041 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00120a002
CHEMBL317755 209449 0 None - 0 Guinea pig 7.4 pIC50 = 7.4 Binding
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)NS(C)(=O)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
44578772 182204 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CCK1 receptorInhibition of 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 182204 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CCK1 receptorInhibition of 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
52949124 861 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
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 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 861 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
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 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 861 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
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 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 861 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
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 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
44336565 108715 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 671 8 2 7 5.7 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C4(C(F)(F)F)N=N4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/s0960-894x(98)00548-4
CHEMBL321700 108715 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 671 8 2 7 5.7 COc1ccc(N(C)C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C4(C(F)(F)F)N=N4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1016/s0960-894x(98)00548-4
10346957 26732 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 531 7 2 4 4.9 CCN(CC)C(=O)C(C)N1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL136436 26732 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 531 7 2 4 4.9 CCN(CC)C(=O)C(C)N1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10002123 78386 1 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
CHEMBL2112748 78386 1 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
14991539 106298 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 859 22 8 8 3.8 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144533 106298 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 859 22 8 8 3.8 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCc1ccc(Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44366345 118967 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.3-5.4 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.3-5.4 uM
ChEMBL 447 6 2 2 5.8 O=C1[C@@H](Cc2c[nH]c3ccccc23)CN(Cc2ccccc2)C[C@H]1Cc1c[nH]c2ccccc12 10.1016/0960-894X(94)80030-8
CHEMBL345327 118967 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.3-5.4 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 3.3-5.4 uM
ChEMBL 447 6 2 2 5.8 O=C1[C@@H](Cc2c[nH]c3ccccc23)CN(Cc2ccccc2)C[C@H]1Cc1c[nH]c2ccccc12 10.1016/0960-894X(94)80030-8
19766221 118371 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 569 7 3 5 5.2 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1021/jm00163a069
CHEMBL342256 118371 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 569 7 3 5 5.2 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1021/jm00163a069
44280116 99158 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 672 12 3 6 5.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL284183 99158 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 672 12 3 6 5.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
10392698 116790 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 546 5 3 3 5.9 Cc1ccc([C@H]2C[C@@H](NC(=O)Nc3cccc(Cl)c3)C(=O)N(CC(=O)NC(C)(C)C)c3cc(C)ccc32)cc1 10.1021/jm00048a015
CHEMBL339678 116790 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 546 5 3 3 5.9 Cc1ccc([C@H]2C[C@@H](NC(=O)Nc3cccc(Cl)c3)C(=O)N(CC(=O)NC(C)(C)C)c3cc(C)ccc32)cc1 10.1021/jm00048a015
53465906 69054 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 456 8 5 4 3.7 O=C(Nc1ccccc1C(=O)NC(CCc1ccccc1)C(=O)NO)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933108 69054 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 456 8 5 4 3.7 O=C(Nc1ccccc1C(=O)NC(CCc1ccccc1)C(=O)NO)c1cc2ccccc2[nH]1 10.1021/jm200438b
44152863 119844 4 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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(c2ccccc2)C1c1ccccc1 10.1016/S0960-894X(00)80684-8
CHEMBL353189 119844 4 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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(c2ccccc2)C1c1ccccc1 10.1016/S0960-894X(00)80684-8
71450860 78174 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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
CHEMBL2112273 78174 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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
14208301 105161 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 412 3 1 4 3.3 CN1C(=O)C(NC(=O)c2ccc(C#N)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL312524 105161 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 412 3 1 4 3.3 CN1C(=O)C(NC(=O)c2ccc(C#N)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
10555571 104085 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 601 8 0 6 5.9 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
CHEMBL310466 104085 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 601 8 0 6 5.9 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
52949124 861 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] 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 861 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] 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 861 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] 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 861 2 None -2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] 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 73286 2 None 2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R T3.28V, T3.29S 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 73286 2 None 2 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-CCK] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R T3.28V, T3.29S 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
155533520 171252 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 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 171252 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 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
10555571 104085 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 0 6 5.9 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL310466 104085 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 0 6 5.9 COc1ccc(N(C(=O)CN2C(=O)C(Cc3nn(C)c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
10841358 205677 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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]c4ccc(F)cc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL94005 205677 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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]c4ccc(F)cc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
44334354 4538 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 517 9 2 4 5.0 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCC(C(=O)c3ccc(F)cc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL102879 4538 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 517 9 2 4 5.0 Cc1cccc(NC(=O)N[C@H](COCc2ccccc2)C(=O)N2CCC(C(=O)c3ccc(F)cc3)CC2)c1 10.1016/0960-894X(95)00537-3
44300744 101470 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 542 6 4 4 4.7 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
CHEMBL301261 101470 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 542 6 4 4 4.7 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
10623795 205543 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 COc1ccccc1NC(=O)NNc1nc2ccccc2c(=O)n1-c1cccc(OC(C)C)c1 10.1021/jm970373j
CHEMBL9319 205543 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 COc1ccccc1NC(=O)NNc1nc2ccccc2c(=O)n1-c1cccc(OC(C)C)c1 10.1021/jm970373j
10478431 9791 7 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
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)c1ccc2ccccc2c1 10.1021/jm00124a003
CHEMBL114325 9791 7 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
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)c1ccc2ccccc2c1 10.1021/jm00124a003
14519981 9950 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
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 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2n1 10.1021/jm00124a003
CHEMBL115269 9950 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
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 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2n1 10.1021/jm00124a003
15104618 108541 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
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 496 13 3 2 6.8 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00116a002
CHEMBL321265 108541 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
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 496 13 3 2 6.8 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00116a002
44281078 99269 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 16 4 8 5.9 CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL284975 99269 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 773 16 4 8 5.9 CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
193319 20561 5 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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 268 1 0 2 2.6 CN1C(=O)CN=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL13095 20561 5 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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 268 1 0 2 2.6 CN1C(=O)CN=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL120632 206853 30 None - 3 Rat 5.4 pIC50 = 5.4 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasConcentration producing half-maximal 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](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/0960-894X(94)85022-4
11729474 4588 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 420 2 2 5 2.1 Cc1cccc(NC(=O)NC2N=C(N3CCN(C)CC3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00530-0
CHEMBL103229 4588 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 420 2 2 5 2.1 Cc1cccc(NC(=O)NC2N=C(N3CCN(C)CC3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00530-0
14208302 67388 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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 1 4 3.3 CN1C(=O)[C@@H](NC(=O)c2ccc(C#N)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907847 67388 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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 1 4 3.3 CN1C(=O)[C@@H](NC(=O)c2ccc(C#N)cc2)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
24785432 180969 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CCK1 receptorInhibition of 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 180969 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CCK1 receptorInhibition of 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
24785176 180971 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CCK1 receptorInhibition of 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 180971 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human CCK1 receptorInhibition of 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
CHEMBL169178 207084 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
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 CCOC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N1CC(=O)N[C@@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
15104613 109813 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 486 13 3 2 6.2 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00116a002
CHEMBL323854 109813 0 None - 0 Guinea pig 6.4 pIC50 = 6.4 Binding
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 486 13 3 2 6.2 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00116a002
10364355 27728 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 412 4 2 3 3.9 C[C@H](NC(=O)NC1N=C(c2ccccc2)c2ccccc2N(C)C1=O)c1ccccc1 10.1021/jm00078a018
CHEMBL137208 27728 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 412 4 2 3 3.9 C[C@H](NC(=O)NC1N=C(c2ccccc2)c2ccccc2N(C)C1=O)c1ccccc1 10.1021/jm00078a018
44280266 98309 0 None - 1 Mouse 6.4 pIC50 = 6.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 729 14 4 7 5.0 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL278217 98309 0 None - 1 Mouse 6.4 pIC50 = 6.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 729 14 4 7 5.0 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
108187 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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 10.1016/S0960-894X(00)80273-5
873 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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 10.1016/S0960-894X(00)80273-5
CHEMBL2062154 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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 10.1016/S0960-894X(00)80273-5
CHEMBL287735 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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 10.1016/S0960-894X(00)80273-5
59923871 73597 1 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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; 1200-8500Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 1200-8500
ChEMBL 614 12 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCC(NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(00)80156-0
CHEMBL2021374 73597 1 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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; 1200-8500Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 1200-8500
ChEMBL 614 12 5 5 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCC(NC(=O)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(00)80156-0
108187 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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/jm00105a062
873 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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/jm00105a062
CHEMBL2062154 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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/jm00105a062
CHEMBL287735 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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/jm00105a062
14802537 85547 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 614 12 5 5 4.9 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)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL2304062 85547 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 614 12 5 5 4.9 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)CCC(=O)O)c1ccccc1 10.1016/S0960-894X(01)80769-1
108187 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(00)80685-X
873 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(00)80685-X
CHEMBL2062154 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(00)80685-X
CHEMBL287735 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)CCC(=O)O 10.1016/S0960-894X(00)80685-X
14802538 96228 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 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(98)00677-5
CHEMBL263969 96228 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 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(98)00677-5
108187 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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 10.1016/S0960-894X(97)00356-9
873 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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 10.1016/S0960-894X(97)00356-9
CHEMBL2062154 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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 10.1016/S0960-894X(97)00356-9
CHEMBL287735 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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 10.1016/S0960-894X(97)00356-9
44368727 118987 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 598 12 5 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00057a005
CHEMBL345511 118987 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 598 12 5 4 4.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00057a005
44153340 31444 5 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 413 3 0 4 3.8 CN1c2ccccc2C(c2ccccc2F)=NCC1CN1C(=O)c2ccccc2C1=O 10.1021/jm00163a069
CHEMBL140516 31444 5 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 413 3 0 4 3.8 CN1c2ccccc2C(c2ccccc2F)=NCC1CN1C(=O)c2ccccc2C1=O 10.1021/jm00163a069
108187 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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/jm970065l
873 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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/jm970065l
CHEMBL2062154 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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/jm970065l
CHEMBL287735 911 30 None 4 5 Rat 5.4 pIC50 = 5.4 Binding
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 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/jm970065l
14802539 76184 1 None - 1 Rat 5.4 pIC50 = 5.4 Binding
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 1200-8500The 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 1200-8500
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)80652-6
CHEMBL2062144 76184 1 None - 1 Rat 5.4 pIC50 = 5.4 Binding
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 1200-8500The 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 1200-8500
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)80652-6
136060577 87234 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
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 495 4 1 5 6.3 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccccc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
CHEMBL233647 87234 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
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 495 4 1 5 6.3 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccccc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
44369595 167951 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 475 7 2 7 4.2 Cc1cccc(NCNC2N=C(c3nccs3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL435447 167951 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 475 7 2 7 4.2 Cc1cccc(NCNC2N=C(c3nccs3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
9978270 78387 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 3 4 3.2 CN1C(=O)[C@H](NC(=O)Nc2cccc(N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2112749 78387 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 3 4 3.2 CN1C(=O)[C@H](NC(=O)Nc2cccc(N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10323637 105692 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 498 7 2 5 3.6 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm00078a018
CHEMBL313813 105692 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 498 7 2 5 3.6 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm00078a018
10323637 105692 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 498 7 2 5 3.6 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm9608523
CHEMBL313813 105692 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 498 7 2 5 3.6 CCN(CC)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm9608523
10973981 78009 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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(c3cccc([N+](=O)[O-])c3)C(=O)C[C@@H]12 10.1021/jm010813d
CHEMBL2111548 78009 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
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(c3cccc([N+](=O)[O-])c3)C(=O)C[C@@H]12 10.1021/jm010813d
46234970 73278 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 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 73278 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
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 620 7 1 5 6.7 O=C1C(Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc2N1CC(=O)N1CCCCC1Cc1ccccc1 10.1016/j.bmcl.2012.02.049
10051431 120600 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 494 6 2 4 5.1 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
CHEMBL357502 120600 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 494 6 2 4 5.1 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
44336487 110499 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 699 9 2 7 6.5 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C4(C(F)(F)F)N=N4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1016/s0960-894x(98)00548-4
CHEMBL326251 110499 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 699 9 2 7 6.5 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C4(C(F)(F)F)N=N4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1016/s0960-894x(98)00548-4
14802525 116214 1 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 626 12 5 5 4.5 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)/C=C/C(=O)O)Cc1ccccc1 10.1021/jm00105a062
CHEMBL337384 116214 1 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 626 12 5 5 4.5 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)/C=C/C(=O)O)Cc1ccccc1 10.1021/jm00105a062
44368613 120476 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 610 12 5 4 4.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CNC(=O)/C=C/C(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL356419 120476 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 610 12 5 4 4.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CNC(=O)/C=C/C(=O)O)Cc1ccccc1 10.1021/jm00057a005
73351319 167590 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 648 12 5 5 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCP(C)(=O)O)c1ccccc1 10.1021/jm00092a007
CHEMBL433148 167590 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 648 12 5 5 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCP(C)(=O)O)c1ccccc1 10.1021/jm00092a007
CHEMBL282175 98850 0 None - 1 Mouse 5.4 pIC50 = 5.4 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 769 16 6 11 4.6 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)NCCCC(=O)NCCSCc3csc(C=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00249-1
44591882 178387 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 466 7 5 3 4.3 O=C(Nc1ccccc1C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL470622 178387 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 466 7 5 3 4.3 O=C(Nc1ccccc1C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
10789229 97915 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 440 6 3 7 3.8 CCOc1cccc(-n2c(NNC(=O)Nc3cccc(C#N)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL275307 97915 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 440 6 3 7 3.8 CCOc1cccc(-n2c(NNC(=O)Nc3cccc(C#N)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
10091467 116192 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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)Nc2ccccn2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL337285 116192 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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)Nc2ccccn2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44362744 34432 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 546 7 4 5 3.5 CC(C)(C)OC(=O)N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@@H](CC(=O)O)Cc3ccccc3)N2C1=O 10.1016/s0960-894x(98)00677-5
CHEMBL143012 34432 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 546 7 4 5 3.5 CC(C)(C)OC(=O)N[C@H]1C[C@@H]2c3[nH]c4ccccc4c3C[C@@H](C(=O)N[C@@H](CC(=O)O)Cc3ccccc3)N2C1=O 10.1016/s0960-894x(98)00677-5
40875375 198356 1 None - 1 Rat 6.4 pIC50 = 6.4 Binding
Concentration required for binding affinity to neuropeptide (CCK-A) receptor in rat pancreaConcentration required for binding affinity to neuropeptide (CCK-A) receptor in rat pancrea
ChEMBL 480 9 4 3 4.8 O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1c[nH]c2ccccc12)OCc1ccccc1 10.1016/S0960-894X(97)00346-6
CHEMBL59561 198356 1 None - 1 Rat 6.4 pIC50 = 6.4 Binding
Concentration required for binding affinity to neuropeptide (CCK-A) receptor in rat pancreaConcentration required for binding affinity to neuropeptide (CCK-A) receptor in rat pancrea
ChEMBL 480 9 4 3 4.8 O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCCc1c[nH]c2ccccc12)OCc1ccccc1 10.1016/S0960-894X(97)00346-6
11801355 116355 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 580 8 3 6 3.6 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@@H](NC(=O)OCc3ccccc3)C(=O)N21 10.1021/jm000959x
CHEMBL338186 116355 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 580 8 3 6 3.6 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@@H](NC(=O)OCc3ccccc3)C(=O)N21 10.1021/jm000959x
44360340 32470 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 457 5 1 4 5.1 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)Cc1cccc2sccc12 10.1021/jm00163a069
CHEMBL141354 32470 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 457 5 1 4 5.1 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)Cc1cccc2sccc12 10.1021/jm00163a069
89913625 140217 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 293 6 1 2 3.4 CCCCCCN1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
CHEMBL3818303 140217 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 293 6 1 2 3.4 CCCCCCN1C(=O)C=C(Cl)C1(O)c1ccccc1 10.1039/C6MD00052E
14802538 96228 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 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 10.1021/jm00092a007
CHEMBL263969 96228 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 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 10.1021/jm00092a007
44334033 107306 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
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 475 6 2 4 4.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
CHEMBL319196 107306 0 None - 0 Guinea pig 5.4 pIC50 = 5.4 Binding
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 475 6 2 4 4.7 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
57390472 67398 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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 431 5 1 4 3.3 COc1cccc(CC(=O)N[C@@H]2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)c1 10.1021/jm00120a002
CHEMBL1907856 67398 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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 431 5 1 4 3.3 COc1cccc(CC(=O)N[C@@H]2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)c1 10.1021/jm00120a002
44359881 118784 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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 473 8 1 5 4.1 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)CCC(=O)OCc1ccccc1 10.1021/jm00163a069
CHEMBL343969 118784 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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 473 8 1 5 4.1 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)CCC(=O)OCc1ccccc1 10.1021/jm00163a069
10574611 205510 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 429 6 3 6 4.3 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3ccccc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL9291 205510 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 429 6 3 6 4.3 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3ccccc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL171310 207094 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
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)OC(C)(C)C)C(=O)N1CC(=O)N[C@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
10010811 106113 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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)c1ccc(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
CHEMBL3142898 106113 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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)c1ccc(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
42636923 178243 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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 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 178243 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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 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
15104624 9890 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 2 4 5.7 CCCCCN(CCCCC)C(=O)[C@@H](CC1C(=O)Nc2ccccc21)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL114913 9890 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 2 4 5.7 CCCCCN(CCCCC)C(=O)[C@@H](CC1C(=O)Nc2ccccc21)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
10341040 116096 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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)Nc2ccc(F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL336749 116096 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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)Nc2ccc(F)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44336539 5060 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]CCK from CCK1R (unknown origin) 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 5060 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]CCK from CCK1R (unknown origin) 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
10393441 171137 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 580 7 3 3 6.5 CC(C)(NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm00048a015
CHEMBL446682 171137 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 580 7 3 3 6.5 CC(C)(NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm00048a015
44362685 121314 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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
CHEMBL358989 121314 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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
14720386 48045 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 463 12 2 4 4.4 CCCN(CCC)C(=O)[C@H](CCC(=O)OCc1ccccc1)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
CHEMBL155406 48045 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 463 12 2 4 4.4 CCCN(CCC)C(=O)[C@H](CCC(=O)OCc1ccccc1)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
44281005 116218 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 787 17 4 8 6.4 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00249-1
CHEMBL33743 116218 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 787 17 4 8 6.4 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00249-1
44592046 178318 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 393 6 3 3 4.0 CC(C)C[C@H](NC(=O)N(C(=O)c1cc2ccccc2[nH]1)c1ccccc1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL469980 178318 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 393 6 3 3 4.0 CC(C)C[C@H](NC(=O)N(C(=O)c1cc2ccccc2[nH]1)c1ccccc1)C(=O)O 10.1016/j.bmc.2009.02.012
10347746 16607 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 558 6 3 3 6.2 CC1(NC(=O)CN2C(=O)[C@H](NC(=O)Nc3cccc(Cl)c3)C[C@H](c3ccccc3)c3ccccc32)CCCCC1 10.1021/jm00048a015
CHEMBL124611 16607 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 558 6 3 3 6.2 CC1(NC(=O)CN2C(=O)[C@H](NC(=O)Nc3cccc(Cl)c3)C[C@H](c3ccccc3)c3ccccc32)CCCCC1 10.1021/jm00048a015
44368633 46267 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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
CHEMBL153787 46267 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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
115208 3746 25 None -91 4 Rat 7.3 pIC50 = 7.3 Binding
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 1 4 4.0 O=C(c1ccsc1)NCC1CN=C(c2c(N1C)cccc2)c1ccccc1F 10.1021/jm00163a069
1667 3746 25 None -91 4 Rat 7.3 pIC50 = 7.3 Binding
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 1 4 4.0 O=C(c1ccsc1)NCC1CN=C(c2c(N1C)cccc2)c1ccccc1F 10.1021/jm00163a069
CHEMBL169703 3746 25 None -91 4 Rat 7.3 pIC50 = 7.3 Binding
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 1 4 4.0 O=C(c1ccsc1)NCC1CN=C(c2c(N1C)cccc2)c1ccccc1F 10.1021/jm00163a069
10769565 17775 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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 580 8 3 6 3.6 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1021/jm000959x
CHEMBL126160 17775 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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 580 8 3 6 3.6 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1Cc2c([nH]c3ccccc23)[C@H]2C[C@H](NC(=O)OCc3ccccc3)C(=O)N12 10.1021/jm000959x
9982757 51181 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 483 5 2 5 4.3 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL158235 51181 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 483 5 2 5 4.3 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
44381562 168038 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 827 22 10 9 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NNC[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
CHEMBL436053 168038 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 827 22 10 9 3.5 Cc1ccccc1NC(=O)NCCCC[C@H](NNC[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
11505691 140381 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
ChEMBL 667 9 2 6 5.8 COc1ccc(N(C)C(=O)CN2C(=O)[C@@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1021/jm049072h
CHEMBL382263 140381 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
ChEMBL 667 9 2 6 5.8 COc1ccc(N(C)C(=O)CN2C(=O)[C@@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1021/jm049072h
9891461 164459 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 483 5 2 5 4.3 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
CHEMBL422604 164459 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 483 5 2 5 4.3 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
15104598 109282 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 481 13 2 2 6.4 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)cc1 10.1021/jm00116a002
CHEMBL323245 109282 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 481 13 2 2 6.4 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc(Cl)cc1 10.1021/jm00116a002
14208258 102470 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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(c2ccccc2)c2ccccc2NC1=O)c1ccc(F)cc1 10.1021/jm00047a021
CHEMBL306394 102470 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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(c2ccccc2)c2ccccc2NC1=O)c1ccc(F)cc1 10.1021/jm00047a021
10769675 205460 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 COc1cccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)c1 10.1021/jm970265x
CHEMBL92586 205460 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 COc1cccc(N(C(=O)CN2C(=O)C(Cc3n[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)c1 10.1021/jm970265x
14208200 203001 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 422 5 3 3 4.0 O=C(CCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00047a021
CHEMBL74181 203001 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 422 5 3 3 4.0 O=C(CCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00047a021
44341613 9507 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 516 13 2 3 6.4 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccc(F)cc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL112622 9507 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 516 13 2 3 6.4 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccc(F)cc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
52940616 17940 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human 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 17940 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human 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
10453063 106495 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 391 2 2 4 3.0 Cc1cccc(NC(=O)NC2N=C(N3CCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL315214 106495 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 391 2 2 4 3.0 Cc1cccc(NC(=O)NC2N=C(N3CCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
21842331 43277 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 522 7 2 4 5.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)CC3CCCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
CHEMBL150869 43277 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 522 7 2 4 5.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)CC3CCCCC3)C2=O)c1 10.1016/0960-894X(95)00556-9
73349791 204083 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 664 13 5 6 5.2 CCOP(=O)(O)CC(=O)N[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1021/jm00092a007
CHEMBL83244 204083 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 664 13 5 6 5.2 CCOP(=O)(O)CC(=O)N[C@H](CNC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1021/jm00092a007
14208258 102470 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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(c2ccccc2)c2ccccc2NC1=O)c1ccc(F)cc1 10.1021/jm00120a002
CHEMBL306394 102470 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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(c2ccccc2)c2ccccc2NC1=O)c1ccc(F)cc1 10.1021/jm00120a002
44370461 119048 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
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 119048 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 488 15 2 4 4.8 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)N1CCCC1)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
10453063 106495 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 391 2 2 4 3.0 Cc1cccc(NC(=O)NC2N=C(N3CCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
CHEMBL315214 106495 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 391 2 2 4 3.0 Cc1cccc(NC(=O)NC2N=C(N3CCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
14208200 203001 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 5 3 3 4.0 O=C(CCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
CHEMBL74181 203001 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 5 3 3 4.0 O=C(CCc1c[nH]c2ccccc12)NC1N=C(c2ccccc2)c2ccccc2NC1=O 10.1021/jm00120a002
19766220 31703 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 4 3.8 CN1c2ccccc2C(c2ccccc2F)NCC1CNC(=O)c1ccsc1 10.1021/jm00163a069
CHEMBL140749 31703 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 4 3.8 CN1c2ccccc2C(c2ccccc2F)NCC1CNC(=O)c1ccsc1 10.1021/jm00163a069
10323073 25192 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 484 7 2 5 3.8 CCOC(=O)CN1C(=O)C(NC(=O)N[C@@H](C)c2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL134987 25192 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 484 7 2 5 3.8 CCOC(=O)CN1C(=O)C(NC(=O)N[C@@H](C)c2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44280252 99378 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 655 11 5 8 3.7 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL285746 99378 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 655 11 5 8 3.7 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
6604124 55296 3 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
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
CHEMBL1315743 55296 3 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
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
CHEMBL162111 55296 3 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
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
70682900 77481 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
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 385 3 2 3 4.6 O=C1Nc2ccccc2C(c2ccccc2F)=NC1C[C@@H]1CNc2ccccc21 10.1021/jm00390a019
CHEMBL2092991 77481 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
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 385 3 2 3 4.6 O=C1Nc2ccccc2C(c2ccccc2F)=NC1C[C@@H]1CNc2ccccc21 10.1021/jm00390a019
20063212 166577 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
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 395 3 0 3 4.5 CN1CC(CC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c2ccccc21 10.1021/jm00390a019
CHEMBL429063 166577 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
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 395 3 0 3 4.5 CN1CC(CC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c2ccccc21 10.1021/jm00390a019
44349353 116329 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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 415 7 3 4 3.0 Cc1cc(C)cc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
CHEMBL338045 116329 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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 415 7 3 4 3.0 Cc1cc(C)cc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
44381852 58719 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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
CHEMBL169398 58719 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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
44361604 31247 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 621 8 3 4 4.9 O=C(N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm991078x
CHEMBL140320 31247 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 621 8 3 4 4.9 O=C(N[C@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C12CC3CC(CC(C3)C1)C2 10.1021/jm991078x
44381730 13836 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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 450 8 2 4 2.5 CN1CCN(C(=O)CCC(NC(=O)c2cccc(Cl)c2)C(=O)NCCC(C)(C)C)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL1196729 13836 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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 450 8 2 4 2.5 CN1CCN(C(=O)CCC(NC(=O)c2cccc(Cl)c2)C(=O)NCCC(C)(C)C)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL557997 13836 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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 450 8 2 4 2.5 CN1CCN(C(=O)CCC(NC(=O)c2cccc(Cl)c2)C(=O)NCCC(C)(C)C)CC1 10.1016/S0960-894X(00)80681-2
10320031 77457 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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
CHEMBL2092868 77457 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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
90663981 106315 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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)c(Cl)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144550 106315 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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)c(Cl)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
70689603 73232 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 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 73232 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 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
52946666 17937 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human 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 17937 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from human 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
44300743 100479 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 572 6 4 6 4.7 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
CHEMBL294161 100479 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 572 6 4 6 4.7 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
11679146 134819 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
ChEMBL 667 9 2 6 5.8 COc1ccc(N(C)C(=O)CN2C(=O)[C@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1021/jm049072h
CHEMBL372773 134819 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
ChEMBL 667 9 2 6 5.8 COc1ccc(N(C)C(=O)CN2C(=O)[C@H](NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)cc1 10.1021/jm049072h
11741582 27738 6 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 398 4 2 3 3.3 CN1C(=O)C(NC(=O)NCc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137213 27738 6 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 398 4 2 3 3.3 CN1C(=O)C(NC(=O)NCc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10029145 97705 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 504 7 2 5 4.6 CCOC(=O)CCN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL273919 97705 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 504 7 2 5 4.6 CCOC(=O)CCN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10693825 205317 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 428 5 3 6 3.9 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(N(C)C)c2)c1 10.1021/jm970373j
CHEMBL9171 205317 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 428 5 3 6 3.9 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(N(C)C)c2)c1 10.1021/jm970373j
6604124 55296 3 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
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 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
CHEMBL1315743 55296 3 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
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 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
CHEMBL162111 55296 3 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
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 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
10528637 96842 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 477 6 3 7 4.4 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(Cl)c2)c1 10.1021/jm970373j
CHEMBL269123 96842 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 477 6 3 7 4.4 CCOC(=O)c1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(Cl)c2)c1 10.1021/jm970373j
14208229 102680 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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 430 3 3 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(F)ccc2[nH]1 10.1021/jm00120a002
CHEMBL308111 102680 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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 430 3 3 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(F)ccc2[nH]1 10.1021/jm00120a002
14208229 102680 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 430 3 3 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(F)ccc2[nH]1 10.1021/jm00047a021
CHEMBL308111 102680 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 430 3 3 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(F)ccc2[nH]1 10.1021/jm00047a021
44306823 201369 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 802 20 9 7 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(CCCCNC(=O)Nc1ccccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
CHEMBL63707 201369 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 802 20 9 7 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NC(CCCCNC(=O)Nc1ccccc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(C)cc1)C(N)=O 10.1021/jm00001a027
3081191 9442 9 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
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 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00124a003
CHEMBL112307 9442 9 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
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 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00124a003
3081191 9442 9 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
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 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL112307 9442 9 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
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 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
44293812 101232 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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 645 5 2 4 5.9 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(Br)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
CHEMBL299523 101232 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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 645 5 2 4 5.9 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(Br)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
11027990 67177 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 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 67177 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 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
44330874 206611 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 2.1 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\c1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL99499 206611 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 2.1 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\c1ccccc1)C(N)=O 10.1021/jm00094a001
10056407 119630 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
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 7 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)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL351364 119630 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
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 7 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)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL318570 209459 0 None - 0 Guinea pig 8.3 pIC50 = 8.3 Binding
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)NC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL438911 212048 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
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
24785180 180948 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human CCK1 receptorInhibition of 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 180948 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human CCK1 receptorInhibition of 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
11803697 106121 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
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)Nc1cccc([N+](=O)[O-])c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
136898911 106121 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
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)Nc1cccc([N+](=O)[O-])c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
CHEMBL3142912 106121 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
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)Nc1cccc([N+](=O)[O-])c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm960509y
15667013 106909 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
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 920 26 10 11 0.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)CNC(=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
CHEMBL318010 106909 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
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 920 26 10 11 0.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)CNC(=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
CHEMBL319439 209462 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
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 CNC(=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
3960 2303 20 None - 1 Rat 7.3 pIC50 = 7.3 Binding
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 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00079a003
891 2303 20 None - 1 Rat 7.3 pIC50 = 7.3 Binding
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 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00079a003
CHEMBL24938 2303 20 None - 1 Rat 7.3 pIC50 = 7.3 Binding
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 458 14 2 3 5.2 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCCC 10.1021/jm00079a003
44349077 117325 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)c1cc(Cl)cc(Cl)c1 10.1021/jm00079a003
CHEMBL340263 117325 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)c1cc(Cl)cc(Cl)c1 10.1021/jm00079a003
10483574 6114 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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 591 8 2 5 5.3 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1016/s0960-894x(98)00548-4
CHEMBL108130 6114 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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 591 8 2 5 5.3 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1016/s0960-894x(98)00548-4
13605417 205824 3 None - 1 Rat 7.3 pIC50 = 7.3 Binding
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 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(00)80681-2
CHEMBL9485 205824 3 None - 1 Rat 7.3 pIC50 = 7.3 Binding
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 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(00)80681-2
10458620 114035 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 499 5 2 4 5.4 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)OC(C)(C)C)C2=O)c1 10.1021/jm00048a015
CHEMBL333718 114035 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 499 5 2 4 5.4 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3)c3ccccc3N(CC(=O)OC(C)(C)C)C2=O)c1 10.1021/jm00048a015
13605417 205824 3 None - 1 Rat 7.3 pIC50 = 7.3 Binding
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 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(00)80687-3
CHEMBL9485 205824 3 None - 1 Rat 7.3 pIC50 = 7.3 Binding
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 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1016/S0960-894X(00)80687-3
14991580 100228 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 829 21 8 9 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C/c1cccs1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL292490 100228 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 829 21 8 9 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C/c1cccs1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
10507109 108727 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
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 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm9601664
CHEMBL321761 108727 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
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 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm9601664
10507109 108727 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
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 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm950626d
CHEMBL321761 108727 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
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 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm950626d
10507109 108727 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
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 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/S0960-894X(97)00062-0
CHEMBL321761 108727 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
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 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/S0960-894X(97)00062-0
44336539 5060 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]BDZ1 from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R 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 5060 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]BDZ1 from CCK1R TM3 (unknown origin) containing T3.28V, T3.29S chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R 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
11039204 78165 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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 588 7 3 6 4.2 CN(C)c1cccc(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
CHEMBL2112231 78165 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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 588 7 3 6 4.2 CN(C)c1cccc(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
14208265 202794 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cc(Cl)cc(Cl)c1 10.1021/jm00120a002
CHEMBL72616 202794 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cc(Cl)cc(Cl)c1 10.1021/jm00120a002
14802530 21402 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 614 12 5 5 4.3 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)CC(=O)O)Cc1ccccc1 10.1021/jm00105a062
CHEMBL131754 21402 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 614 12 5 5 4.3 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)CC(=O)O)Cc1ccccc1 10.1021/jm00105a062
15104607 162849 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 497 13 2 2 6.9 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccc2ccccc12 10.1021/jm00116a002
CHEMBL419585 162849 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 497 13 2 2 6.9 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cccc2ccccc12 10.1021/jm00116a002
44334305 109218 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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)N2CCC(C(=O)Nc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL322913 109218 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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)N2CCC(C(=O)Nc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
101918113 114902 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 650 14 6 7 0.7 CS[C@H]1C[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)N(C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(C)=O)C1 10.1021/jm00001a019
CHEMBL3350334 114902 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 650 14 6 7 0.7 CS[C@H]1C[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)N(C(=O)[C@H](Cc2c[nH]c3ccccc23)NC(C)=O)C1 10.1021/jm00001a019
CHEMBL407736 210923 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00378a012
44211354 12740 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 536 6 1 4 4.2 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL1188705 12740 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 536 6 1 4 4.2 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL537171 12740 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 536 6 1 4 4.2 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
44280740 99928 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 787 17 4 8 6.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL290122 99928 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 787 17 4 8 6.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL289310 209116 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00378a012
20063240 13524 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
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 480 6 2 4 4.7 CC(C)CC(N)C(=O)N1CC(CC2N=C(c3ccccc3)c3ccccc3NC2=O)c2ccccc21 10.1021/jm00390a019
CHEMBL1194526 13524 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
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 480 6 2 4 4.7 CC(C)CC(N)C(=O)N1CC(CC2N=C(c3ccccc3)c3ccccc3NC2=O)c2ccccc21 10.1021/jm00390a019
CHEMBL552817 13524 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
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 480 6 2 4 4.7 CC(C)CC(N)C(=O)N1CC(CC2N=C(c3ccccc3)c3ccccc3NC2=O)c2ccccc21 10.1021/jm00390a019
15614807 67370 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
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 365 3 2 2 4.6 O=C1Nc2ccccc2C(c2ccccc2)=N[C@@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
CHEMBL1907740 67370 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
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 365 3 2 2 4.6 O=C1Nc2ccccc2C(c2ccccc2)=N[C@@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
14208265 202794 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 423 3 2 3 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cc(Cl)cc(Cl)c1 10.1021/jm00047a021
CHEMBL72616 202794 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 423 3 2 3 4.5 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cc(Cl)cc(Cl)c1 10.1021/jm00047a021
887 4035 24 None - 4 Rat 6.3 pIC50 = 6.3 Binding
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 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 10.1021/jm960669+
9870520 4035 24 None - 4 Rat 6.3 pIC50 = 6.3 Binding
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 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 10.1021/jm960669+
CHEMBL324547 4035 24 None - 4 Rat 6.3 pIC50 = 6.3 Binding
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 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 10.1021/jm960669+
DB12355 4035 24 None - 4 Rat 6.3 pIC50 = 6.3 Binding
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 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 10.1021/jm960669+
10649606 49334 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 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 49334 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 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
CHEMBL3142692 209376 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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)Nc1cccc(Cl)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
10070677 161163 13 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
CHEMBL41361 161163 13 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00121a004
10649606 49334 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 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 49334 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 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
54580263 61513 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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-c2cccc(F)c2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773878 61513 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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-c2cccc(F)c2)cc1 10.1016/j.bmcl.2011.03.069
15104611 108757 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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]c2ccccc12)NC(=O)c1cc(O)c2ccccc2n1 10.1021/jm00116a002
CHEMBL321811 108757 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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]c2ccccc12)NC(=O)c1cc(O)c2ccccc2n1 10.1021/jm00116a002
15104601 169850 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 486 13 3 2 6.2 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00116a002
CHEMBL444847 169850 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 486 13 3 2 6.2 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00116a002
CHEMBL99786 214142 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00173a006
73355867 204527 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 680 12 5 6 6.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1ccccc1O)c1ccccc1 10.1021/jm00092a007
CHEMBL86879 204527 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 680 12 5 6 6.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1ccccc1O)c1ccccc1 10.1021/jm00092a007
10501974 96514 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 415 5 3 6 3.9 COc1cccc(-n2c(NNC(=O)Nc3cccc(C)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL266376 96514 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 415 5 3 6 3.9 COc1cccc(-n2c(NNC(=O)Nc3cccc(C)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL436451 211923 0 None - 0 Mouse 4.3 pIC50 = 4.3 Binding
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](N)Cc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
44368522 118963 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 574 11 5 5 4.4 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)NC[C@H](NC(=O)/C=C/C(=O)O)c1ccccc1 10.1021/jm00057a005
CHEMBL345303 118963 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 574 11 5 5 4.4 C[C@H]1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)NC[C@H](NC(=O)/C=C/C(=O)O)c1ccccc1 10.1021/jm00057a005
CHEMBL382349 210545 0 None -3235 4 Human 5.3 pIC50 = 5.3 Binding
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](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
44336539 5060 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 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 5060 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 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
44591825 183514 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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 411 8 4 4 3.4 CSCCC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL482571 183514 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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 411 8 4 4 3.4 CSCCC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
14991576 101731 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 21 9 9 3.4 COc1ccc2[nH]c(C(=O)NCCCC[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)cc2c1 10.1021/jm00089a010
CHEMBL302911 101731 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 21 9 9 3.4 COc1ccc2[nH]c(C(=O)NCCCC[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)cc2c1 10.1021/jm00089a010
51353551 17935 10 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat 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 17935 10 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cellsDisplacement of [125I]CCK8 from rat 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
10414170 170041 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1016/S0960-894X(00)80683-6
CHEMBL445095 170041 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1016/S0960-894X(00)80683-6
44300989 100498 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 625 7 4 6 4.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(C)(=O)=O)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
CHEMBL294252 100498 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 625 7 4 6 4.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(C)(=O)=O)c1)C[C@@H]2C1CCCCC1 10.1016/0960-894X(95)00327-P
44382624 119840 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
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 619 12 4 4 4.0 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)/C=C/c1ccccc1)C(=O)N1CC(=O)N[C@@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
CHEMBL353148 119840 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
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 619 12 4 4 4.0 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)/C=C/c1ccccc1)C(=O)N1CC(=O)N[C@@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
10414170 170041 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00121a004
CHEMBL445095 170041 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 515 5 2 4 4.3 O=C(Nc1ccc(Cl)cc1)NC1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00121a004
15104602 9346 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 486 13 3 2 6.2 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00116a002
CHEMBL111808 9346 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 486 13 3 2 6.2 CCCCCN(CCCCC)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00116a002
44366583 120769 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.1-6.4 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.1-6.4 uM
ChEMBL 420 4 1 5 4.9 CC(C)(C)OC(=O)n1cc(CC2CN(Cc3ccccc3)CCC2O)c2ccccc21 10.1016/0960-894X(94)80030-8
CHEMBL358016 120769 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.1-6.4 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.1-6.4 uM
ChEMBL 420 4 1 5 4.9 CC(C)(C)OC(=O)n1cc(CC2CN(Cc3ccccc3)CCC2O)c2ccccc21 10.1016/0960-894X(94)80030-8
73354294 106472 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 636 11 6 5 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CP(=O)(O)O)c1ccccc1 10.1021/jm00092a007
CHEMBL315055 106472 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 636 11 6 5 4.2 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CP(=O)(O)O)c1ccccc1 10.1021/jm00092a007
15104610 9579 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
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 513 13 3 3 6.6 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2cc(O)ccc2c1 10.1021/jm00116a002
CHEMBL113041 9579 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
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 513 13 3 3 6.6 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc2cc(O)ccc2c1 10.1021/jm00116a002
44280388 116356 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 759 15 4 8 5.0 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL33819 116356 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 759 15 4 8 5.0 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
44334330 4945 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
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
CHEMBL105153 4945 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
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
44381319 120200 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 495 11 4 5 3.6 N#C[C@H](N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
CHEMBL354817 120200 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 495 11 4 5 3.6 N#C[C@H](N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
10626596 112271 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 555 7 1 4 5.6 O=C1C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc2N1CC(=O)N(c1ccccc1)C1CC1 10.1021/jm970265x
CHEMBL330566 112271 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 555 7 1 4 5.6 O=C1C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc2N1CC(=O)N(c1ccccc1)C1CC1 10.1021/jm970265x
44327457 106841 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 11 3 4 5.6 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCC(=O)O)CCc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL317577 106841 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 11 3 4 5.6 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCC(=O)O)CCc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL262767 208793 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 Cc1ccc(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/jm00113a023
CHEMBL262767 208793 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 Cc1ccc(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
CHEMBL262767 208793 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 Cc1ccc(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/jm00173a006
44333311 4179 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 476 6 2 5 3.5 CCCc1cccc(NC(=O)NC2N=C(N3CCN(C)CC3)c3ccccc3N(CCC)C2=O)c1 10.1016/0960-894X(95)00530-0
CHEMBL100502 4179 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 476 6 2 5 3.5 CCCc1cccc(NC(=O)NC2N=C(N3CCN(C)CC3)c3ccccc3N(CCC)C2=O)c1 10.1016/0960-894X(95)00530-0
44303481 100219 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 524 9 3 6 4.3 CC(=O)Nc1nc(CC(C)(NC(=O)OC2C3CC4CC(C3)CC2C4)C(=O)NCCc2ccccc2)cs1 10.1016/S0960-894X(97)00356-9
CHEMBL292422 100219 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 524 9 3 6 4.3 CC(=O)Nc1nc(CC(C)(NC(=O)OC2C3CC4CC(C3)CC2C4)C(=O)NCCc2ccccc2)cs1 10.1016/S0960-894X(97)00356-9
10789887 205684 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 454 6 3 7 4.2 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C#N)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL9405 205684 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 454 6 3 7 4.2 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C#N)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
45482492 196297 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 495 7 4 3 4.9 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cccc(C(F)(F)F)c2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL573560 196297 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 495 7 4 3 4.9 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2cccc(C(F)(F)F)c2[nH]1 10.1016/j.bmc.2009.05.067
10370499 36706 0 None - 1 Rat 6.3 pIC50 = 6.3 Binding
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
CHEMBL145133 36706 0 None - 1 Rat 6.3 pIC50 = 6.3 Binding
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
10370499 36706 0 None - 1 Rat 6.3 pIC50 = 6.3 Binding
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 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1016/s0960-894x(98)00677-5
CHEMBL145133 36706 0 None - 1 Rat 6.3 pIC50 = 6.3 Binding
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 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1016/s0960-894x(98)00677-5
10370499 85549 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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
CHEMBL2304064 85549 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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
10769315 16647 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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
CHEMBL124798 16647 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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
11621814 140695 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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
CHEMBL382953 140695 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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
10507109 108727 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
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 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
CHEMBL321761 108727 0 None -1 2 Human 7.3 pIC50 = 7.3 Binding
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 561 7 2 4 5.3 CC(C)N(C(=O)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
44370473 50574 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
CHEMBL157722 50574 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
44280213 101134 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 685 12 5 9 3.7 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL29888 101134 0 None - 1 Mouse 5.3 pIC50 = 5.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 685 12 5 9 3.7 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
70697518 77438 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
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 367 3 2 3 4.4 O=C1Nc2ccccc2C(c2ccccc2)=NC1C[C@@H]1CNc2ccccc21 10.1021/jm00390a019
CHEMBL2092748 77438 0 None - 0 Guinea pig 4.3 pIC50 = 4.3 Binding
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 367 3 2 3 4.4 O=C1Nc2ccccc2C(c2ccccc2)=NC1C[C@@H]1CNc2ccccc21 10.1021/jm00390a019
10649606 49334 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]CCK from CCK1R (unknown origin) 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 49334 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cellsDisplacement of [125I]CCK from CCK1R (unknown origin) 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
44283087 120298 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 8 2 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)OCCc1ccccc1 10.1021/jm00086a017
CHEMBL35580 120298 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 8 2 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)OCCc1ccccc1 10.1021/jm00086a017
45482494 196298 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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)c1cc2cccc(F)c2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL573561 196298 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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)c1cc2cccc(F)c2[nH]1 10.1016/j.bmc.2009.05.067
54582288 61526 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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-c2ccccc2C)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773893 61526 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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-c2ccccc2C)cc1 10.1016/j.bmcl.2011.03.069
90663977 106304 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 823 21 8 8 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144539 106304 0 None - 0 Guinea pig 7.3 pIC50 = 7.3 Binding
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 823 21 8 8 3.3 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44386117 130816 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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(=C/c1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80273-5
CHEMBL368803 130816 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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(=C/c1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80273-5
44458120 98491 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 377 5 3 3 2.0 O=C(N[C@@H]1C(=O)N(Cc2ccccc2)C[C@@H]1C(=O)O)c1cc2ccccc2[nH]1 10.1016/S0960-894X(00)80224-3
CHEMBL279730 98491 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 377 5 3 3 2.0 O=C(N[C@@H]1C(=O)N(Cc2ccccc2)C[C@@H]1C(=O)O)c1cc2ccccc2[nH]1 10.1016/S0960-894X(00)80224-3
44366587 43430 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.7-7.1 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.7-7.1 uM
ChEMBL 554 10 0 8 7.2 CCOP(=O)(OCC)OC1=CCN(Cc2ccccc2)CC1Cc1cn(C(=O)OC(C)(C)C)c2ccccc12 10.1016/0960-894X(94)80030-8
CHEMBL151022 43430 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.7-7.1 uMBinding affinity towards CCK-A receptor in rat pancreas using [125I]Bolton-Hunter CCK-8 as radioligand; Value ranges from 4.7-7.1 uM
ChEMBL 554 10 0 8 7.2 CCOP(=O)(OCC)OC1=CCN(Cc2ccccc2)CC1Cc1cn(C(=O)OC(C)(C)C)c2ccccc12 10.1016/0960-894X(94)80030-8
CHEMBL441840 212139 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
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)OC(C)(C)C)C(=O)N1CC(=O)N[C@@H](Cc2ccccc2)C1 10.1016/S0960-894X(01)80253-5
14208246 202966 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00120a002
CHEMBL73892 202966 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00120a002
15637194 25719 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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 308 2 2 3 1.5 CN1C(=O)C(NC(N)=O)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135405 25719 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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 308 2 2 3 1.5 CN1C(=O)C(NC(N)=O)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44592484 187519 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 337 5 4 3 2.2 O=C(O)CNC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL498273 187519 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 337 5 4 3 2.2 O=C(O)CNC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
10553207 206521 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 492 6 2 6 4.7 CC(C)Oc1cccc(-n2c(NNC(=O)c3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL9888 206521 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 492 6 2 6 4.7 CC(C)Oc1cccc(-n2c(NNC(=O)c3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
23757281 9743 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 539 8 2 5 5.5 CCN(CC)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
CHEMBL114072 9743 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 539 8 2 5 5.5 CCN(CC)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
10389643 118503 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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 5 3 4 3.8 O=C(O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL342614 118503 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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 5 3 4 3.8 O=C(O)CN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
9984739 114303 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 538 5 3 3 6.2 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
CHEMBL334100 114303 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 538 5 3 3 6.2 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
44280180 102147 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 655 11 5 8 3.6 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
CHEMBL30430 102147 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 655 11 5 8 3.6 CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00248-X
44329304 107619 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 7 3 3 5.5 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL319569 107619 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 7 3 3 5.5 Cc1cccc(NC(=O)N[C@@H]2C[C@H](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
44382749 59382 0 None - 0 Mouse 4.3 pIC50 = 4.3 Binding
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 532 11 4 4 3.0 CC(C)C[C@H](NC(=O)CCc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
CHEMBL172354 59382 0 None - 0 Mouse 4.3 pIC50 = 4.3 Binding
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 532 11 4 4 3.0 CC(C)C[C@H](NC(=O)CCc1c[nH]c2ccccc12)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
10673307 110134 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 511 7 3 5 4.2 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(NC=O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
CHEMBL325746 110134 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 511 7 3 5 4.2 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(NC=O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
14208246 202966 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00047a021
CHEMBL73892 202966 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00047a021
44327455 106848 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 12 3 4 6.0 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCCC(=O)O)CCc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL317626 106848 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 12 3 4 6.0 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCCC(=O)O)CCc1ccccc1 10.1016/S0960-894X(01)80769-1
15104603 9391 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
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 436 13 3 2 5.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc[nH]1 10.1021/jm00116a002
CHEMBL112054 9391 0 None - 0 Guinea pig 5.3 pIC50 = 5.3 Binding
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 436 13 3 2 5.0 CCCCCN(CCCCC)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccc[nH]1 10.1021/jm00116a002
10412837 27401 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 479 5 3 5 4.0 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(Cc3n[nH]c(C)n3)C2=O)c1 10.1021/jm00078a018
CHEMBL136975 27401 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 479 5 3 5 4.0 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(Cc3n[nH]c(C)n3)C2=O)c1 10.1021/jm00078a018
CHEMBL345598 209953 0 None - 0 Guinea pig 6.3 pIC50 = 6.3 Binding
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 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)N(C)C(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
44382562 58776 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 662 13 5 5 5.8 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccc(O)cc1)NCCc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL169710 58776 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 662 13 5 5 5.8 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccc(O)cc1)NCCc1ccccc1 10.1016/S0960-894X(00)80687-3
10408567 118761 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 398 3 2 3 4.0 Cc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00078a018
CHEMBL343767 118761 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 398 3 2 3 4.0 Cc1ccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00078a018
90663991 106324 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 868 22 8 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144560 106324 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 868 22 8 10 3.2 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
14991567 198108 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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)c1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL59404 198108 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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)c1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
44280117 101568 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 672 12 3 6 5.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL30195 101568 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 672 12 3 6 5.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
14423345 202716 1 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 283 1 1 3 1.9 CN1C(=O)C(N)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL72151 202716 1 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 283 1 1 3 1.9 CN1C(=O)C(N)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
10768084 9909 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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+
CHEMBL114991 9909 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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+
44408483 168352 0 None -165 4 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.7 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](Cc1cn(C(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL438739 168352 0 None -165 4 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.7 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](Cc1cn(C(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL262172 208773 0 None -26302 4 Human 5.2 pIC50 = 5.2 Binding
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](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 10.1021/jm050921q
44376112 119675 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 452 4 3 6 2.8 CN1C(=O)[C@@H](NC(=O)Nc2ccc(-c3nn[nH]n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
CHEMBL351854 119675 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 452 4 3 6 2.8 CN1C(=O)[C@@H](NC(=O)Nc2ccc(-c3nn[nH]n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
14208221 79123 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 530 6 2 5 4.2 CN1C(=O)C(NC(=O)C(Cc2ccccc2)NC(=O)OC(C)(C)C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL2114102 79123 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 530 6 2 5 4.2 CN1C(=O)C(NC(=O)C(Cc2ccccc2)NC(=O)OC(C)(C)C)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
44354128 20079 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 4.7 CC(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)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
CHEMBL130578 20079 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 4.7 CC(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)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
14802521 58760 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 628 13 5 5 4.7 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL169616 58760 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 628 13 5 5 4.7 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
10392523 206196 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL96970 206196 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
15104609 110037 0 None - 0 Guinea pig 5.2 pIC50 = 5.2 Binding
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)c1nccc2ccccc12 10.1021/jm00116a002
CHEMBL325160 110037 0 None - 0 Guinea pig 5.2 pIC50 = 5.2 Binding
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)c1nccc2ccccc12 10.1021/jm00116a002
19766222 116089 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 383 5 1 4 3.9 CC(C)COC(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C 10.1021/jm00163a069
CHEMBL336690 116089 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 383 5 1 4 3.9 CC(C)COC(=O)NCC1CN=C(c2ccccc2F)c2ccccc2N1C 10.1021/jm00163a069
14208308 67386 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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)c2ccccc2I)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907845 67386 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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)c2ccccc2I)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
15167811 167317 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 417 3 0 3 4.3 CN1C(=O)C(N(C)C(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL431185 167317 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 417 3 0 3 4.3 CN1C(=O)C(N(C)C(=O)c2ccccc2Cl)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
11607292 165432 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
CHEMBL425392 165432 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
44303526 201445 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 708 14 4 6 6.3 O=C(CCC(=O)OCc1ccccc1)N[C@@H](CNC(=O)C(Cc1c[nH]c2ccc(F)cc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL64155 201445 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 708 14 4 6 6.3 O=C(CCC(=O)OCc1ccccc1)N[C@@H](CNC(=O)C(Cc1c[nH]c2ccc(F)cc12)NC(=O)OC1C2CC3CC(C2)CC1C3)c1ccccc1 10.1016/S0960-894X(97)00356-9
54582313 61576 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 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 61576 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 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
10744359 10047 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 513 6 2 6 4.5 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc([N+](=O)[O-])c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
CHEMBL115833 10047 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 513 6 2 6 4.5 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc([N+](=O)[O-])c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
15689724 106103 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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)Nc1cccc(C(F)(F)F)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142696 106103 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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)Nc1cccc(C(F)(F)F)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44370497 164630 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 453 8 3 3 4.6 O=C(O)CC[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N(C1CCCCC1)C1CCCCC1 10.1021/jm00164a020
CHEMBL422873 164630 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 453 8 3 3 4.6 O=C(O)CC[C@H](NC(=O)c1cc2ccccc2[nH]1)C(=O)N(C1CCCCC1)C1CCCCC1 10.1021/jm00164a020
90663256 106135 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory activity against cholecystokinin type A receptor from rat pancreas binding assayInhibitory activity against cholecystokinin type A receptor from rat pancreas binding assay
ChEMBL 854 17 7 8 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CSC(C)(C)[C@H]1C(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00100a033
CHEMBL3143146 106135 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory activity against cholecystokinin type A receptor from rat pancreas binding assayInhibitory activity against cholecystokinin type A receptor from rat pancreas binding assay
ChEMBL 854 17 7 8 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CSC(C)(C)[C@H]1C(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00100a033
155521287 170001 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]CCK-8s from human CCKA incubated for 60 mins by scintillation counting methodDisplacement of [125I]CCK-8s from human CCKA incubated for 60 mins by scintillation counting method
ChEMBL 478 7 0 6 4.8 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(F)c(Cl)c3)C(=O)C21 10.1021/acs.jmedchem.9b02080
CHEMBL4450506 170001 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]CCK-8s from human CCKA incubated for 60 mins by scintillation counting methodDisplacement of [125I]CCK-8s from human CCKA incubated for 60 mins by scintillation counting method
ChEMBL 478 7 0 6 4.8 CCOP(=O)(OCC)C1(c2ccccc2)N=CC2C(=O)N(c3ccc(F)c(Cl)c3)C(=O)C21 10.1021/acs.jmedchem.9b02080
44283081 99396 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 99396 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 99396 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
14208225 67397 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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
CHEMBL1907855 67397 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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
14208204 202750 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00120a002
CHEMBL72300 202750 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00120a002
14208204 202750 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00047a021
CHEMBL72300 202750 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 407 3 2 3 4.0 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccc(Cl)cc1 10.1021/jm00047a021
44376191 164762 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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 452 4 3 6 2.8 CN1C(=O)[C@H](NC(=O)Nc2ccc(-c3nn[nH]n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
CHEMBL423472 164762 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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 452 4 3 6 2.8 CN1C(=O)[C@H](NC(=O)Nc2ccc(-c3nn[nH]n3)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00032a003
10010890 108237 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
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 874 22 8 8 4.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
CHEMBL320858 108237 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
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 874 22 8 8 4.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00028a015
10409534 28013 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL137398 28013 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
10649606 49334 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 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 49334 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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 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
5311205 12968 1 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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)N[C@H]2N=C(N3CC4CCC(CC4)C3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL1190319 12968 1 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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)N[C@H]2N=C(N3CC4CCC(CC4)C3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL540596 12968 1 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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)N[C@H]2N=C(N3CC4CCC(CC4)C3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
54583260 61529 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1773896 61529 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2011.03.069
11039097 79121 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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
CHEMBL2114084 79121 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
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
24785177 189179 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human CCK1 receptorInhibition of 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 189179 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human CCK1 receptorInhibition of 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
CHEMBL3142697 209377 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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)Nc1ccc(Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44373701 52196 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 541 8 4 4 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N/C(=C\c1ccccc1)C(=O)O 10.1016/S0960-894X(01)81250-6
CHEMBL159138 52196 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 541 8 4 4 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N/C(=C\c1ccccc1)C(=O)O 10.1016/S0960-894X(01)81250-6
9978327 78391 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 400 3 3 4 3.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2112753 78391 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 400 3 3 4 3.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
11765552 113118 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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)CCC(=O)O)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm00017a022
CHEMBL332263 113118 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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)CCC(=O)O)NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm00017a022
44300888 100311 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 580 6 4 6 4.5 Cc1ccc([C@H]2C[C@@H](NC(=O)Nc3cccc(-c4nn[nH]n4)c3)C(=O)N(CC(=O)NC(C)(C)C)c3cc(C)ccc32)cc1 10.1016/0960-894X(95)00327-P
CHEMBL293107 100311 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 580 6 4 6 4.5 Cc1ccc([C@H]2C[C@@H](NC(=O)Nc3cccc(-c4nn[nH]n4)c3)C(=O)N(CC(=O)NC(C)(C)C)c3cc(C)ccc32)cc1 10.1016/0960-894X(95)00327-P
44348808 17738 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 451 7 3 4 3.9 O=C(O)CCC(NC(=O)c1ccc2ccccc2c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
CHEMBL125925 17738 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 451 7 3 4 3.9 O=C(O)CCC(NC(=O)c1ccc2ccccc2c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
71456207 78199 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 655 12 5 7 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1c[nH]nn1)c1ccccc1 10.1021/jm00092a007
CHEMBL2112331 78199 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 655 12 5 7 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1c[nH]nn1)c1ccccc1 10.1021/jm00092a007
9853654 22573 37 None - 2 Rat 6.2 pIC50 = 6.2 Binding
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 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/jm00092a007
CHEMBL1328 22573 37 None - 2 Rat 6.2 pIC50 = 6.2 Binding
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 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/jm00092a007
9853654 22573 37 None - 2 Rat 6.2 pIC50 = 6.2 Binding
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 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/jm00105a062
CHEMBL1328 22573 37 None - 2 Rat 6.2 pIC50 = 6.2 Binding
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 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/jm00105a062
15104627 109976 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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 2 3 4.7 CN(Cc1ccccc1)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL324760 109976 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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 2 3 4.7 CN(Cc1ccccc1)C(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
9853654 22573 37 None - 2 Rat 6.2 pIC50 = 6.2 Binding
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 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/jm00057a005
CHEMBL1328 22573 37 None - 2 Rat 6.2 pIC50 = 6.2 Binding
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 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/jm00057a005
44360121 116232 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 3.3 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(O)c1ccccc1 10.1021/jm00163a069
CHEMBL337530 116232 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 3.3 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)C(O)c1ccccc1 10.1021/jm00163a069
11742520 29398 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 COc1ccccc1NC(=O)NC1N=C(c2ccccc2)c2ccccc2N(C)C1=O 10.1021/jm00078a018
CHEMBL138592 29398 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 COc1ccccc1NC(=O)NC1N=C(c2ccccc2)c2ccccc2N(C)C1=O 10.1021/jm00078a018
10431936 92793 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
CHEMBL2448131 92793 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
14208198 103886 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
CHEMBL310246 103886 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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
44349410 16583 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 394 7 3 3 3.5 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCCCCCC1 10.1021/jm00079a003
CHEMBL124459 16583 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 394 7 3 3 3.5 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCCCCCC1 10.1021/jm00079a003
15556550 67366 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
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 326 3 1 2 4.5 CC(C)C[C@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=O 10.1021/jm00390a019
CHEMBL1907736 67366 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
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 326 3 1 2 4.5 CC(C)C[C@H]1N=C(c2ccccc2)c2cc(Cl)ccc2NC1=O 10.1021/jm00390a019
11571172 140041 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
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 140041 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
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
19018661 28256 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 5 3 4 3.3 CN1C(=O)C(NC(=O)Nc2cccc(CC(=O)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137567 28256 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 5 3 4 3.3 CN1C(=O)C(NC(=O)Nc2cccc(CC(=O)O)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10000984 116130 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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)c3cnccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL336972 116130 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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)c3cnccc3N(C)C2=O)c1 10.1021/jm00078a018
46235271 73286 2 None 2 2 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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 73286 2 None 2 2 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-BDZ-1] from human CCK1R W6.48A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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
10392523 206196 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL96970 206196 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
44280996 99270 0 None - 1 Mouse 5.2 pIC50 = 5.2 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 745 14 4 8 5.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL284976 99270 0 None - 1 Mouse 5.2 pIC50 = 5.2 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 745 14 4 8 5.4 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
15614737 75567 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
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)=NC1Cc1ccc2ccccc2c1 10.1021/jm00390a019
CHEMBL20514 75567 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
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)=NC1Cc1ccc2ccccc2c1 10.1021/jm00390a019
44303299 199556 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 598 11 4 6 5.5 CC(Cc1ccc(Oc2ccccc2)cc1)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)[C@H](O)c1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL60386 199556 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 598 11 4 6 5.5 CC(Cc1ccc(Oc2ccccc2)cc1)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)[C@H](O)c1ccccc1 10.1016/S0960-894X(97)00356-9
52949124 861 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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 861 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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 861 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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 861 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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
14208298 202917 1 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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)c2ccccc2Br)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL73511 202917 1 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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)c2ccccc2Br)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
44210425 164731 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 439 5 2 5 3.5 COc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)OC(C)(C)C)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL423278 164731 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 439 5 2 5 3.5 COc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)OC(C)(C)C)C2=O)c1 10.1016/S0960-894X(00)80683-6
9960703 167464 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 621 6 3 7 4.0 O=C(Nc1cccc(-c2nn[nH]n2)c1)NC1N=C(c2ccccc2F)c2ccccc2N(CC(=O)N2CC3CCC(CC3)C2)C1=O 10.1016/s0960-894x(98)00237-6
CHEMBL432266 167464 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 621 6 3 7 4.0 O=C(Nc1cccc(-c2nn[nH]n2)c1)NC1N=C(c2ccccc2F)c2ccccc2N(CC(=O)N2CC3CCC(CC3)C2)C1=O 10.1016/s0960-894x(98)00237-6
44287087 99985 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 796 19 7 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL290719 99985 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 796 19 7 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
44458113 167601 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 392 4 2 3 2.8 O=C(N[C@@H]1C(=O)N(c2ccccc2F)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
CHEMBL433222 167601 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 392 4 2 3 2.8 O=C(N[C@@H]1C(=O)N(c2ccccc2F)C[C@@H]1C(=O)O)c1ccc2ccccc2c1 10.1016/S0960-894X(00)80224-3
9872735 186434 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 567 5 2 4 5.1 Cc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3ccccc3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
CHEMBL49085 186434 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 567 5 2 4 5.1 Cc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3ccccc3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
44300852 101488 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 566 6 4 6 4.1 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL301418 101488 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 566 6 4 6 4.1 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(-c3nn[nH]n3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
71458004 78203 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 670 12 5 8 4.7 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCn1nn[nH]c1=S)c1ccccc1 10.1021/jm00092a007
CHEMBL2112335 78203 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 670 12 5 8 4.7 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCn1nn[nH]c1=S)c1ccccc1 10.1021/jm00092a007
10323690 100019 0 None - 2 Rat 6.2 pIC50 = 6.2 Binding
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 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
CHEMBL2114401 100019 0 None - 2 Rat 6.2 pIC50 = 6.2 Binding
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 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
CHEMBL291033 100019 0 None - 2 Rat 6.2 pIC50 = 6.2 Binding
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 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
14208299 67385 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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)c2ccccc2Br)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL1907844 67385 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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)c2ccccc2Br)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
10416987 12088 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 539 5 2 4 3.2 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CC[N+](C)(C)CC3)C2=O)c1 10.1021/jm00078a018
CHEMBL1184312 12088 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 539 5 2 4 3.2 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CC[N+](C)(C)CC3)C2=O)c1 10.1021/jm00078a018
CHEMBL343949 12088 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 539 5 2 4 3.2 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CC[N+](C)(C)CC3)C2=O)c1 10.1021/jm00078a018
11607291 170441 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
CHEMBL445662 170441 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
44368594 120525 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 447 8 3 3 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1)C(=O)NCCc1ccccc1 10.1021/jm00057a005
CHEMBL356810 120525 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 447 8 3 3 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1CCCCC1)C(=O)NCCc1ccccc1 10.1021/jm00057a005
44349073 16365 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 395 7 3 4 2.5 CC1(C)CCN(NC(=O)C(CCC(=O)O)NC(=O)c2cccc(Cl)c2)CC1 10.1021/jm00079a003
CHEMBL123785 16365 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 395 7 3 4 2.5 CC1(C)CCN(NC(=O)C(CCC(=O)O)NC(=O)c2cccc(Cl)c2)CC1 10.1021/jm00079a003
11124446 78012 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
CHEMBL2111552 78012 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
14519981 9950 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2n1 10.1021/jm00124a003
CHEMBL115269 9950 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2n1 10.1021/jm00124a003
14519981 9950 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2n1 10.1021/jm00116a002
CHEMBL115269 9950 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 441 14 2 4 4.4 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc2ccccc2n1 10.1021/jm00116a002
44370694 47731 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
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 47731 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 488 15 2 4 4.8 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)N1CCCC1)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
10348659 1766 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 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 10.1021/jm950626d
866 1766 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 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 10.1021/jm950626d
CHEMBL1184355 1766 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 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 10.1021/jm950626d
44306887 101578 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
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
CHEMBL302027 101578 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
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
CHEMBL355778 209983 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
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)OC(C)(C)C)C(=O)N1C[C@H](CCc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
19910130 119273 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 439 14 3 3 4.9 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL348168 119273 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 439 14 3 3 4.9 CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
44578398 181192 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human CCK1 receptorInhibition of 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 181192 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human CCK1 receptorInhibition of 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
CHEMBL172177 207098 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
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)OC(C)(C)C)C(=O)N1C[C@@H](Cc2ccccc2)NC(=O)[C@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
44349064 16328 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 435 7 3 4 3.4 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
CHEMBL123684 16328 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 435 7 3 4 3.4 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NN1CCC2(CCCCC2)CC1 10.1021/jm00079a003
15167820 67357 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
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 393 3 0 3 4.6 CN1C(=O)[C@@H](Cc2cn(C)c3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
CHEMBL1907724 67357 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
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 393 3 0 3 4.6 CN1C(=O)[C@@H](Cc2cn(C)c3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1021/jm00390a019
44327699 205739 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 641 15 2 5 7.2 COC(=O)CCCCCCN(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
CHEMBL94352 205739 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 641 15 2 5 7.2 COC(=O)CCCCCCN(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
52949124 861 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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 861 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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 861 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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 861 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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
44283086 118816 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 482 8 2 2 7.2 CC(/C=C/CCc1ccccc1)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL34422 118816 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 482 8 2 2 7.2 CC(/C=C/CCc1ccccc1)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
10008405 118272 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
CHEMBL342110 118272 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
CHEMBL169174 207083 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
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
44333997 108259 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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 588 10 3 5 5.3 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
CHEMBL320886 108259 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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 588 10 3 5 5.3 CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC(C(=O)c2ccccc2)CC1 10.1016/0960-894X(95)00537-3
10551234 96480 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 443 6 3 6 4.6 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1021/jm970373j
CHEMBL266120 96480 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 443 6 3 6 4.6 Cc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1021/jm970373j
6956374 2363 4 None - 1 Rat 5.2 pIC50 = 5.2 Binding
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
902 2363 4 None - 1 Rat 5.2 pIC50 = 5.2 Binding
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
CHEMBL117281 2363 4 None - 1 Rat 5.2 pIC50 = 5.2 Binding
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
6956374 2363 4 None - 1 Rat 5.2 pIC50 = 5.2 Binding
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
902 2363 4 None - 1 Rat 5.2 pIC50 = 5.2 Binding
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
CHEMBL117281 2363 4 None - 1 Rat 5.2 pIC50 = 5.2 Binding
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
2118 201783 35 None - 2 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 308 1 0 4 3.6 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 10.1021/jm00396a028
CHEMBL661 201783 35 None - 2 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 308 1 0 4 3.6 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 10.1021/jm00396a028
CHEMBL2372078 208429 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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](CCCNCc2ccccc2)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
CHEMBL383458 210556 0 None -10 4 Human 5.2 pIC50 = 5.2 Binding
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](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 10.1021/jm050921q
10409900 103368 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
CHEMBL30919 103368 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
44318205 204070 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 459 3 3 4 3.9 CN1C(=O)[C@H](NC(=O)Nc2ccc3c(c2)CCC3)N=C([C@H]2CC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
CHEMBL83130 204070 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 459 3 3 4 3.9 CN1C(=O)[C@H](NC(=O)Nc2ccc3c(c2)CCC3)N=C([C@H]2CC(C)(C)CCN2)c2ccccc21 10.1021/jm9608523
44303515 101610 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 571 9 2 5 5.3 CN(C)C(=O)c1oc2ccccc2c1CC(C)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL302194 101610 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 571 9 2 5 5.3 CN(C)C(=O)c1oc2ccccc2c1CC(C)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
10363545 204017 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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(c3ccccn3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL82685 204017 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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(c3ccccn3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
10363545 204017 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
CHEMBL82685 204017 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 399 3 2 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
90663984 106318 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 21 8 8 3.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144553 106318 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 21 8 8 3.4 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(F)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
118719193 114946 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 520 7 2 5 3.6 CC(C)(C)OC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm991078x
CHEMBL3350871 114946 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 520 7 2 5 3.6 CC(C)(C)OC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@H]12 10.1021/jm991078x
CHEMBL3142685 209372 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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 Cc1ccccc1NC(=O)NCCC[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
10413618 201094 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
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 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/s0960-894x(00)00198-0
CHEMBL62205 201094 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
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 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/s0960-894x(00)00198-0
9983419 108886 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 499 8 3 3 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
CHEMBL321946 108886 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 499 8 3 3 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00105a062
10413618 201094 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
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 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL62205 201094 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
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 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
44280200 100344 0 None - 1 Mouse 6.2 pIC50 = 6.2 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 785 18 4 7 6.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL29331 100344 0 None - 1 Mouse 6.2 pIC50 = 6.2 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 785 18 4 7 6.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
10413618 201094 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
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 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1021/jm970065l
CHEMBL62205 201094 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
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 499 8 3 3 5.4 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1021/jm970065l
15719750 78059 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 446 9 3 3 4.0 O=C(O)CC[C@H](NC(=O)c1cccc(Cl)c1)C(=O)NCCC12CC3CC(CC(C3)C1)C2 10.1021/jm00079a003
CHEMBL2111825 78059 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 446 9 3 3 4.0 O=C(O)CC[C@H](NC(=O)c1cccc(Cl)c1)C(=O)NCCC12CC3CC(CC(C3)C1)C2 10.1021/jm00079a003
13605417 205824 3 None - 1 Guinea pig 7.2 pIC50 = 7.2 Binding
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 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 205824 3 None - 1 Guinea pig 7.2 pIC50 = 7.2 Binding
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 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
54581301 61575 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 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 61575 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 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
15167812 101713 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 437 3 1 3 3.6 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)[N+]([O-])=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL302825 101713 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 437 3 1 3 3.6 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)[N+]([O-])=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
13605417 205824 3 None - 1 Guinea pig 7.2 pIC50 = 7.2 Binding
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 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00116a002
CHEMBL9485 205824 3 None - 1 Guinea pig 7.2 pIC50 = 7.2 Binding
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 458 14 2 3 5.2 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00116a002
44368382 45069 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 45069 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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
10480792 45528 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 CC1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL153095 45528 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 CC1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3350686 45528 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 CC1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
136242438 78201 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 671 12 6 7 4.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1n[nH]c(=O)[nH]1)c1ccccc1 10.1021/jm00092a007
CHEMBL2112333 78201 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 671 12 6 7 4.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1n[nH]c(=O)[nH]1)c1ccccc1 10.1021/jm00092a007
10699165 110952 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 625 7 1 4 6.9 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(C(F)(F)F)cc1 10.1021/jm970265x
CHEMBL327552 110952 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 625 7 1 4 6.9 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccc(C(F)(F)F)cc1 10.1021/jm970265x
44211352 13857 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 6 1 4 3.8 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL1196916 13857 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 6 1 4 3.8 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
CHEMBL558614 13857 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 6 1 4 3.8 CN1CCN(C(=O)CCC(NC(=O)c2cc(Cl)cc(Cl)c2)C(=O)N2CCC3(CCCC3)CC2)CC1 10.1016/S0960-894X(00)80681-2
11744065 78388 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 3.6 CC(=O)Oc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL2112750 78388 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 3.6 CC(=O)Oc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
15167809 67358 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
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 440 5 2 3 3.6 NC(=O)CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
CHEMBL1907725 67358 0 None - 0 Guinea pig 4.2 pIC50 = 4.2 Binding
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 440 5 2 3 3.6 NC(=O)CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00390a019
135703408 142292 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 511 4 2 6 6.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(O)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
CHEMBL389311 142292 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 511 4 2 6 6.0 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccc(O)cc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
44349254 16639 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 354 10 3 3 2.6 CCCCCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
CHEMBL124751 16639 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 354 10 3 3 2.6 CCCCCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
23129945 9504 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 604 16 2 4 7.8 CCCCCN(CCCCC)C(=O)C(Cc1c[nH]c2ccc(OCc3ccccc3)cc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
CHEMBL112612 9504 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 604 16 2 4 7.8 CCCCCN(CCCCC)C(=O)C(Cc1c[nH]c2ccc(OCc3ccccc3)cc12)NC(=O)c1cnc2ccccc2c1 10.1021/jm00116a002
14888721 76869 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 1055 30 11 14 -0.2 CSCC[C@H](NC(=O)[C@H](Cc1ccc(Cc2nnn[nH]2)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
CHEMBL2079551 76869 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 1055 30 11 14 -0.2 CSCC[C@H](NC(=O)[C@H](Cc1ccc(Cc2nnn[nH]2)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
CHEMBL350222 209966 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 Cc1ccccc1NC(=O)N(C)CCCC[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/jm00031a013
22354599 193127 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 517 6 2 5 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccncc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL538912 193127 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 517 6 2 5 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccncc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 10.1016/0960-894X(95)00557-A
15104600 96626 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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
CHEMBL267339 96626 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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
10484212 99404 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-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 99404 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-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
45482488 196618 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 Cc1cccc2cc(C(=O)Nc3ccccc3C(=O)NC(Cc3ccccc3)C(=O)O)[nH]c12 10.1016/j.bmc.2009.05.067
CHEMBL576021 196618 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 Cc1cccc2cc(C(=O)Nc3ccccc3C(=O)NC(Cc3ccccc3)C(=O)O)[nH]c12 10.1016/j.bmc.2009.05.067
44327458 206111 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 11 3 4 5.6 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCC(=O)O)CCc1ccccc1 10.1016/S0960-894X(01)80769-1
CHEMBL96469 206111 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 11 3 4 5.6 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCC(=O)O)CCc1ccccc1 10.1016/S0960-894X(01)80769-1
44379965 57518 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 496 6 2 5 5.5 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc(C(F)(F)F)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
CHEMBL167169 57518 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 496 6 2 5 5.5 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc(C(F)(F)F)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
44349335 116797 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 401 7 3 4 2.6 Cc1cccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
CHEMBL339707 116797 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 401 7 3 4 2.6 Cc1cccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
52949124 861 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R L7.39H 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 861 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R L7.39H 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 861 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R L7.39H 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 861 2 None -2 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R L7.39H 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
10252366 25665 11 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 434 3 2 3 4.8 CN1C(=O)C(NC(=O)Nc2cccc3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135364 25665 11 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 434 3 2 3 4.8 CN1C(=O)C(NC(=O)Nc2cccc3ccccc23)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10649606 49334 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 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 49334 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 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
70683295 73234 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 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 73234 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 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
73355866 204499 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Compound was evaluated for inhibition of CCK-A receptor by displacing [125I]-Bolton hunter CCK-8 radioligand in the rat pancreasCompound was evaluated for inhibition of CCK-A receptor by displacing [125I]-Bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 717 13 5 6 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCNS(=O)(=O)C(F)(F)F)c1ccccc1 10.1021/jm00092a007
CHEMBL86702 204499 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Compound was evaluated for inhibition of CCK-A receptor by displacing [125I]-Bolton hunter CCK-8 radioligand in the rat pancreasCompound was evaluated for inhibition of CCK-A receptor by displacing [125I]-Bolton hunter CCK-8 radioligand in the rat pancreas
ChEMBL 717 13 5 6 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCNS(=O)(=O)C(F)(F)F)c1ccccc1 10.1021/jm00092a007
71454457 78198 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 655 12 5 7 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1nc[nH]n1)c1ccccc1 10.1021/jm00092a007
CHEMBL2112330 78198 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 655 12 5 7 4.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CSc1nc[nH]n1)c1ccccc1 10.1021/jm00092a007
44370393 119126 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 492 14 2 3 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCCC1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL346784 119126 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 492 14 2 3 5.4 CCCCCN(CCCCC)C(=O)C(CCC(=O)N1CCCC1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
15673149 85551 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 620 to 770The 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 620 to 770
ChEMBL 717 13 5 6 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCNS(=O)(=O)C(F)(F)F)c1ccccc1 10.1016/S0960-894X(00)80652-6
CHEMBL2304151 85551 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 620 to 770The 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 620 to 770
ChEMBL 717 13 5 6 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCNS(=O)(=O)C(F)(F)F)c1ccccc1 10.1016/S0960-894X(00)80652-6
44349412 16671 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 12 3 3 3.6 CCCCC(CC)CNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
CHEMBL124917 16671 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 12 3 3 3.6 CCCCC(CC)CNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
10361419 26234 11 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 364 2 2 3 2.9 CN1C(=O)C(NC(=O)NC(C)(C)C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL135988 26234 11 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 364 2 2 3 2.9 CN1C(=O)C(NC(=O)NC(C)(C)C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44303243 201227 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 545 9 5 5 4.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)[C@H](O)c1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL62832 201227 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 545 9 5 5 4.2 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)[C@H](O)c1ccccc1 10.1016/S0960-894X(97)00356-9
10507071 113098 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
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 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 113098 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
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 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
10553685 118633 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 508 8 3 5 4.2 COC[C@@H]1CCCN1NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
CHEMBL342907 118633 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 508 8 3 5 4.2 COC[C@@H]1CCCN1NC(=O)[C@@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm970065l
9985100 113991 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 552 5 3 3 6.0 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2cccc(Cl)c2)c2ccccc21 10.1021/jm00048a015
CHEMBL333541 113991 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 552 5 3 3 6.0 CC(C)(C)NC(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(Cl)c2)C[C@H](c2cccc(Cl)c2)c2ccccc21 10.1021/jm00048a015
44368611 121467 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 541 10 4 3 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL359292 121467 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 541 10 4 3 4.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1021/jm00057a005
14208273 67381 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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)N[C@H]2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)cc1 10.1021/jm00120a002
CHEMBL1907840 67381 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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)N[C@H]2N=C(c3ccccc3F)c3ccccc3N(C)C2=O)cc1 10.1021/jm00120a002
44334172 4486 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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 556 10 3 5 4.9 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCC(C(=O)Nc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL102526 4486 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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 556 10 3 5 4.9 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCC(C(=O)Nc3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44379640 57267 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 522 6 2 5 5.8 CC(C)Oc1cccc(-n2c(C/N=C(\S)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
CHEMBL166737 57267 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 522 6 2 5 5.8 CC(C)Oc1cccc(-n2c(C/N=C(\S)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
44303470 201565 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 479 8 2 5 4.5 Cc1noc(C)c1CC(C)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL64623 201565 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 479 8 2 5 4.5 Cc1noc(C)c1CC(C)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1 10.1016/S0960-894X(97)00356-9
CHEMBL2372079 208430 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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](CCNCc2ccccc2)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
44286836 161164 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
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 19 6 7 4.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL41364 161164 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
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 19 6 7 4.8 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CCC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
15692562 109135 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
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 473 14 4 6 3.8 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc(O)c2cccc(O)c2n1 10.1021/jm00116a002
CHEMBL322284 109135 0 None - 0 Guinea pig 8.2 pIC50 = 8.2 Binding
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 473 14 4 6 3.8 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc(O)c2cccc(O)c2n1 10.1021/jm00116a002
10700916 173854 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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
CHEMBL4553223 173854 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
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
46235271 73286 2 None 2 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S 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 73286 2 None 2 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from human CCK1R T3.28V, T3.29S 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
CHEMBL2310858 207735 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
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 CCCC1CCN([C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc2ccccc2)C(N)=O)[C@H]1C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)CCc1ccc(OS(=O)(=O)O)cc1 10.1021/jm00094a001
44293999 187831 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 597 6 2 5 5.1 COc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
CHEMBL50216 187831 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 597 6 2 5 5.1 COc1cccc(NC(=O)NC2N=C(c3ccccc3F)c3cccc(C)c3N(CC(=O)N3CC4CCC(CC4)C3)C2=O)c1 10.1016/S0960-894X(96)00609-9
9985667 162797 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 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 10.1021/jm000959x
CHEMBL419237 162797 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 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 10.1021/jm000959x
44293811 184526 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 601 5 2 4 5.8 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(Cl)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
CHEMBL48563 184526 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 601 5 2 4 5.8 Cc1cccc2c1N(CC(=O)N1CC3CCC(CC3)C1)C(=O)C(NC(=O)Nc1cccc(Cl)c1)N=C2c1ccccc1F 10.1016/S0960-894X(96)00609-9
9985667 162797 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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
CHEMBL419237 162797 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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
14590302 100955 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 444 4 1 4 4.3 CC(C)(C)OC(=O)CN1C(=O)C(NC(=O)c2ccc3ccccc3c2)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
CHEMBL297534 100955 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 444 4 1 4 4.3 CC(C)(C)OC(=O)CN1C(=O)C(NC(=O)c2ccc3ccccc3c2)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
367893 51329 1 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
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 51329 1 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 429 14 3 3 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
10048986 27332 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 5 3 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)O)C2=O)c1 10.1021/jm00078a018
CHEMBL136919 27332 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 5 3 4 3.4 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)O)C2=O)c1 10.1021/jm00078a018
10816889 78415 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 570 8 3 6 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)[C@H](C#N)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
CHEMBL2112824 78415 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 570 8 3 6 4.5 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)[C@H](C#N)N[C@@H]1CCCN2C(=O)N(Cc3ccccc3)C(=O)C[C@@H]12 10.1021/jm991078x
136046102 100197 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
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 864 20 9 10 3.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cnc2cccc(O)c2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL292298 100197 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
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 864 20 9 10 3.1 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)c1cnc2cccc(O)c2c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
11742839 12700 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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)N[C@H]2N=C(N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL1188361 12700 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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)N[C@H]2N=C(N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL536245 12700 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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)N[C@H]2N=C(N3CCCCCC3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
10074366 120074 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 120074 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 120074 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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
15514020 78166 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 603 7 3 7 4.0 CC(=O)Oc1cccc(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
CHEMBL2112232 78166 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 603 7 3 7 4.0 CC(=O)Oc1cccc(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
14208234 202983 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 428 3 4 4 3.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(O)ccc2[nH]1 10.1021/jm00047a021
CHEMBL74066 202983 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 428 3 4 4 3.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(O)ccc2[nH]1 10.1021/jm00047a021
46235271 73286 2 None 2 2 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] 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 73286 2 None 2 2 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-CCK] from human CCK1R I6.51V, F6.52Y mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] 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
14208270 67395 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
CHEMBL1907853 67395 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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
13809511 101811 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 512 6 2 5 4.1 CN1C(=O)C(NC(=O)[C@@H](Cc2ccccc2)NC(=O)OC(C)(C)C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL303386 101811 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 512 6 2 5 4.1 CN1C(=O)C(NC(=O)[C@@H](Cc2ccccc2)NC(=O)OC(C)(C)C)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
15060278 120272 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 633 12 3 5 6.5 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)OCc1ccccc1 10.1016/S0960-894X(00)80687-3
CHEMBL355532 120272 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 633 12 3 5 6.5 O=C(CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NCCc1ccccc1)OCc1ccccc1 10.1016/S0960-894X(00)80687-3
44329287 205891 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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](c3ccc(F)cc3)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL95209 205891 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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](c3ccc(F)cc3)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
10815039 112336 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 493 5 2 5 4.5 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C#N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
CHEMBL330917 112336 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 493 5 2 5 4.5 CC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C#N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
15614750 118805 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 3 3 3.9 O=C(NCC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00163a069
CHEMBL344154 118805 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 3 3 3.9 O=C(NCC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2[nH]1 10.1021/jm00163a069
10744557 32492 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1C(=O)O 10.1021/jm970065l
CHEMBL141370 32492 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC1CCCCC1C(=O)O 10.1021/jm970065l
44372047 156576 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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 7 8 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)N(C)C(=O)OC(C)(C)C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
CHEMBL407507 156576 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
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 7 8 4.2 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)N(C)C(=O)OC(C)(C)C)C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00031a013
16100410 141254 0 None -6309 4 Human 5.2 pIC50 = 5.2 Binding
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
CHEMBL386212 141254 0 None -6309 4 Human 5.2 pIC50 = 5.2 Binding
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
11803746 106118 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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)c1ccc(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
CHEMBL3142904 106118 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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)c1ccc(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
14208230 102721 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 446 3 3 3 4.5 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Cl)ccc2[nH]1 10.1021/jm00120a002
CHEMBL308414 102721 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 446 3 3 3 4.5 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(Cl)ccc2[nH]1 10.1021/jm00120a002
14208234 202983 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 428 3 4 4 3.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(O)ccc2[nH]1 10.1021/jm00120a002
CHEMBL74066 202983 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 428 3 4 4 3.6 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2cc(O)ccc2[nH]1 10.1021/jm00120a002
10053201 16400 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 546 6 3 3 5.9 CCc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
CHEMBL124004 16400 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 546 6 3 3 5.9 CCc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
90663986 106320 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 21 8 8 3.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL3144555 106320 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 21 8 8 3.9 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)/C=C\c1ccc(Cl)cc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
90663994 106327 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 837 21 8 8 3.6 Cc1ccc(/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
CHEMBL3144563 106327 0 None - 0 Guinea pig 7.2 pIC50 = 7.2 Binding
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 837 21 8 8 3.6 Cc1ccc(/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
44283030 99181 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 629 12 3 7 5.4 COC(=O)CCC(=O)N[C@H](COC(=O)C(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)c1ccccc1 10.1021/jm00086a017
CHEMBL284361 99181 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 629 12 3 7 5.4 COC(=O)CCC(=O)N[C@H](COC(=O)C(C)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)c1ccccc1 10.1021/jm00086a017
11607229 139894 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
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
CHEMBL380922 139894 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cellsDisplacement of [125I]D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat CCK receptor expressed in CHO cells
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
44370451 50503 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
CHEMBL157658 50503 0 None - 0 Guinea pig 6.2 pIC50 = 6.2 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
19754255 58783 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 2 2 3 4.4 Cn1c(C(=O)Nc2cc3c4ccccc4nc-3c[nH]2)cc2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL169767 58783 1 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 2 2 3 4.4 Cn1c(C(=O)Nc2cc3c4ccccc4nc-3c[nH]2)cc2ccccc21 10.1016/S0960-894X(00)80682-4
10094721 205157 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 439 5 3 7 3.5 CN(C)c1cccc(-n2c(NNC(=O)Nc3cccc(C#N)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL9083 205157 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 439 5 3 7 3.5 CN(C)c1cccc(-n2c(NNC(=O)Nc3cccc(C#N)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
19754256 59279 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 287 2 2 2 3.9 O=C(Nc1cc2c3ccccc3nc-2c[nH]1)c1ccccc1 10.1016/S0960-894X(00)80682-4
CHEMBL171940 59279 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 287 2 2 2 3.9 O=C(Nc1cc2c3ccccc3nc-2c[nH]1)c1ccccc1 10.1016/S0960-894X(00)80682-4
10325557 46230 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 563 9 4 4 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC12C[C@@H]3C[C@@H](C[C@@H](C3)C1)C2Cl)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL153760 46230 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 563 9 4 4 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC12C[C@@H]3C[C@@H](C[C@@H](C3)C1)C2Cl)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
53465907 69055 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 4.7 O=C(Nc1ccccc1NC(=O)C(CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933109 69055 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 4.7 O=C(Nc1ccccc1NC(=O)C(CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
44381830 59009 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 610 15 6 7 2.5 N#C[C@H](N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
CHEMBL170664 59009 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 610 15 6 7 2.5 N#C[C@H](N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1 10.1016/S0960-894X(97)00107-8
10051647 116769 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
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 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2C(C)C 10.1021/jm00048a015
CHEMBL339547 116769 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
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 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2C(C)C 10.1021/jm00048a015
21842400 120448 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 496 7 2 4 5.3 CCC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccc2)c2ccccc21 10.1016/0960-894X(95)00556-9
CHEMBL356191 120448 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 496 7 2 4 5.3 CCC(C)(C)C(=O)CN1C(=O)C(NC(=O)Nc2cccc(C)c2)N=C(c2ccccc2)c2ccccc21 10.1016/0960-894X(95)00556-9
10816869 51561 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 569 8 3 5 5.2 COC(=O)[C@]1(NC(=O)[C@@](C)(Cc2c[nH]c3ccccc23)NC(=O)OC2C3CC4CC(C3)CC2C4)C[C@H]1c1ccccc1 10.1016/S0960-894X(01)81250-6
CHEMBL158547 51561 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 569 8 3 5 5.2 COC(=O)[C@]1(NC(=O)[C@@](C)(Cc2c[nH]c3ccccc23)NC(=O)OC2C3CC4CC(C3)CC2C4)C[C@H]1c1ccccc1 10.1016/S0960-894X(01)81250-6
20063261 22908 12 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 412 3 2 3 4.3 Cc1cc(C)cc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL133087 22908 12 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 412 3 2 3 4.3 Cc1cc(C)cc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
44280713 99557 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 740 15 6 9 3.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL286907 99557 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 740 15 6 9 3.6 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
44382486 59093 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
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 11 4 4 2.8 CCCC[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
CHEMBL171051 59093 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
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 11 4 4 2.8 CCCC[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
CHEMBL2372081 208432 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
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](C)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
44303650 100299 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 548 6 2 3 6.4 O=C(NC1(C(=O)NCCc2ccccc2)CC2(Cc3cccc4cccc(c34)C2)C1)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(97)00356-9
CHEMBL292956 100299 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 548 6 2 3 6.4 O=C(NC1(C(=O)NCCc2ccccc2)CC2(Cc3cccc4cccc(c34)C2)C1)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(97)00356-9
44349354 118033 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
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 415 8 3 4 2.9 CCc1cccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
CHEMBL341505 118033 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
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 415 8 3 4 2.9 CCc1cccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
14208267 202811 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 380 3 2 4 3.1 N#Cc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
CHEMBL72710 202811 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 380 3 2 4 3.1 N#Cc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
10350069 9864 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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)CCC(=O)O)NC(=O)[C@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm00017a022
CHEMBL114774 9864 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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)CCC(=O)O)NC(=O)[C@](C)(Cc1c[nH]c2ccccc12)NC(=O)OC1C2CC3CC(C2)CC1C3 10.1021/jm00017a022
44348902 155209 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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)c1cc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)ccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
CHEMBL405805 155209 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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)c1cc(NC(=O)[C@H](Cc2ccc(S(=O)(=O)O)cc2)NC(=O)O)ccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00099a005
44300862 157318 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 9 4 6 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)Cc3ccccc3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL408392 157318 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 9 4 6 5.2 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(=O)(=O)Cc3ccccc3)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
14208267 202811 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 380 3 2 4 3.1 N#Cc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL72710 202811 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 380 3 2 4 3.1 N#Cc1ccc(C(=O)NC2N=C(c3ccccc3)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
10761732 75578 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 371 4 3 5 3.5 O=C(NNc1nc2ccccc2c(=O)n1-c1ccccc1)Nc1ccccc1 10.1021/jm970373j
CHEMBL2051984 75578 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 371 4 3 5 3.5 O=C(NNc1nc2ccccc2c(=O)n1-c1ccccc1)Nc1ccccc1 10.1021/jm970373j
44349314 16375 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
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)c1cc(Cl)cc(Cl)c1 10.1021/jm00079a003
CHEMBL123852 16375 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
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)c1cc(Cl)cc(Cl)c1 10.1021/jm00079a003
5311201 205653 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
CHEMBL9387 205653 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00032a002
5311201 205653 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00530-0
CHEMBL9387 205653 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00530-0
5311201 205653 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
CHEMBL9387 205653 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80987-2
5311201 205653 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm9506736
CHEMBL9387 205653 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm9506736
5311201 205653 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
CHEMBL9387 205653 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm9608523
44376130 56028 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1ccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00032a003
CHEMBL163049 56028 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1ccc(NC(=O)N[C@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)cc1 10.1021/jm00032a003
44280599 98692 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 694 12 4 5 6.2 O=C(O)CC[C@H](NC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1)C(=O)Nc1cccc2ccccc12 10.1021/jm950372w
CHEMBL281206 98692 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 694 12 4 5 6.2 O=C(O)CC[C@H](NC(=O)CCC(NC(=O)c1cc(Cl)cc(Cl)c1)C(=O)N1CCC2(CCCC2)CC1)C(=O)Nc1cccc2ccccc12 10.1021/jm950372w
5311201 205653 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm970373j
CHEMBL9387 205653 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm970373j
14802510 114606 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 629 13 4 6 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](COC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
CHEMBL334346 114606 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 629 13 4 6 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](COC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
44368298 120502 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 613 13 4 5 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](COC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL356599 120502 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 613 13 4 5 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](COC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00057a005
43811299 116147 11 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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)Nc2cccc(C(F)(F)F)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL337055 116147 11 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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)Nc2cccc(C(F)(F)F)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
5311201 205653 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
CHEMBL9387 205653 30 None 26 6 Rat 6.1 pIC50 = 6.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00078a018
44281205 114307 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 857 17 4 10 5.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL33412 114307 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 857 17 4 10 5.1 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
90663256 106135 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory activity against cholecystokinin type A receptor from bovine striatal binding assayInhibitory activity against cholecystokinin type A receptor from bovine striatal binding assay
ChEMBL 854 17 7 8 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CSC(C)(C)[C@H]1C(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00100a033
CHEMBL3143146 106135 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory activity against cholecystokinin type A receptor from bovine striatal binding assayInhibitory activity against cholecystokinin type A receptor from bovine striatal binding assay
ChEMBL 854 17 7 8 5.3 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CSC(C)(C)[C@H]1C(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00100a033
CHEMBL2372080 208431 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
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](CNCc2ccccc2)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
10504136 204902 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 COc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1021/jm970373j
CHEMBL8922 204902 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 COc1cccc(NC(=O)NNc2nc3ccccc3c(=O)n2-c2cccc(OC(C)C)c2)c1 10.1021/jm970373j
44286835 99808 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 796 20 8 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL289036 99808 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 796 20 8 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCCCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
9916170 76185 2 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 575 10 4 4 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CC(=O)O)Cc1ccc(F)cc1 10.1016/s0960-894x(00)00198-0
CHEMBL2062146 76185 2 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 575 10 4 4 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CC(=O)O)Cc1ccc(F)cc1 10.1016/s0960-894x(00)00198-0
10462874 98367 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 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)80687-3
CHEMBL278780 98367 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 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)80687-3
10074366 120074 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 120074 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 120074 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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
10031013 204748 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human Cholecystokinin type A receptorBinding affinity against human Cholecystokinin type A receptor
ChEMBL 574 8 1 4 6.2 CC(C)N(C(=O)CN1C(=O)C(C)(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
CHEMBL88239 204748 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity against human Cholecystokinin type A receptorBinding affinity against human Cholecystokinin type A receptor
ChEMBL 574 8 1 4 6.2 CC(C)N(C(=O)CN1C(=O)C(C)(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
10031013 204748 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 574 8 1 4 6.2 CC(C)N(C(=O)CN1C(=O)C(C)(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
CHEMBL88239 204748 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 574 8 1 4 6.2 CC(C)N(C(=O)CN1C(=O)C(C)(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960205b
10031013 204748 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 574 8 1 4 6.2 CC(C)N(C(=O)CN1C(=O)C(C)(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/acs.jmedchem.0c00829
CHEMBL88239 204748 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 574 8 1 4 6.2 CC(C)N(C(=O)CN1C(=O)C(C)(CC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/acs.jmedchem.0c00829
44286655 99381 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 808 16 6 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC(=O)N(C(Cc2ccccc2)C(N)=O)CC1 10.1021/jm00037a005
CHEMBL285772 99381 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 808 16 6 7 4.5 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N1CCC(=O)N(C(Cc2ccccc2)C(N)=O)CC1 10.1021/jm00037a005
44329384 206580 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 COc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(C)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
CHEMBL99289 206580 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 COc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(C)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
89913304 140227 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 249 2 1 2 2.0 O=C1C=C(Cl)C(O)(c2ccccc2)N1C1CC1 10.1039/C6MD00052E
CHEMBL3818437 140227 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 249 2 1 2 2.0 O=C1C=C(Cl)C(O)(c2ccccc2)N1C1CC1 10.1039/C6MD00052E
5279123 202826 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00120a002
CHEMBL72841 202826 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00120a002
15614763 67409 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to rat pancreas cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to rat pancreas cholecystokinin receptor
ChEMBL 401 3 3 2 5.1 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)N[C@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
CHEMBL1907932 67409 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Half-maximal inhibition of [125I]CCK-33 binding to rat pancreas cholecystokinin receptorHalf-maximal inhibition of [125I]CCK-33 binding to rat pancreas cholecystokinin receptor
ChEMBL 401 3 3 2 5.1 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)N[C@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
5279123 202826 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00047a021
CHEMBL72841 202826 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1ccccc1Cl 10.1021/jm00047a021
14991538 106330 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
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)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/jm00089a010
CHEMBL3144566 106330 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
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)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/jm00089a010
52949124 861 2 None - 2 Rat 7.1 pIC50 = 7.1 Binding
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 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 861 2 None - 2 Rat 7.1 pIC50 = 7.1 Binding
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 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 861 2 None - 2 Rat 7.1 pIC50 = 7.1 Binding
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 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 861 2 None - 2 Rat 7.1 pIC50 = 7.1 Binding
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 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
10481933 13170 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 524 5 2 5 3.1 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CCN(C)CC3)C2=O)c1 10.1021/jm00078a018
CHEMBL1191818 13170 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 524 5 2 5 3.1 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CCN(C)CC3)C2=O)c1 10.1021/jm00078a018
CHEMBL542967 13170 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 524 5 2 5 3.1 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)N3CCN(C)CC3)C2=O)c1 10.1021/jm00078a018
44279808 98671 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 712 13 6 9 2.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL281082 98671 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 712 13 6 9 2.9 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1 10.1016/S0960-894X(96)00248-X
10369804 16566 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
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 Cc1cccc2c1N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
CHEMBL124340 16566 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
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 Cc1cccc2c1N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(Cl)c1)C[C@@H]2c1ccccc1 10.1021/jm00048a015
9984452 164740 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 4.7 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](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL423329 164740 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 4.7 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](CO)Cc1ccccc1 10.1021/jm00057a005
44283055 116099 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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; 690-850Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 690-850
ChEMBL 515 9 4 4 4.4 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NC(CO)Cc1ccccc1)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80156-0
CHEMBL336769 116099 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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; 690-850Evaluated for in vitro binding affinity to cholecystokinin-A (CCK-A) receptor in homogenized rat pancreas using [125I]bolton hunter CCK-26-33 as radioligand; 690-850
ChEMBL 515 9 4 4 4.4 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NC(CO)Cc1ccccc1)OC1C2CC3CC(C2)CC1C3 10.1016/S0960-894X(00)80156-0
14208282 67329 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 363 5 1 3 3.4 CC(C)CCC(=O)N[C@H]1N=C(c2ccccc2)c2ccccc2N(C)C1=O 10.1021/jm00120a002
CHEMBL1907663 67329 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 363 5 1 3 3.4 CC(C)CCC(=O)N[C@H]1N=C(c2ccccc2)c2ccccc2N(C)C1=O 10.1021/jm00120a002
9984452 164740 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 529 9 4 4 4.7 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](CO)Cc1ccccc1 10.1021/jm00105a062
CHEMBL423329 164740 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 529 9 4 4 4.7 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](CO)Cc1ccccc1 10.1021/jm00105a062
15177358 52940604 16338 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 667 9 4 4 7.1 ClC(Cl)(Cl)Cl.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
CHEMBL1237153 16338 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 667 9 4 4 7.1 ClC(Cl)(Cl)Cl.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
44368624 120607 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 513 9 4 3 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL357564 120607 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 513 9 4 3 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
9984452 29486 0 None - 1 Rat 6.1 pIC50 = 6.1 Binding
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 529 9 4 4 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm970065l
CHEMBL138657 29486 0 None - 1 Rat 6.1 pIC50 = 6.1 Binding
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 529 9 4 4 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm970065l
44368329 120477 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 499 8 3 3 5.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3)C(=O)NCCc1ccccc1 10.1021/jm00057a005
CHEMBL356446 120477 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 499 8 3 3 5.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3)C(=O)NCCc1ccccc1 10.1021/jm00057a005
10483574 6114 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 591 8 2 5 5.3 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm950626d
CHEMBL108130 6114 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 591 8 2 5 5.3 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3ccccc3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm950626d
73351320 105653 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 12 5 5 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCNC(=O)C(F)(F)F)c1ccccc1 10.1021/jm00092a007
CHEMBL313559 105653 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 12 5 5 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCNC(=O)C(F)(F)F)c1ccccc1 10.1021/jm00092a007
6439414 2964 11 None -2454 2 Rat 6.1 pIC50 = 6.1 Binding
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 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 10.1021/jm00105a062
867 2964 11 None -2454 2 Rat 6.1 pIC50 = 6.1 Binding
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 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 10.1021/jm00105a062
CHEMBL3351022 2964 11 None -2454 2 Rat 6.1 pIC50 = 6.1 Binding
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 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 10.1021/jm00105a062
CHEMBL341460 2964 11 None -2454 2 Rat 6.1 pIC50 = 6.1 Binding
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 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 10.1021/jm00105a062
44368728 118988 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 596 11 5 4 4.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)/C=C/C(=O)O)c1ccccc1 10.1021/jm00057a005
CHEMBL345512 118988 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 596 11 5 4 4.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)/C=C/C(=O)O)c1ccccc1 10.1021/jm00057a005
14208306 202477 1 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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)c2ccccc2I)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
CHEMBL70791 202477 1 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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)c2ccccc2I)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00047a021
44451577 95328 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity to mouse CCK1 receptorBinding affinity to mouse CCK1 receptor
ChEMBL 546 6 2 5 2.1 Cc1cccc(NC(=O)NC2C(=O)N(CC(=O)N3CCCC3)c3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
CHEMBL258630 95328 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity to mouse CCK1 receptorBinding affinity to mouse CCK1 receptor
ChEMBL 546 6 2 5 2.1 Cc1cccc(NC(=O)NC2C(=O)N(CC(=O)N3CCCC3)c3ccccc3N(CC(=O)N3CCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
52949124 861 2 None -2 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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 861 2 None -2 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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 861 2 None -2 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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 861 2 None -2 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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
46235271 73286 2 None 2 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R L7.39H 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 73286 2 None 2 2 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-CCK] from human CCK1R L7.39H mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from human CCK1R L7.39H 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
15689723 106100 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
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)Nc1ccccc1C(F)(F)F)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142693 106100 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
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)Nc1ccccc1C(F)(F)F)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
89913313 140246 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 299 3 1 2 3.1 CC(C)CN1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
CHEMBL3818718 140246 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 299 3 1 2 3.1 CC(C)CN1C(=O)C=C(Cl)C1(O)c1ccc(Cl)cc1 10.1039/C6MD00052E
443375 205862 40 None -3 5 Rat 8.1 pIC50 = 8.1 Binding
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 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00163a069
CHEMBL9506 205862 40 None -3 5 Rat 8.1 pIC50 = 8.1 Binding
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 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00163a069
44578305 180578 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human CCK1 receptorInhibition of 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 180578 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human CCK1 receptorInhibition of 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
14991571 201238 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
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 905 21 8 10 3.9 CC(=O)Oc1ccc2cc(C(=O)NCCCC[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)ccc2c1 10.1021/jm00089a010
CHEMBL62887 201238 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
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 905 21 8 10 3.9 CC(=O)Oc1ccc2cc(C(=O)NCCCC[C@H](NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)ccc2c1 10.1021/jm00089a010
104929 2180 8 None - 3 Rat 8.1 pIC50 = 8.1 Binding
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 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00121a004
3477 2180 8 None - 3 Rat 8.1 pIC50 = 8.1 Binding
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 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00121a004
879 2180 8 None - 3 Rat 8.1 pIC50 = 8.1 Binding
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 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00121a004
CHEMBL289498 2180 8 None - 3 Rat 8.1 pIC50 = 8.1 Binding
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 398 3 2 3 4.0 Cc1cccc(c1)NC(=O)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm00121a004
10009894 25409 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 694 13 6 6 4.9 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@@H](NC(=O)OCc3ccccc3)C(=O)N21 10.1016/s0960-894x(01)00630-8
CHEMBL13517 25409 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 694 13 6 6 4.9 Cc1ccccc1NC(=O)NCCCC[C@@H](CC(=O)O)NC(=O)[C@H]1Cc2c([nH]c3ccccc23)[C@@H]2C[C@@H](NC(=O)OCc3ccccc3)C(=O)N21 10.1016/s0960-894x(01)00630-8
10070679 27545 11 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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)Nc2cccc(Cl)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL137066 27545 11 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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)Nc2cccc(Cl)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL407530 210910 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00100a033
14208194 162872 2 None 1122 2 Rat 8.1 pIC50 = 8.1 Binding
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
CHEMBL419764 162872 2 None 1122 2 Rat 8.1 pIC50 = 8.1 Binding
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
14208243 202702 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL72073 202702 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
14208194 162872 2 None 1122 2 Rat 8.1 pIC50 = 8.1 Binding
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 408 3 2 3 3.7 CN1C(=O)[C@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL419764 162872 2 None 1122 2 Rat 8.1 pIC50 = 8.1 Binding
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 408 3 2 3 3.7 CN1C(=O)[C@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
10452597 26705 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 384 3 2 3 3.6 CN1C(=O)C(NC(=O)Nc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL136408 26705 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 384 3 2 3 3.6 CN1C(=O)C(NC(=O)Nc2ccccc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
14208243 202702 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 403 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
CHEMBL72073 202702 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 403 3 1 3 3.9 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(00)80682-4
14208194 162872 2 None 1122 2 Rat 8.1 pIC50 = 8.1 Binding
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
CHEMBL419764 162872 2 None 1122 2 Rat 8.1 pIC50 = 8.1 Binding
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
14208243 202702 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
CHEMBL72073 202702 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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(NC(=O)c2ccc(Cl)cc2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00047a021
10817395 106645 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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 600 8 1 4 6.9 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
CHEMBL316164 106645 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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 600 8 1 4 6.9 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm960249k
10817395 106645 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 600 8 1 4 6.9 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL316164 106645 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 600 8 1 4 6.9 COc1ccc(N(C(=O)CN2C(=O)C(C)(Cc3c[nH]c4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
15689727 106098 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
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 880 20 9 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccc(Cl)cc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
CHEMBL3142690 106098 0 None - 0 Guinea pig 8.1 pIC50 = 8.1 Binding
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 880 20 9 8 4.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)Nc1ccc(Cl)cc1Cl)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00113a023
44578455 181863 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human CCK1 receptorInhibition of 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 181863 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human CCK1 receptorInhibition of 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
10480792 45528 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 CC1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL153095 45528 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 CC1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
CHEMBL3350686 45528 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 CC1CCCCC1OC(=O)N[C@](C)(Cc1c[nH]c2ccccc12)C(=O)N[C@H](CO)Cc1ccccc1 10.1021/jm00057a005
14208210 202493 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 413 3 2 4 4.1 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2o1 10.1021/jm00047a021
CHEMBL70856 202493 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 413 3 2 4 4.1 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2o1 10.1021/jm00047a021
21842365 119236 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 495 6 2 5 4.5 Cc1cccc(NC(=O)NC2N=C(c3cccnc3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL347843 119236 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 495 6 2 5 4.5 Cc1cccc(NC(=O)NC2N=C(c3cccnc3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1016/0960-894X(95)00557-A
11765257 108332 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 695 10 2 6 6.6 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1016/s0960-894x(98)00548-4
CHEMBL320980 108332 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 695 10 2 6 6.6 COc1ccc(N(C(=O)CN2C(=O)C(NC(=O)Nc3cccc(C(=O)c4ccccc4)c3)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1016/s0960-894x(98)00548-4
46234820 73277 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 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 73277 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 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
CHEMBL328422 209540 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 Cc1cccc(C)c1NC(=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
89913684 140225 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 299 3 1 2 3.0 O=C1C=C(Cl)C(O)(c2ccccc2)N1Cc1ccccc1 10.1039/C6MD00052E
CHEMBL3818410 140225 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 299 3 1 2 3.0 O=C1C=C(Cl)C(O)(c2ccccc2)N1Cc1ccccc1 10.1039/C6MD00052E
14208307 77456 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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)c2ccccc2I)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL2092867 77456 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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)c2ccccc2I)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
14208283 67328 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 375 3 1 3 3.5 CN1C(=O)[C@@H](NC(=O)C2CCCCC2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL1907662 67328 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 375 3 1 3 3.5 CN1C(=O)[C@@H](NC(=O)C2CCCCC2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
20190197 31289 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 421 4 1 3 4.6 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1ccc(Cl)cc1 10.1021/jm00163a069
CHEMBL140365 31289 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 421 4 1 3 4.6 CN1c2ccccc2C(c2ccccc2F)=NCC1CNC(=O)c1ccc(Cl)cc1 10.1021/jm00163a069
10075052 189072 0 None - 2 Rat 6.1 pIC50 = 6.1 Binding
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 510 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL515268 189072 0 None - 2 Rat 6.1 pIC50 = 6.1 Binding
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 510 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL515288 189072 0 None - 2 Rat 6.1 pIC50 = 6.1 Binding
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 510 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
44334320 4939 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 531 9 2 4 4.6 Cc1cccc(NC(=O)N[C@H](C[S+]([O-])Cc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL105132 4939 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 531 9 2 4 4.6 Cc1cccc(NC(=O)N[C@H](C[S+]([O-])Cc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
15673150 85553 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 680 to 970The 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 680 to 970
ChEMBL 681 12 5 5 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCNC(=O)C(F)(F)F)c1ccccc1 10.1016/S0960-894X(00)80652-6
CHEMBL2304154 85553 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 680 to 970The 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 680 to 970
ChEMBL 681 12 5 5 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@H](NC(=O)CCNC(=O)C(F)(F)F)c1ccccc1 10.1016/S0960-894X(00)80652-6
44349413 112595 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 410 12 3 3 4.0 CCC(CC)(CC)CCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
CHEMBL331413 112595 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 410 12 3 3 4.0 CCC(CC)(CC)CCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
44360216 32001 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 403 5 3 4 3.3 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)C(O)c1ccccc1 10.1021/jm00163a069
CHEMBL140974 32001 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 403 5 3 4 3.3 O=C(NCC1CNc2ccccc2C(c2ccccc2F)=N1)C(O)c1ccccc1 10.1021/jm00163a069
44349240 117601 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
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 368 11 3 3 3.0 CCCCCCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
CHEMBL340755 117601 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
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 368 11 3 3 3.0 CCCCCCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
9800177 67352 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
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 383 3 2 2 4.7 O=C1Nc2ccccc2C(c2ccccc2F)=N[C@@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
CHEMBL1907714 67352 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
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 383 3 2 2 4.7 O=C1Nc2ccccc2C(c2ccccc2F)=N[C@@H]1Cc1c[nH]c2ccccc12 10.1021/jm00390a019
15614841 67364 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
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 390 5 1 3 4.7 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=N[C@@H]1COCc1ccccc1 10.1021/jm00390a019
CHEMBL1907734 67364 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
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 390 5 1 3 4.7 O=C1Nc2ccc(Cl)cc2C(c2ccccc2)=N[C@@H]1COCc1ccccc1 10.1021/jm00390a019
CHEMBL286843 99547 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 541 8 3 4 7.2 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C1NC=C(CCc2ccccc2)S1 10.1021/jm00086a017
10480605 77942 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 5 4 7 3.7 Cc1ccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)cc1Nc1nn[nH]n1 10.1021/jm9506736
CHEMBL2110201 77942 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 5 4 7 3.7 Cc1ccc(NC(=O)N[C@@H]2N=C(C3CCCCC3)c3ccccc3N(C)C2=O)cc1Nc1nn[nH]n1 10.1021/jm9506736
44349411 16649 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
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 380 7 3 3 3.1 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCCCCC1 10.1021/jm00079a003
CHEMBL124802 16649 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
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 380 7 3 3 3.1 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)NC1CCCCCC1 10.1021/jm00079a003
44283159 99659 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 8 3 3 6.6 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)/C(S)=N/CCc1ccccc1 10.1021/jm00086a017
CHEMBL287682 99659 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 8 3 3 6.6 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)/C(S)=N/CCc1ccccc1 10.1021/jm00086a017
44331065 106729 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
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 25 8 11 1.3 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
CHEMBL316709 106729 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
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 25 8 11 1.3 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00094a001
15667015 161293 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
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 10 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@H](C)C(=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
CHEMBL414793 161293 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
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 10 11 2.0 CCCC[C@H](NC(=O)CCc1ccc(OS(=O)(=O)O)cc1)C(=O)N[C@H](C)C(=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
14208253 202993 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc(Cl)c1 10.1021/jm00120a002
CHEMBL74125 202993 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc(Cl)c1 10.1021/jm00120a002
14208253 202993 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc(Cl)c1 10.1021/jm00047a021
CHEMBL74125 202993 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 389 3 2 3 3.9 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)c1cccc(Cl)c1 10.1021/jm00047a021
14802508 78366 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 615 12 4 6 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCC(OC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL2112695 78366 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 615 12 4 6 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCC(OC(=O)CCC(=O)O)c1ccccc1 10.1021/jm00105a062
15104629 109617 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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
CHEMBL323627 109617 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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
14720386 48045 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 463 12 2 4 4.4 CCCN(CCC)C(=O)[C@H](CCC(=O)OCc1ccccc1)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
CHEMBL155406 48045 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 463 12 2 4 4.4 CCCN(CCC)C(=O)[C@H](CCC(=O)OCc1ccccc1)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
44329055 206215 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 554 7 3 3 6.1 CCc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(C)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
CHEMBL97133 206215 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 554 7 3 3 6.1 CCc1ccccc1[C@H]1C[C@@H](NC(=O)Nc2cccc(C)c2)C(=O)N(CC(=O)NC(C)(C)C)[C@@H](c2ccccc2)C1 10.1016/S0960-894X(01)80832-5
44382706 58696 1 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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
CHEMBL169274 58696 1 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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
11667741 194897 0 None - 2 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCKalpha receptorInhibition of CCKalpha receptor
ChEMBL 366 4 1 5 2.5 Cc1c(CC(=O)O)c2cccnc2n1S(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.06.042
CHEMBL563949 194897 0 None - 2 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCKalpha receptorInhibition of CCKalpha receptor
ChEMBL 366 4 1 5 2.5 Cc1c(CC(=O)O)c2cccnc2n1S(=O)(=O)c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.06.042
10528465 96590 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 4 7 4.0 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C(=O)O)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL267023 96590 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 4 7 4.0 CC(C)Oc1cccc(-n2c(NNC(=O)Nc3cccc(C(=O)O)c3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL2369769 207930 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasConcentration producing half-maximal inhibition of specific binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL None None None C/C=C/CC[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/0960-894X(94)85022-4
11700447 72663 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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
CHEMBL200953 72663 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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
13953716 101113 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 442 3 2 5 4.9 Cc1nnc2n1-c1ccccc1C(c1ccccc1)=NC2NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00396a028
CHEMBL298705 101113 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
ChEMBL 442 3 2 5 4.9 Cc1nnc2n1-c1ccccc1C(c1ccccc1)=NC2NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00396a028
44281292 114283 0 None - 1 Mouse 5.1 pIC50 = 5.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 816 17 5 9 5.0 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCNC(=O)CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
CHEMBL33398 114283 0 None - 1 Mouse 5.1 pIC50 = 5.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 816 17 5 9 5.0 CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCNC(=O)CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00249-1
44329456 110944 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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
CHEMBL327526 110944 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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
10995425 114945 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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
CHEMBL3350859 114945 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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
44592486 187234 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 393 7 4 3 3.6 CC(C)CC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL496067 187234 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 393 7 4 3 3.6 CC(C)CC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1)C(=O)O 10.1016/j.bmc.2009.02.012
155557285 173936 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 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 173936 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 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
44373702 119408 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 555 8 4 4 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@]1(C(=O)O)C[C@H]1c1ccccc1 10.1016/S0960-894X(01)81250-6
CHEMBL349473 119408 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 555 8 4 4 5.1 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@]1(C(=O)O)C[C@H]1c1ccccc1 10.1016/S0960-894X(01)81250-6
44286696 167411 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
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 796 18 6 7 4.4 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL431912 167411 0 None - 0 Guinea pig 7.1 pIC50 = 7.1 Binding
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 796 18 6 7 4.4 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N(C)CC(=O)N(C)C(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL170026 207087 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
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)OC(C)(C)C)C(=O)N1C[C@H](Cc2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
10004579 78092 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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@H](NC(=O)Nc2cccc(Br)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL2111923 78092 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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@H](NC(=O)Nc2cccc(Br)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
15281997 48223 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 486 5 2 6 3.7 Cc1cccc(NC(=O)NC2N=C(c3nccn3C)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL155627 48223 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 486 5 2 6 3.7 Cc1cccc(NC(=O)NC2N=C(c3nccn3C)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL2369762 207925 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Concentration producing half-maximal inhibition of specific binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreasConcentration producing half-maximal inhibition of specific binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
ChEMBL None None None CCCCC[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/0960-894X(94)85022-4
44209152 58835 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 336 2 3 2 5.0 O=C(Nc1ccc(Cl)cc1)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
CHEMBL169953 58835 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 336 2 3 2 5.0 O=C(Nc1ccc(Cl)cc1)Nc1cc2c3ccccc3nc-2c[nH]1 10.1016/S0960-894X(00)80682-4
73349792 156860 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 669 13 5 7 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCSc1nc[nH]n1)c1ccccc1 10.1021/jm00092a007
CHEMBL407857 156860 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 669 13 5 7 5.3 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)CCSc1nc[nH]n1)c1ccccc1 10.1021/jm00092a007
44354100 116256 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 4.7 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)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
CHEMBL337661 116256 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 4.7 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)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
44354100 120285 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 628 13 5 5 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL355656 120285 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 628 13 5 5 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
101823779 1364 29 None - 0 Human 6.1 pIC50 = 6.1 Binding
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
16162108 1364 29 None - 0 Human 6.1 pIC50 = 6.1 Binding
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
8408 1364 29 None - 0 Human 6.1 pIC50 = 6.1 Binding
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
CHEMBL4451154 1364 29 None - 0 Human 6.1 pIC50 = 6.1 Binding
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
44408632 157680 0 None -3630 4 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.8 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](Cc1cn(C(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL408832 157680 0 None -3630 4 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.8 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](Cc1cn(C(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O 10.1021/jm050851n
44283055 99282 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 4.4 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NC(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL285049 99282 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 4.4 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)NC(CO)Cc1ccccc1)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
44591979 178472 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 426 7 4 3 3.2 NC(=O)C(Cc1ccccc1)NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
CHEMBL471465 178472 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 426 7 4 3 3.2 NC(=O)C(Cc1ccccc1)NC(=O)c1ccccc1NC(=O)c1cc2ccccc2[nH]1 10.1016/j.bmc.2009.02.012
54587151 61522 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 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 61522 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 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
5311201 205653 30 None -2570 6 Guinea pig 7.1 pIC50 = 7.1 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00327-P
CHEMBL9387 205653 30 None -2570 6 Guinea pig 7.1 pIC50 = 7.1 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/0960-894X(95)00327-P
5311201 205653 30 None -2570 6 Guinea pig 7.1 pIC50 = 7.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00048a015
CHEMBL9387 205653 30 None -2570 6 Guinea pig 7.1 pIC50 = 7.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00048a015
5311201 205653 30 None -2570 6 Guinea pig 7.1 pIC50 = 7.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL9387 205653 30 None -2570 6 Guinea pig 7.1 pIC50 = 7.1 Binding
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 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL2111881 207466 0 None - 0 Guinea pig 5.1 pIC50 = 5.1 Binding
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
CHEMBL2111882 207467 0 None - 0 Guinea pig 5.1 pIC50 = 5.1 Binding
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
44349278 16414 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 388 10 3 3 3.3 CCCCCNC(=O)C(CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00079a003
CHEMBL124090 16414 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 388 10 3 3 3.3 CCCCCNC(=O)C(CCC(=O)O)NC(=O)c1ccc(Cl)c(Cl)c1 10.1021/jm00079a003
44283177 99827 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 655 16 2 5 7.6 CCOC(=O)CCCCCC(=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
CHEMBL289239 99827 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 655 16 2 5 7.6 CCOC(=O)CCCCCC(=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
44283085 99431 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 484 9 2 2 7.4 CC(CCCCc1ccccc1)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
CHEMBL286093 99431 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 484 9 2 2 7.4 CC(CCCCc1ccccc1)(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00086a017
14208239 202783 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 398 4 3 3 4.2 O=C1Nc2ccccc2C(c2ccccc2F)=NC1NCc1cc2ccccc2[nH]1 10.1021/jm00120a002
CHEMBL72550 202783 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 398 4 3 3 4.2 O=C1Nc2ccccc2C(c2ccccc2F)=NC1NCc1cc2ccccc2[nH]1 10.1021/jm00120a002
10698051 204795 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 557 7 1 4 5.9 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
CHEMBL88545 204795 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 557 7 1 4 5.9 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm960249k
10698051 204795 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 557 7 1 4 5.9 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm970265x
CHEMBL88545 204795 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 557 7 1 4 5.9 CC(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm970265x
70683305 73285 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 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 73285 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 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
14802543 169901 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 600 11 5 5 4.5 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)CC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL2112693 169901 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 600 11 5 5 4.5 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)CC(=O)O)c1ccccc1 10.1021/jm00105a062
CHEMBL444902 169901 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 600 11 5 5 4.5 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)CC(=O)O)c1ccccc1 10.1021/jm00105a062
44336539 5060 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]BDZ1 from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R TM2 (unknown origin) containing N2.61T 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 5060 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]BDZ1 from CCK1R TM2 (unknown origin) containing N2.61T chimeric mutant expressed in CHO cellsDisplacement of [125I]BDZ1 from CCK1R TM2 (unknown origin) containing N2.61T 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
44349044 112795 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 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 10.1021/jm000959x
CHEMBL331532 112795 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 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 10.1021/jm000959x
44349044 112795 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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
CHEMBL331532 112795 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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
15104617 9893 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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)c1cc2ccccc2cn1 10.1021/jm00116a002
CHEMBL114916 9893 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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)c1cc2ccccc2cn1 10.1021/jm00116a002
14720390 49110 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 373 10 3 3 2.8 CCCN(CCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
CHEMBL156415 49110 0 None - 0 Guinea pig 4.1 pIC50 = 4.1 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 373 10 3 3 2.8 CCCN(CCC)C(=O)[C@@H](CCC(=O)O)NC(=O)c1cc2ccccc2[nH]1 10.1021/jm00164a020
44349429 16643 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
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 406 7 3 4 3.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)C1CC2CCCCC2CN1 10.1021/jm00079a003
CHEMBL124780 16643 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
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 406 7 3 4 3.0 O=C(O)CCC(NC(=O)c1cccc(Cl)c1)C(=O)C1CC2CCCCC2CN1 10.1021/jm00079a003
23928173 113636 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 511 6 2 5 4.7 CN(C)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
CHEMBL332931 113636 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 511 6 2 5 4.7 CN(C)c1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm960669+
44381949 120199 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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
CHEMBL354802 120199 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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
14208209 163342 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 402 5 3 4 3.2 O=C(CNc1ccccc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00047a021
CHEMBL420722 163342 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 402 5 3 4 3.2 O=C(CNc1ccccc1)NC1N=C(c2ccccc2F)c2ccccc2NC1=O 10.1021/jm00047a021
10841112 205357 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 0 6 6.1 COc1ccc(N(C(=O)CN2C(=O)C(Cc3noc4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
CHEMBL91986 205357 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 0 6 6.1 COc1ccc(N(C(=O)CN2C(=O)C(Cc3noc4ccccc34)C(=O)N(c3ccccc3)c3ccccc32)C(C)C)cc1 10.1021/jm970265x
10048206 196968 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 428 7 3 4 4.1 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2o1 10.1016/j.bmc.2009.05.067
CHEMBL579245 196968 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cellsDisplacement of [125I]-CCK8 from CCK1 receptor in rat pancreatic acinar cells
ChEMBL 428 7 3 4 4.1 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2o1 10.1016/j.bmc.2009.05.067
10674604 167354 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 571 6 1 4 6.3 CC(C)(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm970265x
CHEMBL431451 167354 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro for binding affinity against human cholecystokinin type A receptor.In vitro for binding affinity against human cholecystokinin type A receptor.
ChEMBL 571 6 1 4 6.3 CC(C)(C)N(C(=O)CN1C(=O)C(Cc2n[nH]c3ccccc23)C(=O)N(c2ccccc2)c2ccccc21)c1ccccc1 10.1021/jm970265x
16100408 141247 0 None -1202 3 Human 5.1 pIC50 = 5.1 Binding
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](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)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
CHEMBL386186 141247 0 None -1202 3 Human 5.1 pIC50 = 5.1 Binding
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](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)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
14208210 202493 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 413 3 2 4 4.1 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2o1 10.1021/jm00120a002
CHEMBL70856 202493 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 413 3 2 4 4.1 O=C(NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1cc2ccccc2o1 10.1021/jm00120a002
14208268 202769 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 418 3 2 4 3.5 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2N)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
CHEMBL72428 202769 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 418 3 2 4 3.5 CN1C(=O)C(NC(=O)c2ccc(Cl)cc2N)N=C(c2ccccc2)c2ccccc21 10.1021/jm00120a002
10073533 22339 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 472 7 3 5 3.5 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCC(=O)O)C2=O)c1 10.1021/jm00078a018
CHEMBL132603 22339 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
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 472 7 3 5 3.5 COc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CCC(=O)O)C2=O)c1 10.1021/jm00078a018
155543846 172631 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 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 172631 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 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
10484212 99404 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-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 99404 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]Cholecystokinin-8 binding to Cholecystokinin type A receptor of rat pancreatic membranesInhibition of [125I]Cholecystokinin-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
CHEMBL3142923 209381 0 None - 0 Guinea pig 8.0 pIC50 = 8.0 Binding
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 COc1cccc(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
53465844 69053 0 None - 2 Rat 8.0 pIC50 = 8.0 Binding
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)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69053 0 None - 2 Rat 8.0 pIC50 = 8.0 Binding
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)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL208479 207445 0 None -3 4 Human 8.0 pIC50 = 8.0 Binding
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](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
46235272 73283 0 None - 0 Human 8.0 pIC50 = 8 Binding
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 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 73283 0 None - 0 Human 8.0 pIC50 = 8 Binding
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 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
54586175 61574 0 None - 0 Human 8.0 pIC50 = 8 Binding
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 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 61574 0 None - 0 Human 8.0 pIC50 = 8 Binding
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 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
15667018 157228 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 998 27 10 11 2.5 CCCC[C@H](NC(=O)c1ccc2cc(OS(=O)(=O)O)ccc2c1)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
CHEMBL408286 157228 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 998 27 10 11 2.5 CCCC[C@H](NC(=O)c1ccc2cc(OS(=O)(=O)O)ccc2c1)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
14208212 102465 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 396 3 3 4 3.0 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)C1Cc2ccccc2N1 10.1021/jm00120a002
CHEMBL306369 102465 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 396 3 3 4 3.0 O=C(NC1N=C(c2ccccc2)c2ccccc2NC1=O)C1Cc2ccccc2N1 10.1021/jm00120a002
44311593 102533 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 402 3 2 3 3.8 CN(C(=O)NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1 10.1021/jm00120a002
CHEMBL306958 102533 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 402 3 2 3 3.8 CN(C(=O)NC1N=C(c2ccccc2F)c2ccccc2NC1=O)c1ccccc1 10.1021/jm00120a002
11114607 114940 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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
CHEMBL3350852 114940 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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
19018662 26292 11 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 424 3 2 3 4.1 CN1C(=O)C(NC(=O)Nc2ccc3c(c2)CCC3)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
CHEMBL136038 26292 11 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 424 3 2 3 4.1 CN1C(=O)C(NC(=O)Nc2ccc3c(c2)CCC3)N=C(c2ccccc2)c2ccccc21 10.1021/jm00078a018
10436569 77477 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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)N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00078a018
CHEMBL2092976 77477 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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)N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(=O)N2CCCC2)C1=O 10.1021/jm00078a018
44280224 104292 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 757 16 4 7 5.8 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL31090 104292 0 None - 1 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 757 16 4 7 5.8 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1 10.1016/S0960-894X(96)00248-X
44334337 4592 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 541 10 2 5 5.1 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL103276 4592 0 None - 0 Guinea pig 6.1 pIC50 = 6.1 Binding
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 541 10 2 5 5.1 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCC(C(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL34853 209958 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 CCS[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
14208300 77455 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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)c2ccccc2Br)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
CHEMBL2092866 77455 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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)c2ccccc2Br)N=C(c2ccccc2F)c2ccccc21 10.1021/jm00120a002
10474221 16655 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
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 368 8 3 3 2.9 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
CHEMBL124822 16655 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
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 368 8 3 3 2.9 CC(C)(C)CCNC(=O)C(CCC(=O)O)NC(=O)c1cccc(Cl)c1 10.1021/jm00079a003
14991565 198648 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 23 8 8 3.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL59759 198648 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 23 8 8 3.6 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CCCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00089a010
CHEMBL408083 210941 0 None -2 4 Human 5.0 pIC50 = 5.0 Binding
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](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
11812882 78169 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 483 5 3 5 2.5 CN1C(=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
CHEMBL2112236 78169 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 483 5 3 5 2.5 CN1C(=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
44591826 191924 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 425 8 3 5 3.4 CSCCC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2n1C)C(=O)O 10.1016/j.bmc.2009.02.012
CHEMBL520997 191924 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 425 8 3 5 3.4 CSCCC(NC(=O)c1ccccc1NC(=O)c1cc2ccccc2n1C)C(=O)O 10.1016/j.bmc.2009.02.012
44279862 98660 0 None - 1 Mouse 5.0 pIC50 = 5.0 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 702 13 3 7 5.9 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL281017 98660 0 None - 1 Mouse 5.0 pIC50 = 5.0 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 702 13 3 7 5.9 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
44286976 141401 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 768 18 8 7 3.7 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
CHEMBL38716 141401 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 768 18 8 7 3.7 Cc1ccccc1NC(=O)NCCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)NCC(=O)NC(Cc1ccccc1)C(N)=O 10.1021/jm00037a005
15670985 205352 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 490 9 3 5 3.2 COc1cccc(N(CC(=O)N(C)c2ccccc2)C(=O)CNC(=O)Nc2cccc(C(=O)O)c2)c1 10.1021/jm970373j
CHEMBL9195 205352 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 490 9 3 5 3.2 COc1cccc(N(CC(=O)N(C)c2ccccc2)C(=O)CNC(=O)Nc2cccc(C(=O)O)c2)c1 10.1021/jm970373j
CHEMBL3142681 209370 0 None - 0 Guinea pig 7.0 pIC50 = 7.0 Binding
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 Cc1ccccc1NC(=O)NCCCCC[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
70681224 73280 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 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 73280 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 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 861 2 None -2 2 Human 7.0 pIC50 = 7.0 Binding
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 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 861 2 None -2 2 Human 7.0 pIC50 = 7.0 Binding
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 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 861 2 None -2 2 Human 7.0 pIC50 = 7.0 Binding
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 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 861 2 None -2 2 Human 7.0 pIC50 = 7.0 Binding
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 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
CHEMBL328422 209540 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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(C)c1NC(=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
44381829 167952 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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](CNN[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)Cc1c[nH]c2ccccc12 10.1016/S0960-894X(00)80680-0
CHEMBL435465 167952 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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](CNN[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)Cc1c[nH]c2ccccc12 10.1016/S0960-894X(00)80680-0
10392523 206196 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
CHEMBL96970 206196 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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](c3ccccc3C)C[C@H](c3ccccc3)N(CC(=O)NC(C)(C)C)C2=O)c1 10.1016/S0960-894X(01)80832-5
44370406 49602 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 529 16 2 4 6.6 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCc1ccccc1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
CHEMBL156814 49602 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibition of binding of [125I]- CCK-33 to rat pancreasInhibition of binding of [125I]- CCK-33 to rat pancreas
ChEMBL 529 16 2 4 6.6 CCCCCN(CCCCC)C(=O)C(CCC(=O)OCc1ccccc1)NC(=O)Nc1ccc(Cl)cc1 10.1021/jm00164a020
70684970 77480 0 None - 0 Guinea pig 4.0 pIC50 = 4.0 Binding
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 395 3 0 3 4.5 CN1C[C@@H](CC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c2ccccc21 10.1021/jm00390a019
CHEMBL2092990 77480 0 None - 0 Guinea pig 4.0 pIC50 = 4.0 Binding
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 395 3 0 3 4.5 CN1C[C@@H](CC2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c2ccccc21 10.1021/jm00390a019
44283515 99699 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 8 2 4 6.5 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)SCCc1ccccc1 10.1021/jm00086a017
CHEMBL288038 99699 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 8 2 4 6.5 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)SCCc1ccccc1 10.1021/jm00086a017
155540415 172360 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 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 172360 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 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
44349348 16739 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
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 412 7 3 5 2.2 N#Cc1cccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
CHEMBL125316 16739 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
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 412 7 3 5 2.2 N#Cc1cccc(C(=O)NC(CCC(=O)O)C(=O)NN2CCC3(CCCC3)CC2)c1 10.1021/jm00079a003
45482490 196453 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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)c1cc2c(F)cccc2[nH]1 10.1016/j.bmc.2009.05.067
CHEMBL574715 196453 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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)c1cc2c(F)cccc2[nH]1 10.1016/j.bmc.2009.05.067
19766168 59230 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 367 4 3 3 2.5 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)O)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL171722 59230 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 367 4 3 3 2.5 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)O)C2=O)c1 10.1016/S0960-894X(00)80683-6
71452691 78204 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 671 12 5 7 3.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)C[S+]([O-])c1nc[nH]n1)c1ccccc1 10.1021/jm00092a007
CHEMBL2112336 78204 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 671 12 5 7 3.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)NC[C@@H](NC(=O)C[S+]([O-])c1nc[nH]n1)c1ccccc1 10.1021/jm00092a007
CHEMBL172635 207101 0 None - 0 Mouse 5.0 pIC50 = 5.0 Binding
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)OC(C)(C)C)C(=O)N1C[C@H](c2ccccc2)NC(=O)[C@@H]1CC(=O)O 10.1016/S0960-894X(01)80253-5
44280372 98915 0 None - 1 Mouse 5.0 pIC50 = 5.0 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 787 17 4 8 5.8 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
CHEMBL282645 98915 0 None - 1 Mouse 5.0 pIC50 = 5.0 Binding
Inhibitory activity against Cholecystokinin type A receptorInhibitory activity against Cholecystokinin type A receptor
ChEMBL 787 17 4 8 5.8 Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1 10.1016/S0960-894X(96)00248-X
136060577 87234 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 495 4 1 5 6.3 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccccc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
CHEMBL233647 87234 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 495 4 1 5 6.3 O=C1c2ccccc2C(=O)N1Cc1c(O)ccc2c(/C=C/c3ccccc3)cc3nc4ccccc4n3c12 10.1016/j.bmcl.2007.02.071
22883501 10307 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 552 6 2 6 5.0 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N3CCCCC3)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm960669+
CHEMBL116300 10307 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 552 6 2 6 5.0 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N3CCCCC3)c2)N=C(c2ccccn2)c2ccccc21 10.1021/jm960669+
54583297 61577 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
CHEMBL1774040 61577 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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(c4cc5ccccc5cc4C(=O)O)CC3)nc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2011.03.069
14208254 202791 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 403 4 2 4 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
CHEMBL72599 202791 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity against cholecystokinin type A receptor of rat pancreasBinding affinity against cholecystokinin type A receptor of rat pancreas
ChEMBL 403 4 2 4 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00047a021
14802520 115780 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 4.7 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)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
CHEMBL335914 115780 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 4.7 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)CCC(=O)O)Cc1ccccc1 10.1021/jm00105a062
14802520 119841 1 None - 1 Rat 6.0 pIC50 = 6.0 Binding
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 628 13 5 5 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
CHEMBL353157 119841 1 None - 1 Rat 6.0 pIC50 = 6.0 Binding
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 628 13 5 5 4.7 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80685-X
44368612 121469 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 612 13 5 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00057a005
CHEMBL359361 121469 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 612 13 5 4 4.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)C1C2CC3CC(C2)CC1C3)C(=O)N[C@H](CNC(=O)CCC(=O)O)Cc1ccccc1 10.1021/jm00057a005
23815458 167221 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 483 5 3 5 4.2 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
CHEMBL430516 167221 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 483 5 3 5 4.2 CC(C)(C)C(=O)CN1C(=O)[C@H](NC(=O)Nc2cccc(N)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm960669+
46235271 73286 2 None 2 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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 73286 2 None 2 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I-BDZ-1] from human CCK1R V3.36A mutant expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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
14208254 202791 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 2 4 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
CHEMBL72599 202791 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 2 4 3.4 COc1ccc(C(=O)NC2N=C(c3ccccc3F)c3ccccc3NC2=O)cc1 10.1021/jm00120a002
44210427 120242 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 459 4 2 4 4.7 CC(C)(C)OC(=O)CN1C(=O)C(NC(=O)Nc2cccc3ccccc23)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
CHEMBL355319 120242 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 459 4 2 4 4.7 CC(C)(C)OC(=O)CN1C(=O)C(NC(=O)Nc2cccc3ccccc23)CCc2ccccc21 10.1016/S0960-894X(00)80683-6
CHEMBL382051 210536 0 None -489 4 Human 7.0 pIC50 = 7.0 Binding
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
10555245 96030 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 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)N21 10.1021/jm000959x
CHEMBL262463 96030 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 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)N21 10.1021/jm000959x
44210426 58791 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 449 4 2 4 2.2 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)N3CCN(C)CC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
CHEMBL169807 58791 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 449 4 2 4 2.2 Cc1cccc(NC(=O)NC2CCc3ccccc3N(CC(=O)N3CCN(C)CC3)C2=O)c1 10.1016/S0960-894X(00)80683-6
44300863 196662 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 619 7 4 6 3.7 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(C)(=O)=O)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
CHEMBL57642 196662 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
Binding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreasBinding activity towards cholecystokinin-A (CCK-A) receptor in guinea pig pancreas
ChEMBL 619 7 4 6 3.7 Cc1ccc2c(c1)N(CC(=O)NC(C)(C)C)C(=O)[C@H](NC(=O)Nc1cccc(C(=O)NS(C)(=O)=O)c1)C[C@@H]2c1ccccc1 10.1016/0960-894X(95)00327-P
73349793 204720 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 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 10.1021/jm00092a007
CHEMBL88090 204720 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 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 10.1021/jm00092a007
44329442 205928 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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](c3ccccc3)C[C@@H](NC(=O)Nc3cccc(C)c3)C(=O)N2CC(=O)NC(C)(C)C)cc1 10.1016/S0960-894X(01)80832-5
CHEMBL95369 205928 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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](c3ccccc3)C[C@@H](NC(=O)Nc3cccc(C)c3)C(=O)N2CC(=O)NC(C)(C)C)cc1 10.1016/S0960-894X(01)80832-5
44334237 107533 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 556 10 3 5 4.4 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCC(NC(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
CHEMBL319466 107533 0 None - 0 Guinea pig 6.0 pIC50 = 6.0 Binding
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 556 10 3 5 4.4 Cc1cccc(NC(=O)N[C@H](CCC(=O)OCc2ccccc2)C(=O)N2CCC(NC(=O)c3ccccc3)CC2)c1 10.1016/0960-894X(95)00537-3
44370473 50574 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
CHEMBL157722 50574 0 None - 0 Guinea pig 5.0 pIC50 = 5.0 Binding
Inhibition of binding of [125I]- CCK-33 to guinea pig cortexInhibition of binding of [125I]- CCK-33 to guinea pig cortex
ChEMBL 435 15 3 4 4.3 CCCCCN(CCCCC)C(=O)[C@@H](CCC(=O)O)NC(=O)Nc1cccc(OC)c1 10.1021/jm00164a020
10673193 97679 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 506 6 2 5 5.3 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
CHEMBL273693 97679 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 506 6 2 5 5.3 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1021/jm970373j
10006792 44656 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 517 6 2 5 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 10.1016/0960-894X(95)00557-A
CHEMBL152306 44656 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 517 6 2 5 4.9 Cc1cccc(NC(=O)NC2N=C(c3ccccn3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 10.1016/0960-894X(95)00557-A
44387108 167680 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 650 9 3 5 4.7 COC(=O)[C@@]1(Cc2ccccc2)C[C@H]2[C@H](NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)C34CC5CC(CC(C5)C3)C4)CCCN2C1=O 10.1016/0960-894X(96)00160-6
CHEMBL433770 167680 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 650 9 3 5 4.7 COC(=O)[C@@]1(Cc2ccccc2)C[C@H]2[C@H](NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)C34CC5CC(CC(C5)C3)C4)CCCN2C1=O 10.1016/0960-894X(96)00160-6
136055865 119678 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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
CHEMBL351891 119678 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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
10673193 97679 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 506 6 2 5 5.3 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
CHEMBL273693 97679 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 506 6 2 5 5.3 CC(C)Oc1cccc(-n2c(CNC(=O)Nc3ccc(Br)cc3)nc3ccccc3c2=O)c1 10.1016/S0960-894X(97)00108-X
44572200 178753 0 None -14 2 Human 8.9 pKd = 8.9 Binding
Binding affinity to human CCK1 receptor expressed in CHO cell membrane by saturation binding assayBinding affinity to human CCK1 receptor expressed in CHO cell membrane by saturation binding assay
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
CHEMBL473612 178753 0 None -14 2 Human 8.9 pKd = 8.9 Binding
Binding affinity to human CCK1 receptor expressed in CHO cell membrane by saturation binding assayBinding affinity to human CCK1 receptor expressed in CHO cell membrane by saturation binding assay
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
CHEMBL475226 178753 0 None -14 2 Human 8.9 pKd = 8.9 Binding
Binding affinity to human CCK1 receptor expressed in CHO cell membrane by saturation binding assayBinding affinity to human CCK1 receptor expressed in CHO cell membrane by saturation binding assay
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
90663557 106202 0 None 6165 2 Rat 10.7 pKi = 10.7 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 1152 31 11 13 2.0 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](CCCCNC(=O)NC(=O)c1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL3143672 106202 0 None 6165 2 Rat 10.7 pKi = 10.7 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 1152 31 11 13 2.0 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](CCCCNC(=O)NC(=O)c1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
443375 205862 40 None -2 5 Human 10.6 pKi = 10.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm051219x
CHEMBL9506 205862 40 None -2 5 Human 10.6 pKi = 10.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm051219x
10819755 164879 0 None 52480 2 Rat 10.5 pKi = 10.5 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
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/jm970477u
CHEMBL423907 164879 0 None 52480 2 Rat 10.5 pKi = 10.5 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
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/jm970477u
9919500 203207 1 None 7413 2 Rat 10.5 pKi = 10.5 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
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/jm970477u
CHEMBL1161142 203207 1 None 7413 2 Rat 10.5 pKi = 10.5 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
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/jm970477u
CHEMBL76248 203207 1 None 7413 2 Rat 10.5 pKi = 10.5 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
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/jm970477u
9919500 203207 1 None 7413 2 Rat 10.5 pKi = 10.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
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/jm990252e
CHEMBL1161142 203207 1 None 7413 2 Rat 10.5 pKi = 10.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
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/jm990252e
CHEMBL76248 203207 1 None 7413 2 Rat 10.5 pKi = 10.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
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/jm990252e
90662930 106076 0 None 3981 2 Rat 10.3 pKi = 10.3 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 1073 29 11 11 2.6 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)NC(=O)c1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL3142366 106076 0 None 3981 2 Rat 10.3 pKi = 10.3 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 1073 29 11 11 2.6 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)NC(=O)c1ccccc1C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
44357046 27835 1 None 18 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 1012 28 9 13 0.7 CSCC[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](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
CHEMBL137280 27835 1 None 18 2 Rat 10.2 pKi = 10.2 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 1012 28 9 13 0.7 CSCC[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](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
4627 807 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL None None None None 10.1021/jm970477u
864 807 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL None None None None 10.1021/jm970477u
9833444 807 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL None None None None 10.1021/jm970477u
CHEMBL1121 807 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL None None None None 10.1021/jm970477u
DB09142 807 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL None None None None 10.1021/jm970477u
4627 807 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
864 807 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
9833444 807 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
CHEMBL1121 807 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
DB09142 807 44 None -1 5 Rat 10.1 pKi = 10.1 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
108187 911 30 None 4 5 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
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/jm990967h
873 911 30 None 4 5 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
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/jm990967h
CHEMBL2062154 911 30 None 4 5 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
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/jm990967h
CHEMBL287735 911 30 None 4 5 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
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/jm990967h
5311201 205653 30 None 26 6 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm990967h
CHEMBL9387 205653 30 None 26 6 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm990967h
443375 205862 40 None -3 5 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against 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 10.1021/jm990967h
CHEMBL9506 205862 40 None -3 5 Rat 9.8 pKi = 9.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against 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 10.1021/jm990967h
11804040 118930 0 None 2137 2 Rat 9.7 pKi = 9.7 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
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@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
CHEMBL345049 118930 0 None 2137 2 Rat 9.7 pKi = 9.7 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
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@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
CHEMBL384035 210559 1 None -8 4 Guinea pig 9.6 pKi = 9.6 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
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/jm00122a026
CHEMBL428666 210559 1 None -8 4 Guinea pig 9.6 pKi = 9.6 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
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/jm00122a026
10581797 62899 0 None 9120 2 Rat 9.6 pKi = 9.6 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 976 26 9 11 1.3 CC[C@H](C)[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](C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/jm970477u
CHEMBL1791002 62899 0 None 9120 2 Rat 9.6 pKi = 9.6 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 976 26 9 11 1.3 CC[C@H](C)[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](C(=O)N(C)[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/jm970477u
4627 807 44 None -2 5 Human 9.6 pKi = 9.6 Binding
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
864 807 44 None -2 5 Human 9.6 pKi = 9.6 Binding
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 807 44 None -2 5 Human 9.6 pKi = 9.6 Binding
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 807 44 None -2 5 Human 9.6 pKi = 9.6 Binding
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 807 44 None -2 5 Human 9.6 pKi = 9.6 Binding
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 807 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm9603072
864 807 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm9603072
9833444 807 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm9603072
CHEMBL1121 807 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm9603072
DB09142 807 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm9603072
4627 807 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brain
ChEMBL None None None None 10.1021/jm00122a026
864 807 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brain
ChEMBL None None None None 10.1021/jm00122a026
9833444 807 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brain
ChEMBL None None None None 10.1021/jm00122a026
CHEMBL1121 807 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brain
ChEMBL None None None None 10.1021/jm00122a026
DB09142 807 44 None -1 5 Guinea pig 9.6 pKi = 9.6 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brain
ChEMBL None None None None 10.1021/jm00122a026
121964 205 28 None 831 2 Rat 9.5 pKi = 9.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
858 205 28 None 831 2 Rat 9.5 pKi = 9.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
CHEMBL323521 205 28 None 831 2 Rat 9.5 pKi = 9.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None None 10.1021/jm990252e
14208194 162872 2 None 1122 2 Rat 9.5 pKi = 9.5 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific 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 10.1021/jm9703247
CHEMBL419764 162872 2 None 1122 2 Rat 9.5 pKi = 9.5 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific 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 10.1021/jm9703247
CHEMBL384035 210559 1 None -8 4 Guinea pig 9.5 pKi = 9.5 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
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 10.1016/j.bmcl.2003.11.001
CHEMBL428666 210559 1 None -8 4 Guinea pig 9.5 pKi = 9.5 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
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 10.1016/j.bmcl.2003.11.001
53465844 69053 0 None 131 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-BH-JMV-179 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [125I]-BH-JMV-179 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69053 0 None 131 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-BH-JMV-179 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [125I]-BH-JMV-179 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
4627 807 44 None -1 5 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm9703247
864 807 44 None -1 5 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm9703247
9833444 807 44 None -1 5 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm9703247
CHEMBL1121 807 44 None -1 5 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm9703247
DB09142 807 44 None -1 5 Rat 9.3 pKi = 9.3 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas
ChEMBL None None None None 10.1021/jm9703247
10701167 62900 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 990 27 8 11 1.8 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](C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/jm970477u
CHEMBL1791005 62900 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 990 27 8 11 1.8 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](C(=O)N(C)[C@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O)[C@@H](C)CC 10.1021/jm970477u
CHEMBL2115177 207506 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None 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)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
4627 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
864 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
9833444 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
CHEMBL1121 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
DB09142 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
10507071 113098 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific 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/jm9703247
CHEMBL332261 113098 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific 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/jm9703247
4627 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm00126a007
864 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm00126a007
9833444 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm00126a007
CHEMBL1121 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm00126a007
DB09142 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm00126a007
4627 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None None 10.1016/S0960-894X(00)80678-2
864 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None None 10.1016/S0960-894X(00)80678-2
9833444 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None None 10.1016/S0960-894X(00)80678-2
CHEMBL1121 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None None 10.1016/S0960-894X(00)80678-2
DB09142 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None None 10.1016/S0960-894X(00)80678-2
4627 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00122a026
864 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00122a026
9833444 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00122a026
CHEMBL1121 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00122a026
DB09142 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00122a026
4627 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Compound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranesCompound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm0000416
864 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Compound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranesCompound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm0000416
9833444 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Compound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranesCompound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm0000416
CHEMBL1121 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Compound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranesCompound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm0000416
DB09142 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Compound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranesCompound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranes
ChEMBL None None None None 10.1021/jm0000416
4627 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00053a022
864 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00053a022
9833444 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00053a022
CHEMBL1121 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00053a022
DB09142 807 44 None -1 5 Guinea pig 9.2 pKi = 9.2 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None None 10.1021/jm00053a022
443375 205862 40 None -3 5 Rat 9.2 pKi = 9.2 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00084a009
CHEMBL9506 205862 40 None -3 5 Rat 9.2 pKi = 9.2 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1021/jm00084a009
5311400 3229 1 None -2 3 Guinea pig 9.1 pKi = 9.1 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
900 3229 1 None -2 3 Guinea pig 9.1 pKi = 9.1 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
CHEMBL262197 3229 1 None -2 3 Guinea pig 9.1 pKi = 9.1 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL None None None None 10.1016/j.bmcl.2003.11.001
CHEMBL384035 210559 1 None -8 4 Guinea pig 9.0 pKi = 9.0 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
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/jm00126a007
CHEMBL428666 210559 1 None -8 4 Guinea pig 9.0 pKi = 9.0 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
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/jm00126a007
CHEMBL384035 210559 1 None -8 4 Guinea pig 9.0 pKi = 9.0 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
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/jm00122a026
CHEMBL428666 210559 1 None -8 4 Guinea pig 9.0 pKi = 9.0 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
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/jm00122a026
44357045 26355 0 None 85 2 Rat 9.0 pKi = 9.0 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 1012 28 9 13 0.7 CSCC[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](CCSC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
CHEMBL136096 26355 0 None 85 2 Rat 9.0 pKi = 9.0 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 1012 28 9 13 0.7 CSCC[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](CCSC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
CHEMBL2369815 207938 0 None 85 2 Rat 9.0 pKi = 9.0 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None CSCC[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](CCSC)C(=O)N[C@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
10557073 16181 0 None 3467 2 Guinea pig 8.9 pKi = 8.9 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 763 20 7 8 2.3 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)CCNC(=O)OC(C)(C)C 10.1021/jm0000416
CHEMBL122934 16181 0 None 3467 2 Guinea pig 8.9 pKi = 8.9 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 763 20 7 8 2.3 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)CCNC(=O)OC(C)(C)C 10.1021/jm0000416
10004216 4660 0 None -11 2 Rat 8.8 pKi = 8.8 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1016/0960-894X(95)00528-2
CHEMBL103750 4660 0 None -11 2 Rat 8.8 pKi = 8.8 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1016/0960-894X(95)00528-2
CHEMBL1172429 206835 0 None 26 4 Human 8.8 pKi = 8.8 Binding
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
44359425 14560 0 None - 1 Guinea pig 8.8 pKi = 8.8 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)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/jm00122a026
CHEMBL1206331 14560 0 None - 1 Guinea pig 8.8 pKi = 8.8 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)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/jm00122a026
CHEMBL262687 14560 0 None - 1 Guinea pig 8.8 pKi = 8.8 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)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/jm00122a026
443375 205862 40 None -2 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/j.bmcl.2007.09.093
CHEMBL9506 205862 40 None -2 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 408 3 2 3 3.7 CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 10.1016/j.bmcl.2007.09.093
44328894 108124 0 None -25 2 Human 8.0 pKi = 8 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)
ChEMBL 587 5 2 4 4.8 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CC(=O)N2CC3CCC(CC3)C2)c2ccccc2N(c2ccccc2F)C1=O 10.1016/S0960-894X(96)00613-0
CHEMBL320624 108124 0 None -25 2 Human 8.0 pKi = 8 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)
ChEMBL 587 5 2 4 4.8 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CC(=O)N2CC3CCC(CC3)C2)c2ccccc2N(c2ccccc2F)C1=O 10.1016/S0960-894X(96)00613-0
3476 1368 8 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm200438b
59751 1368 8 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm200438b
878 1368 8 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm200438b
CHEMBL39263 1368 8 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 408 3 2 3 3.7 O=C(c1cc2c([nH]1)cccc2)NC1N=C(c2ccccc2)c2c(N(C1=O)C)cccc2 10.1021/jm200438b
10840582 167405 0 None 257 2 Rat 8.0 pKi = 8.0 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific 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/jm9703247
CHEMBL431858 167405 0 None 257 2 Rat 8.0 pKi = 8.0 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific 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/jm9703247
45486933 195251 0 None 3 2 Human 7.0 pKi = 7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 520 7 2 6 5.3 CC(CNC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.09.064
CHEMBL566360 195251 0 None 3 2 Human 7.0 pKi = 7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 520 7 2 6 5.3 CC(CNC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.09.064
45487006 197224 0 None -10 2 Human 7.0 pKi = 7 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 666 8 3 6 5.0 O=C(N[C@@H](Cc1ccc(Cl)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
CHEMBL584525 197224 0 None -10 2 Human 7.0 pKi = 7 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 666 8 3 6 5.0 O=C(N[C@@H](Cc1ccc(Cl)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
10767708 14362 0 None -138 2 Rat 7.0 pKi = 7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 500 6 2 3 5.6 O=C(Nc1ccccc1)NC1C(=O)N(CCC2CCCC2)c2ccccc2N(c2ccccc2F)C1=O 10.1021/jm990967h
CHEMBL120296 14362 0 None -138 2 Rat 7.0 pKi = 7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 500 6 2 3 5.6 O=C(Nc1ccccc1)NC1C(=O)N(CCC2CCCC2)c2ccccc2N(c2ccccc2F)C1=O 10.1021/jm990967h
45486994 196037 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 506 7 2 6 4.8 O=C(NCCc1ccc(Cl)cc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL571457 196037 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 506 7 2 6 4.8 O=C(NCCc1ccc(Cl)cc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
44408411 160751 0 None -2089 4 Human 6.0 pKi = 6 Binding
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 160751 0 None -2089 4 Human 6.0 pKi = 6 Binding
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
118719285 114971 0 None -25 3 Guinea pig 6.0 pKi = 6 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL 733 15 5 7 4.7 CN(C)[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C)c1ccccc1 10.1021/jm00053a022
CHEMBL3351057 114971 0 None -25 3 Guinea pig 6.0 pKi = 6 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL 733 15 5 7 4.7 CN(C)[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C)c1ccccc1 10.1021/jm00053a022
44265924 205639 0 None - 1 Rat 6.0 pKi = 6 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 363 5 1 1 5.7 O=C(NCC=C(c1ccccc1)c1ccccc1)c1cccc2ccccc12 10.1021/jm00084a009
CHEMBL9379 205639 0 None - 1 Rat 6.0 pKi = 6 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 363 5 1 1 5.7 O=C(NCC=C(c1ccccc1)c1ccccc1)c1cccc2ccccc12 10.1021/jm00084a009
10440219 168122 0 None -25 2 Guinea pig 6.0 pKi = 6 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL 776 15 6 7 4.4 CN(C)C(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)c1ccccc1 10.1016/S0960-894X(00)80678-2
CHEMBL436722 168122 0 None -25 2 Guinea pig 6.0 pKi = 6 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL 776 15 6 7 4.4 CN(C)C(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)c1ccccc1 10.1016/S0960-894X(00)80678-2
11527738 75621 0 None -10964 4 Human 5.0 pKi = 5 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 518 7 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL205455 75621 0 None -10964 4 Human 5.0 pKi = 5 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 518 7 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL411201 211115 0 None -4786 4 Human 5.0 pKi = 5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determinedBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determined
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)[C@H](CCC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm0303103
44408484 136970 0 None -19498 4 Human 5.0 pKi = 5 Binding
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 136970 0 None -19498 4 Human 5.0 pKi = 5 Binding
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 156328 0 None -19952 4 Human 5.0 pKi = 5 Binding
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 156328 0 None -19952 4 Human 5.0 pKi = 5 Binding
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
9844256 11677 0 None -3 2 Guinea pig 5.0 pKi = 5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 406 7 3 2 4.6 O=C(O)CCNC(=O)c1cc(-c2ccccc2)[nH]c1CC12CC3CC(CC(C3)C1)C2 10.1021/jm049069y
CHEMBL1181869 11677 0 None -3 2 Guinea pig 5.0 pKi = 5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 406 7 3 2 4.6 O=C(O)CCNC(=O)c1cc(-c2ccccc2)[nH]c1CC12CC3CC(CC(C3)C1)C2 10.1021/jm049069y
CHEMBL2067947 11677 0 None -3 2 Guinea pig 5.0 pKi = 5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 406 7 3 2 4.6 O=C(O)CCNC(=O)c1cc(-c2ccccc2)[nH]c1CC12CC3CC(CC(C3)C1)C2 10.1021/jm049069y
44403980 11685 0 None -398 2 Guinea pig 5.0 pKi = 5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 5.2 CN(C(=O)c1cc2[nH]cnc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2)[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1181938 11685 0 None -398 2 Guinea pig 5.0 pKi = 5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 5.2 CN(C(=O)c1cc2[nH]cnc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2)[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067951 11685 0 None -398 2 Guinea pig 5.0 pKi = 5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 5.2 CN(C(=O)c1cc2[nH]cnc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2)[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
10771043 25933 0 None -61 2 Guinea pig 6.0 pKi = 6.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 707 10 4 4 6.9 O=C(O)c1cccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm00021a019
CHEMBL135658 25933 0 None -61 2 Guinea pig 6.0 pKi = 6.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 707 10 4 4 6.9 O=C(O)c1cccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm00021a019
44212464 63792 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 527 8 2 5 3.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808399 63792 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 527 8 2 5 3.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(Cl)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
56673524 63809 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808418 63809 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
10438352 9691 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of 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 10.1021/jm9703247
CHEMBL113699 9691 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of 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 10.1021/jm9703247
10054705 107928 0 None -28 2 Guinea pig 6.0 pKi = 6.0 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 625 10 3 4 6.5 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1Cl)CC(=O)O 10.1021/jm00072a005
CHEMBL319880 107928 0 None -28 2 Guinea pig 6.0 pKi = 6.0 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 625 10 3 4 6.5 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1Cl)CC(=O)O 10.1021/jm00072a005
44357069 155140 0 None -147 2 Guinea pig 5.0 pKi = 5.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 675 9 5 5 5.4 C[C@@H](NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL405062 155140 0 None -147 2 Guinea pig 5.0 pKi = 5.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 675 9 5 5 5.4 C[C@@H](NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm00021a019
10077166 99459 0 None -75 2 Guinea pig 6.0 pKi = 6.0 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 591 10 3 4 5.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1016/s0960-894x(98)00231-5
CHEMBL286247 99459 0 None -75 2 Guinea pig 6.0 pKi = 6.0 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 591 10 3 4 5.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1016/s0960-894x(98)00231-5
44280157 155176 0 None -75 2 Guinea pig 6.0 pKi = 6.0 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 667 8 3 5 6.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N1CC[C@H](Oc2ccc(Cl)cc2Cl)C[C@H]1C(=O)O 10.1016/s0960-894x(98)00231-5
CHEMBL405468 155176 0 None -75 2 Guinea pig 6.0 pKi = 6.0 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 667 8 3 5 6.9 C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N1CC[C@H](Oc2ccc(Cl)cc2Cl)C[C@H]1C(=O)O 10.1016/s0960-894x(98)00231-5
10257865 206686 3 None -173 5 Guinea pig 6.0 pKi = 6.0 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
CHEMBL99939 206686 3 None -173 5 Guinea pig 6.0 pKi = 6.0 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
56683505 63795 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 571 8 2 5 3.7 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(Br)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808402 63795 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 571 8 2 5 3.7 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(Br)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL430298 211860 0 None -2137 4 Human 6.0 pKi = 6.0 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determinedBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determined
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/jm0303103
44331483 106999 0 None -25 2 Rat 6.0 pKi = 6.0 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 541 5 1 4 6.1 O=C(NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(C2CCCCC2)C1=O)Oc1ccccc1 10.1016/S0960-894X(96)00544-6
CHEMBL318569 106999 0 None -25 2 Rat 6.0 pKi = 6.0 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 541 5 1 4 6.1 O=C(NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(C2CCCCC2)C1=O)Oc1ccccc1 10.1016/S0960-894X(96)00544-6
10840039 113281 0 None -16 2 Rat 7.9 pKi = 7.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 6 2 4 6.2 CSc1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
CHEMBL332403 113281 0 None -16 2 Rat 7.9 pKi = 7.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 6 2 4 6.2 CSc1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
CHEMBL218327 207639 0 None -2630 4 Human 6.0 pKi = 6.0 Binding
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
CHEMBL1207511 206857 0 None -2398 2 Guinea pig 6.0 pKi = 6.0 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=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 10.1016/S0960-894X(00)80678-2
CHEMBL412917 206857 0 None -2398 2 Guinea pig 6.0 pKi = 6.0 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=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 10.1016/S0960-894X(00)80678-2
CHEMBL353862 209971 0 None -77 3 Guinea pig 6.0 pKi = 6.0 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None CC(C)(C)OC(=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](Cc1cccc2ccccc12)C(N)=O)c1ccccc1 10.1016/S0960-894X(00)80678-2
CHEMBL3350335 209718 0 None -245 2 Guinea pig 5.0 pKi = 5.0 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
10626579 15321 0 None -38 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 554 6 2 4 6.2 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2cccc(OC(F)(F)F)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL121703 15321 0 None -38 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 554 6 2 4 6.2 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2cccc(OC(F)(F)F)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
10552321 163347 0 None -165 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 470 5 2 3 5.3 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL420728 163347 0 None -165 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 470 5 2 3 5.3 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
11698512 167681 0 None -21 3 Guinea pig 6.0 pKi = 6.0 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 435 8 3 3 5.5 CCCc1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL433776 167681 0 None -21 3 Guinea pig 6.0 pKi = 6.0 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 435 8 3 3 5.5 CCCc1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
3503 1854 8 None -1174 2 Rat 6.0 pKi = 6.0 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 534 5 2 3 6.1 O=C(N[C@H]1C(=O)N(c2ccccc2)c2c(N(C1=O)CC13CC4CC(C3)CC(C1)C4)cccc2)Nc1ccccc1 10.1016/S0960-894X(96)00544-6
5311147 1854 8 None -1174 2 Rat 6.0 pKi = 6.0 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 534 5 2 3 6.1 O=C(N[C@H]1C(=O)N(c2ccccc2)c2c(N(C1=O)CC13CC4CC(C3)CC(C1)C4)cccc2)Nc1ccccc1 10.1016/S0960-894X(96)00544-6
CHEMBL329305 1854 8 None -1174 2 Rat 6.0 pKi = 6.0 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 534 5 2 3 6.1 O=C(N[C@H]1C(=O)N(c2ccccc2)c2c(N(C1=O)CC13CC4CC(C3)CC(C1)C4)cccc2)Nc1ccccc1 10.1016/S0960-894X(96)00544-6
44346296 113986 0 None -1174 2 Rat 6.0 pKi = 6.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 562 6 2 4 5.9 O=Cc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL333517 113986 0 None -1174 2 Rat 6.0 pKi = 6.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 562 6 2 4 5.9 O=Cc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
11527738 75621 0 None -10964 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 518 7 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm051219x
CHEMBL205455 75621 0 None -10964 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 518 7 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm051219x
10257865 206686 3 None -173 5 Guinea pig 6.0 pKi = 6.0 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
CHEMBL99939 206686 3 None -173 5 Guinea pig 6.0 pKi = 6.0 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
10576324 113452 0 None -54 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 470 6 2 3 5.3 CC(C)CC(C)N1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL332595 113452 0 None -54 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 470 6 2 3 5.3 CC(C)CC(C)N1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
135529065 156461 0 None -275 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 588 7 2 7 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)C(=O)N(C2CCCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL407340 156461 0 None -275 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 588 7 2 7 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)C(=O)N(C2CCCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
11511721 75734 0 None -194 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 502 7 2 5 5.5 CNc1cccc(NC(=O)C[C@@H]2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm051219x
CHEMBL205751 75734 0 None -194 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 502 7 2 5 5.5 CNc1cccc(NC(=O)C[C@@H]2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm051219x
10618720 192886 0 None -4 2 Guinea pig 4.9 pKi = 4.9 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 363 4 2 2 4.5 O=C(O)c1cc2ccccc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm9508907
CHEMBL52740 192886 0 None -4 2 Guinea pig 4.9 pKi = 4.9 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 363 4 2 2 4.5 O=C(O)c1cc2ccccc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm9508907
CHEMBL64605 214069 6 None -1288 3 Guinea pig 4.9 pKi = 4.9 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
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/jm0000416
11635377 197121 0 None 39 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 554 7 2 6 6.0 CC(CNC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.09.064
CHEMBL583457 197121 0 None 39 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 554 7 2 6 6.0 CC(CNC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2009.09.064
44346047 112890 0 None -537 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 568 7 2 7 6.4 O=C(Nc1cccc(C2N=NN=N2)c1)NC1C(=O)N(CCC2CCCC2)c2ccccc2N(c2ccccc2F)C1=O 10.1021/jm990967h
CHEMBL331872 112890 0 None -537 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 568 7 2 7 6.4 O=C(Nc1cccc(C2N=NN=N2)c1)NC1C(=O)N(CCC2CCCC2)c2ccccc2N(c2ccccc2F)C1=O 10.1021/jm990967h
CHEMBL3351051 209779 0 None -17 2 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cccc2ccccc12)NC)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
CHEMBL3351053 209781 0 None -426 2 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
44356886 28200 0 None -42 2 Guinea pig 5.9 pKi = 5.9 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 757 11 5 5 7.3 O=C(O)c1cc(NC(=O)[C@@H](CC2CCCCC2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL137525 28200 0 None -42 2 Guinea pig 5.9 pKi = 5.9 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 757 11 5 5 7.3 O=C(O)c1cc(NC(=O)[C@@H](CC2CCCCC2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
10747345 116464 0 None -6 2 Guinea pig 5.9 pKi = 5.9 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 707 10 4 4 6.9 O=C(O)c1ccccc1NC(=O)[C@H](Cc1ccccc1)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
CHEMBL338728 116464 0 None -6 2 Guinea pig 5.9 pKi = 5.9 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 707 10 4 4 6.9 O=C(O)c1ccccc1NC(=O)[C@H](Cc1ccccc1)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
44329798 107050 0 None -100 5 Rat 5.9 pKi = 5.9 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 610 10 2 4 6.5 CC(Cc1c[nH]c2ccccc12)(C(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1Cl)CC(=O)O 10.1021/jm00072a005
CHEMBL318852 107050 0 None -100 5 Rat 5.9 pKi = 5.9 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 610 10 2 4 6.5 CC(Cc1c[nH]c2ccccc12)(C(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1Cl)CC(=O)O 10.1021/jm00072a005
11497371 70271 0 None -40 3 Guinea pig 6.9 pKi = 6.9 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 525 7 3 3 7.4 Cc1cc(C)c(-c2nc(C(=O)Nc3ccc(C)c(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
CHEMBL195007 70271 0 None -40 3 Guinea pig 6.9 pKi = 6.9 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 525 7 3 3 7.4 Cc1cc(C)c(-c2nc(C(=O)Nc3ccc(C)c(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
10552320 116943 0 None -109 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 470 6 2 3 5.2 CC(C)C(C)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL339879 116943 0 None -109 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 470 6 2 3 5.2 CC(C)C(C)CN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
10257865 206686 3 None -204 5 Rat 5.9 pKi = 5.9 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
CHEMBL99939 206686 3 None -204 5 Rat 5.9 pKi = 5.9 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
9960432 39172 6 None -12 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 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 10.1016/j.bmc.2007.12.047
CHEMBL147186 39172 6 None -12 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 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 10.1016/j.bmc.2007.12.047
11571140 71342 0 None -23 3 Guinea pig 6.9 pKi = 6.9 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 489 7 3 3 6.9 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CCCCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL196517 71342 0 None -23 3 Guinea pig 6.9 pKi = 6.9 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 489 7 3 3 6.9 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CCCCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
45487002 195902 0 None -10 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 672 8 3 7 5.1 O=C(N[C@@H](Cc1ccc(Cl)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
CHEMBL570520 195902 0 None -10 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 672 8 3 7 5.1 O=C(N[C@@H](Cc1ccc(Cl)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
9958214 114282 0 None -269 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 517 7 2 4 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
CHEMBL333979 114282 0 None -269 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 517 7 2 4 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
44272156 140998 0 None -45 2 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1194 24 13 13 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL384731 140998 0 None -45 2 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1194 24 13 13 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
44444933 94217 0 None - 1 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 455 6 3 3 5.8 O=C(O)c1cccc(NC(=O)c2nc(-c3ccccc3)[nH]c2CC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm070880t
CHEMBL252559 94217 0 None - 1 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 455 6 3 3 5.8 O=C(O)c1cccc(NC(=O)c2nc(-c3ccccc3)[nH]c2CC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm070880t
9853208 101241 0 None -1071 2 Guinea pig 5.9 pKi = 5.9 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 710 11 6 9 4.5 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2[nH]ccc2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(-c2nn[nH]n2)cc(-c2nn[nH]n2)c1 10.1021/jm9508907
CHEMBL299540 101241 0 None -1071 2 Guinea pig 5.9 pKi = 5.9 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 710 11 6 9 4.5 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2[nH]ccc2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(-c2nn[nH]n2)cc(-c2nn[nH]n2)c1 10.1021/jm9508907
44346825 114262 0 None -77 2 Guinea pig 4.9 pKi = 4.9 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 623 8 3 4 4.7 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3)C(=O)O 10.1021/jm00048a001
CHEMBL333920 114262 0 None -77 2 Guinea pig 4.9 pKi = 4.9 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 623 8 3 4 4.7 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3)C(=O)O 10.1021/jm00048a001
3960 2303 20 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in 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/jm950423p
891 2303 20 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in 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/jm950423p
CHEMBL24938 2303 20 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in 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/jm950423p
16100406 82797 0 None -33 4 Human 6.9 pKi = 6.9 Binding
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 82797 0 None -33 4 Human 6.9 pKi = 6.9 Binding
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
11612498 133026 0 None -5 3 Guinea pig 5.9 pKi = 5.9 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 469 7 3 3 6.2 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccccc3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL371068 133026 0 None -5 3 Guinea pig 5.9 pKi = 5.9 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 469 7 3 3 6.2 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccccc3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
9808153 112164 0 None -36 2 Guinea pig 5.9 pKi = 5.9 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 571 11 3 4 5.6 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCC(=O)O)CCc1ccccc1 10.1021/jm00072a005
CHEMBL330390 112164 0 None -36 2 Guinea pig 5.9 pKi = 5.9 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 571 11 3 4 5.6 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCC(=O)O)CCc1ccccc1 10.1021/jm00072a005
10676550 118844 0 None -12 2 Guinea pig 5.9 pKi = 5.9 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1ccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc1C(=O)O 10.1021/jm00021a019
CHEMBL344396 118844 0 None -12 2 Guinea pig 5.9 pKi = 5.9 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1ccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc1C(=O)O 10.1021/jm00021a019
10257865 206686 3 None -204 5 Rat 5.9 pKi = 5.9 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
CHEMBL99939 206686 3 None -204 5 Rat 5.9 pKi = 5.9 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 591 10 3 4 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1)CC(=O)O 10.1021/jm00072a005
44271859 140981 0 None -4 2 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1292 39 14 16 2.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)CC[C@@H](NC(=O)OC(C)(C)C)C(=O)O)C(=O)N[C@@H](CCCCN)C(=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/jm00126a007
CHEMBL384618 140981 0 None -4 2 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1292 39 14 16 2.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)CC[C@@H](NC(=O)OC(C)(C)C)C(=O)O)C(=O)N[C@@H](CCCCN)C(=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/jm00126a007
CHEMBL1172251 206831 0 None -229 4 Human 5.9 pKi = 5.9 Binding
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](Cc1ccccc1)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
CHEMBL3351058 209784 0 None -83 2 Guinea pig 5.9 pKi = 5.9 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CC(C)(C)OC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12)C1CCCCC1 10.1021/jm00053a022
44265978 205757 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 365 6 2 2 5.3 O=C(NCCN(c1ccccc1)c1ccccc1)Nc1ccc(Cl)cc1 10.1021/jm00084a009
CHEMBL9444 205757 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 365 6 2 2 5.3 O=C(NCCN(c1ccccc1)c1ccccc1)Nc1ccc(Cl)cc1 10.1021/jm00084a009
CHEMBL2370437 208095 0 None -10 2 Guinea pig 4.9 pKi = 4.9 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00174a016
10745516 14227 0 None -60 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 563 5 2 4 5.8 CN(C)c1cccc(NC(=O)NC2C(=O)N(c3ccccc3)c3ccccc3N(C3[C@H]4C[C@@H]5C[C@@H](C[C@H]3C5)C4)C2=O)c1 10.1021/jm990967h
CHEMBL120015 14227 0 None -60 2 Rat 6.9 pKi = 6.9 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 563 5 2 4 5.8 CN(C)c1cccc(NC(=O)NC2C(=O)N(c3ccccc3)c3ccccc3N(C3[C@H]4C[C@@H]5C[C@@H](C[C@H]3C5)C4)C2=O)c1 10.1021/jm990967h
56673524 63809 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808418 63809 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
44331467 106954 0 None -41 2 Rat 5.9 pKi = 5.9 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 529 7 1 4 5.8 CC(C)CCN1C(=O)C(NC(=O)Oc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL318291 106954 0 None -41 2 Rat 5.9 pKi = 5.9 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 529 7 1 4 5.8 CC(C)CCN1C(=O)C(NC(=O)Oc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
44357057 118702 0 None -446 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 769 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccccc2F)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL343367 118702 0 None -446 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 769 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccccc2F)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
10794262 168052 0 None -6 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 645 10 4 4 4.8 O=C(O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
CHEMBL436175 168052 0 None -6 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 645 10 4 4 4.8 O=C(O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
11539356 71321 0 None -69 3 Guinea pig 5.8 pKi = 5.8 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 435 7 3 3 5.6 CC(C)c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL196441 71321 0 None -69 3 Guinea pig 5.8 pKi = 5.8 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 435 7 3 3 5.6 CC(C)c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
56683506 63796 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 511 8 2 5 3.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(F)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808403 63796 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 511 8 2 5 3.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(F)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
19700629 63794 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 561 8 2 5 4.0 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(C(F)(F)F)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808401 63794 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 561 8 2 5 4.0 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(C(F)(F)F)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
10770670 92047 0 None -301 2 Guinea pig 5.8 pKi = 5.8 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 663 11 6 6 4.9 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL2067959 92047 0 None -301 2 Guinea pig 5.8 pKi = 5.8 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 663 11 6 6 4.9 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL24313 92047 0 None -301 2 Guinea pig 5.8 pKi = 5.8 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 663 11 6 6 4.9 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
9850043 112362 1 None -446 3 Rat 5.8 pKi = 5.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL330977 112362 1 None -446 3 Rat 5.8 pKi = 5.8 Binding
Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranesInhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
44346826 113302 0 None -69 2 Guinea pig 4.8 pKi = 4.8 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 595 7 3 4 3.9 O=C(O)CNC(=O)[C@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
CHEMBL332510 113302 0 None -69 2 Guinea pig 4.8 pKi = 4.8 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 595 7 3 4 3.9 O=C(O)CNC(=O)[C@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
CHEMBL334114 209638 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
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)[C@@H](C)N 10.1021/jm0000416
CHEMBL2372623 208522 0 None -16 4 Human 7.8 pKi = 7.8 Binding
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
CHEMBL2370598 208123 0 None -12 2 Guinea pig 5.8 pKi = 5.8 Binding
Displacement of 0.1 nM [3H]Boc[Nle28,31]-CCK27-33 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]Boc[Nle28,31]-CCK27-33 from guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)C[C@@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
44385472 81700 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL 1246 26 13 15 2.2 CCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCCCNC(=O)CC(NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](CN)Cc1ccccc1 10.1021/jm00389a002
CHEMBL216677 81700 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL 1246 26 13 15 2.2 CCCC[C@H](NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCCCNC(=O)CC(NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](CN)Cc1ccccc1 10.1021/jm00389a002
19700643 63673 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 505 9 2 4 4.5 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1807152 63673 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 505 9 2 4 4.5 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
11712880 138381 0 None -114 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell line
ChEMBL 490 6 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm051219x
CHEMBL378388 138381 0 None -114 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell line
ChEMBL 490 6 2 5 5.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm051219x
10769748 112495 0 None -1148 2 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 591 6 3 4 6.1 CC(=O)Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL331119 112495 0 None -1148 2 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 591 6 3 4 6.1 CC(=O)Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
10482868 106907 0 None -107 5 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 557 10 3 4 5.2 CC(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 10.1021/jm00072a005
CHEMBL317999 106907 0 None -107 5 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 557 10 3 4 5.2 CC(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 10.1021/jm00072a005
10460621 106681 0 None -8 2 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 567 8 3 3 6.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Cl)c(Cl)c1 10.1021/jm00072a005
CHEMBL316462 106681 0 None -8 2 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 567 8 3 3 6.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Cl)c(Cl)c1 10.1021/jm00072a005
44451877 95522 0 None -162 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 587 7 1 6 6.9 Cc1nc(-c2cccc(NC(=O)CN3C(=O)N(CC(=O)C(C)(C)C)c4ccccc4N(C4CCCCC4)C3=O)c2)cs1 10.1016/j.bmc.2007.12.047
CHEMBL259557 95522 0 None -162 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 587 7 1 6 6.9 Cc1nc(-c2cccc(NC(=O)CN3C(=O)N(CC(=O)C(C)(C)C)c4ccccc4N(C4CCCCC4)C3=O)c2)cs1 10.1016/j.bmc.2007.12.047
10722460 15008 0 None -309 2 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 612 5 2 3 6.9 O=C(Nc1cccc(Br)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL121028 15008 0 None -309 2 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 612 5 2 3 6.9 O=C(Nc1cccc(Br)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL440259 212104 0 None -4 2 Guinea pig 5.8 pKi = 5.8 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None 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](CCC(=O)O)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/jm00126a007
44318341 204271 0 None -501 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assayBinding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assay
ChEMBL 698 10 5 5 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N)c(I)c1 10.1016/0960-894X(95)00435-V
CHEMBL1628582 204271 0 None -501 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assayBinding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assay
ChEMBL 698 10 5 5 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N)c(I)c1 10.1016/0960-894X(95)00435-V
CHEMBL84864 204271 0 None -501 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assayBinding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assay
ChEMBL 698 10 5 5 5.4 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N)c(I)c1 10.1016/0960-894X(95)00435-V
10698109 106799 0 None 5 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
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 106799 0 None 5 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
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
45486967 195737 0 None 39 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 472 7 2 6 4.1 O=C(NCCc1ccccc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL569616 195737 0 None 39 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 472 7 2 6 4.1 O=C(NCCc1ccccc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
45102806 195078 0 None -15 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 646 8 3 7 5.1 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1cc(Cl)c(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
CHEMBL565324 195078 0 None -15 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 646 8 3 7 5.1 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1cc(Cl)c(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
45486936 195286 0 None -25 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 640 8 3 6 5.1 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1cc(Cl)c(Cl)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
CHEMBL566574 195286 0 None -25 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 640 8 3 6 5.1 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1cc(Cl)c(Cl)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
11700410 197067 0 None -31 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 704 8 3 7 4.4 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(I)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
CHEMBL583035 197067 0 None -31 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 704 8 3 7 4.4 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(I)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
9872866 63807 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 571 7 2 5 4.1 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808416 63807 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 571 7 2 5 4.1 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
44212230 4180 0 None -208 2 Rat 5.8 pKi = 5.8 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 572 8 1 5 5.9 CC(C)CCN1C(=O)C(NC(=O)Oc2cccc(N(C)C)c2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL100509 4180 0 None -208 2 Rat 5.8 pKi = 5.8 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 572 8 1 5 5.9 CC(C)CCN1C(=O)C(NC(=O)Oc2cccc(N(C)C)c2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
10792765 112568 0 None -2754 2 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 550 5 3 4 5.8 O=C(Nc1cccc(O)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL331244 112568 0 None -2754 2 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 550 5 3 4 5.8 O=C(Nc1cccc(O)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
10770670 92047 0 None -301 2 Guinea pig 5.8 pKi = 5.8 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 663 11 6 6 4.9 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067959 92047 0 None -301 2 Guinea pig 5.8 pKi = 5.8 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 663 11 6 6 4.9 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL24313 92047 0 None -301 2 Guinea pig 5.8 pKi = 5.8 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 663 11 6 6 4.9 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
44359447 14519 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(CS(=O)(=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/jm00122a026
CHEMBL1206132 14519 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(CS(=O)(=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/jm00122a026
CHEMBL217767 14519 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(CS(=O)(=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/jm00122a026
CHEMBL216831 207588 0 None -29 2 Guinea pig 5.8 pKi = 5.8 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCCC)NC(=O)[C@H](CCCC)NC(=O)[C@H](Cc1ccc(OS(=O)(=O)O)cc1)NC(=O)[C@@H](CCC(=O)O)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/jm00126a007
10482233 167628 0 None -41 2 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 533 8 3 3 6.0 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Cl)cc1 10.1021/jm00072a005
CHEMBL433407 167628 0 None -41 2 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 533 8 3 3 6.0 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Cl)cc1 10.1021/jm00072a005
10795116 27692 0 None -602 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 743 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCc2ccc3ccccc3c2)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL137180 27692 0 None -602 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 743 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCc2ccc3ccccc3c2)cc(C(=O)O)c1 10.1021/jm00021a019
9850043 112362 1 None -446 3 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL330977 112362 1 None -446 3 Rat 5.8 pKi = 5.8 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
52949124 861 2 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site 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 861 2 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site 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 861 2 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site 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 861 2 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site 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
44356826 118788 0 None -19 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 781 12 5 6 6.6 COc1ccc(C[C@@H](NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)C(=O)Nc2cc(C(=O)O)cc(C(=O)O)c2)cc1 10.1021/jm00021a019
CHEMBL344014 118788 0 None -19 2 Guinea pig 5.8 pKi = 5.8 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 781 12 5 6 6.6 COc1ccc(C[C@@H](NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)C(=O)Nc2cc(C(=O)O)cc(C(=O)O)c2)cc1 10.1021/jm00021a019
56666598 63813 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 575 9 2 4 5.3 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccc(F)cc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808422 63813 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 575 9 2 4 5.3 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccc(F)cc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/j.bmc.2011.05.057
16733645 13055 0 None -416 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 598 9 2 7 5.4 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3cn(CC(=O)O)cn3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL1190962 13055 0 None -416 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 598 9 2 7 5.4 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3cn(CC(=O)O)cn3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL541903 13055 0 None -416 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 598 9 2 7 5.4 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3cn(CC(=O)O)cn3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
44280114 5026 0 None 1 2 Guinea pig 5.8 pKi = 5.8 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
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/s0960-894x(98)00231-5
CHEMBL105618 5026 0 None 1 2 Guinea pig 5.8 pKi = 5.8 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
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/s0960-894x(98)00231-5
44572200 178753 0 None -14 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometryDisplacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometry
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
CHEMBL473612 178753 0 None -14 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometryDisplacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometry
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
CHEMBL475226 178753 0 None -14 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometryDisplacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometry
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
56659685 63806 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 533 7 2 5 3.8 Cc1cccc(NC(=O)NC2C(=O)N(CCN3CCOCC3)c3ccccc3N(CC3CCCCC3)C2=O)c1 10.1016/j.bmc.2011.05.057
CHEMBL1808415 63806 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 533 7 2 5 3.8 Cc1cccc(NC(=O)NC2C(=O)N(CCN3CCOCC3)c3ccccc3N(CC3CCCCC3)C2=O)c1 10.1016/j.bmc.2011.05.057
5311201 205653 30 None -1174 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm051219x
CHEMBL9387 205653 30 None -1174 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm051219x
16732019 84995 0 None -1737 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 542 7 2 7 4.6 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL226533 84995 0 None -1737 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 542 7 2 7 4.6 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
54045469 63803 0 None - 1 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 481 9 2 5 3.2 COc1ccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN(C)C)C2=O)cc1 10.1016/j.bmc.2011.05.057
CHEMBL1808412 63803 0 None - 1 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 481 9 2 5 3.2 COc1ccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN(C)C)C2=O)cc1 10.1016/j.bmc.2011.05.057
10258121 98108 0 None 11 2 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 606 11 4 2 7.1 CC(Cc1c[nH]c2ccccc12)(NC(=O)NC(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm00072a005
CHEMBL276676 98108 0 None 11 2 Guinea pig 5.8 pKi = 5.8 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 606 11 4 2 7.1 CC(Cc1c[nH]c2ccccc12)(NC(=O)NC(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)NCCc1ccccc1 10.1021/jm00072a005
CHEMBL59865 214029 0 None - 1 Guinea pig 7.8 pKi = 7.8 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
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)CN 10.1021/jm0000416
CHEMBL1172253 206833 0 None -138 4 Human 7.8 pKi = 7.8 Binding
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
44265911 205394 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 276 4 2 1 3.6 O=C(NC/C=C/c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
CHEMBL9220 205394 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 276 4 2 1 3.6 O=C(NC/C=C/c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
10004216 4660 0 None -11 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL103750 4660 0 None -11 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
44356887 31087 0 None -776 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 757 11 5 6 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccsc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL140179 31087 0 None -776 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 757 11 5 6 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccsc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
10323690 100019 0 None -21 2 Guinea pig 5.7 pKi = 5.7 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00072a005
CHEMBL2114401 100019 0 None -21 2 Guinea pig 5.7 pKi = 5.7 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00072a005
CHEMBL291033 100019 0 None -21 2 Guinea pig 5.7 pKi = 5.7 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 499 8 3 3 5.4 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccccc1 10.1021/jm00072a005
44272076 168233 0 None -407 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1194 24 13 13 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)[C@H](NC(=O)OC(C)(C)C)CCC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL437661 168233 0 None -407 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1194 24 13 13 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)[C@H](NC(=O)OC(C)(C)C)CCC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
10819816 118223 0 None 7 2 Rat 7.7 pKi = 7.7 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 998 28 10 13 0.4 CSCC[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](CCSC)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
CHEMBL341762 118223 0 None 7 2 Rat 7.7 pKi = 7.7 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
ChEMBL 998 28 10 13 0.4 CSCC[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](CCSC)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm970477u
73354497 88941 0 None 7 2 Rat 7.7 pKi = 7.7 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 998 28 10 13 0.4 CSCC[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](CCSC)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL2369817 88941 0 None 7 2 Rat 7.7 pKi = 7.7 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 998 28 10 13 0.4 CSCC[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](CCSC)C(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
44359447 14519 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(CS(=O)(=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/jm00122a026
CHEMBL1206132 14519 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(CS(=O)(=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/jm00122a026
CHEMBL217767 14519 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](CCCC)NC(=O)[C@@H](Cc1ccc(CS(=O)(=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/jm00122a026
10768579 113354 0 None -32 2 Rat 7.7 pKi = 7.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 531 6 2 4 5.5 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
CHEMBL332568 113354 0 None -32 2 Rat 7.7 pKi = 7.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 531 6 2 4 5.5 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
53465844 69053 0 None 131 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-SR-27897 from human CCK1 R197A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 R197A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69053 0 None 131 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-SR-27897 from human CCK1 R197A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 R197A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
10722460 15008 0 None -309 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 612 5 2 3 6.9 O=C(Nc1cccc(Br)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL121028 15008 0 None -309 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 612 5 2 3 6.9 O=C(Nc1cccc(Br)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
44408526 136409 0 None -2344 4 Human 5.7 pKi = 5.7 Binding
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 136409 0 None -2344 4 Human 5.7 pKi = 5.7 Binding
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 82807 0 None -870 3 Human 5.7 pKi = 5.7 Binding
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 82807 0 None -870 3 Human 5.7 pKi = 5.7 Binding
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
16732916 136417 0 None -338 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 596 8 2 5 6.3 O=C(CN1N=C(C2CCCCC2)c2ccccc2N(CC(=O)C23CC4CC(CC(C4)C2)C3)C1=O)Nc1cccc(C(=O)O)c1 10.1021/jm070139l
CHEMBL374388 136417 0 None -338 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 596 8 2 5 6.3 O=C(CN1N=C(C2CCCCC2)c2ccccc2N(CC(=O)C23CC4CC(CC(C4)C2)C3)C1=O)Nc1cccc(C(=O)O)c1 10.1021/jm070139l
10695854 113491 0 None -25 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 474 6 2 3 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
CHEMBL332646 113491 0 None -25 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 474 6 2 3 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
45486955 195712 0 None -5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 628 8 3 7 5.0 O=C(N[C@@H](Cc1ccc(Cl)c(Br)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL569470 195712 0 None -5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 628 8 3 7 5.0 O=C(N[C@@H](Cc1ccc(Cl)c(Br)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
45486969 195784 0 None 7 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 598 8 3 7 5.4 C[C@H](c1ccc(Cl)c(Cl)c1)[C@@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)C(=O)O 10.1016/j.bmcl.2009.09.064
CHEMBL569849 195784 0 None 7 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 598 8 3 7 5.4 C[C@H](c1ccc(Cl)c(Cl)c1)[C@@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)C(=O)O 10.1016/j.bmcl.2009.09.064
45486947 195217 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 654 8 2 7 5.2 COC(=O)[C@H](Cc1ccc(F)c(Br)c1)NC(=O)c1cc(Cl)c(Cl)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
CHEMBL566177 195217 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 654 8 2 7 5.2 COC(=O)[C@H](Cc1ccc(F)c(Br)c1)NC(=O)c1cc(Cl)c(Cl)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
11693225 197113 0 None -7 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 676 8 3 7 4.8 O=C(N[C@@H](Cc1ccc(Cl)c(Cl)c1)C(=O)O)c1ccc(I)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
CHEMBL583344 197113 0 None -7 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 676 8 3 7 4.8 O=C(N[C@@H](Cc1ccc(Cl)c(Cl)c1)C(=O)O)c1ccc(I)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
16090700 82037 0 None 10 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 541 8 4 4 4.2 O=C(N[C@@H](Cc1ccccc1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cc2ccccc2[nH]1 10.1021/jm060590x
CHEMBL217595 82037 0 None 10 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 541 8 4 4 4.2 O=C(N[C@@H](Cc1ccccc1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cc2ccccc2[nH]1 10.1021/jm060590x
9958214 114282 0 None -269 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 517 7 2 4 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
CHEMBL333979 114282 0 None -269 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 517 7 2 4 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
45486995 196114 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 486 8 2 6 4.5 O=C(NCCCc1ccccc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL572046 196114 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 486 8 2 6 4.5 O=C(NCCCc1ccccc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
45486940 197197 0 None -31 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 550 8 3 7 4.2 O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL584259 197197 0 None -31 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 550 8 3 7 4.2 O=C(N[C@@H](Cc1ccc(Cl)cc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
44444929 94429 0 None - 1 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 788 11 6 5 6.1 O=C(O)c1cc(NC(=O)[C@H](Cc2ccc(I)cc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL254020 94429 0 None - 1 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 788 11 6 5 6.1 O=C(O)c1cc(NC(=O)[C@H](Cc2ccc(I)cc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
10795162 118520 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL2067970 118520 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL342616 118520 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
16090702 165634 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 461 4 2 3 4.4 O=C(c1ccc(Br)cc1NS(=O)(=O)c1cc2ccccc2[nH]1)N1CCCCC1 10.1021/jm060590x
CHEMBL426524 165634 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 461 4 2 3 4.4 O=C(c1ccc(Br)cc1NS(=O)(=O)c1cc2ccccc2[nH]1)N1CCCCC1 10.1021/jm060590x
44331343 4330 0 None -57 2 Rat 5.7 pKi = 5.7 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 606 6 2 3 7.0 O=C(Nc1ccccc1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/S0960-894X(96)00544-6
CHEMBL101456 4330 0 None -57 2 Rat 5.7 pKi = 5.7 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 606 6 2 3 7.0 O=C(Nc1ccccc1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/S0960-894X(96)00544-6
44403984 12190 0 None -125 2 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 5.2 CN(CC12CC3CC(CC(C3)C1)C2)C(=O)c1cc2[nH]cnc2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1185003 12190 0 None -125 2 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 5.2 CN(CC12CC3CC(CC(C3)C1)C2)C(=O)c1cc2[nH]cnc2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067967 12190 0 None -125 2 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 5.2 CN(CC12CC3CC(CC(C3)C1)C2)C(=O)c1cc2[nH]cnc2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
10795162 118520 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067970 118520 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL342616 118520 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
6956374 2363 4 None - 1 Guinea pig 4.7 pKi = 4.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@@H]([C@H]1c1ccccc1)c1ccccc1 10.1021/jm070880t
902 2363 4 None - 1 Guinea pig 4.7 pKi = 4.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@@H]([C@H]1c1ccccc1)c1ccccc1 10.1021/jm070880t
CHEMBL117281 2363 4 None - 1 Guinea pig 4.7 pKi = 4.7 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 435 3 2 2 4.9 Brc1ccc(cc1)NC(=O)N1NC(=O)[C@@H]([C@H]1c1ccccc1)c1ccccc1 10.1021/jm070880t
9939183 113616 0 None -6606 2 Rat 4.7 pKi = 4.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 633 7 2 5 5.9 O=C(Nc1cccc(CN2CCOCC2)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL332850 113616 0 None -6606 2 Rat 4.7 pKi = 4.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 633 7 2 5 5.9 O=C(Nc1cccc(CN2CCOCC2)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
44347144 112554 0 None -12 2 Guinea pig 4.7 pKi = 4.7 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 512 6 2 4 4.0 COC(=O)CNC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
CHEMBL331177 112554 0 None -12 2 Guinea pig 4.7 pKi = 4.7 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 512 6 2 4 4.0 COC(=O)CNC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
CHEMBL386304 210623 0 None -6 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None 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](CCC(=O)O)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/jm00126a007
44272056 97699 0 None -42 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1194 24 13 13 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL273880 97699 0 None -42 2 Guinea pig 5.7 pKi = 5.7 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1194 24 13 13 2.6 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
10794634 112590 0 None 11220 2 Guinea pig 8.7 pKi = 8.7 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 677 19 7 7 0.3 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)CC(N)=O 10.1021/jm0000416
CHEMBL331394 112590 0 None 11220 2 Guinea pig 8.7 pKi = 8.7 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 677 19 7 7 0.3 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)CC(N)=O 10.1021/jm0000416
53465844 69053 0 None 131 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69053 0 None 131 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL333477 209636 0 None -3 3 Guinea pig 8.6 pKi = 8.6 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
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)OC(C)(C)C 10.1016/j.bmcl.2003.11.001
CHEMBL333762 209637 0 None - 1 Guinea pig 8.6 pKi = 8.6 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
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](N)Cc1c[nH]c2ccccc12 10.1021/jm0000416
11216391 162929 0 None 1348 2 Guinea pig 8.6 pKi = 8.6 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 747 23 7 7 2.1 CCCCCNC(=O)CC(=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 10.1016/j.bmcl.2003.11.001
CHEMBL420161 162929 0 None 1348 2 Guinea pig 8.6 pKi = 8.6 Binding
Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranesAbility to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 747 23 7 7 2.1 CCCCCNC(=O)CC(=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 10.1016/j.bmcl.2003.11.001
CHEMBL119992 206846 0 None - 1 Guinea pig 7.7 pKi = 7.7 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
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)[C@H](C)N 10.1021/jm0000416
CHEMBL3350278 209710 0 None 20 2 Guinea pig 6.7 pKi = 6.7 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00174a016
44265932 96541 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 420 5 2 1 6.3 O=C(NCC=C(c1ccc(Cl)cc1)c1ccc(Cl)cc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
CHEMBL266596 96541 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 420 5 2 1 6.3 O=C(NCC=C(c1ccc(Cl)cc1)c1ccc(Cl)cc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
44265967 164310 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 350 11 2 1 6.5 CCCCCC(=CCNC(=O)Nc1ccc(Cl)cc1)CCCCC 10.1021/jm00084a009
CHEMBL422036 164310 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 350 11 2 1 6.5 CCCCCC(=CCNC(=O)Nc1ccc(Cl)cc1)CCCCC 10.1021/jm00084a009
CHEMBL379405 210508 0 None -11 4 Human 5.7 pKi = 5.7 Binding
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
10099504 206462 0 None -14 2 Guinea pig 5.7 pKi = 5.7 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 568 10 2 4 5.8 CC(Cc1cccc2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
CHEMBL98516 206462 0 None -14 2 Guinea pig 5.7 pKi = 5.7 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 568 10 2 4 5.8 CC(Cc1cccc2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
10628607 116261 0 None -467 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 713 11 5 5 6.4 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL337673 116261 0 None -467 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 713 11 5 5 6.4 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm00021a019
19700636 63801 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 491 8 2 4 4.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCN2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808410 63801 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 491 8 2 4 4.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCN2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
9872866 63807 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 571 7 2 5 4.1 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808416 63807 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 571 7 2 5 4.1 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
19700617 63812 0 None - 1 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 543 8 2 4 4.7 CN(C)CCCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808421 63812 0 None - 1 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 543 8 2 4 4.7 CN(C)CCCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/j.bmc.2011.05.057
10370321 12858 0 None -30902 2 Rat 4.7 pKi = 4.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 550 5 3 4 5.8 O=C(Nc1ccc(O)cc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL118954 12858 0 None -30902 2 Rat 4.7 pKi = 4.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 550 5 3 4 5.8 O=C(Nc1ccc(O)cc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
44346909 114072 0 None -10 2 Guinea pig 4.7 pKi = 4.7 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 498 6 3 3 3.9 O=C(O)CNC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
CHEMBL333758 114072 0 None -10 2 Guinea pig 4.7 pKi = 4.7 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 498 6 3 3 3.9 O=C(O)CNC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
44356888 118351 0 None -35 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 765 12 5 5 7.0 O=C(O)c1cc(NC(=O)[C@@H](CCc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL342205 118351 0 None -35 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 765 12 5 5 7.0 O=C(O)c1cc(NC(=O)[C@@H](CCc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
10795162 118520 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL2067970 118520 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL342616 118520 0 None -630 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
11561828 140083 0 None -4 2 Guinea pig 5.7 pKi = 5.7 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 468 7 3 2 6.8 O=C(O)c1cccc(NC(=O)c2cc(-c3ccccc3)[nH]c2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL381426 140083 0 None -4 2 Guinea pig 5.7 pKi = 5.7 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 468 7 3 2 6.8 O=C(O)c1cccc(NC(=O)c2cc(-c3ccccc3)[nH]c2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
44451547 96251 0 None -489 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 587 8 2 8 4.7 CN(c1cccc(NC(=O)CN2C(=O)N(CC(=O)C(C)(C)C)c3ccccc3N(C3CCCCC3)C2=O)c1)c1nn[nH]n1 10.1016/j.bmc.2007.12.047
CHEMBL264150 96251 0 None -489 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 587 8 2 8 4.7 CN(c1cccc(NC(=O)CN2C(=O)N(CC(=O)C(C)(C)C)c3ccccc3N(C3CCCCC3)C2=O)c1)c1nn[nH]n1 10.1016/j.bmc.2007.12.047
16733469 85079 0 None -6309 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 576 10 2 6 5.8 O=C(O)CSc1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1021/jm070139l
CHEMBL227333 85079 0 None -6309 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 576 10 2 6 5.8 O=C(O)CSc1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1021/jm070139l
44296914 100766 0 None -1318 2 Guinea pig 5.7 pKi = 5.7 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 765 12 5 5 7.0 O=C(CC1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL296167 100766 0 None -1318 2 Guinea pig 5.7 pKi = 5.7 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 765 12 5 5 7.0 O=C(CC1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL3351052 209780 0 None -14 2 Guinea pig 5.7 pKi = 5.7 Binding
Affinity of compound on binding of [3H]pCCK-8 to the cholecystokinin type A receptor in guinea pig pancreatic membraneAffinity of compound on binding of [3H]pCCK-8 to the cholecystokinin type A receptor in guinea pig pancreatic membrane
ChEMBL None None None CN(C(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12)C1CCCCC1)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
46235271 73286 2 None 2 2 Human 6.7 pKi = 6.7 Binding
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 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 73286 2 None 2 2 Human 6.7 pKi = 6.7 Binding
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 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
44357058 164295 0 None -173 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 785 11 5 5 7.3 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL421921 164295 0 None -173 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 785 11 5 5 7.3 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
10794888 164689 0 None -15 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 707 10 4 4 6.9 O=C(O)c1ccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc1 10.1021/jm00021a019
CHEMBL422981 164689 0 None -15 2 Guinea pig 5.7 pKi = 5.7 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 707 10 4 4 6.9 O=C(O)c1ccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc1 10.1021/jm00021a019
16732444 142762 0 None -2570 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 572 8 2 7 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3cnn(CC(=O)O)c3c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL389713 142762 0 None -2570 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 572 8 2 7 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3cnn(CC(=O)O)c3c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
44346225 161348 0 None -12022 2 Rat 5.7 pKi = 5.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 564 6 3 4 5.6 O=C(Nc1cccc(CO)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL415240 161348 0 None -12022 2 Rat 5.7 pKi = 5.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 564 6 3 4 5.6 O=C(Nc1cccc(CO)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
9985629 167485 0 None -41 2 Guinea pig 5.7 pKi = 5.7 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 577 8 3 3 6.1 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Br)cc1 10.1021/jm00072a005
CHEMBL432389 167485 0 None -41 2 Guinea pig 5.7 pKi = 5.7 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 577 8 3 3 6.1 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Br)cc1 10.1021/jm00072a005
10768308 14711 0 None -19 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 520 4 2 3 5.7 O=C(Nc1ccccc1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)C1=O 10.1021/jm990967h
CHEMBL120793 14711 0 None -19 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 520 4 2 3 5.7 O=C(Nc1ccccc1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)C1=O 10.1021/jm990967h
10506830 113455 0 None -6 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 548 6 2 3 6.5 O=C(Nc1ccccc1)NC1C(=O)N(CCC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL332601 113455 0 None -6 2 Rat 6.7 pKi = 6.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 548 6 2 3 6.5 O=C(Nc1ccccc1)NC1C(=O)N(CCC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
11664728 133885 0 None -10 2 Guinea pig 5.7 pKi = 5.7 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 482 7 3 2 7.1 Cc1ccccc1-c1cc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL371750 133885 0 None -10 2 Guinea pig 5.7 pKi = 5.7 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 482 7 3 2 7.1 Cc1ccccc1-c1cc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
10554602 15108 0 None -29 2 Rat 7.7 pKi = 7.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 546 7 2 4 6.3 CSc1cccc(NC(=O)NC2C(=O)N(CCC3CCCC3)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
CHEMBL121331 15108 0 None -29 2 Rat 7.7 pKi = 7.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 546 7 2 4 6.3 CSc1cccc(NC(=O)NC2C(=O)N(CCC3CCCC3)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
10505959 112979 0 None -74 2 Rat 7.7 pKi = 7.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 513 6 2 4 5.4 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL331975 112979 0 None -74 2 Rat 7.7 pKi = 7.7 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 513 6 2 4 5.4 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
44345980 113622 0 None -79 2 Rat 7.6 pKi = 7.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 538 6 2 7 6.2 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2cccc(C3N=NN=N3)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL332902 113622 0 None -79 2 Rat 7.6 pKi = 7.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 538 6 2 7 6.2 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2cccc(C3N=NN=N3)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
44387568 61863 0 None -144 3 Guinea pig 5.7 pKi = 5.7 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 660 11 7 6 2.0 C[C@@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm0000416
CHEMBL177799 61863 0 None -144 3 Guinea pig 5.7 pKi = 5.7 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 660 11 7 6 2.0 C[C@@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm0000416
10327028 89011 0 None -144 3 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 660 11 7 6 2.0 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
CHEMBL2371222 89011 0 None -144 3 Guinea pig 5.7 pKi = 5.7 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 660 11 7 6 2.0 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
19700615 63808 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2cc(F)ccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808417 63808 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2cc(F)ccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
10652142 101086 0 None -1819 2 Guinea pig 5.7 pKi = 5.7 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 679 11 5 6 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccsc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL298521 101086 0 None -1819 2 Guinea pig 5.7 pKi = 5.7 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 679 11 5 6 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccsc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
138106885 166347 71 None -1 4 Human 5.6 pKi = 5.6 Binding
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 166347 71 None -1 4 Human 5.6 pKi = 5.6 Binding
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 166347 71 None -1 4 Human 5.6 pKi = 5.6 Binding
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
44331524 163103 0 None -13 2 Rat 6.6 pKi = 6.6 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 530 8 2 3 6.5 CC(CC1CCCC1)N1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(C(C)CC2CCCC2)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL420459 163103 0 None -13 2 Rat 6.6 pKi = 6.6 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 530 8 2 3 6.5 CC(CC1CCCC1)N1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(C(C)CC2CCCC2)c2ccccc21 10.1016/S0960-894X(96)00544-6
10101023 89013 0 None -57 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 675 11 8 7 -0.1 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CC(=O)NCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
CHEMBL2371224 89013 0 None -57 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 675 11 8 7 -0.1 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CC(=O)NCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
CHEMBL3350720 209732 0 None -4 2 Guinea pig 6.6 pKi = 6.6 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(S(=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](CCCNC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00174a016
11541870 71092 0 None -33 3 Guinea pig 5.6 pKi = 5.6 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 433 7 3 3 5.4 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL196141 71092 0 None -33 3 Guinea pig 5.6 pKi = 5.6 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 433 7 3 3 5.4 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
44451622 95457 0 None -371 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 562 9 2 5 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(CCC(=O)O)c2)C(=O)N(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL259276 95457 0 None -371 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 562 9 2 5 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(CCC(=O)O)c2)C(=O)N(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
44451920 95667 0 None -245 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 519 7 2 5 5.5 CNc1cccc(NC(=O)CN2C(=O)N(CC(=O)C(C)(C)C)c3ccccc3N(C3CCCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
CHEMBL260394 95667 0 None -245 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 519 7 2 5 5.5 CNc1cccc(NC(=O)CN2C(=O)N(CC(=O)C(C)(C)C)c3ccccc3N(C3CCCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
10325110 111482 0 None -29 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 544 9 3 5 5.3 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc([N+](=O)[O-])cc1 10.1021/jm00072a005
CHEMBL328852 111482 0 None -29 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 544 9 3 5 5.3 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc([N+](=O)[O-])cc1 10.1021/jm00072a005
10006936 205981 0 None -5 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 521 6 3 3 6.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)Nc1ccc2ccccc2c1 10.1021/jm00072a005
CHEMBL95689 205981 0 None -5 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 521 6 3 3 6.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)Nc1ccc2ccccc2c1 10.1021/jm00072a005
9985004 205874 0 None -26 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 549 8 3 3 6.5 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1cccc2ccccc12 10.1021/jm00072a005
CHEMBL95115 205874 0 None -26 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 549 8 3 3 6.5 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1cccc2ccccc12 10.1021/jm00072a005
44331506 106788 0 None -22 2 Rat 6.6 pKi = 6.6 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 574 5 2 3 6.8 O=C(Nc1cccc(Cl)c1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(C2CCCCC2)C1=O 10.1016/S0960-894X(96)00544-6
CHEMBL317108 106788 0 None -22 2 Rat 6.6 pKi = 6.6 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 574 5 2 3 6.8 O=C(Nc1cccc(Cl)c1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(C2CCCCC2)C1=O 10.1016/S0960-894X(96)00544-6
44346825 114262 0 None -77 2 Guinea pig 4.6 pKi = 4.6 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 623 8 3 4 4.7 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3)C(=O)O 10.1021/jm00048a001
CHEMBL333920 114262 0 None -77 2 Guinea pig 4.6 pKi = 4.6 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 623 8 3 4 4.7 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3)C(=O)O 10.1021/jm00048a001
52949124 861 2 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R at allosteric site 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 861 2 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R at allosteric site 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 861 2 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R at allosteric site 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 861 2 None -2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R at allosteric site 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
CHEMBL3351050 209778 0 None -33 2 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CC(C)(C)OC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12 10.1021/jm00053a022
CHEMBL171594 207095 0 None -33 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1016/S0960-894X(00)80678-2
73347063 89010 0 None -162 3 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 674 11 7 6 2.4 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
CHEMBL2371221 89010 0 None -162 3 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 674 11 7 6 2.4 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
22171089 93536 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 462 8 1 5 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(OC)c3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL248552 93536 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 462 8 1 5 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(OC)c3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
15002730 93577 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 462 8 1 5 5.6 COc1ccc(C(Cc2cc(-c3ccc(Cl)cc3)n(-c3ccc(OC)cc3)n2)C(=O)O)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL248752 93577 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 462 8 1 5 5.6 COc1ccc(C(Cc2cc(-c3ccc(Cl)cc3)n(-c3ccc(OC)cc3)n2)C(=O)O)cc1 10.1016/j.bmcl.2007.09.093
22171039 93578 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(C)cc3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL248754 93578 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(C)cc3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
44444767 93611 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 432 7 1 4 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL248948 93611 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 432 7 1 4 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
10343558 93612 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(Cl)c3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL248949 93612 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(Cl)c3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
15002734 93613 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 442 8 1 5 5.3 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3OC)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL248950 93613 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 442 8 1 5 5.3 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3OC)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
10388627 93655 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 442 8 1 5 5.3 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(OC)c3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL249151 93655 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 442 8 1 5 5.3 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(OC)c3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
10366068 93656 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 442 8 1 5 5.3 COc1ccc(C(Cc2cc(-c3ccc(C)cc3)n(-c3ccc(OC)cc3)n2)C(=O)O)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL249153 93656 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 442 8 1 5 5.3 COc1ccc(C(Cc2cc(-c3ccc(C)cc3)n(-c3ccc(OC)cc3)n2)C(=O)O)cc1 10.1016/j.bmcl.2007.09.093
22171037 93696 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 426 7 1 4 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(C)c3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL249361 93696 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 426 7 1 4 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(C)c3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
10320262 93723 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 426 7 1 4 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(C)cc3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL249560 93723 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 426 7 1 4 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(C)cc3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
44444777 93752 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 412 7 1 4 5.3 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL249763 93752 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 412 7 1 4 5.3 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
11754311 93874 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 466 7 1 4 6.3 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(Cl)cc3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL250576 93874 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 466 7 1 4 6.3 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(Cl)cc3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
22171092 153950 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(C)c3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL399055 153950 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(C)c3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
10433726 153951 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(Cl)cc3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL399056 153951 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 446 7 1 4 5.9 COc1ccc(-n2nc(CC(C(=O)O)c3ccc(Cl)cc3)cc2-c2ccc(C)cc2)cc1 10.1016/j.bmcl.2007.09.093
22171012 154184 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 466 7 1 4 6.3 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(Cl)c3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL399915 154184 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 466 7 1 4 6.3 COc1ccc(-n2nc(CC(C(=O)O)c3cccc(Cl)c3)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
44444763 154318 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 462 8 1 5 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3OC)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
CHEMBL400670 154318 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 462 8 1 5 5.6 COc1ccc(-n2nc(CC(C(=O)O)c3ccccc3OC)cc2-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2007.09.093
45486974 196003 0 None 50 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 580 7 3 7 4.8 C[C@@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)[C@@H](O)c1cccc(Br)c1 10.1016/j.bmcl.2009.09.064
CHEMBL571206 196003 0 None 50 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 580 7 3 7 4.8 C[C@@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)[C@@H](O)c1cccc(Br)c1 10.1016/j.bmcl.2009.09.064
44271963 96264 0 None -4466 2 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1274 26 13 15 2.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)[C@H](NC(=O)OC(C)(C)C)CCC(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL264273 96264 0 None -4466 2 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1274 26 13 15 2.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)[C@H](NC(=O)OC(C)(C)C)CCC(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
11555184 165468 0 None -281 3 Guinea pig 6.6 pKi = 6.6 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 503 7 3 3 7.0 Cc1ccc(NC(=O)c2[nH]c(C3(C)CCCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)cc1C(=O)O 10.1021/jm0490686
CHEMBL425574 165468 0 None -281 3 Guinea pig 6.6 pKi = 6.6 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 503 7 3 3 7.0 Cc1ccc(NC(=O)c2[nH]c(C3(C)CCCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)cc1C(=O)O 10.1021/jm0490686
45255234 197348 0 None -15 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 584 8 3 7 4.9 O=C(N[C@@H](Cc1ccc(Cl)c(Cl)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL585914 197348 0 None -15 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 584 8 3 7 4.9 O=C(N[C@@H](Cc1ccc(Cl)c(Cl)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
45486935 195074 0 None -25 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 612 8 3 7 4.5 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
CHEMBL565298 195074 0 None -25 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 612 8 3 7 4.5 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
45486976 197284 0 None -39 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 656 8 3 7 4.6 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
CHEMBL585157 197284 0 None -39 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 656 8 3 7 4.6 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.065
10792724 14280 0 None -162 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 548 5 2 3 6.4 Cc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL120031 14280 0 None -162 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 548 5 2 3 6.4 Cc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
10793611 15310 0 None -4 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 594 7 2 4 7.2 CSc1cccc(NC(=O)NC2C(=O)N(CCC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL121624 15310 0 None -4 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 594 7 2 4 7.2 CSc1cccc(NC(=O)NC2C(=O)N(CCC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
19043400 98275 0 None -162 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 480 4 2 3 5.1 O=C(Nc1ccccc1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2CC3CCC2C3)C1=O 10.1021/jm990967h
CHEMBL278018 98275 0 None -162 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 480 4 2 3 5.1 O=C(Nc1ccccc1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2CC3CCC2C3)C1=O 10.1021/jm990967h
9869202 71717 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 467 6 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)c1 10.1021/jm0490686
CHEMBL197716 71717 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 467 6 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)c1 10.1021/jm0490686
CHEMBL2067960 71717 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 467 6 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)c1 10.1021/jm0490686
44444930 154371 0 None - 1 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 688 11 6 6 5.7 Nc1cccc2cc(C(=O)N[C@@H](Cc3ccccc3)C(=O)Nc3cc(C(=O)O)cc(C(=O)O)c3)c(C(=O)NCC34CC5CC(CC(C5)C3)C4)cc12 10.1021/jm070880t
CHEMBL400974 154371 0 None - 1 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 688 11 6 6 5.7 Nc1cccc2cc(C(=O)N[C@@H](Cc3ccccc3)C(=O)Nc3cc(C(=O)O)cc(C(=O)O)c3)c(C(=O)NCC34CC5CC(CC(C5)C3)C4)cc12 10.1021/jm070880t
44444931 154394 0 None - 1 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 688 11 6 6 5.7 Nc1cccc2cc(C(=O)NCC34CC5CC(CC(C5)C3)C4)c(C(=O)N[C@@H](Cc3ccccc3)C(=O)Nc3cc(C(=O)O)cc(C(=O)O)c3)cc12 10.1021/jm070880t
CHEMBL401097 154394 0 None - 1 Guinea pig 5.6 pKi = 5.6 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 688 11 6 6 5.7 Nc1cccc2cc(C(=O)NCC34CC5CC(CC(C5)C3)C4)c(C(=O)N[C@@H](Cc3ccccc3)C(=O)Nc3cc(C(=O)O)cc(C(=O)O)c3)cc12 10.1021/jm070880t
16090789 82823 0 None 3 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 521 6 2 7 4.4 O=C(Nc1ccc(C(=O)N2CCCCC2)c(NS(=O)(=O)c2cccc3nsnc23)c1)c1ccccc1 10.1021/jm060590x
CHEMBL218729 82823 0 None 3 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 521 6 2 7 4.4 O=C(Nc1ccc(C(=O)N2CCCCC2)c(NS(=O)(=O)c2cccc3nsnc23)c1)c1ccccc1 10.1021/jm060590x
16733466 85078 0 None -7413 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 558 10 2 5 5.6 O=C(O)CCc1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1021/jm070139l
CHEMBL227330 85078 0 None -7413 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 558 10 2 5 5.6 O=C(O)CCc1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C3CCCC3)C2=O)c1 10.1021/jm070139l
16732165 168371 0 None -3235 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 571 8 2 6 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3c(ccn3CC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL438843 168371 0 None -3235 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 571 8 2 6 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3c(ccn3CC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
9936141 12141 0 None -12 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 510 7 4 3 7.0 O=C(O)c1cc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184700 12141 0 None -12 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 510 7 4 3 7.0 O=C(O)c1cc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067956 12141 0 None -12 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 510 7 4 3 7.0 O=C(O)c1cc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
9869202 71717 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 467 6 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)c1 10.1021/jm049069y
CHEMBL197716 71717 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 467 6 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)c1 10.1021/jm049069y
CHEMBL2067960 71717 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 467 6 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)c1 10.1021/jm049069y
44444932 154300 0 None - 1 Guinea pig 4.6 pKi = 4.6 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 623 8 3 4 4.8 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2)C(=O)O 10.1021/jm070880t
CHEMBL400548 154300 0 None - 1 Guinea pig 4.6 pKi = 4.6 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 623 8 3 4 4.8 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2)C(=O)O 10.1021/jm070880t
44357208 118465 0 None -4 2 Guinea pig 5.6 pKi = 5.6 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 737 10 5 5 6.7 O=C(O)c1cc(NC(=O)[C@H](NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)c2ccccc2)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL342465 118465 0 None -4 2 Guinea pig 5.6 pKi = 5.6 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 737 10 5 5 6.7 O=C(O)c1cc(NC(=O)[C@H](NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)c2ccccc2)cc(C(=O)O)c1 10.1021/jm00021a019
56673524 63809 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808418 63809 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
10842269 101090 0 None -575 2 Guinea pig 5.6 pKi = 5.6 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 681 11 6 6 5.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2F)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL298551 101090 0 None -575 2 Guinea pig 5.6 pKi = 5.6 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 681 11 6 6 5.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2F)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
10698746 116272 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 595 7 3 4 4.0 O=C(O)CNC(=O)[C@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3 10.1021/jm00021a019
CHEMBL337743 116272 0 None -3 2 Guinea pig 5.6 pKi = 5.6 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 595 7 3 4 4.0 O=C(O)CNC(=O)[C@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3 10.1021/jm00021a019
19700615 63808 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2cc(F)ccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808417 63808 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2cc(F)ccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
11799257 112955 0 None -32 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 490 6 2 3 5.1 O=C(Nc1ccccc1)NC1C(=O)N(CCc2ccccc2)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL331929 112955 0 None -32 2 Rat 6.6 pKi = 6.6 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 490 6 2 3 5.1 O=C(Nc1ccccc1)NC1C(=O)N(CCc2ccccc2)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
10795162 118520 0 None -630 2 Guinea pig 5.6 pKi = 5.6 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL2067970 118520 0 None -630 2 Guinea pig 5.6 pKi = 5.6 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL342616 118520 0 None -630 2 Guinea pig 5.6 pKi = 5.6 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 751 11 5 5 6.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
19700643 63673 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 505 9 2 4 4.5 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1807152 63673 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 505 9 2 4 4.5 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
10439779 106191 0 None -5 3 Guinea pig 6.6 pKi = 6.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 710 11 7 8 2.2 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCSSCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
CHEMBL3143501 106191 0 None -5 3 Guinea pig 6.6 pKi = 6.6 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 710 11 7 8 2.2 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCSSCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
52949124 861 2 None -2 2 Human 6.6 pKi = 6.6 Binding
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 861 2 None -2 2 Human 6.6 pKi = 6.6 Binding
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 861 2 None -2 2 Human 6.6 pKi = 6.6 Binding
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 861 2 None -2 2 Human 6.6 pKi = 6.6 Binding
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
56663144 63793 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 507 8 2 5 3.2 Cc1cccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN3CCOCC3)C2=O)c1 10.1016/j.bmc.2011.05.057
CHEMBL1808400 63793 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 507 8 2 5 3.2 Cc1cccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN3CCOCC3)C2=O)c1 10.1016/j.bmc.2011.05.057
46235271 73286 2 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R at allosteric site 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 73286 2 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-CCK] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-CCK] from wild-type human CCK1R at allosteric site 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
887 4035 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 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 10.1021/jm070139l
9870520 4035 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 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 10.1021/jm070139l
CHEMBL324547 4035 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 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 10.1021/jm070139l
DB12355 4035 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 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 10.1021/jm070139l
44451581 95368 0 None -316 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 594 9 2 6 6.0 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(SCC(=O)O)c2)C(=O)N(C2CCCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL258863 95368 0 None -316 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 594 9 2 6 6.0 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(SCC(=O)O)c2)C(=O)N(C2CCCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
10652140 101361 0 None -177 2 Guinea pig 5.6 pKi = 5.6 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 679 11 7 7 4.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL300456 101361 0 None -177 2 Guinea pig 5.6 pKi = 5.6 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 679 11 7 7 4.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
44329398 205944 0 None -12 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 543 10 3 4 4.8 O=C(O)CN(CCc1ccccc1)C(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00072a005
CHEMBL95461 205944 0 None -12 2 Guinea pig 5.6 pKi = 5.6 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 543 10 3 4 4.8 O=C(O)CN(CCc1ccccc1)C(=O)C(Cc1c[nH]c2ccccc12)NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2 10.1021/jm00072a005
10098459 4186 0 None -208 2 Rat 6.5 pKi = 6.5 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 528 7 2 3 5.8 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL100548 4186 0 None -208 2 Rat 6.5 pKi = 6.5 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 528 7 2 3 5.8 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
73354642 89014 0 None -46 3 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 646 11 7 6 1.6 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
CHEMBL2371225 89014 0 None -46 3 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL 646 11 7 6 1.6 C[C@]1(Cc2c[nH]c3ccccc23)NC(=O)CCCCCC[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC1=O 10.1021/jm9603072
11568611 71620 0 None -263 3 Guinea pig 5.5 pKi = 5.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 449 6 3 3 5.8 CC(C)(C)c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL197370 71620 0 None -263 3 Guinea pig 5.5 pKi = 5.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 449 6 3 3 5.8 CC(C)(C)c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
5311188 9697 2 None -1 2 Rat 5.5 pKi = 5.5 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific 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/jm9703247
CHEMBL113718 9697 2 None -1 2 Rat 5.5 pKi = 5.5 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific 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/jm9703247
44265912 204671 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 354 6 2 1 5.1 O=C(NCCC(c1ccccc1)c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
CHEMBL8779 204671 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 354 6 2 1 5.1 O=C(NCCC(c1ccccc1)c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
44346355 157313 0 None -446 3 Guinea pig 5.5 pKi = 5.5 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 1260 26 13 15 1.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCCCNC(=O)C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0000416
CHEMBL408389 157313 0 None -446 3 Guinea pig 5.5 pKi = 5.5 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 1260 26 13 15 1.7 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H]1CCCCNC(=O)C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0000416
CHEMBL2370588 208117 0 None -446 2 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL3350335 209718 0 None -245 2 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
CHEMBL3142843 209380 0 None -6 2 Guinea pig 4.5 pKi = 4.5 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CC(C)(C)OC(=O)NCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00174a016
11495719 70015 0 None -14 3 Guinea pig 6.5 pKi = 6.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 431 7 3 3 5.8 Cc1ccccc1-c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC2CCCCC2)[nH]1 10.1021/jm0490686
CHEMBL194514 70015 0 None -14 3 Guinea pig 6.5 pKi = 6.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 431 7 3 3 5.8 Cc1ccccc1-c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC2CCCCC2)[nH]1 10.1021/jm0490686
10817243 113005 0 None -22 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 591 7 2 4 6.6 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL332128 113005 0 None -22 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 591 7 2 4 6.6 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
16733051 136420 0 None -758 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 595 8 2 7 4.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)NS(C)(=O)=O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL374390 136420 0 None -758 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 595 8 2 7 4.2 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)NS(C)(=O)=O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
11800981 10099 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific 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/jm9703247
CHEMBL116001 10099 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific 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/jm9703247
44379428 57851 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibitory activity against CCK-A receptorInhibitory activity against CCK-A receptor
ChEMBL 557 9 3 6 4.9 C[C@@](N)(Cc1cn(C(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80669-1
CHEMBL168182 57851 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibitory activity against CCK-A receptorInhibitory activity against CCK-A receptor
ChEMBL 557 9 3 6 4.9 C[C@@](N)(Cc1cn(C(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)N[C@H](CC(=O)O)Cc1ccccc1 10.1016/S0960-894X(00)80669-1
CHEMBL1206136 206852 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
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)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/jm00122a026
CHEMBL218455 206852 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
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)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/jm00122a026
10372489 4183 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 692 20 7 7 1.3 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)CCC(=O)O 10.1021/jm0000416
CHEMBL100538 4183 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 692 20 7 7 1.3 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)CCC(=O)O 10.1021/jm0000416
44359425 14560 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)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/jm00122a026
CHEMBL1206331 14560 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)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/jm00122a026
CHEMBL262687 14560 0 None - 1 Guinea pig 8.5 pKi = 8.5 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brainThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig brain
ChEMBL 1031 30 11 11 1.0 CCCC[C@H](NC(=O)[C@H](Cc1ccc(CS(=O)(=O)O)cc1)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/jm00122a026
90662935 106080 0 None 10 2 Rat 8.5 pKi = 8.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 1057 30 11 11 2.6 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=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)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL3142373 106080 0 None 10 2 Rat 8.5 pKi = 8.5 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL 1057 30 11 11 2.6 CCCC[C@H](NC(=O)Cc1ccc(O)cc1)C(=O)NCC(=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)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
53465844 69053 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-SR-27897 from human CCK1 W39A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 W39A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69053 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-SR-27897 from human CCK1 W39A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 W39A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
10075052 189072 0 None 10 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometryDisplacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometry
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
CHEMBL515268 189072 0 None 10 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometryDisplacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometry
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
CHEMBL515288 189072 0 None 10 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometryDisplacement of [125I](S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea from human CCK1 receptor expressed in CHO cells by gamma spectrometry
ChEMBL 510 3 2 3 4.3 CN1C(=O)[C@H](NC(=O)Nc2cccc(I)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm801439x
53465844 69053 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-SR-27897 from human CCK1 F107A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 F107A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69053 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-SR-27897 from human CCK1 F107A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 F107A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
44215880 69050 0 None 3890 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins 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 69050 0 None 3890 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins 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
887 4035 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 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 10.1021/jm051219x
9870520 4035 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 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 10.1021/jm051219x
CHEMBL324547 4035 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 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 10.1021/jm051219x
DB12355 4035 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 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 10.1021/jm051219x
10460632 206579 0 None -43 2 Human 5.5 pKi = 5.5 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 568 10 2 4 5.8 CC(Cc1ccc2ccccc2c1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
CHEMBL99252 206579 0 None -43 2 Human 5.5 pKi = 5.5 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 568 10 2 4 5.8 CC(Cc1ccc2ccccc2c1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
9890720 167894 0 None -2 2 Guinea pig 5.5 pKi = 5.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 466 6 3 2 7.3 O=C(O)c1cccc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)c1 10.1021/jm0490686
CHEMBL2067971 167894 0 None -2 2 Guinea pig 5.5 pKi = 5.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 466 6 3 2 7.3 O=C(O)c1cccc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)c1 10.1021/jm0490686
CHEMBL435127 167894 0 None -2 2 Guinea pig 5.5 pKi = 5.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 466 6 3 2 7.3 O=C(O)c1cccc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)c1 10.1021/jm0490686
44356448 167665 0 None -75 2 Guinea pig 6.5 pKi = 6.5 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 769 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2cccc(F)c2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL433656 167665 0 None -75 2 Guinea pig 6.5 pKi = 6.5 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 769 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2cccc(F)c2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
44356666 168053 0 None -16 2 Guinea pig 6.5 pKi = 6.5 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 799 11 3 11 5.2 O=C(NCC12CC3CC(CC(C3)C1)C2)C1C2c3ccccc3C(c3ccccc32)C1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(-n2cnnn2)cc(-n2cnnn2)c1 10.1021/jm00021a019
CHEMBL436187 168053 0 None -16 2 Guinea pig 6.5 pKi = 6.5 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 799 11 3 11 5.2 O=C(NCC12CC3CC(CC(C3)C1)C2)C1C2c3ccccc3C(c3ccccc32)C1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(-n2cnnn2)cc(-n2cnnn2)c1 10.1021/jm00021a019
11643045 71779 0 None -43 3 Guinea pig 6.5 pKi = 6.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 511 9 3 3 6.8 Cc1ccccc1-c1nc(C(=O)Nc2cccc(CCC(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL197873 71779 0 None -43 3 Guinea pig 6.5 pKi = 6.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 511 9 3 3 6.8 Cc1ccccc1-c1nc(C(=O)Nc2cccc(CCC(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
10793342 112593 0 None -158 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 579 6 2 5 6.0 O=C(Nc1cccc([N+](=O)[O-])c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL331405 112593 0 None -158 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 579 6 2 5 6.0 O=C(Nc1cccc([N+](=O)[O-])c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
44329798 107050 0 None -245 5 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 610 10 2 4 6.5 CC(Cc1c[nH]c2ccccc12)(C(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1Cl)CC(=O)O 10.1021/jm00072a005
CHEMBL318852 107050 0 None -245 5 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 610 10 2 4 6.5 CC(Cc1c[nH]c2ccccc12)(C(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccc(Cl)cc1Cl)CC(=O)O 10.1021/jm00072a005
19700615 63808 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2cc(F)ccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808417 63808 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 589 7 2 5 4.2 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2cc(F)ccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
887 4035 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 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 10.1016/j.bmc.2007.12.047
9870520 4035 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 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 10.1016/j.bmc.2007.12.047
CHEMBL324547 4035 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 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 10.1016/j.bmc.2007.12.047
DB12355 4035 24 None -380 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 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 10.1016/j.bmc.2007.12.047
11534594 197112 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 616 8 2 6 7.0 O=C(NCC(c1ccc(Cl)cc1)c1ccc(Cl)cc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL583343 197112 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 616 8 2 6 7.0 O=C(NCC(c1ccc(Cl)cc1)c1ccc(Cl)cc1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
10071178 74131 1 None 501 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm060590x
CHEMBL202861 74131 1 None 501 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 427 7 4 3 3.8 O=C(Nc1ccccc1C(=O)NC(Cc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm060590x
CHEMBL3350665 209726 0 None -3 2 Guinea pig 6.5 pKi = 6.5 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(S(=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](CCCNC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00174a016
44272041 96623 0 None -338 2 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1274 26 13 15 2.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL267329 96623 0 None -338 2 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1274 26 13 15 2.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
10459641 111733 0 None -26 2 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 529 9 3 4 5.4 COc1ccc(CCNC(=O)C(C)(Cc2c[nH]c3ccccc23)NC(=O)OC2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)cc1 10.1021/jm00072a005
CHEMBL329088 111733 0 None -26 2 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 529 9 3 4 5.4 COc1ccc(CCNC(=O)C(C)(Cc2c[nH]c3ccccc23)NC(=O)OC2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)cc1 10.1021/jm00072a005
45486968 195783 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 550 8 3 7 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL569848 195783 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 550 8 3 7 4.2 O=C(N[C@H](Cc1ccc(Cl)cc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
45486985 196066 0 None -63 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 650 8 3 6 4.5 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
CHEMBL571650 196066 0 None -63 2 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 650 8 3 6 4.5 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
10411553 153349 0 None - 1 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 452 4 3 6 2.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(-c3nnn[nH]3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm070880t
CHEMBL398312 153349 0 None - 1 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 452 4 3 6 2.8 CN1C(=O)[C@H](NC(=O)Nc2cccc(-c3nnn[nH]3)c2)N=C(c2ccccc2)c2ccccc21 10.1021/jm070880t
5311201 205653 30 None -2570 6 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm070880t
CHEMBL9387 205653 30 None -2570 6 Guinea pig 6.5 pKi = 6.5 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm070880t
136036823 155125 0 None -263 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 574 7 2 7 4.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)C(=O)N(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL404967 155125 0 None -263 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 574 7 2 7 4.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)C(=O)N(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
10099495 107234 0 None -117 2 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 567 8 3 3 6.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Cl)cc1Cl 10.1021/jm00072a005
CHEMBL319120 107234 0 None -117 2 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 567 8 3 3 6.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCc1ccc(Cl)cc1Cl 10.1021/jm00072a005
45486958 195901 0 None -19 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 516 8 3 7 3.6 O=C(N[C@H](Cc1ccccc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL570518 195901 0 None -19 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 516 8 3 7 3.6 O=C(N[C@H](Cc1ccccc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
44444928 154067 0 None - 1 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 610 10 6 5 5.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL399252 154067 0 None - 1 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 610 10 6 5 5.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm070880t
16090699 141372 0 None 1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 463 8 4 4 3.4 O=C(N[C@@H](Cc1ccccc1)C(=O)O)c1ccccc1NS(=O)(=O)c1cc2ccccc2[nH]1 10.1021/jm060590x
CHEMBL386985 141372 0 None 1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 463 8 4 4 3.4 O=C(N[C@@H](Cc1ccccc1)C(=O)O)c1ccccc1NS(=O)(=O)c1cc2ccccc2[nH]1 10.1021/jm060590x
10603971 101131 0 None -208 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 624 11 6 5 5.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL298861 101131 0 None -208 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 624 11 6 5 5.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm9508907
9958028 11684 0 None -12 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 511 7 4 4 6.4 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1181937 11684 0 None -12 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 511 7 4 4 6.4 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067950 11684 0 None -12 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 511 7 4 4 6.4 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccc4ccccc4c3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
9956948 11808 0 None 1 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 483 7 4 4 6.0 O=C(Nc1cc(CO)cc(CO)c1)c1[nH]c(-c2ccc3ccccc3c2)nc1CC1CCCCCC1 10.1021/jm049069y
CHEMBL1182723 11808 0 None 1 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 483 7 4 4 6.0 O=C(Nc1cc(CO)cc(CO)c1)c1[nH]c(-c2ccc3ccccc3c2)nc1CC1CCCCCC1 10.1021/jm049069y
CHEMBL2067953 11808 0 None 1 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 483 7 4 4 6.0 O=C(Nc1cc(CO)cc(CO)c1)c1[nH]c(-c2ccc3ccccc3c2)nc1CC1CCCCCC1 10.1021/jm049069y
11576933 12147 0 None -19 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 499 7 4 4 5.5 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184725 12147 0 None -19 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 499 7 4 4 5.5 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067957 12147 0 None -19 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 499 7 4 4 5.5 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
44404005 12164 0 None -100 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 623 11 5 5 5.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184845 12164 0 None -100 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 623 11 5 5 5.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067963 12164 0 None -100 2 Guinea pig 5.5 pKi = 5.5 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 623 11 5 5 5.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2ccccc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL206974 207428 0 None -72 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determinedBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determined
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](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm0303103
CHEMBL1172249 206830 0 None -5 4 Human 7.5 pKi = 7.5 Binding
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
CHEMBL206974 207428 0 None -72 5 Human 6.5 pKi = 6.5 Binding
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](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
CHEMBL3351048 209776 0 None -5 2 Guinea pig 5.5 pKi = 5.5 Binding
Affinity of compound on binding of [3H]pCCK-8 to the cholecystokinin type A receptor in guinea pig pancreatic membraneAffinity of compound on binding of [3H]pCCK-8 to the cholecystokinin type A receptor in guinea pig pancreatic membrane
ChEMBL None None None CN(C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
CHEMBL407057 210878 0 None -1513 4 Human 5.5 pKi = 5.5 Binding
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](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O 10.1021/jm050921q
11513177 72169 0 None -131 3 Guinea pig 6.5 pKi = 6.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 501 7 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(C34CCC(CC3)CC4)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL199091 72169 0 None -131 3 Guinea pig 6.5 pKi = 6.5 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 501 7 3 3 6.7 O=C(O)c1cccc(NC(=O)c2[nH]c(C34CCC(CC3)CC4)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
10004216 4660 0 None -11 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL103750 4660 0 None -11 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
18472063 63811 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 529 7 2 4 4.3 CN(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808420 63811 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 529 7 2 4 4.3 CN(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1206136 206852 0 None - 1 Guinea pig 7.5 pKi = 7.5 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
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)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/jm00122a026
CHEMBL218455 206852 0 None - 1 Guinea pig 7.5 pKi = 7.5 Binding
The compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membraneThe compound was tested for the inhibition of [3H]propionyl specific binding to Cholecystokinin 8 receptor of guinea pig pancreatic membrane
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)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/jm00122a026
54554106 63802 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 451 8 2 4 3.2 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCN(C)C)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808411 63802 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 451 8 2 4 3.2 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCN(C)C)c2ccccc21 10.1016/j.bmc.2011.05.057
10723216 161434 0 None -4466 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 680 11 6 5 5.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2F)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL415936 161434 0 None -4466 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 680 11 6 5 5.6 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2F)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL265595 208900 0 None -1584 4 Human 5.5 pKi = 5.5 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determinedBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determined
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](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CC(=O)O 10.1021/jm0303103
10604664 154684 0 None -602 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 691 9 2 7 5.6 O=C(Nc1cccc(C(=O)OCCN2CCOCC2)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL402702 154684 0 None -602 2 Rat 6.5 pKi = 6.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 691 9 2 7 5.6 O=C(Nc1cccc(C(=O)OCCN2CCOCC2)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
10580234 98564 0 None -251 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]ccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL280248 98564 0 None -251 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]ccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL3350331 209717 0 None 1 2 Guinea pig 6.5 pKi = 6.5 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00174a016
CHEMBL3350665 209726 0 None -3 2 Guinea pig 6.5 pKi = 6.5 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(S(=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](CCCNC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00174a016
44265916 205851 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 352 5 2 1 5.0 O=C(NCC=C(c1ccccc1)c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
CHEMBL9500 205851 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 352 5 2 1 5.0 O=C(NCC=C(c1ccccc1)c1ccccc1)c1cc2ccccc2[nH]1 10.1021/jm00084a009
CHEMBL2371662 208351 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL None None None 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)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00389a002
10031454 108088 0 None -67 2 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 596 10 2 4 5.5 CC(Cc1ccc(Br)cc1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
CHEMBL320399 108088 0 None -67 2 Guinea pig 5.5 pKi = 5.5 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 596 10 2 4 5.5 CC(Cc1ccc(Br)cc1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
56659684 63805 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 519 7 2 5 3.5 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC2CCCCC2)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808414 63805 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 519 7 2 5 3.5 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCOCC2)c2ccccc2N(CC2CCCCC2)C1=O 10.1016/j.bmc.2011.05.057
10508004 11679 0 None -2454 2 Rat 5.5 pKi = 5.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 612 5 2 3 6.9 O=C(Nc1ccc(Br)cc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL118189 11679 0 None -2454 2 Rat 5.5 pKi = 5.5 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 612 5 2 3 6.9 O=C(Nc1ccc(Br)cc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
44382456 119942 0 None -3162 3 Rat 6.5 pKi = 6.5 Binding
The compound was evaluated for the inhibition of binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.The compound was evaluated for the inhibition of binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 572 10 5 5 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N)cc1 10.1016/S0960-894X(00)80686-1
CHEMBL354049 119942 0 None -3162 3 Rat 6.5 pKi = 6.5 Binding
The compound was evaluated for the inhibition of binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.The compound was evaluated for the inhibition of binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 572 10 5 5 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N)cc1 10.1016/S0960-894X(00)80686-1
CHEMBL83942 119942 0 None -3162 3 Rat 6.5 pKi = 6.5 Binding
The compound was evaluated for the inhibition of binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.The compound was evaluated for the inhibition of binding of [125I]Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas.
ChEMBL 572 10 5 5 4.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N)cc1 10.1016/S0960-894X(00)80686-1
CHEMBL3351061 209786 0 None -4 2 Guinea pig 5.5 pKi = 5.5 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CN(C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
9867157 99765 4 None 194 2 Guinea pig 6.5 pKi = 6.5 Binding
In vitro affinity against Cholecystokinin type A receptor in guinea pig pancreatic cellIn vitro affinity against Cholecystokinin type A receptor in guinea pig pancreatic cell
ChEMBL 426 9 3 4 2.3 O=C(O)C[C@H](NS(=O)(=O)c1ccc2ccccc2c1)C(=O)NCCc1ccccc1 10.1016/S0960-894X(00)80008-6
CHEMBL288641 99765 4 None 194 2 Guinea pig 6.5 pKi = 6.5 Binding
In vitro affinity against Cholecystokinin type A receptor in guinea pig pancreatic cellIn vitro affinity against Cholecystokinin type A receptor in guinea pig pancreatic cell
ChEMBL 426 9 3 4 2.3 O=C(O)C[C@H](NS(=O)(=O)c1ccc2ccccc2c1)C(=O)NCCc1ccccc1 10.1016/S0960-894X(00)80008-6
44356825 168057 0 None -1621 2 Guinea pig 5.5 pKi = 5.5 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 767 11 6 6 6.3 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL436209 168057 0 None -1621 2 Guinea pig 5.5 pKi = 5.5 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 767 11 6 6 6.3 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
11798204 192985 0 None -10 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 460 5 2 3 4.5 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2ccccc2cc1C(=O)N1CCC[C@@H]1C(=O)O 10.1021/jm9508907
CHEMBL53129 192985 0 None -10 2 Guinea pig 5.5 pKi = 5.5 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 460 5 2 3 4.5 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2ccccc2cc1C(=O)N1CCC[C@@H]1C(=O)O 10.1021/jm9508907
10815832 14998 0 None -109 2 Rat 7.4 pKi = 7.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 520 7 2 4 5.8 CSc1cccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
CHEMBL121021 14998 0 None -109 2 Rat 7.4 pKi = 7.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 520 7 2 4 5.8 CSc1cccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
CHEMBL218763 207644 0 None -3630 4 Human 5.4 pKi = 5.4 Binding
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
CHEMBL120632 206853 30 None -2187 3 Guinea pig 4.4 pKi = 4.4 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0000416
CHEMBL120632 206853 30 None -2187 3 Guinea pig 4.4 pKi = 4.4 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm9603072
9939572 37243 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL14557 37243 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL2067949 37243 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
16731711 85080 0 None -15 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 570 7 2 5 5.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1021/jm070139l
CHEMBL227369 85080 0 None -15 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 570 7 2 5 5.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1021/jm070139l
10676212 115496 0 None -489 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 701 8 4 5 5.9 O=C(O)c1cc(NC(=O)[C@H]2CCCN2C(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL335587 115496 0 None -489 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 701 8 4 5 5.9 O=C(O)c1cc(NC(=O)[C@H]2CCCN2C(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
44280162 98984 0 None -21 2 Guinea pig 5.4 pKi = 5.4 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 667 8 3 5 6.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N1CC[C@H](Oc2ccc(Cl)cc2Cl)C[C@@H]1C(=O)O 10.1016/s0960-894x(98)00231-5
CHEMBL283040 98984 0 None -21 2 Guinea pig 5.4 pKi = 5.4 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 667 8 3 5 6.9 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N1CC[C@H](Oc2ccc(Cl)cc2Cl)C[C@@H]1C(=O)O 10.1016/s0960-894x(98)00231-5
10324322 107206 0 None -43 2 Guinea pig 5.4 pKi = 5.4 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 518 10 2 4 4.7 CC(Cc1ccccc1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
CHEMBL319085 107206 0 None -43 2 Guinea pig 5.4 pKi = 5.4 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 518 10 2 4 4.7 CC(Cc1ccccc1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
10484529 100950 0 None -707 2 Guinea pig 5.4 pKi = 5.4 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 663 11 5 6 5.8 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccoc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL297480 100950 0 None -707 2 Guinea pig 5.4 pKi = 5.4 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 663 11 5 6 5.8 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccoc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
44272042 96586 0 None -131 2 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1274 26 13 15 2.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
CHEMBL266990 96586 0 None -131 2 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranesDisplacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes
ChEMBL 1274 26 13 15 2.1 CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](Cc2ccc(OS(=O)(=O)O)cc2)C(=O)N[C@@H](CCCC)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00126a007
16732021 167900 0 None -549 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 588 9 2 8 5.3 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(SCc3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL435143 167900 0 None -549 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 588 9 2 8 5.3 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(SCc3nn[nH]n3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
44451843 158880 0 None -1230 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 562 8 2 5 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(CC(=O)O)c2)C(=O)N(C2CCCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL410114 158880 0 None -1230 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 562 8 2 5 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(CC(=O)O)c2)C(=O)N(C2CCCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
53465844 69053 0 None 131 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-SR-27897 from human CCK1 I352A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 I352A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69053 0 None 131 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-SR-27897 from human CCK1 I352A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 I352A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL132314 206950 0 None -6456 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determinedBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determined
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)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/jm0303103
44461961 105117 0 None -446 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assayBinding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assay
ChEMBL 724 11 4 5 6.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N=[N+]=[N-])c(I)c1 10.1016/0960-894X(95)00435-V
CHEMBL2079605 105117 0 None -446 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assayBinding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assay
ChEMBL 724 11 4 5 6.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N=[N+]=[N-])c(I)c1 10.1016/0960-894X(95)00435-V
CHEMBL312252 105117 0 None -446 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assayBinding affinity towards CCK-A receptor in rat pancreas membrane using Hunter labelled CCK-8S assay
ChEMBL 724 11 4 5 6.8 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N[C@@H](CC(=O)O)Cc1ccc(N=[N+]=[N-])c(I)c1 10.1016/0960-894X(95)00435-V
11547802 135467 0 None -177 2 Guinea pig 6.4 pKi = 6.4 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 497 8 3 3 6.4 Cc1ccccc1-c1nc(C(=O)Nc2cccc(CC(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL373168 135467 0 None -177 2 Guinea pig 6.4 pKi = 6.4 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 497 8 3 3 6.4 Cc1ccccc1-c1nc(C(=O)Nc2cccc(CC(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
45486941 195079 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 516 7 2 6 4.2 O=C(NCCc1ccccc1)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL565325 195079 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 516 7 2 6 4.2 O=C(NCCc1ccccc1)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
45486964 195708 0 None -39 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 606 8 3 6 4.4 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
CHEMBL569391 195708 0 None -39 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from human CCK-1R after 100 mins by liquid scintillation counting
ChEMBL 606 8 3 6 4.4 O=C(N[C@@H](Cc1ccc(F)c(Br)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nccnc12 10.1016/j.bmcl.2009.09.065
887 4035 24 None -5011 4 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 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 10.1021/jm070880t
9870520 4035 24 None -5011 4 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 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 10.1021/jm070880t
CHEMBL324547 4035 24 None -5011 4 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 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 10.1021/jm070880t
DB12355 4035 24 None -5011 4 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 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 10.1021/jm070880t
45486949 195260 0 None -50 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 516 8 3 7 3.6 O=C(N[C@@H](Cc1ccccc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL566390 195260 0 None -50 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 516 8 3 7 3.6 O=C(N[C@@H](Cc1ccccc1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
45486970 195942 0 None -3 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 578 8 3 7 5.0 CC(C)(c1ccc(Cl)cc1)[C@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)C(=O)O 10.1016/j.bmcl.2009.09.064
CHEMBL570761 195942 0 None -3 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 578 8 3 7 5.0 CC(C)(c1ccc(Cl)cc1)[C@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)C(=O)O 10.1016/j.bmcl.2009.09.064
45486997 196096 0 None -12 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 486 7 1 6 4.5 CN(CCc1ccccc1)C(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL571832 196096 0 None -12 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 486 7 1 6 4.5 CN(CCc1ccccc1)C(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
9939572 37243 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL14557 37243 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL2067949 37243 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
10327180 37386 0 None - 1 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 676 11 5 6 5.5 Cn1ccc2cc(C(=O)N[C@@H](Cc3ccccc3)C(=O)Nc3cc(C(=O)O)cc(C(=O)O)c3)c(C(=O)NCC34CC5CC(CC(C5)C3)C4)cc21 10.1021/jm070880t
CHEMBL14571 37386 0 None - 1 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 676 11 5 6 5.5 Cn1ccc2cc(C(=O)N[C@@H](Cc3ccccc3)C(=O)Nc3cc(C(=O)O)cc(C(=O)O)c3)c(C(=O)NCC34CC5CC(CC(C5)C3)C4)cc21 10.1021/jm070880t
44425006 141536 0 None -3311 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 544 8 2 5 5.6 CC1CCCC1C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL388068 141536 0 None -3311 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 544 8 2 5 5.6 CC1CCCC1C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
44404001 11813 0 None -6 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 635 11 6 6 4.5 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2nc[nH]c2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(CO)cc(CO)c1 10.1021/jm049069y
CHEMBL1182744 11813 0 None -6 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 635 11 6 6 4.5 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2nc[nH]c2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(CO)cc(CO)c1 10.1021/jm049069y
CHEMBL2067969 11813 0 None -6 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 635 11 6 6 4.5 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2nc[nH]c2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(CO)cc(CO)c1 10.1021/jm049069y
44403982 12157 0 None -7 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 4.9 CN(C(=O)[C@H](Cc1ccccc1)NC(=O)c1cc2[nH]cnc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2)c1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184798 12157 0 None -7 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 4.9 CN(C(=O)[C@H](Cc1ccccc1)NC(=O)c1cc2[nH]cnc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2)c1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067958 12157 0 None -7 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 677 11 5 6 4.9 CN(C(=O)[C@H](Cc1ccccc1)NC(=O)c1cc2[nH]cnc2cc1C(=O)NCC12CC3CC(CC(C3)C1)C2)c1cc(C(=O)O)cc(C(=O)O)c1 10.1021/jm049069y
9939572 37243 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL14557 37243 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067949 37243 0 None -3548 3 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 662 11 6 5 5.5 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3cc[nH]c3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
9890720 167894 0 None -2 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 466 6 3 2 7.3 O=C(O)c1cccc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)c1 10.1021/jm049069y
CHEMBL2067971 167894 0 None -2 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 466 6 3 2 7.3 O=C(O)c1cccc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)c1 10.1021/jm049069y
CHEMBL435127 167894 0 None -2 2 Guinea pig 5.4 pKi = 5.4 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 466 6 3 2 7.3 O=C(O)c1cccc(NC(=O)c2cc(-c3ccc4ccccc4c3)[nH]c2CC2CCCCCC2)c1 10.1021/jm049069y
10509945 88940 0 None 229 2 Rat 8.4 pKi = 8.4 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
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/jm990252e
CHEMBL2369816 88940 0 None 229 2 Rat 8.4 pKi = 8.4 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
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/jm990252e
CHEMBL384035 210559 1 None -22 4 Rat 8.4 pKi = 8.4 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
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/jm00389a002
CHEMBL428666 210559 1 None -22 4 Rat 8.4 pKi = 8.4 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
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/jm00389a002
10508430 16148 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 648 18 6 6 1.8 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)CC 10.1021/jm0000416
CHEMBL122872 16148 0 None - 1 Guinea pig 8.4 pKi = 8.4 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
ChEMBL 648 18 6 6 1.8 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)CC 10.1021/jm0000416
44332766 107837 0 None 48 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 474 6 2 3 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2cc(F)ccc21 10.1016/0960-894X(95)00528-2
CHEMBL319795 107837 0 None 48 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 474 6 2 3 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2cc(F)ccc21 10.1016/0960-894X(95)00528-2
19043395 4690 0 None 194 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 490 6 2 3 5.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2cc(Cl)ccc21 10.1016/0960-894X(95)00528-2
CHEMBL103968 4690 0 None 194 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 490 6 2 3 5.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2cc(Cl)ccc21 10.1016/0960-894X(95)00528-2
53465844 69053 0 None 131 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-SR-27897 from human CCK1 F330A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 F330A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69053 0 None 131 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-SR-27897 from human CCK1 F330A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 F330A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
44265985 205929 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 376 6 2 1 6.0 O=C(NCCC=C(c1ccccc1)c1ccccc1)Nc1ccc(Cl)cc1 10.1021/jm00084a009
CHEMBL9538 205929 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 376 6 2 1 6.0 O=C(NCCC=C(c1ccccc1)c1ccccc1)Nc1ccc(Cl)cc1 10.1021/jm00084a009
44265913 204857 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 381 5 1 1 5.9 O=C(NCC=C(c1ccccc1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1021/jm00084a009
CHEMBL8893 204857 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 381 5 1 1 5.9 O=C(NCC=C(c1ccccc1)c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1021/jm00084a009
10604230 114700 0 None -5 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 645 10 4 4 4.8 O=C(O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
CHEMBL334523 114700 0 None -5 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 645 10 4 4 4.8 O=C(O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
10676196 118722 0 None -234 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 699 11 5 5 6.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC2CCCCC2)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL343515 118722 0 None -234 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 699 11 5 5 6.0 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC2CCCCC2)cc(C(=O)O)c1 10.1021/jm00021a019
56673523 63804 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 479 10 2 4 3.9 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808413 63804 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 479 10 2 4 3.9 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/j.bmc.2011.05.057
16732018 85029 0 None -741 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 548 9 2 6 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(OCC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL226729 85029 0 None -741 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 548 9 2 6 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(OCC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
10769001 112669 0 None -13803 2 Rat 5.4 pKi = 5.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 549 5 3 4 5.7 Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL331468 112669 0 None -13803 2 Rat 5.4 pKi = 5.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 549 5 3 4 5.7 Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
10390666 206554 0 None -17 2 Guinea pig 5.4 pKi = 5.4 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 485 7 3 3 5.3 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCc1ccccc1 10.1021/jm00072a005
CHEMBL99076 206554 0 None -17 2 Guinea pig 5.4 pKi = 5.4 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 485 7 3 3 5.3 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCc1ccccc1 10.1021/jm00072a005
19043358 4280 0 None 22 2 Rat 7.4 pKi = 7.4 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 490 6 2 3 5.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccc(Cl)cc21 10.1016/0960-894X(95)00528-2
CHEMBL101125 4280 0 None 22 2 Rat 7.4 pKi = 7.4 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 490 6 2 3 5.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccc(Cl)cc21 10.1016/0960-894X(95)00528-2
44408524 155152 0 None -169 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1134 30 12 15 2.6 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](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL405192 155152 0 None -169 4 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1134 30 12 15 2.6 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](Cc1cn(C(=O)OC(C)(C)C)c2ccccc12)C(=O)O 10.1021/jm050851n
11605694 168077 0 None -70 3 Guinea pig 6.4 pKi = 6.4 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 497 7 3 3 6.8 Cc1ccc(NC(=O)c2[nH]c(-c3ccccc3C)nc2CCC23CC4CC(CC(C4)C2)C3)cc1C(=O)O 10.1021/jm0490686
CHEMBL436314 168077 0 None -70 3 Guinea pig 6.4 pKi = 6.4 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 497 7 3 3 6.8 Cc1ccc(NC(=O)c2[nH]c(-c3ccccc3C)nc2CCC23CC4CC(CC(C4)C2)C3)cc1C(=O)O 10.1021/jm0490686
10818497 25633 0 None -58 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 701 8 4 5 5.9 O=C(O)c1cc(NC(=O)[C@@H]2CCCN2C(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL135344 25633 0 None -58 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 701 8 4 5 5.9 O=C(O)c1cc(NC(=O)[C@@H]2CCCN2C(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL3351054 209782 0 None -812 2 Guinea pig 5.4 pKi = 5.4 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccc2ccccc2c1)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
9983949 205997 0 None -23 2 Guinea pig 5.4 pKi = 5.4 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 513 9 3 3 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCCc1ccccc1 10.1021/jm00072a005
CHEMBL95793 205997 0 None -23 2 Guinea pig 5.4 pKi = 5.4 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 513 9 3 3 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)NCCCc1ccccc1 10.1021/jm00072a005
52949124 861 2 None -2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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 861 2 None -2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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 861 2 None -2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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 861 2 None -2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] 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
10531553 116117 0 None -31 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 595 7 3 4 4.0 O=C(O)CNC(=O)[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3 10.1021/jm00021a019
CHEMBL336896 116117 0 None -31 2 Guinea pig 5.4 pKi = 5.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 595 7 3 4 4.0 O=C(O)CNC(=O)[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12C[C@H]3C[C@@H](C1)C[C@@H](C2)C3 10.1021/jm00021a019
44346345 112572 0 None -43 2 Rat 7.4 pKi = 7.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 523 5 2 4 5.1 CN(C)c1cccc(NC(=O)NC2C(=O)N(c3ccccc3)c3ccccc3N(C3CC4CCC3C4)C2=O)c1 10.1021/jm990967h
CHEMBL331262 112572 0 None -43 2 Rat 7.4 pKi = 7.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 523 5 2 4 5.1 CN(C)c1cccc(NC(=O)NC2C(=O)N(c3ccccc3)c3ccccc3N(C3CC4CCC3C4)C2=O)c1 10.1021/jm990967h
10747623 168903 0 None -29 2 Guinea pig 6.4 pKi = 6.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 746 12 6 5 6.1 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCCc2c[nH]c3ccccc23)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL443028 168903 0 None -29 2 Guinea pig 6.4 pKi = 6.4 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 746 12 6 5 6.1 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCCc2c[nH]c3ccccc23)cc(C(=O)O)c1 10.1021/jm00021a019
44451519 95300 0 None -58 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 518 6 1 4 6.1 Cc1cccc(NC(=O)CN2C(=O)N(CC(=O)C(C)(C)C)c3ccccc3N(C3CCCCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
CHEMBL258486 95300 0 None -58 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 518 6 1 4 6.1 Cc1cccc(NC(=O)CN2C(=O)N(CC(=O)C(C)(C)C)c3ccccc3N(C3CCCCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
10579091 14242 0 None -398 2 Rat 6.4 pKi = 6.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 577 6 2 4 6.2 CN(C)c1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL120021 14242 0 None -398 2 Rat 6.4 pKi = 6.4 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 577 6 2 4 6.2 CN(C)c1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
44265914 204942 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 363 5 1 1 5.7 O=C(NCC=C(c1ccccc1)c1ccccc1)c1ccc2ccccc2c1 10.1021/jm00084a009
CHEMBL8949 204942 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 363 5 1 1 5.7 O=C(NCC=C(c1ccccc1)c1ccccc1)c1ccc2ccccc2c1 10.1021/jm00084a009
16732162 141549 0 None -1862 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 584 8 2 6 6.4 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3ccc(C(=O)O)o3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL388144 141549 0 None -1862 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 584 8 2 6 6.4 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3ccc(C(=O)O)o3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
10004216 4660 0 None -11 2 Rat 5.3 pKi = 5.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL103750 4660 0 None -11 2 Rat 5.3 pKi = 5.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 456 6 2 3 4.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
44346255 116368 0 None -30 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 564 6 2 7 6.7 CC(C)(C1CCCC1)N1C(=O)C(NC(=O)Nc2cccc(C3N=NN=N3)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL338278 116368 0 None -30 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 564 6 2 7 6.7 CC(C)(C1CCCC1)N1C(=O)C(NC(=O)Nc2cccc(C3N=NN=N3)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
19700643 63673 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 505 9 2 4 4.5 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1807152 63673 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 505 9 2 4 4.5 CCN(CC)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CC2CCCCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
135423404 85073 0 None -4365 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 570 8 2 7 5.0 O=C(CN1N=C(C2CCCCC2)c2ccccc2N(CC(=O)C2CCCC2)C1=O)Nc1cccc(-c2noc(=O)[nH]2)c1 10.1021/jm070139l
CHEMBL227276 85073 0 None -4365 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 570 8 2 7 5.0 O=C(CN1N=C(C2CCCCC2)c2ccccc2N(CC(=O)C2CCCC2)C1=O)Nc1cccc(-c2noc(=O)[nH]2)c1 10.1021/jm070139l
5311201 205653 30 None -2570 6 Guinea pig 6.3 pKi = 6.3 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00048a001
CHEMBL9387 205653 30 None -2570 6 Guinea pig 6.3 pKi = 6.3 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 398 3 2 3 4.0 Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1 10.1021/jm00048a001
115208 3746 25 None -91 4 Rat 7.3 pKi = 7.3 Binding
Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.
ChEMBL 393 4 1 4 4.0 O=C(c1ccsc1)NCC1CN=C(c2c(N1C)cccc2)c1ccccc1F 10.1021/jm950423p
1667 3746 25 None -91 4 Rat 7.3 pKi = 7.3 Binding
Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.
ChEMBL 393 4 1 4 4.0 O=C(c1ccsc1)NCC1CN=C(c2c(N1C)cccc2)c1ccccc1F 10.1021/jm950423p
CHEMBL169703 3746 25 None -91 4 Rat 7.3 pKi = 7.3 Binding
Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.Binding affinity against Cholecystokinin type A receptor using [125I](BH)-CCK-8 as radioligand in rat pancreas.
ChEMBL 393 4 1 4 4.0 O=C(c1ccsc1)NCC1CN=C(c2c(N1C)cccc2)c1ccccc1F 10.1021/jm950423p
44346126 15082 0 None -27 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 514 4 2 3 5.7 O=C(Nc1cccc(Cl)c1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2CC3CCC2C3)C1=O 10.1021/jm990967h
CHEMBL121267 15082 0 None -27 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 514 4 2 3 5.7 O=C(Nc1cccc(Cl)c1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2CC3CCC2C3)C1=O 10.1021/jm990967h
10792618 163790 0 None -70 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 543 7 2 4 5.7 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC3CCCC3)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
CHEMBL421271 163790 0 None -70 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 543 7 2 4 5.7 CN(C)c1cccc(NC(=O)NC2C(=O)N(CCC3CCCC3)c3ccccc3N(c3ccccc3F)C2=O)c1 10.1021/jm990967h
44265917 205870 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 364 5 1 2 5.1 O=C(NCC=C(c1ccccc1)c1ccccc1)c1ccc2ccccc2n1 10.1021/jm00084a009
CHEMBL9510 205870 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranesDisplacement of [3H]L-364718 from Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 364 5 1 2 5.1 O=C(NCC=C(c1ccccc1)c1ccccc1)c1ccc2ccccc2n1 10.1021/jm00084a009
9850043 112362 1 None -446 3 Rat 6.3 pKi = 6.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL330977 112362 1 None -446 3 Rat 6.3 pKi = 6.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
10603576 14331 0 None -19 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 594 8 2 7 5.6 CC(C)Cn1nnc(-c2cccc(NC(=O)NC3C(=O)N(CCC(C)(C)C)c4ccccc4N(c4ccccc4)C3=O)c2)n1 10.1021/jm990967h
CHEMBL120168 14331 0 None -19 2 Rat 7.3 pKi = 7.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 594 8 2 7 5.6 CC(C)Cn1nnc(-c2cccc(NC(=O)NC3C(=O)N(CCC(C)(C)C)c4ccccc4N(c4ccccc4)C3=O)c2)n1 10.1021/jm990967h
10747599 25641 0 None -46 2 Guinea pig 6.3 pKi = 6.3 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 743 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCc2cccc3ccccc23)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL135350 25641 0 None -46 2 Guinea pig 6.3 pKi = 6.3 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 743 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCc2cccc3ccccc23)cc(C(=O)O)c1 10.1021/jm00021a019
13605417 205824 3 None - 1 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
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/jm00084a009
CHEMBL9485 205824 3 None - 1 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
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/jm00084a009
53465844 69053 0 None 131 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-BH-JMV-179 from human CCK1 receptor N333A mutant expressed in COS7 cells after 60 mins by gamma countingDisplacement of [125I]-BH-JMV-179 from human CCK1 receptor N333A mutant expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69053 0 None 131 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-BH-JMV-179 from human CCK1 receptor N333A mutant expressed in COS7 cells after 60 mins by gamma countingDisplacement of [125I]-BH-JMV-179 from human CCK1 receptor N333A mutant expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
53465844 69053 0 None 131 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-SR-27897 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69053 0 None 131 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-SR-27897 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from wild type human CCK1 receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
10507109 108727 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
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 108727 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
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
11512151 195101 0 None 158 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 534 7 2 6 5.5 CC(C)(CNC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.09.064
CHEMBL565511 195101 0 None 158 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 534 7 2 6 5.5 CC(C)(CNC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.09.064
44328951 164034 0 None -3 2 Human 7.3 pKi = 7.3 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line (n=1)
ChEMBL 533 5 2 4 3.8 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(c2ccccc2F)C1=O 10.1016/S0960-894X(96)00613-0
CHEMBL421575 164034 0 None -3 2 Human 7.3 pKi = 7.3 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line (n=1)
ChEMBL 533 5 2 4 3.8 O=C(Nc1ccc(F)cc1)NC1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(c2ccccc2F)C1=O 10.1016/S0960-894X(96)00613-0
11556194 195872 0 None -3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 598 8 3 7 5.4 C[C@H](c1ccc(Cl)c(Cl)c1)[C@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)C(=O)O 10.1016/j.bmcl.2009.09.064
CHEMBL570297 195872 0 None -3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 598 8 3 7 5.4 C[C@H](c1ccc(Cl)c(Cl)c1)[C@H](NC(=O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12)C(=O)O 10.1016/j.bmcl.2009.09.064
9832467 143749 0 None -602 5 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 477 7 3 4 5.9 O=C(O)c1cccc(NC(=O)c2nc(C3CCCCC3)[nH]c2COC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm070880t
CHEMBL390519 143749 0 None -602 5 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 477 7 3 4 5.9 O=C(O)c1cccc(NC(=O)c2nc(C3CCCCC3)[nH]c2COC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm070880t
11555110 11846 0 None -5 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 500 7 5 4 5.7 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccc4[nH]ccc4c3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1182962 11846 0 None -5 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 500 7 5 4 5.7 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccc4[nH]ccc4c3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067954 11846 0 None -5 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 500 7 5 4 5.7 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccc4[nH]ccc4c3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
44403999 12163 0 None -12 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 619 10 5 5 5.2 O=C(O)c1cccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm049069y
CHEMBL1184841 12163 0 None -12 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 619 10 5 5 5.2 O=C(O)c1cccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm049069y
CHEMBL2067962 12163 0 None -12 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 619 10 5 5 5.2 O=C(O)c1cccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm049069y
11605951 12165 0 None -25 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 512 8 4 3 6.5 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184851 12165 0 None -25 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 512 8 4 3 6.5 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067961 12165 0 None -25 2 Guinea pig 5.3 pKi = 5.3 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 512 8 4 3 6.5 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
73356071 88942 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
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@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL2369818 88942 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
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@@H](CC(=O)O)C(=O)N(C)[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm990252e
CHEMBL382349 210545 0 None -3235 4 Human 5.3 pKi = 5.3 Binding
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](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
56663145 63798 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 541 8 2 5 3.9 Cc1cccc(Cl)c1NC(=O)NC1C(=O)N(CCC(C)C)c2ccccc2N(CCN2CCOCC2)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808407 63798 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 541 8 2 5 3.9 Cc1cccc(Cl)c1NC(=O)NC1C(=O)N(CCC(C)C)c2ccccc2N(CCN2CCOCC2)C1=O 10.1016/j.bmc.2011.05.057
19700618 63799 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 523 9 2 6 2.9 COc1ccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN3CCOCC3)C2=O)cc1 10.1016/j.bmc.2011.05.057
CHEMBL1808408 63799 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 523 9 2 6 2.9 COc1ccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN3CCOCC3)C2=O)cc1 10.1016/j.bmc.2011.05.057
118719287 114972 0 None -6 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL 727 17 4 7 4.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cccc2ccccc12)N(C)C)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
CHEMBL3351059 114972 0 None -6 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL 727 17 4 7 4.8 CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cccc2ccccc12)N(C)C)C(=O)N(C)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
CHEMBL3142842 209379 0 None -2 2 Guinea pig 5.3 pKi = 5.3 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CC(C)(C)OC(=O)NCCC[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/jm00174a016
53465844 69053 0 None 131 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SR-27897 from human CCK1 R336A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 R336A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69053 0 None 131 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SR-27897 from human CCK1 R336A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 R336A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
11518283 165596 0 None -74 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 461 7 3 3 6.2 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL426290 165596 0 None -74 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 461 7 3 3 6.2 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
10482868 106907 0 None -37 5 Rat 6.3 pKi = 6.3 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 557 10 3 4 5.2 CC(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 10.1021/jm00072a005
CHEMBL317999 106907 0 None -37 5 Rat 6.3 pKi = 6.3 Binding
Tested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligandTested for binding affinity towards cholecystokinin type A receptor in rat pancreas by displacement of [3H]pCCK-8 radioligand
ChEMBL 557 10 3 4 5.2 CC(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 10.1021/jm00072a005
11613212 71742 0 None -39 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 513 7 3 4 6.4 Cc1cc(C)c(-c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(COC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
CHEMBL197780 71742 0 None -39 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 513 7 3 4 6.4 Cc1cc(C)c(-c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(COC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
56666597 63797 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 585 8 2 5 4.0 Cc1cc(Br)ccc1NC(=O)NC1C(=O)N(CCC(C)C)c2ccccc2N(CCN2CCOCC2)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808405 63797 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 585 8 2 5 4.0 Cc1cc(Br)ccc1NC(=O)NC1C(=O)N(CCC(C)C)c2ccccc2N(CCN2CCOCC2)C1=O 10.1016/j.bmc.2011.05.057
118719284 114970 0 None -72 2 Guinea pig 5.3 pKi = 5.3 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL 739 15 5 7 4.9 CN(C)[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C)C1CCCCC1 10.1021/jm00053a022
CHEMBL3351056 114970 0 None -72 2 Guinea pig 5.3 pKi = 5.3 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL 739 15 5 7 4.9 CN(C)[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C)C1CCCCC1 10.1021/jm00053a022
16733185 141548 0 None -346 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 594 8 2 5 6.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3cccc(C(=O)O)c3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL388143 141548 0 None -346 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 594 8 2 5 6.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3cccc(C(=O)O)c3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
16732164 142759 0 None -1862 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 571 8 2 6 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3ccn(CC(=O)O)c3c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL389711 142759 0 None -1862 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 571 8 2 6 5.5 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3ccn(CC(=O)O)c3c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
10623068 112330 0 None -89 2 Rat 6.3 pKi = 6.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 442 6 2 3 4.7 CCCCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL330854 112330 0 None -89 2 Rat 6.3 pKi = 6.3 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 442 6 2 3 4.7 CCCCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL1172246 206829 0 None 1 4 Human 6.3 pKi = 6.3 Binding
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
44408483 168352 0 None -165 4 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.7 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](Cc1cn(C(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL438739 168352 0 None -165 4 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.7 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](Cc1cn(C(=O)OC2C3CC4CC(C3)CC2C4)c2ccccc12)C(=O)O 10.1021/jm050851n
11511706 71902 0 None -12 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 501 7 3 3 6.6 Cc1ccccc1-c1nc(C(=O)Nc2ccc(F)c(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL198225 71902 0 None -12 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 501 7 3 3 6.6 Cc1ccccc1-c1nc(C(=O)Nc2ccc(F)c(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
11571142 135270 0 None -346 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 489 7 3 3 6.7 CC1(c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)CCCCC1 10.1021/jm0490686
CHEMBL373050 135270 0 None -346 3 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 489 7 3 3 6.7 CC1(c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)CCCCC1 10.1021/jm0490686
9832467 143749 0 None -602 5 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 477 7 3 4 5.9 O=C(O)c1cccc(NC(=O)c2nc(C3CCCCC3)[nH]c2COC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL390519 143749 0 None -602 5 Guinea pig 6.3 pKi = 6.3 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 477 7 3 4 5.9 O=C(O)c1cccc(NC(=O)c2nc(C3CCCCC3)[nH]c2COC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
10256780 112169 0 None -234 2 Rat 6.3 pKi = 6.3 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 540 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(C2CCCCC2)C1=O 10.1016/S0960-894X(96)00544-6
CHEMBL330409 112169 0 None -234 2 Rat 6.3 pKi = 6.3 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 540 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(C2CCCCC2)C1=O 10.1016/S0960-894X(96)00544-6
CHEMBL262172 208773 0 None -26302 4 Human 5.2 pKi = 5.2 Binding
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](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 10.1021/jm050921q
10626665 10149 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific 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/jm9703247
CHEMBL116127 10149 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific 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/jm9703247
11540160 71089 0 None -117 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 475 7 3 3 6.6 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CCCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL196133 71089 0 None -117 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 475 7 3 3 6.6 O=C(O)c1cccc(NC(=O)c2[nH]c(C3CCCCC3)nc2CCC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
16732443 85058 0 None -1202 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 532 7 2 5 5.6 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL227147 85058 0 None -1202 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 532 7 2 5 5.6 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(C(=O)O)c2)N=C(C2CCCCCC2)c2ccccc21 10.1021/jm070139l
135610887 85003 0 None -2951 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 558 7 2 7 4.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL226583 85003 0 None -2951 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 558 7 2 7 4.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
11656338 75577 0 None -389 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 504 7 2 5 5.0 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(CO)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm051219x
CHEMBL205198 75577 0 None -389 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 504 7 2 5 5.0 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(CO)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm051219x
10071178 74131 1 None 501 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins 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 74131 1 None 501 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins 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
10367509 106943 0 None -14 2 Guinea pig 5.2 pKi = 5.2 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 471 6 3 3 5.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)Nc1ccccc1 10.1021/jm00072a005
CHEMBL318238 106943 0 None -14 2 Guinea pig 5.2 pKi = 5.2 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 471 6 3 3 5.7 CC(Cc1c[nH]c2ccccc12)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)Nc1ccccc1 10.1021/jm00072a005
44331505 4272 0 None -25 2 Rat 7.2 pKi = 7.2 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 450 8 2 3 4.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL101063 4272 0 None -25 2 Rat 7.2 pKi = 7.2 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 450 8 2 3 4.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/S0960-894X(96)00544-6
10794691 116548 0 None 1 2 Guinea pig 6.2 pKi = 6.2 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 684 10 5 4 5.3 O=C(O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
CHEMBL339177 116548 0 None 1 2 Guinea pig 6.2 pKi = 6.2 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 684 10 5 4 5.3 O=C(O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm00021a019
11679213 133007 0 None -61 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 497 7 3 3 6.8 Cc1ccc(-c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
CHEMBL370882 133007 0 None -61 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 497 7 3 3 6.8 Cc1ccc(-c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
44451522 157757 0 None -26 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 531 6 1 4 5.1 Cc1cccc(NC(=O)CN2C(=O)N(CC(=O)N3CCCC3)c3ccccc3N(C3CCCCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
CHEMBL408915 157757 0 None -26 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 531 6 1 4 5.1 Cc1cccc(NC(=O)CN2C(=O)N(CC(=O)N3CCCC3)c3ccccc3N(C3CCCCCC3)C2=O)c1 10.1016/j.bmc.2007.12.047
CHEMBL1206334 206854 0 None -1023 2 Guinea pig 7.2 pKi = 7.2 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](N)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@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80678-2
CHEMBL262894 206854 0 None -1023 2 Guinea pig 7.2 pKi = 7.2 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](N)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@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/S0960-894X(00)80678-2
11541048 195290 0 None 7 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 530 7 2 6 4.8 C[C@H](CNC(=O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccccc1 10.1016/j.bmcl.2009.09.064
CHEMBL566604 195290 0 None 7 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 530 7 2 6 4.8 C[C@H](CNC(=O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccccc1 10.1016/j.bmcl.2009.09.064
44444934 154395 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 749 16 6 7 4.8 COc1ccc(CCNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)cc1 10.1021/jm070880t
CHEMBL401098 154395 0 None - 1 Guinea pig 7.2 pKi = 7.2 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 749 16 6 7 4.8 COc1ccc(CCNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC(C)(C)C)cc1 10.1021/jm070880t
11801315 114263 0 None -50 2 Rat 7.2 pKi = 7.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 577 6 2 4 6.0 CN(C)c1cccc(NC(=O)NC2C(=O)N(CC3[C@H]4C[C@@H]5C[C@@H](C[C@H]3C5)C4)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL333930 114263 0 None -50 2 Rat 7.2 pKi = 7.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 577 6 2 4 6.0 CN(C)c1cccc(NC(=O)NC2C(=O)N(CC3[C@H]4C[C@@H]5C[C@@H](C[C@H]3C5)C4)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
108187 911 30 None -4265 5 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic 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/jm070880t
873 911 30 None -4265 5 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic 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/jm070880t
CHEMBL2062154 911 30 None -4265 5 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic 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/jm070880t
CHEMBL287735 911 30 None -4265 5 Guinea pig 6.2 pKi = 6.2 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic 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/jm070880t
10698427 14370 0 None -645 2 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 578 6 3 4 5.8 O=C(Nc1cccc(C(=O)O)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL120363 14370 0 None -645 2 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 578 6 3 4 5.8 O=C(Nc1cccc(C(=O)O)c1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
10555899 112861 0 None -2344 2 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 623 8 5 6 5.2 CC(O)C(O)Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL331763 112861 0 None -2344 2 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 623 8 5 6 5.2 CC(O)C(O)Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL3351062 209787 0 None -173 2 Guinea pig 5.2 pKi = 5.2 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
11535277 12158 0 None -10 2 Guinea pig 5.2 pKi = 5.2 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 513 8 4 4 5.9 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184817 12158 0 None -10 2 Guinea pig 5.2 pKi = 5.2 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 513 8 4 4 5.9 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067964 12158 0 None -10 2 Guinea pig 5.2 pKi = 5.2 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 513 8 4 4 5.9 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
10457639 107213 0 None - 1 Guinea pig 5.2 pKi = 5.2 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 474 8 4 2 5.3 CC(Cc1c[nH]c2ccccc12)(NC(=O)Nc1ccc(Cl)cc1)C(=O)NCCc1ccccc1 10.1021/jm00072a005
CHEMBL319096 107213 0 None - 1 Guinea pig 5.2 pKi = 5.2 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 474 8 4 2 5.3 CC(Cc1c[nH]c2ccccc12)(NC(=O)Nc1ccc(Cl)cc1)C(=O)NCCc1ccccc1 10.1021/jm00072a005
16732911 142672 0 None -999 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 564 9 2 6 5.6 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(SCC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL389639 142672 0 None -999 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 564 9 2 6 5.6 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(SCC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
16732017 85028 0 None -6025 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 561 9 2 6 5.0 CN(CC(=O)O)c1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm070139l
CHEMBL226726 85028 0 None -6025 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 561 9 2 6 5.0 CN(CC(=O)O)c1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm070139l
16732020 85071 0 None -3311 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 571 8 2 8 4.7 CN(c1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1)c1nn[nH]n1 10.1021/jm070139l
CHEMBL227254 85071 0 None -3311 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 571 8 2 8 4.7 CN(c1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1)c1nn[nH]n1 10.1021/jm070139l
CHEMBL383458 210556 0 None -10 4 Human 5.2 pKi = 5.2 Binding
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](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 10.1021/jm050921q
44331468 4207 0 None -16 2 Rat 7.2 pKi = 7.2 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 470 7 2 3 4.8 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(Cc2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL100685 4207 0 None -16 2 Rat 7.2 pKi = 7.2 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 470 7 2 3 4.8 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(Cc2ccccc2)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL2370441 208096 0 None -2 2 Guinea pig 6.2 pKi = 6.2 Binding
Apparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranesApparent affinity to inhibit binding of [3H]pCCK-8 to Cholecystokinin type A receptor of guinea pig pancreatic membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccc(S(=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](CCCNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm00174a016
11542079 71363 0 None -11 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 483 7 3 3 6.5 Cc1ccccc1-c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
CHEMBL196580 71363 0 None -11 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 483 7 3 3 6.5 Cc1ccccc1-c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC23CC4CC(CC(C4)C2)C3)[nH]1 10.1021/jm0490686
11685703 71561 0 None -25 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 391 7 3 3 4.9 Cc1ccccc1-c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC(C)C)[nH]1 10.1021/jm0490686
CHEMBL197205 71561 0 None -25 3 Guinea pig 6.2 pKi = 6.2 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 391 7 3 3 4.9 Cc1ccccc1-c1nc(C(=O)Nc2cccc(C(=O)O)c2)c(CCC(C)C)[nH]1 10.1021/jm0490686
16733307 168246 0 None -1819 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 585 8 2 7 5.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(C(=O)O)co3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL437736 168246 0 None -1819 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 585 8 2 7 5.8 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(-c3nc(C(=O)O)co3)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
10697783 117117 0 None -141 2 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 543 7 2 4 5.7 CN(C)c1ccc(NC(=O)NC2C(=O)N(CCC3CCCC3)c3ccccc3N(c3ccccc3F)C2=O)cc1 10.1021/jm990967h
CHEMBL340107 117117 0 None -141 2 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 543 7 2 4 5.7 CN(C)c1ccc(NC(=O)NC2C(=O)N(CCC3CCCC3)c3ccccc3N(c3ccccc3F)C2=O)cc1 10.1021/jm990967h
56673429 63585 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 537 9 2 6 3.3 COc1ccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN3CCOCC3)C2=O)c(C)c1 10.1016/j.bmc.2011.05.057
CHEMBL1806517 63585 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 537 9 2 6 3.3 COc1ccc(NC(=O)NC2C(=O)N(CCC(C)C)c3ccccc3N(CCN3CCOCC3)C2=O)c(C)c1 10.1016/j.bmc.2011.05.057
19700612 63791 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 493 8 2 5 2.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808398 63791 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 493 8 2 5 2.9 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
16732594 14237 0 None -2511 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 572 8 2 7 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc3c2cnn3CC(=O)O)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL1161950 14237 0 None -2511 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 572 8 2 7 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc3c2cnn3CC(=O)O)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL1200187 14237 0 None -2511 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 572 8 2 7 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc3c2cnn3CC(=O)O)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
44303372 200981 0 None - 1 Mouse 8.2 pKi = 8.2 Binding
Binding affinity in Cholecystokinin type A receptor binding assay (iv) in miceBinding affinity in Cholecystokinin type A receptor binding assay (iv) in mice
ChEMBL 317 7 2 3 2.0 CCCCNC(=O)[C@@H]1Cc2ccccc2N1C(=O)CC(N)CC 10.1021/jm980521l
CHEMBL61498 200981 0 None - 1 Mouse 8.2 pKi = 8.2 Binding
Binding affinity in Cholecystokinin type A receptor binding assay (iv) in miceBinding affinity in Cholecystokinin type A receptor binding assay (iv) in mice
ChEMBL 317 7 2 3 2.0 CCCCNC(=O)[C@@H]1Cc2ccccc2N1C(=O)CC(N)CC 10.1021/jm980521l
10768190 112320 0 None -15 2 Rat 8.1 pKi = 8.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 516 6 2 4 6.0 CSc1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL330773 112320 0 None -15 2 Rat 8.1 pKi = 8.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 516 6 2 4 6.0 CSc1cccc(NC(=O)NC2C(=O)N(CCC(C)(C)C)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
53465844 69053 0 None 131 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-SR-27897 from human CCK1 M195A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 M195A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933104 69053 0 None 131 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-SR-27897 from human CCK1 M195A mutant receptor expressed in COS7 cells after 60 mins by gamma countingDisplacement of [3H]-SR-27897 from human CCK1 M195A mutant receptor expressed in COS7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
10460632 206579 0 None 43 2 Guinea pig 7.2 pKi = 7.2 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 568 10 2 4 5.8 CC(Cc1ccc2ccccc2c1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
CHEMBL99252 206579 0 None 43 2 Guinea pig 7.2 pKi = 7.2 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 568 10 2 4 5.8 CC(Cc1ccc2ccccc2c1)(NC(=O)OC1[C@H]2C[C@@H]3C[C@@H](C[C@H]1C3)C2)C(=O)N(CCc1ccccc1)CC(=O)O 10.1021/jm00072a005
10696354 112978 0 None -74 2 Rat 7.2 pKi = 7.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 488 5 2 3 5.5 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
CHEMBL331971 112978 0 None -74 2 Rat 7.2 pKi = 7.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 488 5 2 3 5.5 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
16100410 141254 0 None -6309 4 Human 5.2 pKi = 5.2 Binding
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
CHEMBL386212 141254 0 None -6309 4 Human 5.2 pKi = 5.2 Binding
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
9850043 112051 1 None -309 2 Rat 6.2 pKi = 6.2 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(c2ccccc2)C1=O 10.1016/S0960-894X(96)00544-6
CHEMBL329984 112051 1 None -309 2 Rat 6.2 pKi = 6.2 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc2N(c2ccccc2)C1=O 10.1016/S0960-894X(96)00544-6
9850043 112362 1 None -446 3 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL330977 112362 1 None -446 3 Rat 6.2 pKi = 6.2 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.1 O=C(Nc1ccccc1)NC1C(=O)N(CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
44425005 141910 0 None -79 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 478 7 2 5 4.2 CC(C)C1=NN(CC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(CC(=O)C(C)(C)C)c2ccccc21 10.1021/jm070139l
CHEMBL389019 141910 0 None -79 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 478 7 2 5 4.2 CC(C)C1=NN(CC(=O)Nc2cccc(C(=O)O)c2)C(=O)N(CC(=O)C(C)(C)C)c2ccccc21 10.1021/jm070139l
136036821 95351 0 None -3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 602 9 2 7 5.6 CC(C)(C)C(=O)CN1C(=O)N(CCCC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)C(=O)N(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
CHEMBL258782 95351 0 None -3 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO-K1 cells
ChEMBL 602 9 2 7 5.6 CC(C)(C)C(=O)CN1C(=O)N(CCCC(=O)Nc2cccc(-c3nc(=O)o[nH]3)c2)C(=O)N(C2CCCCC2)c2ccccc21 10.1016/j.bmc.2007.12.047
9958214 114282 0 None -269 2 Rat 7.1 pKi = 7.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 517 7 2 4 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
CHEMBL333979 114282 0 None -269 2 Rat 7.1 pKi = 7.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 517 7 2 4 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(c2ccccc2F)c2ccccc21 10.1021/jm990967h
11613179 71429 0 None -83 3 Guinea pig 6.1 pKi = 6.1 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 511 7 3 3 7.1 Cc1cc(C)c(-c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
CHEMBL196745 71429 0 None -83 3 Guinea pig 6.1 pKi = 6.1 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 511 7 3 3 7.1 Cc1cc(C)c(-c2nc(C(=O)Nc3cccc(C(=O)O)c3)c(CCC34CC5CC(CC(C5)C3)C4)[nH]2)c(C)c1 10.1021/jm0490686
11555166 139287 0 None -54 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 502 7 2 5 5.5 CNc1cccc(NC(=O)C[C@H]2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm051219x
CHEMBL379902 139287 0 None -54 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cell line
ChEMBL 502 7 2 5 5.5 CNc1cccc(NC(=O)C[C@H]2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm051219x
44356654 27884 0 None 1 2 Guinea pig 5.1 pKi = 5.1 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 691 9 3 3 7.8 Cc1ccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc1C 10.1021/jm00021a019
CHEMBL137308 27884 0 None 1 2 Guinea pig 5.1 pKi = 5.1 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 691 9 3 3 7.8 Cc1ccc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc1C 10.1021/jm00021a019
10555899 112861 0 None -2344 2 Rat 5.1 pKi = 5.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 623 8 5 6 5.2 CC(O)C(O)Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL331763 112861 0 None -2344 2 Rat 5.1 pKi = 5.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 623 8 5 6 5.2 CC(O)C(O)Nc1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
9986662 101545 6 None -977 2 Guinea pig 5.1 pKi = 5.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 643 11 6 6 4.8 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2F)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL301777 101545 6 None -977 2 Guinea pig 5.1 pKi = 5.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 643 11 6 6 4.8 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2F)NC(=O)c2cc3[nH]cnc3cc2C(=O)NCC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm9508907
44346825 114262 0 None -77 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 623 8 3 4 4.7 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3)C(=O)O 10.1021/jm00048a001
CHEMBL333920 114262 0 None -77 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 623 8 3 4 4.7 C[C@@H](NC(=O)C[C@@H]1CCCN1C(=O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3)C(=O)O 10.1021/jm00048a001
11802426 99806 0 None -50 2 Guinea pig 6.1 pKi = 6.1 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 653 8 3 5 6.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N1C[C@H](Oc2ccc(Cl)cc2Cl)C[C@@H]1C(=O)O 10.1016/s0960-894x(98)00231-5
CHEMBL289021 99806 0 None -50 2 Guinea pig 6.1 pKi = 6.1 Binding
Binding affinity against CCK-A receptor in guinea pig pancreatic membranesBinding affinity against CCK-A receptor in guinea pig pancreatic membranes
ChEMBL 653 8 3 5 6.5 C[C@](Cc1c[nH]c2ccccc12)(NC(=O)OC1C2CC3CC(C2)CC1C3)C(=O)N1C[C@H](Oc2ccc(Cl)cc2Cl)C[C@@H]1C(=O)O 10.1016/s0960-894x(98)00231-5
10255015 206552 0 None 4 2 Guinea pig 6.1 pKi = 6.1 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 490 8 4 2 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)Nc1ccc2ccccc2c1)C(=O)NCCc1ccccc1 10.1021/jm00072a005
CHEMBL99065 206552 0 None 4 2 Guinea pig 6.1 pKi = 6.1 Binding
Tested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranesTested for inhibition of [3H]-pCCK-8 specific binding to cholecystokinin type A receptor in guinea pig pancreatic membranes
ChEMBL 490 8 4 2 5.8 CC(Cc1c[nH]c2ccccc12)(NC(=O)Nc1ccc2ccccc2c1)C(=O)NCCc1ccccc1 10.1021/jm00072a005
44346176 112822 0 None -21 2 Rat 7.1 pKi = 7.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 496 6 3 3 6.2 CC(CC1CCCC1)c1cccc2c1NC(=O)C(NC(=O)Nc1ccccc1)C(=O)N2c1ccccc1 10.1021/jm990967h
CHEMBL331651 112822 0 None -21 2 Rat 7.1 pKi = 7.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 496 6 3 3 6.2 CC(CC1CCCC1)c1cccc2c1NC(=O)C(NC(=O)Nc1ccccc1)C(=O)N2c1ccccc1 10.1021/jm990967h
11498528 72116 0 None -1096 3 Guinea pig 6.1 pKi = 6.1 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 503 7 3 4 6.1 O=C(O)c1cccc(NC(=O)c2[nH]c(C34CCC(CC3)CC4)nc2COC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL198933 72116 0 None -1096 3 Guinea pig 6.1 pKi = 6.1 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 503 7 3 4 6.1 O=C(O)c1cccc(NC(=O)c2[nH]c(C34CCC(CC3)CC4)nc2COC23CC4CC(CC(C4)C2)C3)c1 10.1021/jm0490686
CHEMBL384035 210559 1 None -8 4 Guinea pig 7.1 pKi = 7.1 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
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 10.1016/S0960-894X(00)80678-2
CHEMBL428666 210559 1 None -8 4 Guinea pig 7.1 pKi = 7.1 Binding
Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pigTested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor in pancreatic membranes of guinea-pig
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 10.1016/S0960-894X(00)80678-2
9914672 108042 0 None -31 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 521 5 2 4 3.7 O=C(Nc1ccc(F)cc1)N[C@H]1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(C2CCCCC2)C1=O 10.1016/j.bmc.2007.12.047
CHEMBL320141 108042 0 None -31 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to human CCK1 receptorBinding affinity to human CCK1 receptor
ChEMBL 521 5 2 4 3.7 O=C(Nc1ccc(F)cc1)N[C@H]1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(C2CCCCC2)C1=O 10.1016/j.bmc.2007.12.047
11534407 195250 0 None 6 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 584 8 3 7 4.9 O=C(N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL566359 195250 0 None 6 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 584 8 3 7 4.9 O=C(N[C@H](Cc1ccc(Cl)c(Cl)c1)C(=O)O)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
11627917 195843 0 None 7 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 530 7 2 6 4.8 CC(CNC(=O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccccc1 10.1016/j.bmcl.2009.09.064
CHEMBL570163 195843 0 None 7 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 530 7 2 6 4.8 CC(CNC(=O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccccc1 10.1016/j.bmcl.2009.09.064
45487003 195903 0 None 100 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 540 7 2 6 5.4 O=C(NCCc1ccc(Cl)c(Cl)c1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
CHEMBL570521 195903 0 None 100 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 540 7 2 6 5.4 O=C(NCCc1ccc(Cl)c(Cl)c1)c1ccc(Cl)cc1NS(=O)(=O)c1cccc2nsnc12 10.1016/j.bmcl.2009.09.064
11584582 197180 0 None 19 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 530 7 2 6 4.8 C[C@@H](CNC(=O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccccc1 10.1016/j.bmcl.2009.09.064
CHEMBL584063 197180 0 None 19 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation countingDisplacement of [125I]-CCK-8S from CCK1R after 100 mins by liquid scintillation counting
ChEMBL 530 7 2 6 4.8 C[C@@H](CNC(=O)c1ccc(Br)cc1NS(=O)(=O)c1cccc2nsnc12)c1ccccc1 10.1016/j.bmcl.2009.09.064
9914672 108042 0 None -31 2 Human 7.1 pKi = 7.1 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)
ChEMBL 521 5 2 4 3.7 O=C(Nc1ccc(F)cc1)N[C@H]1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(C2CCCCC2)C1=O 10.1016/S0960-894X(96)00613-0
CHEMBL320141 108042 0 None -31 2 Human 7.1 pKi = 7.1 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)
ChEMBL 521 5 2 4 3.7 O=C(Nc1ccc(F)cc1)N[C@H]1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(C2CCCCC2)C1=O 10.1016/S0960-894X(96)00613-0
44329156 205890 0 None -50 2 Human 7.1 pKi = 7.1 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)
ChEMBL 535 5 2 4 4.0 O=C(Nc1ccc(F)cc1)N[C@H]1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(C2CCCCCC2)C1=O 10.1016/S0960-894X(96)00613-0
CHEMBL95200 205890 0 None -50 2 Human 7.1 pKi = 7.1 Binding
Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)Tested for its selectivity against human Cholecystokinin type A receptor isolated from a human gallbladder cDNA library and stably transfected into a COSM6 cell line; (n=1)
ChEMBL 535 5 2 4 4.0 O=C(Nc1ccc(F)cc1)N[C@H]1C(=O)N(CC(=O)N2CCCC2)c2ccccc2N(C2CCCCCC2)C1=O 10.1016/S0960-894X(96)00613-0
11505870 72147 0 None -2 3 Guinea pig 6.1 pKi = 6.1 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 526 8 3 4 6.6 Cc1ccccc1-c1nc(CCC23CC4CC(CC(C4)C2)C3)c(C(=O)Nc2ccc(N(C)C)c(C(=O)O)c2)[nH]1 10.1021/jm0490686
CHEMBL199032 72147 0 None -2 3 Guinea pig 6.1 pKi = 6.1 Binding
Concentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptorConcentration required to inhibit the binding of 20 pM [125I]BH-CCK-8S radioligand to guinea pig pancreas CCK1 receptor
ChEMBL 526 8 3 4 6.6 Cc1ccccc1-c1nc(CCC23CC4CC(CC(C4)C2)C3)c(C(=O)Nc2ccc(N(C)C)c(C(=O)O)c2)[nH]1 10.1021/jm0490686
10652143 94150 0 None - 1 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 679 11 5 6 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3sccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL252150 94150 0 None - 1 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 679 11 5 6 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3sccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
11802624 101553 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL2067966 101553 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
CHEMBL301810 101553 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm070880t
44331479 4291 0 None -27 2 Rat 6.1 pKi = 6.1 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 494 9 1 5 4.7 CC(C)CCN1C(=O)C(NC(=O)Oc2cccc(N(C)C)c2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL101208 4291 0 None -27 2 Rat 6.1 pKi = 6.1 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 494 9 1 5 4.7 CC(C)CCN1C(=O)C(NC(=O)Oc2cccc(N(C)C)c2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/S0960-894X(96)00544-6
11802624 101553 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067966 101553 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL301810 101553 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
10555325 12825 0 None -45 2 Guinea pig 5.1 pKi = 5.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 585 7 2 5 4.2 CC(=O)N1[C@H](C(=O)NCC(=O)O)CC(=O)c2ccccc2N(Cc2ccccc2)C(=O)[C@H]1CC12CC3CC(CC(C3)C1)C2 10.1021/jm070880t
CHEMBL118930 12825 0 None -45 2 Guinea pig 5.1 pKi = 5.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 585 7 2 5 4.2 CC(=O)N1[C@H](C(=O)NCC(=O)O)CC(=O)c2ccccc2N(Cc2ccccc2)C(=O)[C@H]1CC12CC3CC(CC(C3)C1)C2 10.1021/jm070880t
44272229 98278 0 None - 1 Guinea pig 5.1 pKi = 5.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 635 15 6 6 3.5 CC(C)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)NCCc1ccccc1 10.1021/jm070880t
CHEMBL278032 98278 0 None - 1 Guinea pig 5.1 pKi = 5.1 Binding
Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cellsDisplacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells
ChEMBL 635 15 6 6 3.5 CC(C)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)NCCc1ccccc1 10.1021/jm070880t
16090701 141210 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 383 4 2 3 3.6 O=C(c1ccccc1NS(=O)(=O)c1cc2ccccc2[nH]1)N1CCCCC1 10.1021/jm060590x
CHEMBL385963 141210 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]CCK-8S from human CCK1RDisplacement of [125I]CCK-8S from human CCK1R
ChEMBL 383 4 2 3 3.6 O=C(c1ccccc1NS(=O)(=O)c1cc2ccccc2[nH]1)N1CCCCC1 10.1021/jm060590x
16732755 85011 0 None -10000 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 544 8 2 5 5.7 O=C(CN1N=C(C2CCCCC2)c2ccccc2N(CC(=O)C2CCCCC2)C1=O)Nc1cccc(C(=O)O)c1 10.1021/jm070139l
CHEMBL226622 85011 0 None -10000 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 544 8 2 5 5.7 O=C(CN1N=C(C2CCCCC2)c2ccccc2N(CC(=O)C2CCCCC2)C1=O)Nc1cccc(C(=O)O)c1 10.1021/jm070139l
11518254 11681 0 None -31 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 460 7 4 3 5.8 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1181918 11681 0 None -31 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 460 7 4 3 5.8 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067948 11681 0 None -31 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 460 7 4 3 5.8 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
9870515 12140 0 None -63 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 498 7 4 3 6.1 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184696 12140 0 None -63 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 498 7 4 3 6.1 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067955 12140 0 None -63 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 498 7 4 3 6.1 O=C(O)c1cc(NC(=O)c2cc(-c3ccccc3)[nH]c2CC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm049069y
11554414 12159 0 None -7 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 461 7 4 4 5.2 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL1184820 12159 0 None -7 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 461 7 4 4 5.2 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL2067965 12159 0 None -7 2 Guinea pig 5.1 pKi = 5.1 Binding
Inhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptorInhibition of 20 pM [125I]BH-CCK-8S binding to guinea pig pancreas membrane Cholecystokinin 1 receptor
ChEMBL 461 7 4 4 5.2 O=C(O)c1cc(NC(=O)c2[nH]c(-c3ccccc3)nc2CC2CCCCCC2)cc(C(=O)O)c1 10.1021/jm049069y
CHEMBL320868 209473 0 None 70 2 Rat 8.1 pKi = 8.1 Binding
Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissueInhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue
ChEMBL None None None 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(N)=O 10.1021/jm990252e
CHEMBL3351060 209785 0 None 20 2 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CN(C(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12)c1ccccc1)[C@@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
4627 807 44 None -1 5 Rat 8.1 pKi = 8.1 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL None None None None 10.1021/jm00389a002
864 807 44 None -1 5 Rat 8.1 pKi = 8.1 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL None None None None 10.1021/jm00389a002
9833444 807 44 None -1 5 Rat 8.1 pKi = 8.1 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL None None None None 10.1021/jm00389a002
CHEMBL1121 807 44 None -1 5 Rat 8.1 pKi = 8.1 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL None None None None 10.1021/jm00389a002
DB09142 807 44 None -1 5 Rat 8.1 pKi = 8.1 Binding
Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nMEvaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM
ChEMBL None None None None 10.1021/jm00389a002
10027864 106785 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 474 6 2 3 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccc(F)cc21 10.1016/0960-894X(95)00528-2
CHEMBL317081 106785 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 474 6 2 3 5.1 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2ccc(F)cc21 10.1016/0960-894X(95)00528-2
44265928 205534 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 342 5 2 1 5.2 Cc1cccc(NC(=O)NCC=C(c2ccccc2)c2ccccc2)c1 10.1021/jm00084a009
CHEMBL9312 205534 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 342 5 2 1 5.2 Cc1cccc(NC(=O)NCC=C(c2ccccc2)c2ccccc2)c1 10.1021/jm00084a009
CHEMBL3351049 209777 0 None -2 2 Guinea pig 5.1 pKi = 5.1 Binding
Affinity of compound on binding of [3H]pCCK-8 to the cholecystokinin type A receptor in guinea pig pancreatic membraneAffinity of compound on binding of [3H]pCCK-8 to the cholecystokinin type A receptor in guinea pig pancreatic membrane
ChEMBL None None None CN(C(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1ccccc1)[C@H](Cc1c[nH]c2ccccc12)C(=O)OC(C)(C)C 10.1021/jm00053a022
10651325 13750 0 None -275 2 Rat 6.1 pKi = 6.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 606 7 2 5 6.3 CCOC(=O)c1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
CHEMBL119608 13750 0 None -275 2 Rat 6.1 pKi = 6.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 606 7 2 5 6.3 CCOC(=O)c1cccc(NC(=O)NC2C(=O)N(CC34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)c3ccccc3N(c3ccccc3)C2=O)c1 10.1021/jm990967h
16732592 143038 0 None -870 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 572 8 2 7 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3c(cnn3CC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL389933 143038 0 None -870 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHOK1 cells
ChEMBL 572 8 2 7 4.9 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2ccc3c(cnn3CC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
44296980 101539 0 None -9 2 Guinea pig 5.1 pKi = 5.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 538 5 2 3 4.9 O=C(NCC12CC3CC(CC(C3)C1)C2)C1C2c3ccccc3C(c3ccccc32)C1C(=O)N1CCC[C@@H]1C(=O)O 10.1021/jm9508907
CHEMBL301740 101539 0 None -9 2 Guinea pig 5.1 pKi = 5.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 538 5 2 3 4.9 O=C(NCC12CC3CC(CC(C3)C1)C2)C1C2c3ccccc3C(c3ccccc32)C1C(=O)N1CCC[C@@H]1C(=O)O 10.1021/jm9508907
44346952 113601 0 None -9 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 538 5 2 3 4.8 O=C(NCC1C2CC3CC(C2)CC1C3)C1C2c3ccccc3C(c3ccccc32)C1C(=O)N1CCC[C@@H]1C(=O)O 10.1021/jm00048a001
CHEMBL332782 113601 0 None -9 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 538 5 2 3 4.8 O=C(NCC1C2CC3CC(C2)CC1C3)C1C2c3ccccc3C(c3ccccc32)C1C(=O)N1CCC[C@@H]1C(=O)O 10.1021/jm00048a001
10674395 110271 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific 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/jm9703247
CHEMBL326064 110271 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreasInhibition of [3H]pCCK-8 specific 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/jm9703247
44331489 4195 0 None -32 2 Rat 7.1 pKi = 7.1 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 493 9 2 4 4.7 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL100618 4195 0 None -32 2 Rat 7.1 pKi = 7.1 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 493 9 2 4 4.7 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(CCC(C)C)c2ccccc21 10.1016/S0960-894X(96)00544-6
10768658 114291 0 None -42 2 Rat 7.1 pKi = 7.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.0 O=C(Nc1ccccc1)NC1C(=O)N(CC2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
CHEMBL334020 114291 0 None -42 2 Rat 7.1 pKi = 7.1 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 534 5 2 3 6.0 O=C(Nc1ccccc1)NC1C(=O)N(CC2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)c2ccccc2N(c2ccccc2)C1=O 10.1021/jm990967h
16100408 141247 0 None -1202 3 Human 5.1 pKi = 5.1 Binding
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](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)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
CHEMBL386186 141247 0 None -1202 3 Human 5.1 pKi = 5.1 Binding
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](Cc1cc2ccccc2[nH]1)NC(=O)OC(C)(C)C)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
19700621 63800 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 509 8 3 6 2.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(O)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
CHEMBL1808409 63800 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 509 8 3 6 2.6 CC(C)CCN1C(=O)C(NC(=O)Nc2ccc(O)cc2)C(=O)N(CCN2CCOCC2)c2ccccc21 10.1016/j.bmc.2011.05.057
15249830 101452 0 None -15 2 Guinea pig 5.1 pKi = 5.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 441 4 2 2 4.9 O=C(O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm9508907
CHEMBL301095 101452 0 None -15 2 Guinea pig 5.1 pKi = 5.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 441 4 2 2 4.9 O=C(O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC12CC3CC(CC(C3)C1)C2 10.1021/jm9508907
44347142 113619 0 None -15 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 441 4 2 2 4.8 O=C(O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
CHEMBL332873 113619 0 None -15 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 441 4 2 2 4.8 O=C(O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1C2CC3CC(C2)CC1C3 10.1021/jm00048a001
44408632 157680 0 None -3630 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.8 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](Cc1cn(C(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O 10.1021/jm050851n
CHEMBL408832 157680 0 None -3630 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cellsDisplacement of [125I]CCK8 from human CCK1 receptor expressed in HEK293 cells
ChEMBL 1212 31 12 15 3.8 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](Cc1cn(C(=O)OC23CC4CC(CC(C4)C2)C3)c2ccccc12)C(=O)O 10.1021/jm050851n
11802624 101553 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL2067966 101553 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
CHEMBL301810 101553 0 None -64 2 Guinea pig 6.1 pKi = 6.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 673 11 5 5 6.2 O=C(O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)c2cc3ccccc3cc2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm9508907
16733463 13874 0 None -1380 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 547 9 3 6 5.0 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(NCC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL1197033 13874 0 None -1380 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 547 9 3 6 5.0 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(NCC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
CHEMBL559157 13874 0 None -1380 2 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cellsDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in PC3 cells
ChEMBL 547 9 3 6 5.0 CC(C)(C)C(=O)CN1C(=O)N(CC(=O)Nc2cccc(NCC(=O)O)c2)N=C(C2CCCCC2)c2ccccc21 10.1021/jm070139l
44346947 15111 0 None 1 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 389 4 2 2 4.3 O=C(O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1CCCCC1 10.1021/jm00048a001
CHEMBL121342 15111 0 None 1 2 Guinea pig 5.1 pKi = 5.1 Binding
Tested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cellsTested for its receptor affinity from competition with 20 pM [125I]BH-CCK-8S for Cholecystokinin type A receptor binding sites on guinea pig-pancreatic cells
ChEMBL 389 4 2 2 4.3 O=C(O)C1C2c3ccccc3C(c3ccccc32)C1C(=O)NCC1CCCCC1 10.1021/jm00048a001
CHEMBL336381 209827 0 None -354 5 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determinedBinding affinity towards Cholecystokinin type A receptor (CCK-A) receptor was determined
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)CNC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm0303103
11584903 140195 0 None -295 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell line
ChEMBL 560 10 2 6 5.1 CNCCN(C)c1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm051219x
CHEMBL381805 140195 0 None -295 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell lineDisplacement of [3H]L-364718 from human recombinant CCK1 receptor expressed in CHO cell line
ChEMBL 560 10 2 6 5.1 CNCCN(C)c1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 10.1021/jm051219x
10604847 193001 0 None -218 2 Guinea pig 6.1 pKi = 6.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 711 11 6 10 3.8 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2nc[nH]c2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(-c2nn[nH]n2)cc(-c2nn[nH]n2)c1 10.1021/jm9508907
CHEMBL53237 193001 0 None -218 2 Guinea pig 6.1 pKi = 6.1 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 711 11 6 10 3.8 O=C(NCC12CC3CC(CC(C3)C1)C2)c1cc2nc[nH]c2cc1C(=O)N[C@@H](Cc1ccccc1)C(=O)Nc1cc(-c2nn[nH]n2)cc(-c2nn[nH]n2)c1 10.1021/jm9508907
CHEMBL1172252 206832 0 None -12 4 Human 8.1 pKi = 8.1 Binding
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
CHEMBL208479 207445 0 None -3 4 Human 8.0 pKi = 8.0 Binding
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](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
19043361 4536 0 None 162 2 Rat 8.0 pKi = 8.0 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 524 6 2 3 6.2 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2cc(Cl)c(Cl)cc21 10.1016/0960-894X(95)00528-2
CHEMBL102867 4536 0 None 162 2 Rat 8.0 pKi = 8.0 Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreasBinding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
ChEMBL 524 6 2 3 6.2 CC(C)CCN1C(=O)C(NC(=O)Nc2ccccc2)C(=O)N(c2ccccc2)c2cc(Cl)c(Cl)cc21 10.1016/0960-894X(95)00528-2
44265973 205529 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 362 5 2 1 5.6 O=C(NCC=C(c1ccccc1)c1ccccc1)Nc1ccc(Cl)cc1 10.1021/jm00084a009
CHEMBL9308 205529 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranesInhibition of [3H]L-364718 binding to cholecystokinin type A receptor in rat pancreas membranes
ChEMBL 362 5 2 1 5.6 O=C(NCC=C(c1ccccc1)c1ccccc1)Nc1ccc(Cl)cc1 10.1021/jm00084a009
CHEMBL408083 210941 0 None -2 4 Human 6.0 pKi = 6.0 Binding
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](CCCC)NC(=O)[C@@H](N)Cc1ccc(O)cc1 10.1021/jm050921q
46235271 73286 2 None 2 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site 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 73286 2 None 2 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site expressed in CHO cells after 60 mins by scintillation counterDisplacement of [125I-BDZ-1] from wild-type human CCK1R at allosteric site 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
10580503 101207 0 None -234 2 Guinea pig 6.0 pKi = 6.0 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 691 11 6 10 3.7 O=C(NCC1CCCCCC1)c1cc2nc[nH]c2cc1C(=O)N[C@@H](Cc1ccccc1F)C(=O)Nc1cc(-c2nn[nH]n2)cc(-c2nn[nH]n2)c1 10.1021/jm9508907
CHEMBL299387 101207 0 None -234 2 Guinea pig 6.0 pKi = 6.0 Binding
In vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cellsIn vitro inhibitory activity against Cholecystokinin type A receptor using [125I]BH-CCK-8S as radioligand in guinea pig pancreatic cells
ChEMBL 691 11 6 10 3.7 O=C(NCC1CCCCCC1)c1cc2nc[nH]c2cc1C(=O)N[C@@H](Cc1ccccc1F)C(=O)Nc1cc(-c2nn[nH]n2)cc(-c2nn[nH]n2)c1 10.1021/jm9508907
44356430 114719 0 None -70 2 Guinea pig 6.0 pKi = 6.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 769 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
CHEMBL334714 114719 0 None -70 2 Guinea pig 6.0 pKi = 6.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 769 11 5 5 6.7 O=C(O)c1cc(NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)O)c1 10.1021/jm00021a019
21476261 4215 0 None -169 2 Rat 6.0 pKi = 6.0 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 571 8 2 4 5.9 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
CHEMBL100776 4215 0 None -169 2 Rat 6.0 pKi = 6.0 Binding
Evaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptorEvaluated in vitro for Cholecystokinin type A receptor affinity by measuring its ability to displace tritiated CCK-8S bound on rat pancreas Cholecystokinin type A receptor
ChEMBL 571 8 2 4 5.9 CC(C)CCN1C(=O)C(NC(=O)Nc2cccc(N(C)C)c2)C(=O)N(CC23CC4CC(CC(C4)C2)C3)c2ccccc21 10.1016/S0960-894X(96)00544-6
44357011 116057 0 None 1 2 Guinea pig 5.0 pKi = 5.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 779 11 3 7 6.8 COC(=O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)OC)c1 10.1021/jm00021a019
CHEMBL336453 116057 0 None 1 2 Guinea pig 5.0 pKi = 5.0 Binding
Competition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cellsCompetition with 20 pM [125I]BH-CCK-8S at Cholecystokinin type A receptor binding sites on guinea pig pancreatic cells
ChEMBL 779 11 3 7 6.8 COC(=O)c1cc(NC(=O)[C@H](Cc2ccccc2)NC(=O)C2C3c4ccccc4C(c4ccccc43)C2C(=O)NCC23CC4CC(CC(C4)C2)C3)cc(C(=O)OC)c1 10.1021/jm00021a019
44212463 63810 0 None - 1 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 555 7 2 4 4.9 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL1808419 63810 0 None - 1 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation countingDisplacement of [3H]CCK8 from rat pancreas CCK1 receptor at by liquid scintillation counting
ChEMBL 555 7 2 4 4.9 O=C(Nc1ccccc1)NC1C(=O)N(CCN2CCCC2)c2ccccc2N(CC23CC4CC(CC(C4)C2)C3)C1=O 10.1016/j.bmc.2011.05.057
CHEMBL411271 211118 0 None -630 3 Guinea pig 7.0 pKi = 7.0 Binding
Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.Affinity against Cholecystokinin type A receptor on guinea pig pancreatic membranes.
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)[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0000416
10838957 12351 0 None -151 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 495 5 2 4 5.2 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2cccc(C#N)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
CHEMBL118622 12351 0 None -151 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 495 5 2 4 5.2 CC(C)(C)CCN1C(=O)C(NC(=O)Nc2cccc(C#N)c2)C(=O)N(c2ccccc2)c2ccccc21 10.1021/jm990967h
44346326 112827 0 None -46 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 588 5 2 7 6.5 O=C(Nc1cccc(C2N=NN=N2)c1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)C1=O 10.1021/jm990967h
CHEMBL331688 112827 0 None -46 2 Rat 7.0 pKi = 7.0 Binding
In vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranesIn vitro inhibition of binding of [3H]pCCK-8 against Cholecystokinin type A receptor of rat pancreatic membranes
ChEMBL 588 5 2 7 6.5 O=C(Nc1cccc(C2N=NN=N2)c1)NC1C(=O)N(c2ccccc2)c2ccccc2N(C2[C@H]3C[C@@H]4C[C@@H](C[C@H]2C4)C3)C1=O 10.1021/jm990967h
53465843 69052 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL1933103 69052 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma countingDisplacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting
ChEMBL 441 8 4 3 4.2 O=C(Nc1ccccc1C(=O)N[C@@H](CCc1ccccc1)C(=O)O)c1cc2ccccc2[nH]1 10.1021/jm200438b
CHEMBL382051 210536 0 None -489 4 Human 7.0 pKi = 7.0 Binding
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
CHEMBL3351055 209783 0 None -70 2 Guinea pig 6.0 pKi = 6 Binding
Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membraneDisplacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane
ChEMBL None None None CC(C)(C)OC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)Cc1cccc2ccccc12)c1ccccc1 10.1021/jm00053a022
2118 201783 35 None - 2 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
Drug Central 308 1 0 4 3.6 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 None
CHEMBL661 201783 35 None - 2 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
Drug Central 308 1 0 4 3.6 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2 None
5556 201560 26 None - 1 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
Drug Central 342 1 0 4 4.2 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1Cl)=NC2 None
CHEMBL646 201560 26 None - 1 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreasDisplacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
Drug Central 342 1 0 4 4.2 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1Cl)=NC2 None
11954224 214164 0 None - 60 Mouse 8.4 pIC50 = 8.4 Binding
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
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
9853654 22573 37 None - 2 Rat 8.2 pIC50 = 8.2 Binding
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
Drug Central 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 None
CHEMBL1328 22573 37 None - 2 Rat 8.2 pIC50 = 8.2 Binding
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
Drug Central 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 None
1614 2307 60 None - 1 Human 8.2 pIC50 = 8.2 Binding
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
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 2307 60 None - 1 Human 8.2 pIC50 = 8.2 Binding
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
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 2307 60 None - 1 Human 8.2 pIC50 = 8.2 Binding
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
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 2307 60 None - 1 Human 8.2 pIC50 = 8.2 Binding
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
Drug Central 460 14 2 4 4.0 CCCCCN(C(=O)C(NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC None
16129670 802 0 None 3 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 6256771
860 802 0 None 3 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 6256771
91898395 802 0 None 3 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 6256771
3476 1368 8 None 2 3 Human 9.7 pKd = 9.7 Binding
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 3018478
59751 1368 8 None 2 3 Human 9.7 pKd = 9.7 Binding
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 3018478
878 1368 8 None 2 3 Human 9.7 pKd = 9.7 Binding
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 3018478
CHEMBL39263 1368 8 None 2 3 Human 9.7 pKd = 9.7 Binding
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 3018478
4627 807 44 None -1 5 Rat 8.0 pKi = 8 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
Drug Central None None None None None
864 807 44 None -1 5 Rat 8.0 pKi = 8 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
Drug Central None None None None None
9833444 807 44 None -1 5 Rat 8.0 pKi = 8 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
Drug Central None None None None None
CHEMBL1121 807 44 None -1 5 Rat 8.0 pKi = 8 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
Drug Central None None None None None
DB09142 807 44 None -1 5 Rat 8.0 pKi = 8 Binding
Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissueBinding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue
Drug Central None None None None None
138106885 166347 71 None -1 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
Drug Central 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 None
36314 166347 71 None -1 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
Drug Central 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 None
CHEMBL428647 166347 71 None -1 4 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
Drug Central 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 None
4627 807 44 None -2 5 Human 8.0 pKi = 8.0 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
Drug Central None None None None None
864 807 44 None -2 5 Human 8.0 pKi = 8.0 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
Drug Central None None None None None
9833444 807 44 None -2 5 Human 8.0 pKi = 8.0 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
Drug Central None None None None None
CHEMBL1121 807 44 None -2 5 Human 8.0 pKi = 8.0 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
Drug Central None None None None None
DB09142 807 44 None -2 5 Human 8.0 pKi = 8.0 Binding
Displacement of radiolabeled CCK-8s from human CCK1 receptorDisplacement of radiolabeled CCK-8s from human CCK1 receptor
Drug Central None None None None None
4627 807 44 None -1 5 Guinea pig 8.0 pKi = 8.0 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
Drug Central None None None None None
864 807 44 None -1 5 Guinea pig 8.0 pKi = 8.0 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
Drug Central None None None None None
9833444 807 44 None -1 5 Guinea pig 8.0 pKi = 8.0 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
Drug Central None None None None None
CHEMBL1121 807 44 None -1 5 Guinea pig 8.0 pKi = 8.0 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
Drug Central None None None None None
DB09142 807 44 None -1 5 Guinea pig 8.0 pKi = 8.0 Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranesInhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
Drug Central None None None None None
859 469 0 None 7943 2 Rat 10.5 pKi None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476993
3074331 910 0 None - 1 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 493 6 4 4 4.6 O=C(N[C@@](C(=O)N[C@H]1CCCC[C@@H]1O)(Cc1c[nH]c2c1cccc2)C)OC12CC3CC(C2)CC(C1)C3 9438020
872 910 0 None - 1 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 493 6 4 4 4.6 O=C(N[C@@](C(=O)N[C@H]1CCCC[C@@H]1O)(Cc1c[nH]c2c1cccc2)C)OC12CC3CC(C2)CC(C1)C3 9438020
132980 2200 8 None - 1 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 7969084
881 2200 8 None - 1 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 7969084
CHEMBL420783 2200 8 None - 1 Rat 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 445 2 2 4 4.0 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(N2CC3CCC(C2)CC3)c2c(N(C1=O)C)cccc2 7969084
6439414 2964 11 None -2454 2 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 7516969
867 2964 11 None -2454 2 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 7516969
CHEMBL3351022 2964 11 None -2454 2 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 7516969
CHEMBL341460 2964 11 None -2454 2 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 612 11 5 5 4.6 O=C(N[C@H](c1ccccc1)CNC(=O)[C@@](Cc1c[nH]c2c1cccc2)(NC(=O)OC1C2CC3CC1CC(C2)C3)C)/C=C/C(=O)O 7516969
122130 4039 33 None - 1 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 7910212
888 4039 33 None - 1 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 7910212
CHEMBL115121 4039 33 None - 1 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 516 6 2 4 5.5 Cc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccc2)c2c(N(C1=O)CC(=O)c1ccccc1C)cccc2 7910212
65937 1371 0 None - 1 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 17684117
834 1371 0 None - 1 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 17684117
889 1371 0 None - 1 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 17684117
CHEMBL550781 1371 0 None - 1 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 17684117
DB04856 1371 0 None - 1 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 460 14 2 4 4.0 CCCCCN(C(=O)[C@H](NC(=O)c1ccc(c(c1)Cl)Cl)CCC(=O)O)CCCOC 17684117
11488979 2096 0 None - 1 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 7 1 4 6.6 COc1ccc(cc1)n1nc(cc1c1ccc(c(c1)Cl)Cl)C[C@@H](c1cccc(c1)C)C(=O)O 17684117
877 2096 0 None - 1 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 7 1 4 6.6 COc1ccc(cc1)n1nc(cc1c1ccc(c(c1)Cl)Cl)C[C@@H](c1cccc(c1)C)C(=O)O 17684117
CHEMBL400111 2096 0 None - 1 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 7 1 4 6.6 COc1ccc(cc1)n1nc(cc1c1ccc(c(c1)Cl)Cl)C[C@@H](c1cccc(c1)C)C(=O)O 17684117
885 3775 0 None 1584 2 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 10 3 6 5.1 O=C([C@@H](NC(=O)c1cc2c([nH]1)cccc2)CSc1ncccc1C(=O)O)N1CCN(CC1)C(c1ccccc1)c1ccccc1 8730754
9873836 3775 0 None 1584 2 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 10 3 6 5.1 O=C([C@@H](NC(=O)c1cc2c([nH]1)cccc2)CSc1ncccc1C(=O)O)N1CCN(CC1)C(c1ccccc1)c1ccccc1 8730754