Ligand source activities (1 row/activity)



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

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
51353551 24906 16 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 24906 16 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 24906 16 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 24906 16 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 56390 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 56390 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 56390 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 56390 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 11916 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 11916 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 172221 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 172221 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 195483 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 195483 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 194970 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 194970 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 195468 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 195468 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 56390 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 56390 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 195402 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 195402 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 194969 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 194969 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 194969 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 11916 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 11916 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 195918 5 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 195918 5 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 195830 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 195830 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 195506 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 195506 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 195506 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 195506 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 195506 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 195506 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 178341 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 178341 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 68698 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 68698 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 185498 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 185498 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 68630 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 68630 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 177632 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 177632 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 195468 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 195468 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 195654 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 195654 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 195834 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 195834 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 179250 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 179250 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 195416 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 195416 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 179468 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 179468 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 195530 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 195530 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 195530 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 195564 12 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 195564 12 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 195564 12 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 195564 12 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 195564 12 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 195564 12 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 195564 12 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 195564 12 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 178230 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 178230 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 195424 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 195424 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 195708 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 195708 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 195782 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 195782 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 179485 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 179485 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 179567 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 179567 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 219166 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 178793 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 178793 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 179097 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 179097 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 178527 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 178527 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 179468 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 179468 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 195830 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 195830 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 181151 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 181151 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 181371 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 181371 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 11916 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 11916 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 196410 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 196410 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 68630 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 68630 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 80423 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 80423 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 176868 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 176868 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 181715 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 181715 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 186237 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 186237 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 195648 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 195648 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 195483 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 195483 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 178951 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 178951 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 179697 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 179697 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 195541 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 195541 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 182047 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 182047 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 177717 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 177717 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 178361 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 178361 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 177981 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 177981 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 181643 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 181643 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 178624 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 178624 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 178782 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 178782 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 178829 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 178829 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 179432 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 179432 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 180847 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 180847 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 24906 16 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 24906 16 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 179913 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 179913 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 68697 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 68697 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 179435 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 179435 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 176649 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 176649 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 176644 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 176644 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 180796 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 180796 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 68688 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 68688 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 179286 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 179286 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 186152 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 186152 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 195399 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 195399 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 176649 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 176649 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 187591 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 187591 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 80423 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 80423 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 179612 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 179612 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 180065 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 180065 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 195506 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 195506 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 195506 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 176936 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 176936 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 180455 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 180455 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 180421 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 180421 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 80423 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 80423 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 176728 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 176728 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 182519 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 182519 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 180102 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 180102 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 180511 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 180511 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 181386 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 181386 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 182620 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 182620 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 181113 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 181113 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 179237 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 179237 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 80423 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 80423 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 195708 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 195708 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 177002 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 177002 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 181871 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 181871 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 182857 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 182857 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 196529 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 196529 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 68698 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 68698 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 68687 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 68687 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 178534 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 178534 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 180295 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 180295 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 180295 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 180295 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 180295 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 180295 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 68642 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 68642 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 195497 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 195497 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 24906 16 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 24906 16 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 197488 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 197488 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 197693 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 197693 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 179991 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 179991 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 189065 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 189065 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 197520 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 197520 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 186130 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 186130 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 189705 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 189705 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 179715 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 179715 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 197477 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 197477 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 197487 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 197487 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 219546 2 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 197415 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 197415 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 68638 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 68638 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 195564 12 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 195564 12 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 195564 12 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 195564 12 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 219924 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 181215 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 181215 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 180707 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 180707 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 68647 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 68647 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 186131 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 186131 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 68692 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 68692 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 196437 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 196437 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 196375 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 196375 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 178410 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 178410 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 180954 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 180954 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 181935 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 181935 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 80421 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 80421 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 116004 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 116004 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 80371 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 80371 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 179341 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 179341 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 147362 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 147362 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 24907 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 24907 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 80412 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 80412 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 68690 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 68690 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 188340 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 188340 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 25056 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 25056 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 68645 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 68645 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 216151 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 80420 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 80420 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 188318 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 188318 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 196560 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 196560 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 217483 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 68639 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 68639 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 80413 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 80413 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 181297 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 181297 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 180906 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 180906 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 187949 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 187949 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 80423 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 80423 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 215978 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 215978 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 80416 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 80416 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 68640 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 68640 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 8178 35 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 8178 35 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 8178 35 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 8178 35 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 68689 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 68689 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 218997 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 24906 16 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 24906 16 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 68635 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 68635 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 24909 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 24909 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 219072 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 216158 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 80423 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 80423 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 179898 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 179898 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 219072 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 189575 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 189575 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 80417 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 80417 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 195465 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 195465 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 68637 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 68637 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 68644 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 68644 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 68631 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 68631 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 80419 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 80419 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 46198 5 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 46198 5 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 114073 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 114073 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 186107 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 186107 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 80370 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 80370 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 68693 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 68693 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 68636 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 68636 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 80418 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 80418 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 24908 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 24908 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 188341 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 188341 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 188313 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 188313 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 24911 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 24911 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 80414 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 80414 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 80423 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 80423 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 188319 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 188319 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 68694 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 68694 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 80369 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 80369 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 24911 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 24911 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 189063 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 189063 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 217559 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 188563 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 188563 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 80411 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 80411 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 68695 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 68695 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 68643 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 68643 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 196589 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 196589 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 196497 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 196497 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 216593 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 179718 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 179718 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 68646 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 68646 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 24910 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 24910 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 24906 16 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 24906 16 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 24908 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 24908 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 188342 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 188342 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 80422 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 80422 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 80423 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 80423 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 188315 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 188315 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 68691 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 68691 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 189211 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 189211 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 196438 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 196438 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 178607 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 178607 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 188122 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 188122 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 80415 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 80415 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 68641 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 68641 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 188733 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 188733 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 96159 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 96159 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 189234 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 189234 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 189566 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 189566 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 68696 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 68696 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 11916 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 11916 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 24909 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 24909 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 176990 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 176990 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 189553 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 189553 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 214385 45 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 214385 45 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 131164 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 131164 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 74306 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 74306 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 131164 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 131164 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 106244 15 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 106244 15 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 131164 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 131164 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 131164 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 131164 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 120387 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 120387 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 134394 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 134394 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 74306 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 74306 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 74306 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 74306 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 74306 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 74306 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 134394 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 134394 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 134394 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 134394 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 131164 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 131164 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 218997 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 131164 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 131164 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 134394 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 134394 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 131164 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 131164 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 74306 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 74306 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 74306 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 74306 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 74306 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 74306 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 74306 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 74306 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 74306 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 74306 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 134394 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 134394 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 131164 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 131164 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 131164 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 131164 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 74306 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 74306 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 134394 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 134394 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 131164 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 131164 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 134394 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 134394 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 74306 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 74306 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 134394 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 134394 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 134394 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 134394 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 134394 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 134394 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 131164 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 131164 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 134394 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 134394 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 108838 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 108838 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 164654 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 164654 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 105483 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 105483 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 109107 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 109107 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 108860 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 108860 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 10070 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 10070 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 10070 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 10070 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 10070 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 9128 67 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 9128 67 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 9128 67 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 9128 67 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 8185 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 8185 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 8185 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 8185 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 8185 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 7606 0 None -158 2 Rat 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
861 7606 0 None -158 2 Rat 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
16168172 8552 0 None -158 2 Rat 6.1 pIC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
3559 8552 0 None -158 2 Rat 6.1 pIC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
444007 9817 0 None -794 2 Rat 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
870 9817 0 None -794 2 Rat 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
DB00183 9817 0 None -794 2 Rat 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
3960 9124 23 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 9124 23 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 9124 23 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 9124 23 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 9124 23 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 9124 23 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 8677 7 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 8677 7 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 8677 7 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 8903 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7654246
5311196 8903 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7654246
122077 9102 51 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 9102 51 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 9102 51 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 9102 51 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 6995 34 None 4265 2 Rat 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1636779
858 6995 34 None 4265 2 Rat 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1636779
CHEMBL323521 6995 34 None 4265 2 Rat 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1636779
904 9800 10 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 9800 10 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 9800 10 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 9800 10 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 7607 0 None -1 2 Mouse 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12370550
127948 10491 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 10491 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 8182 9 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 8182 9 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 8182 9 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 8182 9 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 7609 50 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
864 7609 50 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
9833444 7609 50 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
CHEMBL1121 7609 50 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
DB09142 7609 50 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
2281 9949 82 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 9949 82 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 9949 82 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 9949 82 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 9949 82 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 10070 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 10070 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 10070 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 10070 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 10070 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 7713 37 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 7713 37 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 7713 37 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 7713 37 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 9797 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 9797 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 9019 5 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 9019 5 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 9019 5 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 9128 67 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 9128 67 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 9128 67 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 9128 67 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 9000 9 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 9000 9 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 9000 9 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 9000 9 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 10771 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 10771 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 10771 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 10882 33 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 10882 33 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 10882 33 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 10882 33 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 7609 50 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
864 7609 50 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
9833444 7609 50 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
CHEMBL1121 7609 50 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
DB09142 7609 50 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
10348659 8585 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 8585 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 8585 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 10313 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 10313 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 8845 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 8845 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 8845 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 10439 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 10439 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 10439 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 9935 16 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 9935 16 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 9935 16 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 9102 51 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 9102 51 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 9102 51 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 9102 51 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 (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

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 DOI
45138674 23418 50 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 572 6 1 7 5.7 COc1cccc(N2CCN(C3=Nc4c(F)cccc4[C@H](CC(=O)O)N3c3cc(C(F)(F)F)ccc3OC)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1241951 23418 50 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 572 6 1 7 5.7 COc1cccc(N2CCN(C3=Nc4c(F)cccc4[C@H](CC(=O)O)N3c3cc(C(F)(F)F)ccc3OC)CC2)c1 10.1038/s41467-023-40064-9
25181577 84994 56 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
CHEMBL2105695 84994 56 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
3062316 40349 121 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 487 7 3 9 3.3 Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1 10.1038/s41467-023-40064-9
CHEMBL1421 40349 121 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 487 7 3 9 3.3 Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1 10.1038/s41467-023-40064-9
10184653 17769 107 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 8 2 7 4.4 CN(C)C/C=C/C(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1O[C@H]1CCOC1 10.1038/s41467-023-40064-9
CHEMBL1173655 17769 107 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 8 2 7 4.4 CN(C)C/C=C/C(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1O[C@H]1CCOC1 10.1038/s41467-023-40064-9
25025298 84926 39 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 546 8 3 8 4.5 Cc1ccn(-c2cc(Cl)ccc2[C@@H](Oc2cc(-c3ccc(C[C@H](N)C(=O)O)cc3)nc(N)n2)C(F)(F)F)n1 10.1038/s41467-023-40064-9
CHEMBL2103855 84926 39 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 546 8 3 8 4.5 Cc1ccn(-c2cc(Cl)ccc2[C@@H](Oc2cc(-c3ccc(C[C@H](N)C(=O)O)cc3)nc(N)n2)C(F)(F)F)n1 10.1038/s41467-023-40064-9
213046 9164 59 None - 9 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
4168 9164 59 None - 9 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
7461 9164 59 None - 9 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
CHEMBL1237021 9164 59 None - 9 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
DB08815 9164 59 None - 9 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
392622 63086 95 None - 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
CHEMBL163 63086 95 None - 4 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
6436173 61890 45 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL1617 61890 45 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
1890 9535 49 None - 16 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
4449 9535 49 None - 16 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
7247 9535 49 None - 16 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
CHEMBL623 9535 49 None - 16 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
DB01149 9535 49 None - 16 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
10831 123741 25 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 397 7 2 5 4.3 O=C(Nc1ccccc1)OCC(CN1CCCCC1)OC(=O)Nc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL338667 123741 25 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 397 7 2 5 4.3 O=C(Nc1ccccc1)OCC(CN1CCCCC1)OC(=O)Nc1ccccc1 10.1038/s41467-023-40064-9
2713 212050 82 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353524 212050 82 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5360566 212050 82 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
88536661 212050 82 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
9552079 212050 82 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1330113 212050 82 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL790 212050 82 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353627 91316 8 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 411 8 3 4 4.6 CC(C)n1c(/C=C/C(O)CC(O)CC(=O)O)c(-c2ccc(F)cc2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL2220442 91316 8 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 411 8 3 4 4.6 CC(C)n1c(/C=C/C(O)CC(O)CC(=O)O)c(-c2ccc(F)cc2)c2ccccc21 10.1038/s41467-023-40064-9
104850 10103 96 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
4150 10103 96 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
743 10103 96 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL111 10103 96 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
DB06155 10103 96 None - 6 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
135398735 143746 32 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
136262914 143746 32 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL374478 143746 32 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
148192 17192 81 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 704 14 5 9 4.2 COC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)[C@@H](O)CN(Cc1ccc(-c2ccccn2)cc1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL1163 17192 81 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 704 14 5 9 4.2 COC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)[C@@H](O)CN(Cc1ccc(-c2ccccn2)cc1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C(C)(C)C 10.1038/s41467-023-40064-9
4150 7575 39 None - 12 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
5288 7575 39 None - 12 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
644019 7575 39 None - 12 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
CHEMBL190461 7575 39 None - 12 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
DB09061 7575 39 None - 12 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1038/s41467-023-40064-9
135564886 21265 5 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
135673376 21265 5 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
137157436 21265 5 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
145948239 21265 5 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
71587099 21265 5 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
CHEMBL1201304 21265 5 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
2540 11173 111 None - 4 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
CHEMBL1014 11173 111 None - 4 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
2179 174297 76 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL1256655 174297 76 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL43 174297 76 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 5 2 5 4.5 COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
2351 11072 49 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1008 11072 49 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1257078 11072 49 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
30323 69259 57 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL1563 69259 57 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL178 69259 57 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
2583 10548 118 None - 1 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
592 10548 118 None - 1 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
65999 10548 118 None - 1 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
CHEMBL1017 10548 118 None - 1 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
DB00966 10548 118 None - 1 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
123879 10060 82 None - 4 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
1910 10060 82 None - 4 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
1911 10060 82 None - 4 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
2354 10060 82 None - 4 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
CHEMBL361812 10060 82 None - 4 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
DB13036 10060 82 None - 4 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 416 6 2 4 3.1 OC(=O)CCn1c2CC[C@H](Cc2c2c1cccc2)NS(=O)(=O)c1ccc(cc1)F 10.1038/s41467-023-40064-9
54682461 91461 62 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 602 11 2 6 7.3 CCC[C@@]1(CCc2ccccc2)CC(O)=C([C@H](CC)c2cccc(NS(=O)(=O)c3ccc(C(F)(F)F)cn3)c2)C(=O)O1 10.1038/s41467-023-40064-9
CHEMBL222559 91461 62 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 602 11 2 6 7.3 CCC[C@@]1(CCc2ccccc2)CC(O)=C([C@H](CC)c2cccc(NS(=O)(=O)c3ccc(C(F)(F)F)cn3)c2)C(=O)O1 10.1038/s41467-023-40064-9
CHEMBL2103737 84915 0 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
8550 21196 57 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 578 7 1 9 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC 10.1038/s41467-023-40064-9
CHEMBL1200515 21196 57 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 578 7 1 9 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC 10.1038/s41467-023-40064-9
4846 34760 53 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 1 2 6 2.2 O=C(O)c1cc(O)c2c3nc4ccccc4oc-3cc(=O)c2n1 10.1038/s41467-023-40064-9
CHEMBL1372341 34760 53 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 1 2 6 2.2 O=C(O)c1cc(O)c2c3nc4ccccc4oc-3cc(=O)c2n1 10.1038/s41467-023-40064-9
4495 203314 92 None - 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL56367 203314 92 None - 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 10.1038/s41467-023-40064-9
16362 9899 71 None - 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 9899 71 None - 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 9899 71 None - 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 9899 71 None - 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 9899 71 None - 29 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
41684 37995 105 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
CHEMBL1401 37995 105 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
5329102 201505 86 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 201505 86 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
71496458 122342 87 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
CHEMBL3353410 122342 87 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
176870 202264 106 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 10 1 7 3.4 C#Cc1cccc(Nc2ncnc3cc(OCCOC)c(OCCOC)cc23)c1 10.1038/s41467-023-40064-9
CHEMBL553 202264 106 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human CCKAR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 393 10 1 7 3.4 C#Cc1cccc(Nc2ncnc3cc(OCCOC)c(OCCOC)cc23)c1 10.1038/s41467-023-40064-9
4627 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 174814 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 174814 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 217996 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 195468 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 195468 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 195830 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 195830 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 179468 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 179468 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 195530 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 195530 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 195530 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 195834 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 195834 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 68630 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 68630 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 195708 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 195708 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 195506 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 195506 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 195506 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 180102 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 180102 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 194970 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 194970 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 182620 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 182620 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 172221 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 172221 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 219641 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 6995 34 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 6995 34 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 6995 34 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 180065 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 180065 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 185498 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 185498 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 176649 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 176649 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 195483 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 195483 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 195506 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 195506 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 195506 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 179612 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 179612 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 176644 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 176644 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 179286 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 179286 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 179567 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 179567 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 195918 5 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 195918 5 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 176728 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 176728 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 182519 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 182519 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 181643 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 181643 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 214385 45 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 214385 45 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 180455 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 180455 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 181871 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 181871 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 194969 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 194969 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 194969 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 195402 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 195402 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 195648 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 195648 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 214385 45 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 214385 45 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 178951 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 178951 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 181151 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 181151 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 178829 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 178829 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 131164 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 131164 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 122234 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 122234 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 195654 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 195654 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 181113 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 181113 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 217557 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 214385 45 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 214385 45 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 214385 45 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 214385 45 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 214385 45 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 214385 45 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 178534 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 178534 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 176936 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 176936 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 195416 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 195416 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 177002 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 177002 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 168346 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 168346 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 178230 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 178230 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 187591 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 187591 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 195564 12 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 195564 12 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 195564 12 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 195564 12 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 195564 12 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 195564 12 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 195564 12 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 195564 12 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 179250 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 179250 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 179697 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 179697 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 195782 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 195782 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 180847 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 180847 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 68642 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 68642 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 179913 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 179913 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 219858 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 201595 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 201595 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 196410 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 196410 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 179432 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 179432 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 68698 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 68698 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 186237 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 186237 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 195399 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 195399 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 195541 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 195541 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 176868 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 176868 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 177632 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 177632 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 174625 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 174625 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 179485 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 179485 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 68688 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 68688 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 85288 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 85288 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 182857 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 182857 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 181715 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 181715 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 74458 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 74458 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 179097 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 179097 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 178793 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 178793 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 74525 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 74525 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 195424 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 195424 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 65642 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 65642 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 189065 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 189065 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 179435 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 179435 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 180295 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 180295 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 180295 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 180295 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 180295 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 180295 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 166140 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 166140 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 74173 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 74173 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 195497 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 195497 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 181371 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 181371 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 214385 45 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 214385 45 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 104063 4 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 104063 4 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 104063 4 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 104063 4 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 178341 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 178341 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 177717 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 177717 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 178361 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 178361 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 186131 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 186131 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 9102 51 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 9102 51 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 9102 51 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 9102 51 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 196529 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 196529 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 134394 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 134394 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 134394 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 134394 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 220576 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 85206 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 85206 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 216566 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 186152 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 186152 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 217513 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 74528 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 74528 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 178782 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 178782 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 114035 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 114035 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 9935 16 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 9935 16 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 9935 16 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 214385 45 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 179237 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 179237 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 211470 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 211470 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 211470 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 211470 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 114036 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 114036 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 114036 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 114036 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 8182 9 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 8182 9 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 8182 9 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 8182 9 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 211014 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 211014 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 211408 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 211408 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 178527 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 178527 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 215365 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 8182 9 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 8182 9 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 8182 9 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 8182 9 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 74520 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 74520 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 74523 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 74523 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 80423 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 80423 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 211263 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 211263 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 195859 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 195859 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 8845 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 8845 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 8845 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 219095 4 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 219095 4 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 177981 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 177981 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 86320 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 86320 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 103432 1 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 103432 1 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 103432 1 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 103432 1 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 211177 12 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 211177 12 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 21945 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 21945 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 211177 12 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 211177 12 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 186130 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 186130 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 115290 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 115290 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 182047 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 182047 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 216098 30 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 216098 30 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 115366 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 115366 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 114120 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 114120 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 114842 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 114842 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 115481 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 115481 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 74306 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 74306 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 39690 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 39690 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 39690 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 39690 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 178624 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 178624 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 211443 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 211443 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 109041 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 109041 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 84597 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 84597 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 173413 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 173413 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 85290 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 85290 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 181386 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 181386 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 189705 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 189705 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 113982 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 113982 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 122231 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 122231 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 109041 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 109041 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 219652 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 68687 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 68687 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 210918 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 210918 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 211025 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 211025 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 211413 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 211413 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 115232 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 115232 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 211025 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 211025 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 211025 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 211025 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 211413 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 211413 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 80423 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 80423 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 109884 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 109884 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 215366 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 16577 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 16577 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 16577 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 16577 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 173024 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 173024 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 16577 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 16577 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 16577 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 16577 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 215269 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 113964 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 113964 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 33004 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 33004 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 11685 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 11685 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 7713 37 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 7713 37 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 7713 37 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 7713 37 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 33004 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 33004 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 33004 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 33004 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 118214 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 118214 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 186107 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 186107 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 188318 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 188318 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 196438 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 196438 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 196589 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 196589 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 128471 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 128471 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 80423 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 80423 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 215363 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 122860 2 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 122860 2 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 111648 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 111648 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 115068 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 115068 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 11916 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 11916 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 111648 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 111648 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 213321 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 213321 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 17541 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 17541 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 74513 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 74513 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 213321 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 213321 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 109986 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 109986 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 176071 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 176071 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 113377 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 113377 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 126313 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 126313 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 108860 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 108860 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 109107 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 109107 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 169117 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 169117 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 176071 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 176071 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 116500 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 116500 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 85368 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 85368 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 127113 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 127113 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 205840 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 205840 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 171705 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 171705 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 216027 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 80423 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 80423 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 80423 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 80423 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 56390 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 56390 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 171705 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 171705 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 211421 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 211421 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 127912 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 127912 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 126379 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 126379 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 125753 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 125753 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 177397 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 177397 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 127246 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 127246 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 219045 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 74484 32 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 74484 32 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 74493 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 74493 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 38562 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 38562 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 125965 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 125965 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 127402 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 127402 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 127403 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 127403 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 23593 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 23593 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 211298 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 211298 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 66314 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 66314 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 109808 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 109808 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 170248 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 170248 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 211298 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 211298 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 74482 4 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 74482 4 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 74487 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 74487 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 174087 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 174087 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 39103 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 39103 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 123407 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 123407 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 66314 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 66314 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 91159 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 91159 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 91159 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 137473 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 137473 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 123832 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 123832 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 204829 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 204829 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 168089 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 168089 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 144286 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 144286 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 163661 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 163661 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 218170 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 32801 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 32801 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 80423 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 80423 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 126466 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 126466 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 7713 37 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 7713 37 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 7713 37 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 7713 37 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 215948 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 126327 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 126327 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 24906 16 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 24906 16 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 123554 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 123554 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 85259 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 85259 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 205379 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 205379 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 106950 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 106950 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 214311 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 214311 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 76184 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 76184 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 174672 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 174672 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 92768 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 92768 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 114378 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 114378 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 28918 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 28918 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 127579 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 127579 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 40312 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 40312 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 109122 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 109122 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 211387 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 211387 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 109754 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 109754 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 109700 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 109700 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 109849 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 109849 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 216173 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 74513 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 74513 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 176258 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 176258 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 174253 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 174253 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 219978 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 117116 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 117116 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 34504 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 34504 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 56390 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 56390 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 107122 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 107122 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 163202 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 163202 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 109122 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 109122 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 163202 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 163202 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 211387 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 211387 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 32971 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 32971 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 127533 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 127533 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 163202 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 163202 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 113576 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 113576 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 170023 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 170023 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 127057 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 127057 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 107634 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 107634 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 65865 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 65865 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 109849 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 109849 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 210901 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 210901 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 74462 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 74462 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 74511 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 74511 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 125243 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 125243 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 16805 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 16805 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 171862 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 171862 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 122284 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 122284 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 113580 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 113580 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 115690 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 115690 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 65865 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 65865 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 126754 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 126754 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 16302 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 16302 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 171270 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 171270 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 215236 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 84602 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 84602 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 74485 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 74485 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 204790 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 204790 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 128458 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 128458 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 128458 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 128458 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 16920 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 16920 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 123793 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 123793 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 118251 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 118251 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 95976 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 95976 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 95976 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 204977 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 204977 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 213415 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 213415 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 95976 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 95976 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 95976 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 117434 1 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 117434 1 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 16864 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 16864 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 173690 75 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 173690 75 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 173690 75 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 185922 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 185922 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 123861 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 123861 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 106630 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 106630 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
44591978 190688 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 190688 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 39977 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 39977 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 127115 18 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 127115 18 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 56438 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 56438 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 125341 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 125341 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 107237 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 107237 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 52113 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 52113 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 168846 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 168846 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 16671 9 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 16671 9 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 147524 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 147524 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 16671 9 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 16671 9 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 85207 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 85207 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 127376 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 127376 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 127376 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 174814 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 174814 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 201455 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 201455 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 147618 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 147618 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 211296 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 211296 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 117229 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 117229 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 84011 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 84011 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 54784 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 54784 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 35182 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 35182 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 123026 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 123026 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 113598 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 113598 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 113604 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 113604 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 109961 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 109961 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 120276 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 120276 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 211296 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 211296 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 174565 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 174565 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 125819 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 125819 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 214287 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 214287 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 52817 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 52817 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 204657 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 204657 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 66246 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 66246 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 126379 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 126379 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 125819 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 125819 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 168503 15 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 168503 15 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 214287 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 214287 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 218383 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 92772 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 92772 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 217908 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 73849 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 73849 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 74515 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 74515 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 106115 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 106115 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 213992 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 213992 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 131835 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 131835 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 32266 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 32266 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 105847 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 105847 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 85303 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 85303 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 126208 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 126208 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 214347 4 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 214347 4 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 175445 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 175445 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 46198 5 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 46198 5 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 215360 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 103805 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 103805 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 23445 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 23445 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 105644 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 105644 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 177396 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 177396 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 84064 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 84064 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 205121 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 205121 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 24906 16 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 24906 16 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 56390 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 56390 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 113899 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 113899 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 18502 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 18502 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 18502 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 91824 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 91824 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 117280 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 117280 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 68690 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 68690 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 117149 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 117149 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 195203 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 195203 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 113601 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 113601 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 213324 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 213324 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 213324 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 213324 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 118375 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 118375 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 122229 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 122229 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 66009 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 66009 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 103411 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 103411 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 215023 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 215023 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 107328 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 107328 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 31909 2 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 31909 2 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 195465 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 195465 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 113587 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 113587 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 205483 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 205483 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 208698 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 208698 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 16304 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 16304 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 23598 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 23598 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 124841 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 124841 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 116136 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 116136 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 112914 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 112914 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 212867 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 212867 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 211280 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 211280 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 164110 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 164110 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 164110 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 32836 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 32836 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 35873 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 35873 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
44356710 123389 8 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 123389 8 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 106668 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 106739 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 106739 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 11472 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 11472 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 11827 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 11827 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 11842 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 11842 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 116032 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 116032 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 170266 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 170266 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 49200 11 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 49200 11 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 172415 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 172415 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 23126 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 23126 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 211328 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 211328 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 37497 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 37497 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 203475 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 203475 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 24906 16 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 24906 16 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 89999 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 89999 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 174780 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 174780 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 174780 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 174780 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 204891 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 204891 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 106987 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 106987 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 56390 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 56390 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 73952 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 73952 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 175068 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 175068 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 124837 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 124837 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 106353 13 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 106353 13 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 106353 13 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 106353 13 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 56228 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 56228 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 119531 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 119531 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 126137 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 126137 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 170202 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 170202 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 65827 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 65827 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 106655 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 106655 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 218518 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 217917 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 106655 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 106655 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 33707 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 33707 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 189211 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 189211 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 107487 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 107487 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 107561 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 107561 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 220439 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 11916 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 11916 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 118282 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 118282 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 80423 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 80423 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 125996 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 125996 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 214445 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 214445 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 168075 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 168075 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 168075 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 168075 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 127541 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 127541 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 215972 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 126569 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 126569 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 188313 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 188313 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 113579 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 113579 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 113599 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 113599 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 174765 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 174765 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 65991 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 65991 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 127993 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 127993 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 108886 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 108886 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 127095 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 127095 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 39830 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 39830 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 32662 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 32662 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 35471 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 35471 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 106244 15 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 106244 15 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 116544 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 116544 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 170102 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 170102 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 23303 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 23303 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 108686 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 108686 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 125527 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 125527 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 106914 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 106914 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 108886 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 108886 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 35951 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 35951 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 95976 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 95976 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 95976 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 126739 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 126739 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 23354 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 23354 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 119868 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 119868 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 33131 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 33131 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 126303 15 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 126303 15 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 10887 39 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 10887 39 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 10887 39 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 10887 39 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 10887 39 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 10887 39 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 172024 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 172024 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 116241 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 116241 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 175445 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 175445 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 64296 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 64296 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 25422 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 25422 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 185610 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 185610 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 113391 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 113391 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 24910 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 24910 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 74518 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 74518 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 211420 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 211420 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 85370 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 85370 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 208028 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 208028 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 211420 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 211420 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 134394 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 134394 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 86433 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 86433 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 63291 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 63291 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 96159 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 96159 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 76183 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 76183 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 127779 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 127779 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 217056 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 211183 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 211183 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 105612 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 105612 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 214976 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 214976 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 215008 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 215008 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 210929 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 210929 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 19775 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 19775 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 19775 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 112723 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 112723 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 210923 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 210923 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 16792 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 16792 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 117299 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 117299 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 11760 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 11760 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 85226 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 85226 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 35860 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 35860 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 219410 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 216959 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 172227 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 172227 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 106164 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 106164 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 37034 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 37034 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 204656 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 204656 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 11916 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 11916 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 109883 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 109883 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 109883 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 109883 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 29426 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 29426 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 212736 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 212736 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 22031 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 22031 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 36929 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 36929 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 85136 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 85136 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 11916 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 11916 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 128741 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 128741 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 114073 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 114073 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 114073 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 114073 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 214053 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 214053 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 170111 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 170111 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 85676 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 85676 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 11428 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 11428 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 123522 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 123522 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 35881 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 35881 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 119629 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 119629 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 214174 35 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 214174 35 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 110577 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 110577 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 119124 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 119124 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 44998 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 44998 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 205189 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 205189 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 125945 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 125945 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 113369 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 113369 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 113380 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 113380 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 222706 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 154364 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 154364 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 222706 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 222706 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 66298 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 66298 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 105483 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 105483 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 216268 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 188341 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 188341 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 113574 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 113574 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 180707 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 180707 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 215588 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 68689 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 68689 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 118292 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 118292 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 113378 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 113378 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 116821 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 116821 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 195812 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 195812 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 125954 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 125954 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 85592 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 85592 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 189553 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 189553 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 113582 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 113582 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 127412 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 127412 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 74457 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 74457 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 110577 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 110577 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 65038 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 65038 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 189639 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 189639 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 9020 12 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 9020 12 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 9020 12 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 24720 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 24720 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 51335 2 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 51335 2 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 74496 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 74496 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 56661 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 56661 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 9020 12 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 9020 12 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 9020 12 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 9020 12 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 9020 12 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 9020 12 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 85541 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 85541 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 103778 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 103778 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 106765 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 106765 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 103778 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 103778 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 68641 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 68641 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 65647 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 65647 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 94267 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 94267 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 81270 2 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 81270 2 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 68635 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 68635 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 117317 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 117317 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 85367 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 85367 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 35378 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 35378 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 85257 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 85257 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 179898 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 179898 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 106626 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 106626 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 37549 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 37549 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 24510 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 24510 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 103279 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 103279 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 11916 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 11916 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 85590 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 85590 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 80413 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 80413 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 80423 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 80423 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 185684 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 185684 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 74527 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 74527 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 211308 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 211308 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 126868 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 126868 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 107151 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 107151 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 24908 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 24908 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 115984 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 115984 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 108530 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 108530 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 188733 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 188733 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 127404 1 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 127404 1 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 118425 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 118425 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 118307 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 118307 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 68643 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 68643 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 113379 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 113379 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 217910 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 92173 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 92173 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 9124 23 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 9124 23 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 9124 23 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 126587 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 126587 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 84024 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 84024 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 126344 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 126344 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 35417 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 35417 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 65283 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 65283 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 85402 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 85402 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 213141 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 213141 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 74527 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 74527 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 211308 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 211308 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 119625 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 119625 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 11882 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 11882 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 211416 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 211416 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 74491 1 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 74491 1 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 18962 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 18962 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 18962 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 23695 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 23695 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 175420 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 175420 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 104142 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 104142 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 68645 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 68645 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 29561 41 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 29561 41 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 18849 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 18849 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 18849 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 107328 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 107328 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 111157 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 111157 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 204759 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 204759 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 205844 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 205844 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 205844 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 205844 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 86490 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 86490 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 106642 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 106642 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 210936 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 210936 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 116426 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 116426 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 9124 23 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 9124 23 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 9124 23 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 127376 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 127376 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 127376 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 39797 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 39797 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 105873 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 105873 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 17042 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 17042 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 107328 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 107328 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 16337 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 16337 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 125769 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 125769 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 32544 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 32544 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 113573 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 113573 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 217958 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 222635 7 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 19670 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 19670 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 19670 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 222635 7 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 222635 7 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 222635 7 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 111157 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 111157 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 222635 7 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 205844 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 205844 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 222635 7 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 11236 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 11236 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 11331 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 11331 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 222635 7 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 92771 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 92771 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 29923 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 29923 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 83327 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 83327 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 107254 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 107254 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 53068 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 53068 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 16886 16 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 16886 16 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 204623 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 204623 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 92764 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 92764 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 19624 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 19624 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 19624 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 114133 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 114133 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 39800 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 39800 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 114133 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 114133 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 39800 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 39800 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 205141 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 205141 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 56390 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 56390 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 23903 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 23903 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 127156 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 127156 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 146041 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 146041 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 32763 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 32763 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 113386 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 113386 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 16304 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 16304 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 107077 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 107077 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 113386 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 113386 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 68691 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 68691 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 74521 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 74521 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 84603 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 84603 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 115509 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 115509 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 16304 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 16304 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 107767 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 107767 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 74521 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 74521 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 178410 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 178410 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 24907 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 24907 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 126690 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 126690 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 109672 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 109672 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 172027 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 172027 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 109443 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 109443 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 215364 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 217996 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 207482 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 207482 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 216098 30 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 216098 30 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 127530 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 127530 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 16787 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 16787 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 32448 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 32448 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 196375 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 196375 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 103700 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 103700 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 105953 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 105953 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 114563 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 114563 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 210882 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 210882 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 6995 34 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 6995 34 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 6995 34 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 170633 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 170633 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 58394 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 58394 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 143723 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 143723 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 90009 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 90009 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 109011 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 109011 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 175327 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 175327 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 85604 8 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 85604 8 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 219044 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 9128 67 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 9128 67 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 9128 67 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 9128 67 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 127855 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 127855 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 81270 2 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 81270 2 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 94267 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 94267 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 81270 2 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 81270 2 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 81270 2 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 81270 2 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 81270 2 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 81270 2 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 106647 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 106647 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 106647 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 214621 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 214621 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 207469 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 207469 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 126113 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 126113 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 109917 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 109917 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 54334 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 54334 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 211360 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 211360 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 24909 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 24909 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 68697 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 68697 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 170640 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 170640 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 214174 35 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 214174 35 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 109777 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 109777 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 92893 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 92893 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 109777 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 109777 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 134394 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 134394 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 119883 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 119883 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 168108 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 168108 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 119107 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 119107 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 180421 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 180421 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 161921 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 161921 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 161921 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 161921 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 215251 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 196497 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 196497 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 217339 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 68638 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 68638 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 68639 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 68639 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 74525 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 74525 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 189566 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 189566 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 84601 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 84601 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 215971 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 180796 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 180796 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 148606 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 148606 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 170352 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 170352 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 9800 10 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 9800 10 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 9800 10 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 9800 10 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 9800 10 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 9800 10 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 9800 10 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 9800 10 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 119376 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 119376 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 9800 10 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 9800 10 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 9800 10 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 9800 10 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 131164 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 131164 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 122232 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 122232 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 74525 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 74525 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 84600 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 84600 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 84601 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 84601 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 85209 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 85209 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 209594 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 209594 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 65824 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 65824 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 107043 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 107043 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 147530 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 147530 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 109672 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 109672 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 172027 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 172027 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 127376 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 127376 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 127376 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 80423 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 80423 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 211411 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 211411 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 163297 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 163297 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 58394 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 58394 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 108498 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 108498 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 147559 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 147559 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 109917 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 109917 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 65045 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 65045 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 85372 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 85372 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 58054 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 58054 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 33938 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 33938 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 123558 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 123558 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 179341 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 179341 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 115663 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 115663 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 124000 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 124000 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 147580 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 147580 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 106606 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 106606 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 115550 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 115550 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 65957 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 65957 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 211360 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 211360 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 34429 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 34429 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 25056 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 25056 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 9182 33 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 9182 33 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 9182 33 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 9182 33 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 9182 33 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 9182 33 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 205380 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 205380 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 16606 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 16606 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 185838 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 185838 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 171293 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 171293 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 112130 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 112130 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 217906 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 24911 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 24911 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 211411 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 211411 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 16403 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 16403 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 168466 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 168466 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 84025 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 84025 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 85589 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 85589 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 168494 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 168494 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 121240 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 121240 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 84026 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 84026 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 34772 2 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 34772 2 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 65931 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 65931 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 216720 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 32394 1 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 32394 1 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 33120 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 33120 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 123442 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 123442 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 114079 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 114079 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 217664 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 110938 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 110938 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 181935 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 181935 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 103264 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 103264 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 113389 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 113389 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 113389 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 113389 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 113389 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 113389 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 9124 23 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 9124 23 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 9124 23 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 210928 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 210928 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 188122 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 188122 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 113575 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 113575 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 148713 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 148713 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 171289 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 171289 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 120387 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 120387 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 130824 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 130824 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 17033 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 17033 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 17033 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 17033 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 8677 7 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 8677 7 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 8677 7 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 8677 7 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 8677 7 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 8677 7 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 206333 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 206333 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 217913 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 169760 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 169760 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 108721 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 108721 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 110938 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 110938 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 128285 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 128285 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 169760 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 169760 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 113590 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 113590 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 9124 23 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 9124 23 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 9124 23 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 39110 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 39110 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 65865 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 65865 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 11368 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 11368 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 11863 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 11863 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 108739 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 108739 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 179528 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 179528 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 39019 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 39019 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 122120 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 122120 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 123638 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 123638 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 36867 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 36867 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 213462 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 213462 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 123499 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 123499 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 174815 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 174815 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 113373 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 113373 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 215231 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 215231 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 215231 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 214955 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 214955 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 16895 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 16895 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 216564 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 217909 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 65969 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 65969 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 58394 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 58394 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 214174 35 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 214174 35 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 174765 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 174765 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 122285 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 122285 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 125227 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 125227 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 74490 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 74490 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 175087 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 175087 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 11916 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 11916 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 214113 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 214113 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 118363 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 118363 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 16571 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 16571 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 174631 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 174631 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 115604 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 115604 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 108896 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 108896 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 127155 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 127155 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 24909 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 24909 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 11916 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 11916 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 108896 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 108896 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 32897 9 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 32897 9 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 32913 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 32913 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 11390 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 11390 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 36086 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 36086 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 65986 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 65986 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 123316 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 123316 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 105340 1 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 105340 1 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 24912 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 24912 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 211358 31 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 211358 31 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 216962 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 80412 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 80412 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 68637 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 68637 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 23013 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 23013 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 9798 9 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 9798 9 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 9798 9 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 9798 9 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 9800 10 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 9800 10 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 9800 10 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 9800 10 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 9798 9 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 9798 9 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 9798 9 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 9798 9 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 9798 9 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 9798 9 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 9798 9 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 9798 9 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 9798 9 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 9798 9 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 9798 9 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 9798 9 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 79242 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 79242 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 107538 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 107538 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 116004 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 116004 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 127250 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 127250 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 74461 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 74461 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 126422 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 126422 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 113585 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 113585 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 115324 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 115324 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 126474 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 126474 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 147502 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 147502 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 147525 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 147525 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 85565 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 85565 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 118137 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 118137 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 65857 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 65857 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 74536 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 74536 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 114004 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 114004 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 115064 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 115064 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 11244 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 11244 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 196147 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 196147 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 175514 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 175514 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 128066 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 128066 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 106738 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 106738 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 126359 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 126359 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 215362 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 214252 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 214252 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 23179 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 23179 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 117648 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 117648 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 204715 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 204715 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 123828 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 123828 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 213882 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 213882 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 205162 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 205162 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 122186 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 122186 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 214156 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 214156 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 176990 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 176990 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 123310 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 123310 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 106738 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 106738 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 56390 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 56390 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 113391 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 113391 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 218002 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 126670 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 126670 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 127533 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 127533 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 218002 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 104862 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 104862 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 32958 13 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 32958 13 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 127533 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 127533 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 11916 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 11916 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 126727 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 126727 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 210666 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 210666 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 126900 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 126900 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 127014 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 127014 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 216960 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 169698 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 169698 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 107265 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 107265 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 52113 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 52113 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 214209 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 214209 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 175514 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 175514 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 216961 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 211447 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 211447 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 167553 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 167553 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 167745 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 167745 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 185922 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 185922 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 204174 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 204174 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 80423 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 80423 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 113376 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 113376 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 218510 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 211447 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 211447 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 214385 45 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 214385 45 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 125637 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 125637 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 107485 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 107485 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 217918 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 113333 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 113333 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 110474 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 110474 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 66296 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 66296 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 189099 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 189099 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 92770 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 92770 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 211494 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 211494 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 171862 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 171862 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 135890 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 135890 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 23400 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 23400 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 23616 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 23616 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 194605 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 194605 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 185892 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 185892 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 168795 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 168795 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 123491 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 123491 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 24051 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 24051 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 205083 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 205083 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 127279 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 127279 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 109480 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 109480 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 174894 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 174894 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 107415 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 107415 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 211532 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 211532 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 215629 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 146948 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 146948 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 84622 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 84622 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 38430 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 38430 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 107431 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 107431 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 124056 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 124056 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 194605 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 194605 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 25290 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 25290 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 127376 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 127376 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 127376 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 175514 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 175514 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 23606 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 23606 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 172012 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 172012 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 211532 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 211532 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 16229 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 16229 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 109445 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 109445 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 213651 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 213651 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 115864 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 115864 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 92537 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 92537 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 85292 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 85292 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 113583 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 113583 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 11452 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 11452 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 37561 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 37561 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 125574 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 125574 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 35824 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 35824 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 68632 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 68632 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 50864 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 50864 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 205206 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 205206 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 149614 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 149614 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 213368 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 213368 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 210905 4 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 210905 4 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 210905 4 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 210905 4 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 210992 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 210992 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 174647 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 174647 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 215584 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 84027 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 84027 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 123123 13 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 123123 13 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 175109 8 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 175109 8 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 210905 4 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 210905 4 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 179715 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 179715 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 188315 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 188315 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 107803 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 107803 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 211500 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 211500 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 74524 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 74524 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 113374 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 113374 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 68291 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 68291 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 215584 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 66229 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 66229 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 215584 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 215584 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 217995 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 218008 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 218008 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 217995 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 218008 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 127616 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 127616 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 218008 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 131164 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 131164 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 217995 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 168521 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 168521 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 86489 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 86489 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 217982 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 127376 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 127376 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 127376 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 85210 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 85210 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 127238 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 127238 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 9798 9 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 9798 9 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 9798 9 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 9798 9 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 23624 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 23624 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 65830 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 65830 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 215970 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 189063 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 189063 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 109214 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 109214 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 113592 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 113592 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 23558 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 23558 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 65847 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 65847 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 196505 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 196505 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 147599 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 147599 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 112953 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 112953 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 210997 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 210997 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 210911 1 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 210911 1 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 65687 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 65687 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 65811 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 65811 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 66004 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 66004 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 90242 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 90242 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 127177 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 127177 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 35434 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 35434 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 110757 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 110757 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 112934 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 112934 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 220701 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 74486 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 74486 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 74498 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 74498 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 74502 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 74502 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 58054 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 58054 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 16659 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 16659 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 214019 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 214019 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 204976 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 204976 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 210997 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 210997 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 56390 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 56390 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 125933 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 125933 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 127503 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 127503 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 213518 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 213518 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 213518 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 213518 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 35403 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 35403 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 113222 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 113222 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 126754 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 126754 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 164654 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 164654 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 215361 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 108364 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 108364 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 117459 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 117459 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 32395 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 32395 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 32748 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 32748 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 34767 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 34767 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 113569 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 113569 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 175012 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 175012 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 163341 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 163341 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 109984 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 109984 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 85279 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 85279 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 83327 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 83327 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 175085 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 175085 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 103464 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 103464 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 35190 2 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 35190 2 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 122776 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 122776 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 64906 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 64906 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 174874 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 103464 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 103464 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 76185 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 76185 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 205126 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 205126 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 25334 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 25334 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 19048 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 19048 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 19048 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 219140 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 204655 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 204655 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 185683 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 185683 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 215961 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 56390 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 56390 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 104154 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 104154 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 219414 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 171531 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 171531 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 76181 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 76181 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 24718 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 24718 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 216958 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 211430 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 211430 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 107274 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 107274 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 107274 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 85616 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 85616 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 164755 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 164755 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 16302 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 16302 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 121319 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 121319 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 16302 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 16302 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 11197 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 11197 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 65888 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 65888 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 126727 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 126727 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 37967 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 37967 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 105337 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 105337 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 146948 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 146948 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 23539 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 23539 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 68634 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 68634 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 113589 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 113589 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 169959 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 169959 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 56390 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 56390 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 74463 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 74463 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 103216 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 103216 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 110621 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 110621 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 65868 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 65868 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 80853 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 80853 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 11916 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 11916 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 24547 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 24547 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 38642 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 38642 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 66131 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 66131 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 174980 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 174980 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 174829 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 174829 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 204883 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 204883 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 108667 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 108667 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 113392 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 113392 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 113392 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 113392 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 121837 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 121837 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 121998 8 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 121998 8 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 85614 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 85614 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 80418 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 80418 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 211274 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 211274 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 74149 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 74149 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 34387 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 34387 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 105743 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 105743 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 74464 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 74464 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 174829 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 174829 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 210955 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 210955 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 106275 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 106275 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 171972 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 171972 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 174753 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 174753 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 8363 14 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 8363 14 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 8363 14 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 8363 14 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 8363 14 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 105675 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 105675 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 214235 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 214235 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 35999 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 35999 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 127267 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 127267 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 213862 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 213862 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 80423 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 80423 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 68633 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 68633 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 68636 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 68636 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 68646 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 68646 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 105130 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 105130 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 196437 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 196437 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 172345 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 172345 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 114130 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 114130 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 185225 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 185225 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 117394 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 117394 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 16320 14 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 16320 14 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 105521 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 105521 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 105521 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 105521 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 127128 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 127128 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 175108 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 175108 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 113908 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 113908 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 212624 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 212624 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 168505 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 168505 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 168564 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 168564 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 204654 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 204654 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 204858 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 204858 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 20757 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 20757 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 20757 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 213522 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 213522 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 80421 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 80421 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 11916 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 11916 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 103262 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 103262 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 180954 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 180954 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 166539 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 166539 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 80370 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 80370 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 174925 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 174925 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 147575 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 147575 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 175411 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 175411 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 220444 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 147501 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 147501 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 110464 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 110464 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 109805 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 109805 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 123422 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 123422 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 74538 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 74538 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 107836 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 107836 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 123598 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 123598 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 216178 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 107626 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 107626 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 29648 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 29648 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 148186 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 148186 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 205130 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 205130 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 148186 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 148186 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 117327 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 117327 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 122233 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 122233 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 148186 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 148186 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 56164 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 56164 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 80411 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 80411 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 209570 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 209570 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 107274 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 107274 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 107274 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 205052 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 205052 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 127024 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 127024 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 113581 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 113581 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 80419 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 80419 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 106830 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 106830 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 113907 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 113907 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 107274 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 107274 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 107274 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 84023 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 84023 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 105902 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 105902 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 209570 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 209570 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 123814 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 123814 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 11823 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 11823 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 85289 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 85289 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 106855 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 106855 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 126109 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 126109 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 85260 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 85260 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 65389 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 65389 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 64332 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 64332 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 85371 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 85371 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 11883 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 11883 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 107479 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 107479 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 113602 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 113602 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 176497 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 176497 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 11916 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 11916 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 116561 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 116561 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 216565 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 31779 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 31779 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 113584 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 113584 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 106809 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 106809 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 210039 27 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 210039 27 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 196505 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 196505 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 175395 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 175395 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 170047 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 170047 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 181548 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 181548 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 121414 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 121414 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 116453 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 116453 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 65781 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 65781 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 104114 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 104114 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 24882 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 24882 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 175013 4 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 175013 4 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 80416 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 80416 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 180511 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 180511 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 215584 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 74290 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 74290 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 86318 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 86318 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 108405 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 108405 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 31430 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 31430 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 119178 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 119178 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 85619 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 85619 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 113371 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 113371 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 57564 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 57564 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 105575 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 105575 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 109773 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 109773 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 211460 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 211460 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 105369 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 105369 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 68696 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 68696 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 175829 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 175829 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 109773 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 109773 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 211460 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 211460 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 175829 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 175829 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 105369 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 105369 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 105369 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 105369 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 210905 4 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 210905 4 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 217996 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 175016 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 175016 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 127287 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 127287 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 113586 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 113586 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 66208 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 66208 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 11916 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 11916 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 211538 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 211538 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 180906 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 180906 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 121606 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 121606 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 124867 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 124867 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 9019 5 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 9019 5 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 9019 5 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 16777 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 16777 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 123533 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 123533 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 113572 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 113572 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 126448 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 126448 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 215614 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 145143 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 145143 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 147566 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 147566 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 39493 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 39493 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 31740 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 31740 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 215614 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 211193 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 211193 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 145143 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 145143 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 107673 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 107673 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 172290 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 172290 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 212114 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 212114 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 85261 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 85261 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 171661 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 171661 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 162484 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 162484 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 64526 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 64526 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 113404 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 113404 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 211538 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 211538 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 217984 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 189575 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 189575 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 115992 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 115992 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 33726 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 33726 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 85586 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 85586 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 113571 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 113571 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 126263 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 126263 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 125667 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 125667 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 106408 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 106408 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 124084 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 124084 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 76187 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 76187 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 127141 7 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 127141 7 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 85374 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 85374 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 112431 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 112431 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 111354 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 111354 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 80423 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 80423 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 178607 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 178607 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 111354 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 111354 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 214199 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 214199 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 11393 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 11393 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 108730 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 108730 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 214063 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 214063 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 16671 9 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 16671 9 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 16832 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 16832 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 115818 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 115818 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 106519 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 106519 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 27548 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 27548 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 215384 33 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 11443 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 11443 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 74519 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 74519 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 188340 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 188340 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 188342 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 188342 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 215616 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 117092 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 117092 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 34724 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 34724 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 105553 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 105553 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 7713 37 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 7713 37 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 7713 37 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 7713 37 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 80735 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 80735 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 7713 37 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 7713 37 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 7713 37 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 7713 37 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 92763 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 92763 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 7713 37 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 7713 37 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 7713 37 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 7713 37 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 103464 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 103464 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 7713 37 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 7713 37 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 7713 37 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 7713 37 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 126283 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 126283 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 38448 6 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 38448 6 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 7713 37 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 7713 37 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 7713 37 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 7713 37 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 83327 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 83327 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 94451 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 94451 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 175306 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 175306 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 85587 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 85587 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 112963 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 112963 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 112963 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 112963 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 85208 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 85208 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 80415 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 80415 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 127904 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 127904 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 117778 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 117778 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 123505 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 123505 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 127780 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 127780 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 174943 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 174943 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 106097 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 185754 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 185754 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 105156 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 105156 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 123483 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 123483 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 41444 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 41444 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 206828 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 206828 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 123646 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 123646 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 39478 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 39478 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 147539 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 147539 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 103464 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 103464 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 114582 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 114582 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 74529 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 74529 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 126080 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 126080 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 214030 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 214030 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 215626 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 113385 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 113385 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 185610 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 185610 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 16772 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 16772 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 123387 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 123387 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 11916 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 11916 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 178492 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 178492 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 128619 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 128619 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 55098 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 55098 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 123509 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 123509 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 185685 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 185685 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 23573 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 23573 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 53319 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 53319 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 10590 28 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 10590 28 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 10590 28 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 24745 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 24745 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 58245 1 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 58245 1 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 175393 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 175393 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 147703 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 147703 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 171801 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 171801 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 116560 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 116560 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 109733 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 109733 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 213978 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 213978 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 211496 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 211496 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 16385 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 16385 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 24911 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 24911 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 113768 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 113768 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 50312 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 50312 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 212586 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 212586 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 109733 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 109733 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 126344 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 126344 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 113768 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 113768 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 211496 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 211496 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 38708 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 38708 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 32183 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 32183 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 106629 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 106629 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 62374 5 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 62374 5 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 62374 5 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 84624 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 84624 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 173920 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 173920 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 123620 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 123620 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 65817 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 65817 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 38251 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 38251 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 20736 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 20736 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 20736 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 84600 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 84600 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 113588 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 113588 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 80369 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 80369 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 24908 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 24908 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 107737 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 107737 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 142133 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 142133 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 34734 9 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 34734 9 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 104946 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 104946 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 213835 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 213835 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 62374 5 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 62374 5 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 62374 5 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 104079 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 104079 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 109945 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 109945 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 109945 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 109945 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 209846 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 209846 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 16320 14 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 16320 14 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 16320 14 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 16320 14 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 108492 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 108492 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 74306 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 74306 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 215141 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 215141 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 126926 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 126926 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 217994 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 220585 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 188319 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 188319 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 113393 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 113393 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 113393 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 114183 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 114183 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 217997 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 9124 23 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 9124 23 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 9124 23 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 124619 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 124619 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 12978 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 12978 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 214347 4 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 214347 4 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 121324 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 121324 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 214347 4 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 214347 4 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 107484 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 107484 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 116004 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 116004 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 116004 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 116004 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 116004 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 116004 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 11916 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 11916 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 85365 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 85365 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 211288 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 211288 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 28389 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 28389 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 170192 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 170192 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 116496 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 116496 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 122192 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 122192 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 219459 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 19636 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 19636 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 19636 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 107183 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 107183 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 217650 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 20422 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 20422 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 20422 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 74501 1 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 74501 1 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 211288 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 211288 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 10882 33 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 10882 33 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 10882 33 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 10882 33 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 56390 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 56390 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 217911 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 168503 15 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 168503 15 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 56390 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 56390 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 68631 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 68631 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 116034 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 116034 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 177208 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 177208 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 222708 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 213039 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 213039 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 103750 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 103750 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 220460 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 126259 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 126259 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 219081 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 11916 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 11916 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 190885 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 190885 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 108991 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 108991 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 24906 16 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 24906 16 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 177397 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 177397 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 107757 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 107757 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 127137 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 127137 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 177397 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 177397 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 16224 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 16224 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 128073 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 128073 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 113745 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 113745 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 16458 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 16458 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 123647 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 123647 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 11801 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 11801 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 127503 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 127503 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 119558 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 119558 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 114115 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 114115 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 217327 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 217327 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 217327 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 11031 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 11031 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 107475 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 107475 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 214206 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 214206 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 204763 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 204763 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 43726 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 43726 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 43726 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 43726 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 92765 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 92765 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 23613 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 23613 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 148017 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 148017 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 116004 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 116004 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 57636 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 57636 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 108395 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 108395 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 84581 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 84581 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 56390 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 56390 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 127602 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 127602 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 204764 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 204764 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 68644 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 68644 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 113577 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 113577 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 138129 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 138129 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 105737 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 105737 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 50466 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 50466 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 220676 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 211461 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 211461 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 32711 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 32711 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 194891 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 194891 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 215051 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 215051 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 16623 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 16623 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 125799 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 125799 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 121592 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 121592 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 109410 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 109410 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 114895 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 114895 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 66483 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 66483 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 117413 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 117413 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 211461 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 211461 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 114122 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 114122 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 16269 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 16269 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 34396 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 34396 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 218489 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 65874 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 65874 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 126057 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 126057 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 113597 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 113597 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 206579 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 206579 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 108828 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 108828 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 211210 2 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 211210 2 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 16791 1 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 16791 1 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 175708 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 175708 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 217307 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 126971 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 126971 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 86323 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 86323 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 27066 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 27066 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 65858 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 65858 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 214723 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 214723 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 117316 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 117316 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 123380 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 123380 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 74517 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 74517 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 174670 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 174670 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 172775 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 172775 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 209923 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 209923 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 68694 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 68694 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 16929 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 16929 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 113375 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 113375 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 171972 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 171972 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 113407 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 113407 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 177357 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 177357 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 106647 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 106647 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 106647 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 74528 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 74528 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 211244 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 211244 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 211244 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 211244 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 172104 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 172104 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 115514 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 115514 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 35012 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 35012 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 56390 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 56390 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 19866 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 19866 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 19866 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 68647 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 68647 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 86321 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 86321 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 196560 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 196560 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 217912 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 59265 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 59265 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 85591 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 85591 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 120407 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 120407 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 107568 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 107568 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 24707 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 24707 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 85399 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 85399 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 29561 41 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 29561 41 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 29561 41 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 29561 41 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 117255 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 117255 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 29561 41 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 29561 41 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 123523 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 123523 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 36399 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 36399 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 100013 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 100013 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 111155 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 111155 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 23549 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 23549 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 74497 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 74497 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 147362 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 147362 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 35256 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 35256 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 123421 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 123421 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 80423 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 80423 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 214723 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 214723 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 106520 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 106520 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 82710 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 82710 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 208030 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 208030 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 211412 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 211412 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 172073 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 172073 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 174817 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 174817 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 107240 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 107240 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 174954 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 174954 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 193806 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 193806 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 108748 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 108748 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 85403 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 85403 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 107274 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 107274 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 107274 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 74516 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 74516 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 18981 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 18981 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 18981 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 177797 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 177797 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 127829 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 127829 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 23329 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 23329 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 85211 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 85211 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 16832 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 16832 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 16832 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 16832 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 54784 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 54784 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 8585 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 8585 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 8585 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 108838 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 108838 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 218519 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 126569 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 126569 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 188563 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 188563 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 215630 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 23292 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 23292 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 74488 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 74488 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 214261 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 214261 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 126112 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 126112 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 125568 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 125568 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 215615 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 115536 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 115536 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 103716 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 103716 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 9184 5 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 9184 5 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 9184 5 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 9184 5 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 9184 5 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 9184 5 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 210264 36 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 210264 36 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 216963 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 219092 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 110635 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 110635 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 212573 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 212573 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 108870 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 108870 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 212520 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 212520 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 212520 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 212520 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 113591 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 113591 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 122236 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 122236 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 217907 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 209570 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 209570 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 116164 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 116164 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 209570 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 209570 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 107601 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 107601 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 209570 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 209570 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 85258 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 85258 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 214347 4 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 214347 4 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 68693 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 68693 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 108973 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 108973 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 214347 4 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 214347 4 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 52113 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 52113 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 52574 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 52574 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 52574 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 85401 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 85401 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 118230 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 118230 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 20757 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 20757 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 20757 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 85588 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 85588 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 74489 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 74489 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 149614 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 149614 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 23605 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 23605 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 16382 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 16382 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 84012 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 84012 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 218502 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 201584 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 201584 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 103861 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 103861 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 106655 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 106655 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 205084 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 205084 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 214636 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 214636 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 64612 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 64612 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 124091 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 124091 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 32656 14 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 32656 14 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 56390 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 56390 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 80371 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 80371 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 213011 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 213011 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 85398 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 85398 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 126422 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 126422 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 92767 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 92767 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 23637 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 23637 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 33226 13 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 33226 13 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 209704 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 209704 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 120387 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 120387 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 125929 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 125929 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 121280 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 121280 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 128772 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 128772 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 74512 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 74512 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 11341 1 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 11341 1 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 64360 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 64360 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 210044 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 210044 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 216964 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 168504 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 168504 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 116413 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 116413 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 181215 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 181215 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 80423 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 80423 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 216269 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 195204 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 195204 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 170140 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 170140 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 191898 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 191898 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 170140 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 170140 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 108215 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 108215 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 58394 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 58394 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 34327 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 34327 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 85615 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 85615 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 107453 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 107453 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 19596 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 19596 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 19596 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 127376 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 127376 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 127376 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 85366 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 85366 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 211478 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 211478 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 80423 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 80423 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 74526 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 74526 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 109071 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 109071 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 127576 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 127576 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 214414 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 214414 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 119624 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 119624 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 126101 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 126101 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 39500 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 39500 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 163909 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 163909 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 148576 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 148576 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 113390 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 113390 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 109986 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 109986 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 211478 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 211478 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 23364 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 23364 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 113593 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 113593 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 113600 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 113600 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 106431 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 106431 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 147215 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 147215 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 57564 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 57564 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 65881 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 65881 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 213673 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 213673 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 66380 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 66380 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 53282 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 53282 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 76188 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 76188 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 66110 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 66110 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 124063 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 124063 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 127752 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 127752 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 58627 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 58627 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 29897 14 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 29897 14 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 106808 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 106808 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 66194 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 66194 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 216966 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 107556 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 107556 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 125329 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 125329 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 211305 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 211305 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 16745 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 16745 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 162541 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 162541 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 164651 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 164651 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 211305 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 211305 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 82721 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 82721 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 23339 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 23339 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 63110 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 63110 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 105938 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 105938 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 214174 35 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 214174 35 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 121895 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 121895 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 127806 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 127806 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 123438 13 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 123438 13 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 214174 35 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 214174 35 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 121596 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 121596 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 113407 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 113407 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 216965 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 213417 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 213417 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 107061 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 107061 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 83328 3 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 83328 3 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 105612 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 105612 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 127376 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 127376 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 127376 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 213263 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 213263 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 213263 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 213263 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 213263 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 213263 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 106632 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 106632 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 215110 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 215110 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 147549 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 147549 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 211320 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 211320 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 74540 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 74540 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 211320 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 211320 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 113603 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 113603 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 20068 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 20068 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 20068 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 105917 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 105917 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 23532 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 23532 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 172082 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 172082 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 123390 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 123390 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 74460 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 74460 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 172082 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 172082 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 23302 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 23302 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 127911 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 127911 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 36487 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 36487 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 127781 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 127781 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 12978 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 12978 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 112923 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 112923 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 9799 14 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 9799 14 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 9799 14 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 9799 14 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 126284 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 126284 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 210966 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 210966 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 102560 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 102560 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 80423 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 80423 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 113372 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 113372 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 147568 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 147568 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 214385 45 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 214385 45 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 187949 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 187949 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 209715 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 209715 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 9000 9 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 9000 9 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 9000 9 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 9000 9 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 32400 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 32400 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 34541 13 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 34541 13 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 219446 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 170215 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 170215 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 211196 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 211196 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 170215 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 170215 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 33699 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 33699 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 211196 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 211196 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 170215 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 170215 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 211196 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 211196 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 113919 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 113919 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 113919 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 113919 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 113370 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 113370 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 189234 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 189234 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 52574 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 52574 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 52574 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 210982 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 210982 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 126532 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 126532 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 115609 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 115609 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 80414 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 80414 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 218075 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 147547 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 147547 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 84599 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 84599 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 74459 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 74459 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 38293 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 38293 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 196453 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 196453 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 196453 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 11795 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 11795 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 92769 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 92769 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 119884 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 119884 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 39006 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 39006 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 124895 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 124895 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 74483 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 74483 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 74495 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 74495 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 106798 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 85135 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 85135 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 23615 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 23615 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 106910 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 106910 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 114003 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 114003 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 168633 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 168633 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 211488 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 211488 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 211488 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 211488 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 85566 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 85566 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 116896 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 116896 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 55098 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 55098 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 214743 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 214743 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 65794 2 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 65794 2 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 203361 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 203361 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 103825 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 103825 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 216464 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 79799 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 79799 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 108374 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 108374 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 121572 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 121572 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 118222 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 118222 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 122235 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 122235 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 194606 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 194606 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 181297 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 181297 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 126704 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 126704 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 174764 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 174764 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 215619 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 85291 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 85291 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 55276 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 55276 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 216459 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 65936 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 65936 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 164193 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 164193 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 123547 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 123547 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 127589 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 127589 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 8178 35 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 8178 35 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 8178 35 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 8178 35 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 165016 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 165016 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 106532 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 106532 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 185839 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 185839 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 68640 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 68640 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 214174 35 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 215999 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 216000 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 23378 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 23378 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 107080 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 107080 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 106682 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 106682 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 211277 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 211277 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 213310 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 213310 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 213310 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 213310 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 80422 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 80422 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 177258 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 177258 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 177258 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 11916 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 11916 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 120084 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 120084 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 120084 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 120084 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 16775 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 16775 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 56164 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 56164 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 23609 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 23609 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 120925 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 120925 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 127502 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 127502 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 170684 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 170684 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 213875 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 213875 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 205434 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 205434 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 174707 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 174707 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 148569 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 148569 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 210982 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 210982 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 211263 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 211263 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 29326 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 29326 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 179991 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 179991 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 106655 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 106655 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 217916 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 76186 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 76186 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 215978 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 80420 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 80420 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 68692 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 68692 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 164561 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 164561 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 109728 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 109728 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 109797 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 109797 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 122230 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 122230 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 33285 14 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 33285 14 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 84620 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 84620 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 111561 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 111561 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 11447 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 11447 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 218494 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 84598 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 84598 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 23621 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 23621 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 207121 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 207121 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 219477 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 85369 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 85369 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 199311 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 199311 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 105906 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 105906 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 148723 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 148723 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 213870 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 213870 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 217905 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 80417 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 80417 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 218075 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 175307 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 175307 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 214723 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 214723 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 56661 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 56661 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 84623 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 84623 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 106951 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 106951 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 179718 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 179718 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 23707 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 23707 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 204919 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 204919 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 66331 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 66331 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 85404 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 85404 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 215633 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 106163 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 106163 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 94451 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 94451 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 17193 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 17193 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 68695 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 68695 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 211285 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 211285 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 123071 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 123071 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 127138 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 127138 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 128774 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 128774 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 174574 1 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 174574 1 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 80423 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 80423 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 211285 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 211285 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 127546 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 127546 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 219072 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 103265 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 103265 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 65892 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 65892 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 205128 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 205128 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 213235 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 213235 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 214451 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 214451 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 114809 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 114809 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 57636 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 57636 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 104920 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 104920 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 51699 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 51699 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 175033 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 175033 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 126974 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 126974 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 104920 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 104920 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 186122 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 186122 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 186122 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 113474 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 113474 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 214385 45 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 214385 45 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 172221 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 172221 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 211704 3 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 211704 3 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 211704 3 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 211704 3 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 211704 3 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 211704 3 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 113348 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 113348 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 34832 2 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 34832 2 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7713 37 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 7713 37 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 7713 37 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 7713 37 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 214174 35 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 214174 35 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 214385 45 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 214385 45 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 126226 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 126226 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 219095 4 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 219095 4 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 70018 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 70018 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 6995 34 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 6995 34 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 6995 34 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 170215 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 170215 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 219095 4 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 219095 4 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 76186 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 76186 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 70019 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 70019 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 216039 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 120387 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 120387 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 214385 45 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 214385 45 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 10066 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 10066 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 10066 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 219095 4 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 219095 4 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 219095 4 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 219095 4 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 33348 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 33348 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 216472 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 23144 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 23144 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 11515 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 11515 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 215366 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 21516 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 21516 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 21516 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 214385 45 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 214385 45 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 115401 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 115401 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 8182 9 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 8182 9 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 8182 9 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 8182 9 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 174758 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 174758 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 203715 1 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 203715 1 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 205691 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 205691 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 21318 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 21318 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 204503 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 204503 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 168089 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 168089 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 122261 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 122261 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 214160 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 214160 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 175477 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 175477 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 82764 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 82764 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 219651 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 144286 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 144286 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 163661 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 163661 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 18569 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 18569 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 18569 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 18577 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 18577 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 18577 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 32925 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 32925 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 70912 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 70912 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 70929 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 70929 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 16571 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 16571 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 115204 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 115204 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 162472 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 162472 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 106710 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 106710 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 162508 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 162508 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 215217 4 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 215217 4 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 70915 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 70915 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 220397 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 114275 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 114275 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 120570 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 120570 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 216173 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 215388 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 215388 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 218507 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 218253 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 22283 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 22283 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 170689 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 170689 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 175034 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 175034 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 8674 16 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 8674 16 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 8674 16 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 121275 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 121275 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 82764 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 82764 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 215217 4 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 215217 4 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 120741 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 120741 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 163794 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 163794 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 82877 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 82877 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 200570 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 200570 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 222635 7 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 205588 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 205588 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 120179 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 120179 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 218314 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 218316 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 35200 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 35200 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 123756 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 123756 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 114326 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 114326 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 77405 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 77405 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 124237 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 124237 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 215217 4 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 215217 4 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 46198 5 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 46198 5 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 78476 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 78476 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 204368 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 204368 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 121571 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 121571 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 148320 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 148320 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 101443 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 101443 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 108501 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 108501 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 121551 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 121551 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 9124 23 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 9124 23 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 9124 23 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 89999 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 89999 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 140340 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 140340 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 119451 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 119451 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 126140 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 126140 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 215217 4 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 215217 4 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 148303 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 148303 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 215362 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 218319 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 214279 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 214279 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 216629 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 21129 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 21129 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 70929 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 70929 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 114230 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 114230 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 125998 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 125998 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 175407 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 175407 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 78455 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 78455 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 70916 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 70916 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 70914 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 70914 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 99268 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 99268 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 99268 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 119650 2 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 119650 2 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 120591 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 120591 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 218173 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 217056 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 216657 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 88901 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 88901 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 70793 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 70793 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 145701 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 145701 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 119784 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 119784 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 114181 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 114181 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 113955 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 113955 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 102756 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 102756 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 21964 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 21964 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 220641 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 212778 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 212778 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 212778 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 114073 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 114073 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 204202 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 204202 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 203542 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 203542 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 203750 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 203750 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 205534 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 205534 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 70927 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 70927 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 11032 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 11032 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 119857 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 119857 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 99268 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 99268 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 99268 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 21475 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 21475 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 21475 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 216122 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 174981 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 174981 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 34688 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 34688 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 119650 2 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 119650 2 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 126084 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 126084 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 70933 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 70933 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 19953 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 19953 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 19953 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 11882 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 11882 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 186122 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 186122 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 186122 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 70926 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 70926 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 214174 35 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 214174 35 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 92209 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 92209 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 70923 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 70923 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 105349 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 105349 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 222595 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 215364 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 213912 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 213912 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 11515 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 11515 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 38091 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 38091 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 107274 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 107274 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 107274 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 175588 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 175588 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 125519 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 125519 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 96160 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 96160 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 21475 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 21475 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 21475 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 120643 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 120643 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 76186 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 76186 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 21964 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 21964 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 143723 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 143723 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 90009 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 90009 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 143731 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 143731 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 120780 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 120780 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 204177 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 204177 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 204249 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 204249 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 203681 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 203681 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 205580 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 205580 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 89238 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 89238 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 121571 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 121571 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 204580 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 204580 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 205664 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 205664 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 101658 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 101658 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 125816 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 125816 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 125816 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 172977 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 172977 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 11183 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 11183 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 19083 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 19083 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 19083 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 125816 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 125816 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 125816 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 9184 5 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 9184 5 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 9184 5 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 120905 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 120905 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 119843 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 119843 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 219159 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 104940 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 104940 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 119879 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 119879 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 76186 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 76186 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 218171 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 218172 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 170272 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 170272 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 215377 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 218245 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 103777 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 103777 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 171652 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 171652 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 219044 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 214992 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 214992 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 123552 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 123552 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 70921 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 70921 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 70927 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 70927 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 70932 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 70932 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 19754 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 19754 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 121361 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 121361 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 125647 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 125647 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 125816 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 125816 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 125816 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 147405 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 147405 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 103487 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 103487 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 92293 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 92293 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 108026 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 108026 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 218315 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 80423 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 80423 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 171637 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 171637 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 172031 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 172031 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 150084 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 150084 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 168688 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 168688 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 174838 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 174838 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 21667 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 21667 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 120744 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 120744 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 141199 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 141199 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 22065 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 22065 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 120268 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 120268 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 120911 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 120911 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 68981 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 68981 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 96230 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 96230 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 70928 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 70928 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 108347 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 108347 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 173690 75 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 173690 75 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 173690 75 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 170445 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 170445 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 96232 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 96232 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 218267 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 78226 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 78226 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 102691 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 102691 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 102901 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 102901 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 118764 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 118764 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 214504 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 214504 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 214397 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 214397 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 114062 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 114062 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 121551 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 121551 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 218313 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 215627 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 96229 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 96229 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 100758 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 100758 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 100799 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 100799 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 100800 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 100800 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 100833 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 100833 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 100834 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 100834 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 100835 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 100835 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 100877 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 100877 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 100878 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 100878 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 100918 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 100918 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 100945 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 100945 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 100974 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 100974 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 101098 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 101098 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 161278 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 161278 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 161279 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 161279 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 161513 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 161513 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 161648 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 161648 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 204469 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 204469 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 103500 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 103500 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 172811 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 172811 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 205815 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 205815 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 203538 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 203538 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 205751 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 205751 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 21182 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 21182 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 22271 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 22271 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 105518 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 105518 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 78851 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 78851 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 78851 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 161701 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 161701 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 161724 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 161724 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 90025 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 90025 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 92292 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 92292 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 175727 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 175727 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 19034 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 19034 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 19034 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 78851 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 78851 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 78851 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 161629 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 161629 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 125761 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 125761 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 70929 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 70929 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 108351 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 108351 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 123563 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 123563 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 70928 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 70928 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 120244 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 120244 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 125816 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 125816 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 125816 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 70793 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 70793 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 113463 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 113463 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 70913 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 70913 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 80423 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 80423 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 10882 33 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 10882 33 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 10882 33 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 10882 33 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 102600 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 102600 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 108621 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 108621 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 214467 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 214467 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 11038 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 11038 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 96233 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 96233 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 78754 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 78754 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 16577 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 16577 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 213186 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 213186 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 164646 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 164646 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 216651 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 218253 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 217915 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 77148 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 77148 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 120294 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 120294 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 143734 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 143734 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 16982 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 16982 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 64948 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 64948 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 215383 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 215383 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 11035 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 11035 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 21516 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 21516 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 21516 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 113352 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 113352 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 76186 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 76186 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 196453 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 196453 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 196453 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 76186 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 76186 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 76183 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 76183 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 10882 33 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 10882 33 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 10882 33 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 10882 33 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 215109 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 215109 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 175249 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 175249 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 175249 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 175018 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 175018 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 175408 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 175408 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 78913 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 78913 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 119882 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 119882 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 114326 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 114326 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 70928 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 70928 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 10882 33 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 10882 33 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 10882 33 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 10882 33 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 205579 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 205579 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 81270 2 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 81270 2 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 218261 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 103858 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 103858 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 119015 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 119015 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 204248 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 204248 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 204532 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 204532 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 160674 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 160674 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 214174 35 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 214174 35 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 162457 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 162457 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 114510 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 114510 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 204367 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 204367 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 161395 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 161395 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 148694 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 148694 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 108392 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 108392 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 18576 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 18576 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 18576 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 18700 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 18700 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 18700 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 19040 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 19040 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 19040 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 19057 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 19057 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 19057 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 215961 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 215361 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 215961 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 218311 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 219414 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 79304 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 79304 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 11515 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 11515 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 70931 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 70931 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 215383 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 215383 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 70922 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 70922 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 168774 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 168774 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 217434 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 162014 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 162014 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 105810 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 105810 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 218252 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 218261 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 214374 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 214374 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 216885 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 115365 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 115365 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 70925 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 70925 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 18571 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 18571 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 127239 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 127239 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 127239 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 218321 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 107018 7 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 107018 7 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 175412 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 175412 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 201372 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 201372 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 21954 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 21954 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 216178 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 215384 33 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 215384 33 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 44265 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 44265 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 44265 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 92294 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 92294 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 122787 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 122787 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 106232 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 106232 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 114482 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 114482 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 108210 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 108210 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 103821 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 103821 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 175255 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 175255 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 166218 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 166218 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 76186 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 76186 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 215481 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 112386 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 112386 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 112386 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 142781 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 142781 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 203543 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 203543 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 204173 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 204173 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 10882 33 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 10882 33 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 10882 33 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 10882 33 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 203724 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 203724 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 204408 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 204408 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 204562 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 204562 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 44265 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 44265 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 44265 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 44408 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 44408 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 148858 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 148858 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 18705 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 18705 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 18705 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 19050 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 19050 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 19050 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 44265 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 44265 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 44265 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 175249 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 175249 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 175249 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 96159 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 96159 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 219095 4 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 219095 4 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 23111 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 23111 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 115113 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 115113 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 11545 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 11545 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 76186 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 76186 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 214452 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 214452 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 213372 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 213372 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 121990 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 121990 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 126018 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 126018 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 70924 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 70924 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 92243 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 92243 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 119958 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 119958 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 215084 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 215084 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 11133 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 11133 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 162484 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 162484 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 175432 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 175432 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 32624 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 32624 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 218317 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 214520 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 214520 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 7663 4 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 7663 4 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 7663 4 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 7663 4 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 123408 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 123408 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 119861 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 119861 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 176260 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 176260 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 102532 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 102532 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 21144 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 21144 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 213458 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 213458 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 148871 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 148871 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 11515 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 11515 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 123659 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 123659 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 70793 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 70793 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 92287 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 92287 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 214174 35 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 214174 35 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 10590 28 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 10590 28 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 10590 28 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 22038 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 22038 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 171132 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 171132 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 214393 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 214393 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 119650 2 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 119650 2 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 21284 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 21284 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 32632 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 32632 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 214347 4 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 214347 4 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 76186 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 76186 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 76186 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 76186 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 116004 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 116004 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 203565 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 203565 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 171376 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 171376 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 204338 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 204338 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 151071 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 151071 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 18738 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 18738 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 18738 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 19056 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 19056 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 19056 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 19058 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 19058 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 19058 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 96161 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 96161 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 219081 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 70918 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 70918 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 70919 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 70919 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 122262 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 122262 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 217914 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 76186 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 76186 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 172939 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 172939 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 114181 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 114181 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 78876 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 78876 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 70917 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 70917 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 122260 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 122260 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 148870 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 148870 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 150081 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 150081 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 119618 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 119618 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 215360 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 175708 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 175708 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 79036 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 79036 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 142584 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 142584 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 151071 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 151071 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 119456 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 119456 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 217307 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 17033 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 17033 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 78223 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 78223 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 92272 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 92272 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 92217 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 92217 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 82720 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 82720 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 81270 2 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 81270 2 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 114219 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 114219 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 11125 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 11125 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 123840 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 123840 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 140321 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 140321 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 165093 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 165093 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 215385 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 215385 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 203754 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 203754 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 161725 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 161725 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 121552 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 121552 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 7713 37 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 7713 37 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 7713 37 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 7713 37 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 21326 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 21326 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 120150 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 120150 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 218322 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 19051 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 19051 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 19051 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 114489 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 114489 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 149994 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 149994 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 92242 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 92242 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 92285 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 92285 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 219092 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 11059 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 11059 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 216630 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 78497 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 78497 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 78695 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 78695 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 175601 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 175601 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 124411 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 124411 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 70705 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 70705 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 70911 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 70911 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 21139 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 21139 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 21139 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 209456 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 209456 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 119608 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 119608 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 76186 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 76186 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 215109 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 215109 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 120267 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 120267 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 148576 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 148576 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 119333 2 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 119333 2 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 119650 2 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 119650 2 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 149232 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 149232 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 102583 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 102583 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 121571 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 121571 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 78563 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 78563 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 146608 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 146608 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 34882 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 34882 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 120150 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 120150 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 108805 10 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 108805 10 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 121551 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 121551 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 107059 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 107059 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 215082 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 215082 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 120111 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 120111 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 79251 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 79251 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 219095 4 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 219095 4 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 115319 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 115319 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 203714 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 203714 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 204309 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 204309 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 204369 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 204369 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 205647 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 205647 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 115319 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 115319 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 214413 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 214413 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 79282 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 79282 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 101375 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 101375 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 108813 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 108813 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 108813 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 11144 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 11144 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 108813 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 108813 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 108813 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 19721 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 19721 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 105521 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 105521 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 148532 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 148532 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 92225 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 92225 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 18573 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 18573 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 18573 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 19033 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 19033 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 19033 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 19052 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 19052 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 19052 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 218008 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 218320 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 114059 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 114059 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 214054 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 214054 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 218312 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 20650 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 20650 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 150360 1 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 150360 1 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 108799 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 108799 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 120890 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 120890 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 117550 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 117550 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 11047 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 11047 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 121580 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 121580 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 148569 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 148569 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 70920 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 70920 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 108712 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 108712 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 120908 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 120908 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 165016 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 165016 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 108813 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 108813 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 108813 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 20774 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 20774 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 20774 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 22069 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 22069 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 218362 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 147517 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 147517 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 201456 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 201456 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 215363 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 215978 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 11391 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 11391 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 214049 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 214049 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 219477 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 80423 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 80423 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 108467 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 108467 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 122009 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 122009 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 11067 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 11067 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 123348 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 123348 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 70930 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 70930 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 219654 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 19244 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 19244 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 120116 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 120116 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 76185 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 76185 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 219072 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 218318 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 210264 36 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 210264 36 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 210039 27 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 210039 27 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 222732 0 None - 59 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 29561 41 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 29561 41 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 9128 67 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 9128 67 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 9128 67 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 9128 67 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 7603 0 None 3 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 6256771
860 7603 0 None 3 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 6256771
91898395 7603 0 None 3 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 6256771
3476 8182 9 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 8182 9 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 8182 9 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 8182 9 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 173690 75 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 173690 75 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 173690 75 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7609 50 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 7260 0 None 7943 2 Rat 10.5 pKi None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476993
3074331 7712 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 7712 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 9020 12 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 9020 12 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 9020 12 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 9799 14 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 9799 14 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 9799 14 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 9799 14 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 10887 39 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 10887 39 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 10887 39 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 8185 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 8185 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 8185 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 8185 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 8185 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 8917 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 8917 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 8917 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 10620 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 10620 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