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 18134 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 18134 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 18134 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 18134 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 49616 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 49616 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 49616 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 49616 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 5144 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 5144 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 165442 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 165442 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 188704 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 188704 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 188191 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 188191 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 188689 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 188689 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 49616 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 49616 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 188623 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 188623 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 822 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
864 822 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 822 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 822 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 822 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 188190 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 188190 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 188190 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 5144 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 5144 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 189139 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 189139 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 189051 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 189051 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 188727 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 188727 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 188727 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 188727 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 188727 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 188727 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 171562 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 171562 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 61924 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 61924 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 178719 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 178719 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 61856 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 61856 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 170853 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 170853 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 188689 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 188689 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 188875 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 188875 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 189055 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 189055 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 172471 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 172471 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 188637 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 188637 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 172689 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 172689 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 188751 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 188751 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 188751 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 188785 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 188785 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 188785 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 188785 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 188785 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 188785 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 188785 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 188785 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 171451 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 171451 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 188645 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 188645 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 188929 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 188929 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 189003 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 189003 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 172706 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 172706 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 172788 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 172788 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 212387 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 172014 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 172014 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 172318 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 172318 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 171748 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 171748 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 172689 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 172689 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 189051 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 189051 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 174372 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 174372 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 174592 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 174592 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 5144 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 5144 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 189631 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 189631 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 61856 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 61856 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 73648 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 73648 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 170089 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 170089 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 174936 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 174936 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 179458 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 179458 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 188869 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 188869 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 188704 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 188704 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 172172 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 172172 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 172918 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 172918 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 188762 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 188762 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 175268 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 175268 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 170938 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 170938 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 171582 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 171582 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 171202 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 171202 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 174864 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 174864 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 171845 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 171845 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 172003 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 172003 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 172050 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 172050 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 172653 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 172653 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 174068 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 174068 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 18134 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 18134 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 173134 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 173134 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 61923 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 61923 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 172656 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 172656 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 169870 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 169870 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 169865 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 169865 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 174017 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 174017 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 61914 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 61914 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 172507 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 172507 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 179373 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 179373 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 188620 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 188620 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 169870 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 169870 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 180812 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 180812 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 73648 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 73648 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 172833 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 172833 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 173286 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 173286 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 188727 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 188727 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 188727 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 170157 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 170157 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 173676 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 173676 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 173642 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 173642 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 73648 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 73648 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 169949 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 169949 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 175740 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 175740 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 173323 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 173323 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 173732 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 173732 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 174607 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 174607 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 175841 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 175841 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 174334 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 174334 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 172458 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 172458 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 73648 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 73648 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 188929 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 188929 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 170223 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 170223 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 175092 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 175092 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 176078 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 176078 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 876 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 876 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 876 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 876 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 189750 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 189750 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 61924 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 61924 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 61913 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 61913 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 171755 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 171755 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 173516 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 173516 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 173516 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 173516 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 173516 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 173516 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 61868 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 61868 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 188718 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 188718 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 18134 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 18134 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 190709 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 190709 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 190914 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 190914 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 173212 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 173212 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 182286 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 182286 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 190741 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 190741 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 179351 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 179351 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 182926 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 182926 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 172936 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 172936 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 190698 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 190698 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 190708 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 190708 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 212767 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 190636 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 190636 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 61864 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 61864 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 188785 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 188785 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 188785 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 188785 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 876 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 876 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 876 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 876 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 213145 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 876 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 876 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 876 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 876 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 174436 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 174436 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 173928 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 173928 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 61873 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 61873 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 876 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 876 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 876 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 876 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 179352 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 179352 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 61918 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 61918 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 189658 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 189658 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 189596 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 189596 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 171631 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 171631 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 174175 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 174175 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 175156 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 175156 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 73646 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 73646 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 876 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 876 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 876 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 876 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 109227 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 109227 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 73596 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 73596 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 172562 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 172562 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 140584 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 140584 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 18135 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 18135 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 73637 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 73637 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 61916 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 61916 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 181561 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 181561 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 18284 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 18284 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 61871 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 61871 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 209372 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 73645 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 73645 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 181539 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 181539 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 189781 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 189781 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 210704 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 61865 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 61865 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 73638 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 73638 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 174518 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 174518 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 174127 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 174127 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 181170 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 181170 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 73648 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 73648 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 209199 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 209199 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 73641 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 73641 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 61866 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 61866 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 1396 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 1396 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 1396 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 1396 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 61915 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 61915 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 212218 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 18134 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 18134 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 61861 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 61861 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 18137 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 18137 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 212293 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 209379 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 73648 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 73648 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 173119 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 173119 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 212293 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 182796 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 182796 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 73642 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 73642 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 876 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 876 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 876 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 876 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 188686 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 188686 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 61863 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 61863 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 61870 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 61870 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 61857 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 61857 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 73644 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 73644 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 39424 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 39424 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 107296 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 107296 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 179328 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 179328 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 73595 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 73595 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 61919 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 61919 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 876 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 876 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 876 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 876 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 61862 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 61862 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 73643 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 73643 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 18136 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 18136 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 181562 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 181562 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 876 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 876 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 876 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 876 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 181534 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 181534 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 18139 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 18139 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 73639 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 73639 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 73648 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 73648 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 181540 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 181540 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 61920 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 61920 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 73594 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 73594 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 18139 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 18139 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 182284 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 182284 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 210780 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 181784 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 181784 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 73636 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 73636 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 61921 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 61921 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 61869 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 61869 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 189810 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 189810 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 189718 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 189718 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 209814 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 172939 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 172939 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 61872 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 61872 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 18138 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 18138 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 18134 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 18134 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 18136 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 18136 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 181563 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 181563 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 73647 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 73647 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 73648 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 73648 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 181536 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 181536 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 61917 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 61917 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 182432 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 182432 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 189659 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 189659 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 171828 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 171828 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 181343 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 181343 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 73640 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 73640 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 61867 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 61867 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 181954 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 181954 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 89384 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 89384 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 182455 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 182455 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 182787 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 182787 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 61922 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 61922 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 5144 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 5144 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 18137 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 18137 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 170211 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 170211 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 182774 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 182774 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 207606 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 207606 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 124386 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 124386 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 67532 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 67532 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 124386 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 124386 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 99468 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 99468 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 124386 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 124386 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 124386 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 124386 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 113610 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 113610 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 127616 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 127616 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 67532 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 67532 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 67532 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 67532 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 67532 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 67532 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 127616 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 127616 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 127616 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 127616 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 124386 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 124386 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 212218 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 124386 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 124386 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 876 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 876 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 876 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 876 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 127616 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 127616 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 124386 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 124386 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 67532 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 67532 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 67532 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 67532 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 67532 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 67532 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 67532 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 67532 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 67532 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 67532 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 127616 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 127616 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 124386 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 124386 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 124386 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 124386 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 67532 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 67532 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 127616 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 127616 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 124386 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 124386 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 127616 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 127616 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 67532 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 67532 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 127616 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 127616 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 127616 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 127616 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 127616 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 127616 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 124386 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 124386 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 127616 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 127616 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 102061 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 102061 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 157875 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 157875 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 98707 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 98707 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 102330 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 102330 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 102083 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 102083 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 3297 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 3297 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 3297 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 3297 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 3297 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 2349 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 2349 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 2349 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 2349 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 1403 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 1403 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 1403 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 1403 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 1403 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 819 0 None -158 2 Rat 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
861 819 0 None -158 2 Rat 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
16168172 1771 0 None -158 2 Rat 6.1 pIC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
3559 1771 0 None -158 2 Rat 6.1 pIC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
444007 3043 0 None -794 2 Rat 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
870 3043 0 None -794 2 Rat 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
DB00183 3043 0 None -794 2 Rat 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
3960 2345 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 2345 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 2345 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 2345 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 2345 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 2345 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 876 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 876 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 876 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 876 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 1896 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 1896 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 1896 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 2122 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7654246
5311196 2122 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7654246
122077 2322 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 2322 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 2322 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 2322 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 207 34 None 4265 2 Rat 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1636779
858 207 34 None 4265 2 Rat 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1636779
CHEMBL323521 207 34 None 4265 2 Rat 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1636779
904 3026 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 3026 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 3026 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 3026 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
862 821 0 None -1 2 Mouse 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12370550
127948 3719 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 3719 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 1400 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 1400 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 1400 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 1400 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 822 50 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
864 822 50 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
9833444 822 50 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
CHEMBL1121 822 50 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
DB09142 822 50 None -2 6 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
2281 3175 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 3175 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 3175 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 3175 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 3175 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 3297 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 3297 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 3297 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 3297 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 3297 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 926 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
873 926 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 926 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 926 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 3023 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 3023 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 2239 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 2239 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 2239 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 2349 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 2349 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 2349 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 2349 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 2219 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 2219 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 2219 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 2219 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 3999 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 3999 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 3999 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 4110 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 4110 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 4110 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 4110 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 822 50 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
864 822 50 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
9833444 822 50 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
CHEMBL1121 822 50 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
DB09142 822 50 None -2 6 Rat 7.2 pIC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1975695
10348659 1804 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 1804 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 1804 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 3540 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 3540 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 2064 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 2064 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 2064 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 3667 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 3667 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 3667 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 3161 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 3161 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 3161 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 2322 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 2322 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 2322 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 2322 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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 Smiles

 DOI
45138674 16646 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 16646 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 78219 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 78219 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 33575 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 33575 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 10997 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 10997 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 78151 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 78151 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 2385 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 2385 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 2385 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 2385 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 2385 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 56312 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 56312 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 55116 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 55116 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 2759 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 2759 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 2759 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 2759 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 2759 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 116963 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 116963 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 205271 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 205271 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 205271 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 205271 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 205271 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 205271 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 205271 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 84541 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 84541 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 3330 96 None - 5 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 3330 96 None - 5 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 3330 96 None - 5 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 3330 96 None - 5 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 3330 96 None - 5 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 136968 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 136968 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 136968 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 10420 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 10420 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 788 39 None - 11 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 788 39 None - 11 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 788 39 None - 11 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 788 39 None - 11 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 788 39 None - 11 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 14493 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 14493 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 14493 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 14493 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 14493 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 14493 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 4401 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 4401 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 167518 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 167518 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 167518 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 4300 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 4300 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 4300 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 62485 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 62485 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 62485 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 3776 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 3776 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 3776 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 3776 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 3776 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 3287 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 3287 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 3287 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 3287 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 3287 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 3287 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 84686 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 84686 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 78140 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 14424 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 14424 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 27987 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 27987 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 196535 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 196535 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 3125 71 None - 30 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 3125 71 None - 30 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 3125 71 None - 30 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 3125 71 None - 30 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 3125 71 None - 30 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 31221 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 31221 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 194726 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 194726 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 115564 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 115564 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 195485 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 195485 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 822 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
864 822 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 822 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 822 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 822 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 168035 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 168035 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 211217 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 188689 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 188689 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 189051 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 189051 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 172689 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 172689 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 188751 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 188751 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 188751 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 189055 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 189055 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 61856 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 61856 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 188929 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 188929 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 188727 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 188727 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 188727 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 173323 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 173323 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 188191 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 188191 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 175841 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 175841 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 165442 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 165442 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 212862 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 207 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
858 207 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 207 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 173286 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 173286 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 178719 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 178719 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 169870 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 169870 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 188704 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 188704 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 188727 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 188727 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 188727 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 172833 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 172833 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 169865 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 169865 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 172507 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 172507 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 172788 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 172788 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 189139 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 189139 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 169949 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 169949 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 175740 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 175740 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 174864 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 174864 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 207606 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 207606 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 173676 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 173676 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 175092 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 175092 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 207606 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 207606 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 207606 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 207606 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 207606 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 207606 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 207606 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 207606 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 207606 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 207606 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 207606 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 207606 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 207606 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 207606 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 207606 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 207606 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 188190 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 188190 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 188190 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 188623 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 188623 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 188869 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 188869 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 207606 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 207606 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 172172 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 172172 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 174372 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 174372 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 172050 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 172050 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 124386 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 124386 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 115456 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 115456 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 188875 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 188875 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 174334 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 174334 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 210778 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 207606 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 207606 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 822 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
864 822 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 822 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 822 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 822 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 207606 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 207606 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 822 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
864 822 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 822 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 822 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 822 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 207606 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 207606 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 171755 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 171755 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 170157 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 170157 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 188637 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 188637 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 822 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
864 822 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 822 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 822 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 822 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 170223 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 170223 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 161567 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 161567 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 171451 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 171451 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 180812 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 180812 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 188785 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 188785 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 188785 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 188785 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 188785 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 188785 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 188785 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 188785 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 172471 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 172471 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 172918 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 172918 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 189003 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 189003 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 174068 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 174068 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 61868 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 61868 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 173134 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 173134 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 213079 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 194816 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 194816 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 189631 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 189631 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 172653 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 172653 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 61924 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 61924 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 179458 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 179458 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 188620 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 188620 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 188762 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 188762 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 170089 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 170089 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 170853 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 170853 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 167846 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 167846 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 172706 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 172706 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 61914 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 61914 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 78513 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 78513 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 176078 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 176078 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 174936 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 174936 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 822 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
864 822 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 822 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 822 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 822 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 67684 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 67684 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 172318 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 172318 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 172014 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 172014 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 67751 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 67751 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 188645 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 188645 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 58868 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 58868 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 182286 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 182286 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 172656 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 172656 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 173516 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 173516 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 173516 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 173516 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 173516 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 173516 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 159361 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 159361 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 67399 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 67399 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 188718 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 188718 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 174592 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 174592 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 207606 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 207606 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 822 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
864 822 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 822 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 822 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 822 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 97288 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 97288 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 97288 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 97288 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 171562 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 171562 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 170938 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 170938 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 171582 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 171582 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 179352 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 179352 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 2322 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 2322 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 2322 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 2322 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 189750 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 189750 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 127616 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 127616 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 127616 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 127616 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 213797 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 78431 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 78431 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 209787 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 179373 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 179373 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 210734 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 67754 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 67754 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 172003 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 172003 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 107258 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 107258 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 3161 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 3161 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 3161 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 207606 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 207606 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 207606 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 207606 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 207606 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 207606 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 172458 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 172458 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 204691 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 204691 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 204691 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 204691 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 107259 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 107259 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 107259 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 107259 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 1400 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 1400 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 1400 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 1400 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 204235 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 204235 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 204629 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 204629 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 171748 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 171748 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 208586 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 822 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
864 822 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 822 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 822 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 822 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 1400 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 1400 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 1400 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 1400 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 67746 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 67746 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 67749 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 67749 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 73648 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 73648 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 204484 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 204484 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 189080 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 189080 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 2064 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 2064 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 2064 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 212316 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 212316 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 171202 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 171202 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 79545 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 79545 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 96657 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 96657 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 96657 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 96657 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 204398 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 204398 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 822 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
864 822 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 822 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 822 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 822 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 15173 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 15173 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 204398 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 204398 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 179351 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 179351 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 108513 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 108513 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 175268 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 175268 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 209319 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 209319 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 822 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
864 822 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 822 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 822 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 822 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 108589 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 108589 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 107343 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 107343 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 108065 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 108065 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 108704 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 108704 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 67532 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 67532 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 32916 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 32916 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 32916 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 32916 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 171845 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 171845 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 822 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
864 822 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 822 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 822 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 822 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 204664 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 204664 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 102264 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 102264 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 77822 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 77822 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 166634 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 166634 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 78515 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 78515 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 174607 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 174607 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 182926 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 182926 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 107205 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 107205 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 115453 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 115453 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 102264 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 102264 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 212873 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 61913 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 61913 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 204139 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 204139 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 204246 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 204246 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 204634 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 204634 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 108455 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 108455 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 204246 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 204246 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 204246 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 204246 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 204634 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 204634 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 73648 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 73648 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 103107 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 103107 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 208587 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 9805 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 9805 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 9805 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 9805 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 166245 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 166245 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 9805 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 9805 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 9805 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 9805 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 208490 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 107187 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 107187 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 26232 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 26232 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 4913 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 4913 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 926 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
873 926 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 926 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 926 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 26232 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 26232 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 26232 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 26232 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 111437 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 111437 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 179328 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 179328 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 181539 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 181539 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 189659 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 189659 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 189810 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 189810 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 876 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 876 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 876 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 876 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 121693 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 121693 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 73648 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 73648 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 208584 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 116082 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 116082 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 104871 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 104871 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 108291 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 108291 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 5144 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 5144 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 104871 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 104871 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 206542 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 206542 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 10769 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 10769 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 67739 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 67739 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 206542 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 206542 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 103209 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 103209 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 169292 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 169292 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 106600 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 106600 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 119535 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 119535 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 102083 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 102083 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 102330 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 102330 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 162338 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 162338 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 169292 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 169292 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 109723 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 109723 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 78593 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 78593 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 120335 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 120335 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 199061 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 199061 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 164926 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 164926 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 209248 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 876 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 876 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 876 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 876 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 73648 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 73648 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 73648 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 73648 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 49616 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 49616 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 164926 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 164926 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 204642 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 204642 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 121134 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 121134 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 119601 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 119601 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 118975 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 118975 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 170618 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 170618 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 120468 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 120468 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 212266 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 67710 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 67710 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 67719 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 67719 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 31788 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 31788 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 119187 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 119187 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 120624 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 120624 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 120625 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 120625 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 16821 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 16821 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 204519 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 204519 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 59540 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 59540 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 103031 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 103031 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 163469 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 163469 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 204519 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 204519 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 67708 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 67708 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 67713 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 67713 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 167308 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 167308 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 32329 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 32329 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 116629 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 116629 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 59540 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 59540 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 84384 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 84384 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 84384 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 130695 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 130695 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 117054 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 117054 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 198050 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 198050 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 161310 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 161310 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 137508 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 137508 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 156882 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 156882 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 211391 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 26029 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 26029 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 73648 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 73648 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 119688 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 119688 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 926 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
873 926 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 926 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 926 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 209169 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 119549 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 119549 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 18134 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 18134 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 116776 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 116776 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 78484 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 78484 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 198600 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 198600 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 100174 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 100174 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 207532 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 207532 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 69409 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 69409 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 167893 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 167893 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 85993 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 85993 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 107601 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 107601 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 22146 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 22146 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 120801 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 120801 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 33538 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 33538 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 102345 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 102345 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 204608 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 204608 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 102977 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 102977 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 102923 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 102923 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 103072 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 103072 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 209394 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 67739 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 67739 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 169479 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 169479 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 167474 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 167474 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 213199 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 110339 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 110339 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 27731 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 27731 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 49616 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 49616 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 100346 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 100346 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 156423 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 156423 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 102345 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 102345 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 156423 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 156423 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 204608 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 204608 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 26199 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 26199 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 120755 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 120755 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 156423 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 156423 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 106799 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 106799 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 163244 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 163244 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 120279 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 120279 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 100857 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 100857 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 59091 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 59091 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 103072 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 103072 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 204122 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 204122 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 67688 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 67688 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 67737 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 67737 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 118465 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 118465 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 10033 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 10033 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 165083 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 165083 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 115506 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 115506 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 106803 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 106803 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 108913 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 108913 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 59091 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 59091 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 119976 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 119976 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 9530 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 9530 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 164491 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 164491 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 208457 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 77827 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 77827 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 67711 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 67711 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 198011 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 198011 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 121680 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 121680 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 121680 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 121680 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 10148 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 10148 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 117015 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 117015 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 207395 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 207395 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 207395 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 207395 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 111474 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 111474 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 89201 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 89201 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 89201 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 198198 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 198198 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 206636 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 206636 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 89201 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 89201 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 89201 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 110657 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 110657 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 10092 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 10092 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 166911 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 166911 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 166911 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 179143 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 179143 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 117083 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 117083 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 99854 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 99854 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 183909 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 183909 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 33203 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 33203 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 120337 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 120337 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 49664 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 49664 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 118563 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 118563 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 100461 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 100461 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 45339 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 45339 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 162067 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 162067 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 9899 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 9899 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 140746 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 140746 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 9899 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 9899 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 78432 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 78432 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 120598 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 120598 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 120598 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 168035 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 168035 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 876 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 876 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 876 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 876 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 194676 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 194676 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 140840 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 140840 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 204517 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 204517 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 110452 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 110452 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 77236 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 77236 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 48010 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 48010 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 28409 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 28409 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 116248 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 116248 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 106821 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 106821 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 106827 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 106827 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 103184 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 103184 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 113499 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 113499 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 204517 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 204517 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 167786 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 167786 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 119041 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 119041 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 207508 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 207508 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 46043 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 46043 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 197878 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 197878 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 59472 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 59472 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 119601 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 119601 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 119041 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 119041 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 161724 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 161724 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 207508 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 207508 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 211604 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 85997 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 85997 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 211129 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 67075 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 67075 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 67741 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 67741 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 99339 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 99339 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 207213 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 207213 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 125057 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 125057 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 25494 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 25494 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 99071 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 99071 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 78528 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 78528 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 119430 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 119430 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 207568 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 207568 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 168666 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 168666 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 39424 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 39424 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 208581 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 97030 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 97030 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 16673 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 16673 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 98868 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 98868 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 170617 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 170617 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 77289 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 77289 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 198342 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 198342 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 18134 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 18134 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 49616 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 49616 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 107122 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 107122 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 11730 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 11730 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 11730 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 85049 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 85049 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 110503 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 110503 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 61916 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 61916 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 110372 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 110372 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 188424 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 188424 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 106824 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 106824 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 206545 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 206545 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 206545 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 206545 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 111598 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 111598 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 115451 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 115451 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 59235 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 59235 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 96636 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 96636 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 208244 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 208244 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 100552 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 100552 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 25137 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 25137 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 188686 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 188686 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 106810 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 106810 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 198704 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 198704 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 201919 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 201919 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 9532 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 9532 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 16826 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 16826 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 118063 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 118063 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 109359 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 109359 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 106137 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 106137 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 206088 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 206088 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 204501 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 204501 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 157331 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 157331 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 157331 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 26064 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 26064 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 29100 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 29100 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 116611 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 116611 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 99892 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 99963 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 99963 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 4700 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 4700 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 5055 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 5055 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 5070 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 5070 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 109255 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 109255 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 163487 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 163487 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 42426 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 42426 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 165636 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 165636 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 16354 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 16354 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 204549 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 204549 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 30724 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 30724 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 196696 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 196696 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 18134 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 18134 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 83224 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 83224 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 168001 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 168001 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 168001 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 168001 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 198112 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 198112 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 100211 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 100211 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 49616 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 49616 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 67178 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 67178 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 168289 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 168289 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 118059 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 118059 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 99577 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 99577 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 99577 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 99577 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 49454 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 49454 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 112754 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 112754 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 119359 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 119359 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 163423 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 163423 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 59053 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 59053 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 99879 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 99879 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 211739 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 211138 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 99879 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 99879 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 26934 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 26934 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 182432 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 182432 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 100711 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 100711 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 100784 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 100784 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 213660 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 5144 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 5144 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 111505 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 111505 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 73648 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 73648 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 119218 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 119218 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 207666 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 207666 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 161296 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 161296 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 161296 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 161296 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 120763 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 120763 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 209193 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 119791 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 119791 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 181534 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 181534 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 106802 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 106802 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 106822 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 106822 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 167986 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 167986 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 59217 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 59217 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 121215 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 121215 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 102109 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 102109 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 120317 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 120317 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 33056 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 33056 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 25890 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 25890 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 28698 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 28698 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 99468 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 99468 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 109767 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 109767 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 163323 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 163323 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 16531 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 16531 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 101909 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 101909 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 118749 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 118749 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 100138 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 100138 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 102109 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 102109 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 29178 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 29178 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 89201 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 89201 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 89201 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 119961 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 119961 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 16582 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 16582 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 113091 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 113091 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 26359 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 26359 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 119525 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 119525 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 4115 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 4115 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 4115 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 4115 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 4115 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 4115 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 165245 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 165245 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 109464 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 109464 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 168666 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 168666 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 57522 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 57522 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 18650 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 18650 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 178831 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 178831 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 106614 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 106614 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 18138 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 18138 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 67744 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 67744 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 204641 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 204641 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 78595 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 78595 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 201249 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 201249 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 204641 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 204641 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 876 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 876 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 876 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 876 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 127616 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 127616 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 79658 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 79658 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 56517 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 56517 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 89384 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 89384 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 69408 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 69408 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 121001 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 121001 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 210277 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 204404 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 204404 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 98836 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 98836 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 208197 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 208197 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 208229 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 208229 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 204150 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 204150 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 13003 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 13003 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 13003 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 105946 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 105946 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 204144 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 204144 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 10020 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 10020 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 110522 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 110522 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 4988 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 4988 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 78451 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 78451 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 29087 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 29087 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 212631 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 210180 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 165448 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 165448 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 99388 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 99388 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 30261 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 30261 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 197877 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 197877 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 5144 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 5144 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 103106 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 103106 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 103106 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 103106 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 22654 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 22654 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 205957 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 205957 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 15259 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 15259 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 30156 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 30156 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 78361 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 78361 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 5144 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 5144 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 121963 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 121963 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 107296 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 107296 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 107296 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 107296 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 207274 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 207274 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 163332 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 163332 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 78901 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 78901 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 4656 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 4656 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 116744 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 116744 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 29108 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 29108 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 112852 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 112852 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 207395 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 207395 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 103800 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 103800 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 112347 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 112347 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 38224 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 38224 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 198410 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 198410 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 119167 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 119167 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 106592 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 106592 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 106603 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 106603 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 215927 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 147586 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 147586 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 215927 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 215927 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 59524 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 59524 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 98707 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 98707 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 209489 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 181562 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 181562 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 106797 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 106797 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 173928 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 173928 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 208809 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 876 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 876 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 876 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 876 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 61915 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 61915 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 111515 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 111515 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 106601 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 106601 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 110044 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 110044 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 189033 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 189033 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 119176 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 119176 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 78817 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 78817 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 182774 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 182774 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 106805 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 106805 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 120634 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 120634 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 67683 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 67683 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 103800 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 103800 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 58264 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 58264 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 182860 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 182860 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 2240 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 2240 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 2240 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 17948 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 17948 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 44561 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 44561 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 67722 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 67722 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 49887 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 49887 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 2240 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 2240 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 2240 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 2240 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 2240 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 2240 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 78766 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 78766 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 97003 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 97003 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 99989 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 99989 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 97003 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 97003 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 61867 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 61867 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 58873 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 58873 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 87492 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 87492 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 74495 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 74495 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 61861 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 61861 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 110540 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 110540 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 78592 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 78592 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 28605 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 28605 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 78482 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 78482 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 876 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 876 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 876 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 876 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 173119 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 173119 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 99850 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 99850 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 30776 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 30776 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 17738 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 17738 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 96504 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 96504 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 5144 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 5144 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 78815 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 78815 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 73638 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 73638 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 73648 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 73648 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 178905 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 178905 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 67753 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 67753 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 204529 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 204529 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 120090 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 120090 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 100375 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 100375 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 18136 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 18136 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 109207 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 109207 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 101753 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 101753 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 181954 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 181954 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 120626 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 120626 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 111648 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 111648 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 111530 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 111530 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 61869 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 61869 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 106602 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 106602 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 211131 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 85398 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 85398 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 2345 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 2345 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 2345 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 119809 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 119809 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 77249 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 77249 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 119566 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 119566 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 28644 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 28644 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 58509 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 58509 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 78627 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 78627 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 206362 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 206362 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 67753 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 67753 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 204529 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 204529 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 112848 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 112848 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 5110 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 5110 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 204637 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 204637 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 67717 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 67717 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 12190 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 12190 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 12190 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 16923 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 16923 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 168641 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 168641 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 97367 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 97367 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 61871 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 61871 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 22789 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 22789 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 12077 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 12077 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 12077 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 100552 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 100552 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 104380 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 104380 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 197980 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 197980 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 199065 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 199065 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 199065 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 199065 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 79715 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 79715 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 99866 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 99866 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 204157 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 204157 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 109649 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 109649 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 2345 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 2345 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 2345 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 120598 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 120598 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 120598 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 33023 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 33023 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 99097 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 99097 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 10270 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 10270 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 100552 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 100552 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 9565 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 9565 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 118991 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 118991 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 25772 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 25772 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 106796 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 106796 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 211179 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 215856 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 12898 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 12898 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 12898 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 215856 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 215856 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 215856 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 104380 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 104380 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 215856 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 199065 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 199065 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 215856 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 4464 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 4464 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 4559 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 4559 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 215856 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 85996 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 85996 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 23151 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 23151 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 76552 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 76552 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 100478 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 100478 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 46294 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 46294 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 10114 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 10114 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 197844 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 197844 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 85989 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 85989 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 12852 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 12852 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 12852 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 107356 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 107356 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 33026 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 33026 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 107356 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 107356 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 33026 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 33026 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 198362 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 198362 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 49616 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 49616 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 17131 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 17131 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 120378 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 120378 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 139263 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 139263 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 25991 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 25991 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 106609 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 106609 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 9532 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 9532 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 100301 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 100301 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 106609 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 106609 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 61917 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 61917 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 67747 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 67747 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 77828 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 77828 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 108732 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 108732 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 9532 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 9532 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 100990 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 100990 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 67747 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 67747 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 171631 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 171631 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 18135 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 18135 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 119912 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 119912 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 102895 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 102895 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 165248 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 165248 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 102666 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 102666 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 208585 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 211217 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 200703 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 200703 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 209319 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 209319 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 120752 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 120752 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 10015 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 10015 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 25676 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 25676 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 189596 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 189596 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 96925 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 96925 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 99177 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 99177 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 107786 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 107786 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 204103 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 204103 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 207 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
858 207 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 207 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 163854 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 163854 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 51620 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 51620 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 136945 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 136945 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 83234 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 83234 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 102234 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 102234 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 168548 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 168548 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 78829 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 78829 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 212265 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 2349 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 2349 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 2349 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 2349 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 121077 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 121077 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 74495 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 74495 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 87492 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 87492 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 74495 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 74495 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 74495 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 74495 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 74495 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 74495 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 99871 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 99871 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 99871 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 207842 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 207842 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 200690 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 200690 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 119335 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 119335 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 103140 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 103140 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 47560 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 47560 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 204581 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 204581 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 18137 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 18137 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 61923 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 61923 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 163861 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 163861 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 207395 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 207395 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 103000 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 103000 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 86118 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 86118 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 103000 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 103000 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 127616 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 127616 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 113106 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 113106 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 161329 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 161329 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 112330 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 112330 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 173642 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 173642 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 155142 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 155142 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 155142 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 155142 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 208472 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 189718 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 189718 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 210560 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 61864 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 61864 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 61865 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 61865 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 67751 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 67751 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 182787 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 182787 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 77826 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 77826 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 209192 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 174017 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 174017 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 141828 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 141828 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 163573 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 163573 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 3026 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 3026 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 3026 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 3026 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 3026 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 3026 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 3026 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 3026 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 112599 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 112599 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 3026 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 3026 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 3026 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 3026 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 124386 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 124386 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 115454 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 115454 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 67751 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 67751 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 77825 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 77825 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 77826 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 77826 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 78434 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 78434 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 202815 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 202815 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 59050 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 59050 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 100267 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 100267 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 140752 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 140752 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 102895 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 102895 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 165248 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 165248 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 120598 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 120598 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 120598 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 73648 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 73648 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 204632 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 204632 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 156518 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 156518 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 51620 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 51620 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 101721 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 101721 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 140781 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 140781 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 103140 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 103140 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 58271 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 58271 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 78597 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 78597 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 51280 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 51280 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 27165 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 27165 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 116780 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 116780 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 172562 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 172562 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 108886 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 108886 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 117222 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 117222 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 140802 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 140802 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 99830 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 99830 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 108773 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 108773 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 59183 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 59183 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 204581 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 204581 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 27656 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 27656 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 18284 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 18284 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 2403 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 2403 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 2403 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 2403 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 2403 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 2403 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 198601 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 198601 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 9834 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 9834 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 179059 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 179059 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 164514 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 164514 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 105353 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 105353 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 211127 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 18139 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 18139 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 204632 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 204632 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 9631 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 9631 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 161687 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 161687 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 77250 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 77250 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 78814 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 78814 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 161715 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 161715 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 114462 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 114462 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 77251 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 77251 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 27999 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 27999 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 59157 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 59157 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 209941 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 25622 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 25622 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 26348 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 26348 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 116664 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 116664 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 107302 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 107302 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 210885 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 104161 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 104161 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 175156 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 175156 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 96489 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 96489 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 106612 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 106612 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 106612 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 106612 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 106612 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 106612 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 2345 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 2345 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 2345 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 204149 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 204149 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 181343 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 181343 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 106798 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 106798 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 141935 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 141935 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 164510 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 164510 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 876 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 876 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 876 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 876 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 113610 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 113610 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 124046 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 124046 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 10261 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 10261 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 10261 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 10261 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 1896 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 1896 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 1896 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 1896 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 1896 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 1896 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 199554 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 199554 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 211134 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 162981 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 162981 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 101944 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 101944 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 104161 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 104161 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 121507 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 121507 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 162981 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 162981 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 106813 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 106813 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 2345 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 2345 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 2345 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 32336 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 32336 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 59091 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 59091 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 4596 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 4596 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 5091 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 5091 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 101962 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 101962 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 172749 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 172749 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 32245 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 32245 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 115342 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 115342 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 116860 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 116860 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 30094 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 30094 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 206683 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 206683 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 116721 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 116721 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 168036 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 168036 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 106596 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 106596 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 208452 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 208452 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 208452 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 208176 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 208176 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 10123 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 10123 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 209785 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 876 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 876 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 876 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 876 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 211130 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 207395 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 207395 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 207395 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 207395 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 59195 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 59195 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 51620 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 51620 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 207395 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 207395 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 167986 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 167986 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 115507 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 115507 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 118449 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 118449 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 67716 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 67716 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 168308 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 168308 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 5144 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 5144 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 207334 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 207334 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 111586 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 111586 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 9799 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 9799 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 167852 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 167852 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 108827 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 108827 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 102119 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 102119 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 120377 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 120377 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 18137 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 18137 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 5144 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 5144 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 102119 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 102119 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 26125 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 26125 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 26141 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 26141 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 4618 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 4618 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 29313 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 29313 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 59212 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 59212 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 116538 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 116538 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 98564 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 98564 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 18140 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 18140 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 204579 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 204579 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 210183 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 73637 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 73637 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 61863 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 61863 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 16241 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 16241 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 3024 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 3024 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 3024 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 3024 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 3026 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 3026 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 3026 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 3026 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 3024 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 3024 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 3024 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 3024 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 3024 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 3024 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 3024 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 3024 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 3024 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 3024 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 3024 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 3024 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 72467 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 72467 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 100761 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 100761 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 109227 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 109227 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 120472 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 120472 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 67687 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 67687 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 119644 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 119644 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 106808 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 106808 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 108547 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 108547 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 119696 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 119696 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 140724 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 140724 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 140747 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 140747 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 78790 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 78790 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 111360 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 111360 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 59083 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 59083 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 67762 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 67762 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 107227 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 107227 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 108287 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 108287 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 4472 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 4472 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 189368 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 189368 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 168735 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 168735 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 121288 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 121288 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 99962 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 99962 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 119581 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 119581 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 208583 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 207473 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 207473 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 16407 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 16407 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 110871 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 110871 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 197936 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 197936 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 117050 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 117050 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 207103 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 207103 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 198383 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 198383 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 115408 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 115408 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 207377 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 207377 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 170211 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 170211 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 116532 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 116532 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 99962 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 99962 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 49616 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 49616 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 106614 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 106614 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 211223 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 119892 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 119892 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 120755 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 120755 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 211223 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 98086 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 98086 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 26186 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 26186 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 120755 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 120755 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 5144 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 5144 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 876 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 876 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 876 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 876 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 119949 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 119949 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 203887 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 203887 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 120122 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 120122 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 120236 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 120236 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 210181 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 162919 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 162919 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 100489 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 100489 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 45339 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 45339 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 207430 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 207430 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 168735 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 168735 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 210182 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 204668 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 204668 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 876 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 876 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 876 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 876 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 160774 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 160774 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 160966 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 160966 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 179143 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 179143 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 197395 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 197395 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 73648 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 73648 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 106599 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 106599 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 211731 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 204668 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 204668 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 207606 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 207606 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 118859 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 118859 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 100709 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 100709 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 211139 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 106556 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 106556 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 103697 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 103697 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 59522 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 59522 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 182320 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 182320 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 85995 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 85995 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 204715 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 204715 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 165083 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 165083 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 129112 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 129112 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 16628 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 16628 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 16844 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 16844 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 187826 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 187826 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 179113 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 179113 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 162016 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 162016 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 116713 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 116713 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 17279 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 17279 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 198304 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 198304 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 120501 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 120501 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 102703 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 102703 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 168115 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 168115 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 100639 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 100639 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 204753 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 204753 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 207395 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 207395 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 207395 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 207395 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 207395 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 207395 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 207395 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 207395 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 207395 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 207395 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 207395 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 207395 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 208850 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 140170 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 140170 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 77847 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 77847 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 31656 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 31656 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 100655 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 100655 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 117278 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 117278 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 187826 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 187826 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 18518 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 18518 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 120598 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 120598 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 120598 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 168735 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 168735 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 16834 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 16834 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 165233 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 165233 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 204753 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 204753 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 9457 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 9457 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 102668 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 102668 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 206872 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 206872 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 109087 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 109087 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 85762 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 85762 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 78517 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 78517 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 106806 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 106806 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 4680 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 4680 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 30788 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 30788 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 118796 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 118796 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 29051 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 29051 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 61858 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 61858 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 44090 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 44090 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 198427 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 198427 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 142836 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 142836 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 206589 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 206589 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 204126 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 204126 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 204126 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 204126 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 204213 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 204213 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 167868 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 167868 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 208805 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 77252 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 77252 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 116345 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 116345 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 168330 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 168330 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 204126 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 204126 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 172936 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 172936 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 181536 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 181536 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 101026 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 101026 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 204721 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 204721 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 67750 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 67750 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 106597 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 106597 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 61517 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 61517 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 208805 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 59455 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 59455 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 208805 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 208805 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 211216 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 211229 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 211229 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 211216 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 211229 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 120838 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 120838 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 211229 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 124386 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 124386 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 211216 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 161742 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 161742 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 79714 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 79714 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 211203 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 120598 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 120598 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 120598 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 78435 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 78435 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 120460 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 120460 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 3024 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 3024 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 3024 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 3024 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 16852 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 16852 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 59056 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 59056 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 209191 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 182284 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 182284 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 102437 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 102437 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 106815 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 106815 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 16786 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 16786 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 59073 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 59073 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 189726 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 189726 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 140821 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 140821 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 106176 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 106176 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 204218 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 204218 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 204132 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 204132 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 58913 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 58913 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 59037 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 59037 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 59230 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 59230 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 83467 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 83467 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 120399 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 120399 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 28661 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 28661 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 103980 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 103980 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 106157 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 106157 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 213922 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 67712 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 67712 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 67724 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 67724 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 67728 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 67728 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 51280 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 51280 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 9887 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 9887 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 207240 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 207240 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 198197 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 198197 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 204218 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 204218 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 49616 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 49616 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 119155 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 119155 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 120725 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 120725 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 206739 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 206739 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 206739 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 206739 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 28630 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 28630 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 106445 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 106445 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 119976 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 119976 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 157875 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 157875 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 208582 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 876 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 876 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 876 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 876 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 101587 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 101587 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 110682 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 110682 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 25623 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 25623 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 25976 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 25976 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 27994 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 27994 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 106792 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 106792 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 168233 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 168233 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 156562 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 156562 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 103207 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 103207 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 78504 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 78504 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 76552 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 76552 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 168306 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 168306 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 96689 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 96689 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 28417 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 28417 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 115998 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 115998 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 58132 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 58132 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 168095 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 96689 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 96689 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 69410 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 69410 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 198347 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 198347 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 18562 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 18562 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 12276 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 12276 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 12276 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 212361 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 197876 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 197876 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 178904 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 178904 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 209182 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 49616 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 49616 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 97379 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 97379 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 212635 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 164752 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 164752 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 69406 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 69406 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 17946 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 17946 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 210179 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 204651 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 204651 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 100498 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 100498 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 100498 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 78841 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 78841 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 157976 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 157976 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 9530 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 9530 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 114541 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 114541 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 9530 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 9530 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 4425 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 4425 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 59114 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 59114 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 119949 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 119949 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 31193 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 31193 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 98561 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 98561 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 140170 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 140170 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 16767 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 16767 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 61860 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 61860 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 106812 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 106812 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 163180 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 163180 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 49616 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 49616 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 67689 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 67689 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 96441 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 96441 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 103844 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 103844 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 59094 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 59094 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 74078 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 74078 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 5144 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 5144 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 17775 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 17775 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 31868 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 31868 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 59357 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 59357 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 168201 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 168201 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 168050 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 168050 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 198104 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 198104 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 101890 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 101890 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 106615 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 106615 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 106615 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 106615 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 115059 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 115059 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 115220 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 115220 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 78839 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 78839 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 73643 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 73643 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 204495 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 204495 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 67375 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 67375 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 27614 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 27614 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 98967 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 98967 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 67690 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 67690 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 168050 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 168050 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 204176 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 204176 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 99499 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 99499 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 165193 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 165193 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 167974 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 167974 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 1582 14 None - 28 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 1582 14 None - 28 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 1582 14 None - 28 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 1582 14 None - 28 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 1582 14 None - 28 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 98899 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 98899 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 207456 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 207456 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 29226 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 29226 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 120489 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 120489 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 207083 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 207083 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 73648 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 73648 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 61859 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 61859 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 61862 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 61862 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 61872 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 61872 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 98354 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 98354 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 189658 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 189658 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 165566 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 165566 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 107353 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 107353 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 178446 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 178446 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 110617 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 110617 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 9548 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 9548 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 98745 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 98745 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 98745 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 98745 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 120350 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 120350 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 168329 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 168329 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 107131 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 107131 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 205845 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 205845 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 161726 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 161726 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 161785 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 161785 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 197875 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 197875 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 198079 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 198079 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 13985 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 13985 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 13985 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 206743 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 206743 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 73646 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 73646 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 5144 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 5144 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 96487 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 96487 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 174175 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 174175 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 159760 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 159760 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 73595 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 73595 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 168146 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 168146 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 140797 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 140797 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 168632 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 168632 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 213665 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 140723 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 140723 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 103687 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 103687 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 103028 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 103028 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 116644 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 116644 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 67764 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 67764 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 101059 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 101059 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 116820 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 116820 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 209399 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 100849 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 100849 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 22876 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 22876 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 876 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 876 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 876 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 876 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 141408 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 141408 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 198351 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 198351 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 141408 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 141408 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 110550 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 110550 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 115455 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 115455 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 141408 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 141408 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 49390 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 49390 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 73636 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 73636 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 202791 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 202791 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 100498 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 100498 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 100498 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 198273 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 198273 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 120246 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 120246 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 106804 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 106804 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 73644 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 73644 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 100054 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 100054 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 107130 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 107130 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 100498 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 100498 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 100498 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 77248 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 77248 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 99126 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 99126 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 202791 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 202791 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 117036 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 117036 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 5051 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 5051 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 78514 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 78514 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 100079 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 100079 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 119331 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 119331 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 78485 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 78485 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 58615 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 58615 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 57558 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 57558 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 78596 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 78596 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 5111 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 5111 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 100703 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 100703 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 106825 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 106825 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 169718 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 169718 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 5144 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 5144 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 109784 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 109784 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 209786 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 25007 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 25007 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 106807 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 106807 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 100033 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 100033 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 203260 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 203260 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 189726 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 189726 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 168616 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 168616 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 163268 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 163268 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 174769 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 174769 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 114636 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 114636 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 109676 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 109676 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 59007 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 59007 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 97339 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 97339 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 18110 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 18110 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 168234 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 168234 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 73641 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 73641 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 173732 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 173732 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 208805 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 67516 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 67516 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 79543 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 79543 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 101628 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 101628 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 24658 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 24658 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 112401 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 112401 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 78844 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 78844 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 876 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 876 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 876 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 876 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 106594 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 106594 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 50790 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 50790 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 98799 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 98799 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 102996 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 102996 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 204681 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 204681 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 98593 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 98593 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 61922 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 61922 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 169050 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 169050 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 102996 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 102996 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 204681 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 204681 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 169050 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 169050 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 98593 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 98593 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 98593 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 98593 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 204126 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 204126 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 211217 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 168237 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 168237 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 120509 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 120509 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 106809 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 106809 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 59434 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 59434 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 5144 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 5144 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 204759 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 204759 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 174127 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 174127 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 114828 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 114828 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 118089 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 118089 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 2239 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 2239 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 2239 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 10005 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 10005 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 116755 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 116755 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 106795 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 106795 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 119670 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 119670 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 208835 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 138365 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 138365 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 140788 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 140788 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 32719 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 32719 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 24968 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 24968 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 208835 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 204414 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 204414 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 138365 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 138365 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 100896 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 100896 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 165511 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 165511 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 205335 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 205335 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 78486 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 78486 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 164882 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 164882 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 155705 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 155705 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 57752 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 57752 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 106627 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 106627 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 204759 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 204759 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 211205 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 182796 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 182796 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 876 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 876 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 876 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 876 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 109215 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 109215 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 26953 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 26953 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 78811 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 78811 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 106794 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 106794 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 119485 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 119485 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 118889 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 118889 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 99632 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 99632 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 117306 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 117306 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 69412 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 69412 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 120363 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 120363 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 78599 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 78599 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 105654 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 105654 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 104577 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 104577 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 876 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 876 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 876 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 876 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 73648 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 73648 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 171828 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 171828 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 104577 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 104577 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 207420 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 207420 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 4621 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 4621 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 101953 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 101953 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 207284 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 207284 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 9899 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 9899 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 10060 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 10060 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 109041 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 109041 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 99743 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 99743 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 20776 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 20776 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 208605 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 4671 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 4671 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 67745 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 67745 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 181561 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 181561 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 181563 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 181563 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 208837 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 110315 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 110315 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 27951 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 27951 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 98777 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 98777 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 926 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
873 926 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 926 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 926 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 73960 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 73960 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 926 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
873 926 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 926 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 926 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 85988 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 85988 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 926 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
873 926 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 926 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 926 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 96689 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 96689 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 926 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
873 926 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 926 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 926 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 119505 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 119505 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 31674 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 31674 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 926 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
873 926 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 926 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 926 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 76552 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 76552 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 87676 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 87676 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 168527 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 168527 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 78812 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 78812 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 106186 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 106186 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 106186 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 106186 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 78433 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 78433 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 73640 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 73640 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 121126 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 121126 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 111001 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 111001 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 116727 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 116727 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 121002 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 121002 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 168164 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 168164 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 99321 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 178975 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 178975 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 98380 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 98380 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 116705 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 116705 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 34670 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 34670 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 200049 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 200049 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 116868 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 116868 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 32704 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 32704 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 140761 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 140761 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 96689 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 96689 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 107805 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 107805 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 67755 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 67755 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 119302 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 119302 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 207251 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 207251 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 208847 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 106608 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 106608 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 178831 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 178831 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 10000 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 10000 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 116609 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 116609 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 5144 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 5144 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 171713 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 171713 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 121841 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 121841 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 48324 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 48324 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 116731 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 116731 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 178906 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 178906 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 16801 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 16801 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 46545 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 46545 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 3818 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 3818 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 3818 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 17973 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 17973 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 51471 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 51471 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 168614 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 168614 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 140925 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 140925 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 165022 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 165022 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 109783 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 109783 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 102956 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 102956 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 207199 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 207199 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 204717 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 204717 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 9613 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 9613 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 18139 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 18139 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 106991 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 106991 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 43538 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 43538 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 205807 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 205807 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 102956 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 102956 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 119566 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 119566 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 106991 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 106991 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 204717 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 204717 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 31934 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 31934 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 25411 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 25411 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 99853 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 99853 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 55600 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 55600 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 55600 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 77849 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 77849 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 167141 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 167141 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 116842 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 116842 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 59043 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 59043 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 31477 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 31477 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 13964 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 13964 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 13964 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 77825 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 77825 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 106811 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 106811 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 73594 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 73594 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 18136 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 18136 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 100960 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 100960 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 135355 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 135355 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 27961 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 27961 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 98170 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 98170 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 207056 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 207056 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 55600 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 55600 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 55600 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 97304 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 97304 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 103168 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 103168 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 103168 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 103168 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 203067 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 203067 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 9548 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 9548 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 9548 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 9548 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 101715 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 101715 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 67532 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 67532 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 208362 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 208362 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 120148 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 120148 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 211215 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 213806 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 181540 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 181540 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 106616 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 106616 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 106616 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 107406 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 107406 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 211218 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 2345 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 2345 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 2345 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 117841 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 117841 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 6206 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 6206 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 207568 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 207568 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 114546 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 114546 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 207568 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 207568 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 100708 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 100708 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 109227 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 109227 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 109227 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 109227 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 109227 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 109227 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 5144 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 5144 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 78590 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 78590 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 204509 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 204509 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 21617 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 21617 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 163413 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 163413 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 109719 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 109719 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 115414 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 115414 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 212680 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 12864 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 12864 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 12864 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 100407 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 100407 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 210871 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 13650 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 13650 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 13650 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 67727 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 67727 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 204509 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 204509 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 4110 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 4110 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 4110 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 4110 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 49616 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 49616 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 211132 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 161724 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 161724 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 49616 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 49616 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 61857 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 61857 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 109257 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 109257 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 170429 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 170429 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 215929 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 206260 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 206260 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 96975 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 96975 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 213681 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 119481 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 119481 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 212302 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 5144 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 5144 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 184106 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 184106 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 102214 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 102214 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 18134 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 18134 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 170618 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 170618 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 100980 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 100980 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 120359 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 120359 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 170618 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 170618 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 9452 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 9452 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 121295 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 121295 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 106968 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 106968 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 9686 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 9686 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 116869 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 116869 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 5029 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 5029 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 120725 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 120725 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 112781 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 112781 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 107338 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 107338 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 210548 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 210548 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 210548 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 4259 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 4259 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 100699 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 100699 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 207427 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 207427 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 197984 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 197984 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 36952 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 36952 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 36952 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 36952 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 85990 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 85990 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 16841 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 16841 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 141239 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 141239 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 109227 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 109227 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 50862 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 50862 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 101618 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 101618 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 77806 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 77806 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 49616 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 49616 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 120824 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 120824 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 197985 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 197985 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 61870 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 61870 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 106800 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 106800 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 131351 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 131351 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 98961 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 98961 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 43692 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 43692 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 213897 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 204682 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 204682 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 25939 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 25939 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 188112 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 188112 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 208272 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 208272 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 9851 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 9851 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 119021 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 119021 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 114814 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 114814 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 102633 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 102633 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 108118 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 108118 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 59709 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 59709 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 110636 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 110636 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 204682 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 204682 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 107345 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 107345 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 9497 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 9497 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 27623 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 27623 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 211710 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 59100 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 59100 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 119279 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 119279 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 106820 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 106820 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 199800 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 199800 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 102051 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 102051 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 204431 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 204431 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 10019 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 10019 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 168929 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 168929 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 210528 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 120193 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 120193 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 79548 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 79548 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 20294 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 20294 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 59084 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 59084 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 207944 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 207944 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 110539 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 110539 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 116602 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 116602 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 67743 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 67743 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 167891 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 167891 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 165996 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 165996 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 203144 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 203144 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 61920 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 61920 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 10157 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 10157 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 106598 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 106598 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 165193 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 165193 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 106630 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 106630 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 170578 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 170578 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 99871 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 99871 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 99871 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 67754 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 67754 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 204465 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 204465 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 204465 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 204465 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 165325 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 165325 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 108737 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 108737 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 28239 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 28239 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 49616 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 49616 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 13094 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 13094 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 13094 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 61873 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 61873 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 79546 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 79546 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 189781 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 189781 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 211133 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 52491 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 52491 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 78816 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 78816 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 113630 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 113630 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 100791 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 100791 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 17935 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 17935 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 78624 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 78624 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 22789 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 22789 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 22789 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 22789 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 110478 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 110478 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 22789 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 22789 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 116745 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 116745 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 29626 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 29626 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 93238 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 93238 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 104378 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 104378 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 16777 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 16777 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 67723 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 67723 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 140584 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 140584 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 28483 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 28483 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 116643 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 116643 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 73648 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 73648 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 207944 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 207944 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 99744 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 99744 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 75935 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 75935 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 201251 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 201251 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 876 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 876 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 876 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 876 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 204633 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 204633 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 165294 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 165294 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 168038 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 168038 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 100464 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 100464 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 168175 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 168175 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 187027 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 187027 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 101971 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 101971 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 78628 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 78628 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 100498 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 100498 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 100498 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 67742 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 67742 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 12209 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 12209 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 12209 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 171018 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 171018 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 121051 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 121051 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 16557 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 16557 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 78436 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 78436 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 10060 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 10060 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 10060 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 10060 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 48010 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 48010 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 1804 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 1804 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 1804 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 102061 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 102061 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 211740 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 119791 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 119791 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 181784 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 181784 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 208851 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 16520 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 16520 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 67714 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 67714 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 207482 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 207482 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 876 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 876 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 876 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 876 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 119334 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 119334 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 118790 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 118790 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 208836 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 108759 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 108759 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 96941 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 96941 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 2405 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 2405 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 2405 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 2405 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 2405 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 2405 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 203485 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 203485 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 210184 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 212313 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 103858 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 103858 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 205794 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 205794 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 102093 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 102093 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 205741 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 205741 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 205741 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 205741 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 106814 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 106814 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 115458 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 115458 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 211128 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 202791 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 202791 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 109387 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 109387 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 202791 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 202791 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 100824 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 100824 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 202791 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 202791 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 78483 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 78483 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 207568 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 207568 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 61919 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 61919 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 102196 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 102196 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 207568 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 207568 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 45339 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 45339 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 45800 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 45800 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 45800 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 78626 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 78626 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 111453 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 111453 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 13985 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 13985 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 13985 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 78813 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 78813 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 67715 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 67715 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 142836 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 142836 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 16833 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 16833 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 9610 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 9610 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 77237 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 77237 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 211723 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 194805 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 194805 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 97086 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 97086 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 99879 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 99879 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 198305 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 198305 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 207857 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 207857 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 57838 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 57838 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 117313 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 117313 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 876 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 876 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 876 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 876 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 25884 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 25884 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 49616 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 49616 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 73596 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 73596 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 206232 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 206232 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 78623 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 78623 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 119644 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 119644 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 85992 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 85992 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 16865 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 16865 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 26453 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 26453 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 202925 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 202925 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 113610 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 113610 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 119151 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 119151 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 114502 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 114502 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 121994 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 121994 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 67738 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 67738 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 4569 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 4569 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 57586 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 57586 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 203265 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 203265 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 210185 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 161725 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 161725 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 109636 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 109636 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 174436 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 174436 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 73648 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 73648 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 209490 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 188425 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 188425 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 163361 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 163361 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 185119 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 185119 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 163361 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 163361 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 101438 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 101438 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 51620 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 51620 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 27554 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 27554 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 78840 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 78840 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 100677 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 100677 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 12824 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 12824 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 12824 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 120598 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 120598 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 120598 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 78591 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 78591 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 204699 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 204699 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 73648 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 73648 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 67752 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 67752 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 102294 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 102294 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 120798 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 120798 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 207635 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 207635 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 112847 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 112847 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 119323 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 119323 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 32726 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 32726 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 157130 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 157130 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 141798 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 141798 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 106613 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 106613 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 103209 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 103209 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 204699 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 204699 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 16592 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 16592 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 106816 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 106816 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 106823 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 106823 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 99655 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 99655 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 140437 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 140437 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 50790 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 50790 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 59107 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 59107 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 206894 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 206894 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 59606 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 59606 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 46508 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 46508 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 69413 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 69413 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 59336 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 59336 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 117285 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 117285 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 120974 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 120974 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 51853 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 51853 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 23125 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 23125 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 100032 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 100032 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 59420 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 59420 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 210187 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 100779 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 100779 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 118551 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 118551 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 204526 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 204526 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 9973 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 9973 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 155762 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 155762 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 157872 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 157872 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 204526 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 204526 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 75946 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 75946 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 16567 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 16567 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 207395 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 207395 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 207395 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 207395 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 207395 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 207395 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 207395 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 207395 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 207395 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 207395 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 56336 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 56336 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 99162 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 99162 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 207395 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 207395 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 115117 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 115117 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 121028 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 121028 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 116660 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 116660 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 207395 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 207395 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 114818 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 114818 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 106630 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 106630 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 210186 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 206638 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 206638 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 100285 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 100285 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 76553 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 76553 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 98836 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 98836 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 120598 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 120598 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 120598 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 206484 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 206484 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 206484 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 206484 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 206484 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 206484 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 99856 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 99856 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 208331 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 208331 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 140771 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 140771 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 204541 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 204541 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 67766 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 67766 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 204541 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 204541 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 106826 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 106826 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 876 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 876 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 876 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 876 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 13296 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 13296 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 13296 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 99141 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 99141 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 16760 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 16760 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 165303 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 165303 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 116612 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 116612 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 67686 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 67686 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 165303 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 165303 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 16530 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 16530 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 121133 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 121133 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 29714 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 29714 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 121003 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 121003 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 6206 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 6206 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 106146 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 106146 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 3025 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 3025 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 3025 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 3025 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 119506 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 119506 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 204187 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 204187 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 95785 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 95785 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 876 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 876 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 876 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 876 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 73648 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 73648 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 106595 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 106595 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 140790 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 140790 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 207606 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 207606 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 181170 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 181170 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 202936 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 202936 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 2219 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 2219 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 2219 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 2219 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 25628 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 25628 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 27768 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 27768 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 212667 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 163436 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 163436 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 204417 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 204417 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 163436 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 163436 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 26926 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 26926 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 204417 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 204417 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 163436 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 163436 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 204417 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 204417 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 107142 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 107142 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 107142 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 107142 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 106593 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 106593 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 182455 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 182455 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 45800 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 45800 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 45800 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 204203 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 204203 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 119754 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 119754 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 108832 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 108832 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 73639 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 73639 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 211296 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 140769 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 140769 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 77824 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 77824 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 67685 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 67685 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 31519 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 31519 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 189674 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 189674 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 189674 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 5023 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 5023 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 85994 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 85994 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 113107 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 113107 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 32232 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 32232 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 118117 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 118117 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 67709 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 67709 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 67721 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 67721 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 100022 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 78360 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 78360 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 16843 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 16843 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 100134 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 100134 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 107226 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 107226 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 161854 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 161854 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 204709 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 204709 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 204709 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 204709 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 78791 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 78791 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 110119 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 110119 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 48324 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 48324 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 207964 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 207964 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 59020 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 59020 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 196582 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 196582 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 97050 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 97050 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 209685 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 73024 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 73024 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 101597 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 101597 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 114794 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 114794 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 111445 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 111445 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 115457 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 115457 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 187827 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 187827 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 174518 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 174518 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 119926 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 119926 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 167985 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 167985 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 208840 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 78516 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 78516 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 48502 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 48502 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 209680 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 59162 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 59162 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 157414 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 157414 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 116769 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 116769 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 120811 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 120811 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 1396 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 1396 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 1396 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 1396 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 158237 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 158237 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 99756 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 99756 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 179060 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 179060 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 61866 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 61866 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 207395 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 207395 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 207395 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 207395 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 207395 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 207395 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 209220 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 209221 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 16606 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 16606 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 100304 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 100304 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 99906 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 99906 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 204498 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 204498 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 206531 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 206531 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 206531 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 206531 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 73647 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 73647 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 170479 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 170479 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 170479 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 5144 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 5144 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 113307 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 113307 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 113307 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 113307 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 10003 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 10003 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 49390 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 49390 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 16837 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 16837 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 114148 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 114148 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 120724 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 120724 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 163905 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 163905 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 207096 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 207096 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 198655 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 198655 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 167928 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 167928 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 141791 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 141791 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 204203 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 204203 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 204484 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 204484 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 22554 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 22554 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 173212 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 173212 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 99879 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 99879 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 211137 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 69411 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 69411 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 209199 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 73645 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 73645 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 61918 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 61918 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 157782 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 157782 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 102951 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 102951 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 103020 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 103020 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 115452 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 115452 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 26512 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 26512 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 77845 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 77845 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 104784 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 104784 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 4675 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 4675 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 211715 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 77823 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 77823 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 16849 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 16849 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 200342 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 200342 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 212698 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 78594 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 78594 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 192532 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 192532 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 99130 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 99130 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 141945 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 141945 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 207091 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 207091 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 211126 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 73642 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 73642 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 876 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 876 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 876 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 876 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 211296 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 168528 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 168528 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 207944 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 207944 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 49887 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 49887 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 77848 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 77848 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 100175 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 100175 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 172939 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 172939 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 16935 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 16935 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 198140 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 198140 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 59557 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 59557 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 78629 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 78629 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 208854 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 99387 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 99387 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 87676 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 87676 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 10421 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 10421 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 61921 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 61921 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 204506 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 204506 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 116293 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 116293 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 120360 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 120360 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 121996 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 121996 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 167795 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 167795 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 73648 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 73648 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 204506 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 204506 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 120768 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 120768 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 212293 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 96490 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 96490 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 59118 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 59118 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 198349 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 198349 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 206456 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 206456 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 207672 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 207672 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 108032 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 108032 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 50862 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 50862 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 98144 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 98144 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 44925 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 44925 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 168254 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 168254 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 120196 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 120196 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 98144 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 98144 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 179343 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 179343 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 179343 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 106697 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 106697 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 207606 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 207606 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 165442 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 165442 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 204925 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 204925 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 204925 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 204925 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 204925 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 204925 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 106571 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 106571 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 28059 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 28059 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 926 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
873 926 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 926 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 926 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 207395 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 207395 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 207606 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 207606 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 119448 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 119448 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 212316 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 212316 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 63244 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 63244 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 207 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
858 207 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 207 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 163436 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 163436 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 212316 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 212316 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 69411 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 69411 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 822 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
864 822 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 822 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 822 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 822 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 63245 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 63245 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 209260 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 822 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
864 822 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 822 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 822 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 822 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 113610 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 113610 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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 207606 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 207606 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 3293 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 3293 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 3293 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 212316 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 212316 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 212316 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 212316 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 26575 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 26575 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 209693 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 16372 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 16372 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 4743 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 4743 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 208587 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 14744 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 14744 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 14744 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 207606 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 207606 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 108624 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 108624 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 1400 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 1400 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 1400 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 1400 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 167979 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 167979 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 196936 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 196936 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 198912 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 198912 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 14546 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 14546 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 197724 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 197724 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 161310 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 161310 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 115483 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 115483 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 207381 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 207381 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 168698 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 168698 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 75989 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 75989 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 212872 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 137508 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 137508 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 156882 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 156882 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 11797 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 11797 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 11797 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 11805 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 11805 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 11805 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 26153 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 26153 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 64138 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 64138 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 64155 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 64155 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 9799 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 9799 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 108427 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 108427 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 155693 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 155693 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 99934 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 99934 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 155729 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 155729 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 208438 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 208438 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 64141 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 64141 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 213618 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 107498 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 107498 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 113793 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 113793 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 209394 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 208609 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 208609 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 211728 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 211474 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 15511 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 15511 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 163910 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 163910 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 168255 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 168255 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 1893 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 1893 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 1893 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 114497 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 114497 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 75989 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 75989 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 208438 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 208438 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 113964 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 113964 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 157015 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 157015 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 76102 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 76102 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 193791 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 193791 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 215856 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 198809 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 198809 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 113402 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 113402 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 211535 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 211537 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 28427 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 28427 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 116978 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 116978 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 107549 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 107549 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 70630 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 70630 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 117459 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 117459 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 208438 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 208438 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 39424 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 39424 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 71701 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 71701 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 197589 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 197589 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 114793 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 114793 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 141542 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 141542 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 94668 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 94668 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 101724 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 101724 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 114773 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 114773 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 2345 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 2345 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 2345 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 83224 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 83224 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 133562 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 133562 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 112674 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 112674 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 119362 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 119362 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 208438 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 208438 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 141525 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 141525 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 208583 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 211540 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 207500 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 207500 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 209850 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 14357 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 14357 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 64155 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 64155 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 107453 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 107453 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 119220 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 119220 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 168628 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 168628 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 71680 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 71680 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 64142 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 64142 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 64140 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 64140 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 92493 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 92493 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 92493 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 112873 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 112873 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 113814 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 113814 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 211394 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 210277 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 209878 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 82126 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 82126 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 64019 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 64019 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 138923 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 138923 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 113007 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 113007 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 107404 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 107404 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 107178 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 107178 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 95981 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 95981 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 15192 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 15192 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 213862 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 205999 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 205999 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 205999 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 107296 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 107296 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 197423 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 197423 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 196763 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 196763 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 196971 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 196971 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 198755 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 198755 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 64153 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 64153 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 4260 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 4260 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 113080 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 113080 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 92493 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 92493 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 92493 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 14703 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 14703 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 14703 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 209343 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 168202 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 168202 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 27915 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 27915 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 112873 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 112873 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 876 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 876 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 876 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 876 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 119306 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 119306 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 64159 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 64159 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 13181 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 13181 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 13181 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 5110 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 5110 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 179343 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 179343 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 179343 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 64152 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 64152 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 207395 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 207395 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 85434 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 85434 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 64149 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 64149 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 98573 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 98573 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 215816 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 208585 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 207133 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 207133 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 4743 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 4743 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 31317 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 31317 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 100498 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 100498 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 100498 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 168809 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 168809 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 118741 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 118741 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 89385 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 89385 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 14703 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 14703 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 14703 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 113866 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 113866 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 69411 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 69411 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 15192 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 15192 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 136945 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 136945 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 83234 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 83234 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 136953 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 136953 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 114003 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 114003 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 197398 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 197398 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 197470 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 197470 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 196902 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 196902 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 198801 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 198801 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 82463 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 82463 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 114793 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 114793 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 197801 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 197801 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 198885 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 198885 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 94883 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 94883 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 119038 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 119038 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 119038 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 166198 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 166198 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 4411 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 4411 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 12311 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 12311 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 12311 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 119038 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 119038 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 119038 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 2405 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 2405 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 2405 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 114128 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 114128 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 113066 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 113066 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 212380 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 98164 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 98164 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 113102 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 113102 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 69411 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 69411 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 211392 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 211393 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 163493 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 163493 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 208598 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 211466 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 97002 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 97002 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 164873 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 164873 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 212265 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 208213 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 208213 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 116774 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 116774 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 64147 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 64147 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 64153 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 64153 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 64158 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 64158 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 12982 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 12982 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 114583 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 114583 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 118869 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 118869 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 119038 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 119038 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 119038 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 140627 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 140627 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 96712 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 96712 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 85518 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 85518 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 101249 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 101249 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 211536 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 73648 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 73648 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 164858 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 164858 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 165252 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 165252 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 143306 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 143306 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 161909 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 161909 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 168059 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 168059 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 14895 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 14895 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 113967 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 113967 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 134421 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 134421 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 15293 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 15293 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 113491 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 113491 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 114134 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 114134 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 62207 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 62207 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 89455 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 89455 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 64154 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 64154 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 101570 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 101570 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 166911 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 166911 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 166911 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 163666 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 163666 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 89457 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 89457 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 211488 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 71451 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 71451 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 95916 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 95916 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 96126 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 96126 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 111987 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 111987 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 207725 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 207725 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 207618 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 207618 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 107285 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 107285 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 114773 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 114773 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 876 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 876 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 876 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 876 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 211534 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 208848 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 89454 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 89454 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 93983 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 93983 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 94024 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 94024 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 94025 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 94025 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 94058 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 94058 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 94059 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 94059 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 94060 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 94060 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 94102 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 94102 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 94103 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 94103 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 94143 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 94143 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 94170 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 94170 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 94199 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 94199 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 94323 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 94323 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 154499 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 154499 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 154500 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 154500 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 154734 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 154734 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 154869 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 154869 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 197690 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 197690 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 96725 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 96725 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 166032 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 166032 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 199036 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 199036 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 196759 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 196759 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 198972 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 198972 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 14410 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 14410 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 15499 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 15499 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 98742 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 98742 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 72076 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 72076 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 72076 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 154922 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 154922 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 154945 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 154945 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 83250 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 83250 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 85517 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 85517 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 168948 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 168948 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 12262 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 12262 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 12262 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 72076 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 72076 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 72076 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 154850 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 154850 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 118983 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 118983 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 64155 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 64155 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 101574 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 101574 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 116785 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 116785 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 64154 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 64154 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 113467 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 113467 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 119038 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 119038 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 119038 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 64019 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 64019 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 106686 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 106686 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 876 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 876 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 876 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 876 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 64139 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 64139 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 73648 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 73648 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 4110 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 4110 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 4110 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 4110 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 95825 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 95825 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 101844 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 101844 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 207688 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 207688 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 4266 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 4266 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 89458 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 89458 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 71979 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 71979 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 9805 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 9805 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 206407 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 206407 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 157867 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 157867 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 209872 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 211474 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 211136 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 70373 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 70373 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 113517 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 113517 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 136956 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 136956 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 10210 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 10210 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 58174 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 58174 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 208604 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 208604 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 4263 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 4263 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 14744 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 14744 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 14744 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 106575 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 106575 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 69411 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 69411 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 189674 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 189674 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 189674 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 69411 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 69411 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 69408 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 69408 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 4110 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 4110 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 4110 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 4110 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 208330 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 208330 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 168470 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 168470 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 168470 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 168239 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 168239 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 168629 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 168629 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 72138 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 72138 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 113105 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 113105 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 107549 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 107549 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 64154 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 64154 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 4110 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 4110 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 4110 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 4110 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 198800 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 198800 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 74495 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 74495 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 211482 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 97083 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 97083 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 112238 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 112238 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 197469 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 197469 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 197753 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 197753 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 153895 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 153895 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 207395 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 207395 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 155678 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 155678 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 107733 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 107733 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 197588 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 197588 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 154616 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 154616 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 141916 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 141916 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 101615 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 101615 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 11804 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 11804 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 11804 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 11928 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 11928 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 11928 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 12268 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 12268 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 12268 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 12285 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 12285 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 12285 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 209182 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 208582 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 209182 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 211532 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 212635 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 72529 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 72529 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 4743 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 4743 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 64157 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 64157 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 208604 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 208604 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 64148 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 64148 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 161995 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 161995 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 210655 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 155235 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 155235 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 99034 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 99034 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 211473 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 211482 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 207595 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 207595 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 210106 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 108588 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 108588 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 64151 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 64151 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 11799 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 11799 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 120461 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 120461 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 120461 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 211542 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 100242 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 100242 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 168633 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 168633 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 194593 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 194593 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 15182 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 15182 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 209399 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 208605 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 208605 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 37491 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 37491 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 37491 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 85519 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 85519 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 116009 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 116009 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 99456 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 99456 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 107705 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 107705 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 101433 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 101433 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 97046 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 97046 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 168476 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 168476 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 159439 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 159439 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 69411 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 69411 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 208702 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 105609 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 105609 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 105609 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 136003 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 136003 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 196764 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 196764 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 197394 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 197394 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 4110 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 4110 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 4110 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 4110 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 196945 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 196945 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 197629 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 197629 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 197783 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 197783 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 37491 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 37491 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 37491 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 37634 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 37634 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 142080 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 142080 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 11933 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 11933 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 11933 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 12278 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 12278 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 12278 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 37491 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 37491 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 37491 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 168470 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 168470 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 168470 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 89384 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 89384 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 212316 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 212316 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 16339 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 16339 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 108336 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 108336 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 4773 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 4773 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 69411 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 69411 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 207673 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 207673 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 206593 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 206593 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 115212 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 115212 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 119240 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 119240 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 64150 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 64150 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 85468 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 85468 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 113181 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 113181 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 208305 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 208305 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 4361 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 4361 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 155705 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 155705 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 168653 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 168653 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 25852 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 25852 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 211538 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 207741 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 207741 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 876 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 876 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 876 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 876 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 116630 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 116630 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 113084 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 113084 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 169481 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 169481 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 95757 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 95757 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 14372 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 14372 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 206679 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 206679 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 142093 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 142093 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 4743 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 4743 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 116881 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 116881 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 64019 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 64019 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 85512 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 85512 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 207395 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 207395 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 3818 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 3818 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 3818 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 15266 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 15266 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 164353 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 164353 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 207614 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 207614 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 112873 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 112873 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 14512 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 14512 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 25860 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 25860 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 207568 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 207568 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 69411 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 69411 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 69411 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 69411 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 109227 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 109227 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 196786 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 196786 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 164597 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 164597 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 197559 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 197559 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 144293 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 144293 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 11966 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 11966 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 11966 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 12284 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 12284 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 12284 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 12286 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 12286 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 12286 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 89386 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 89386 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 212302 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 64144 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 64144 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 64145 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 64145 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 115484 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 115484 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 211135 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 69411 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 69411 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 166160 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 166160 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 107404 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 107404 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 72101 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 72101 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 64143 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 64143 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 115482 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 115482 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 142092 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 142092 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 143303 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 143303 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 112841 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 112841 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 208581 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 168929 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 168929 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 72261 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 72261 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 135806 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 135806 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 144293 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 144293 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 112679 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 112679 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 210528 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 10261 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 10261 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 71448 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 71448 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 85497 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 85497 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 85442 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 85442 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 75945 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 75945 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 74495 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 74495 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 107442 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 107442 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 4353 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 4353 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 117062 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 117062 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 133543 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 133543 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 158314 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 158314 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 208606 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 208606 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 196975 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 196975 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 154946 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 154946 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 114774 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 114774 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 926 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
873 926 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 926 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 926 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 14554 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 14554 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 113373 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 113373 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 211543 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 12279 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 12279 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 12279 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 107712 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 107712 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 143216 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 143216 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 85467 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 85467 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 85510 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 85510 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 212313 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 4287 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 4287 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 209851 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 71722 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 71722 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 71920 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 71920 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 168822 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 168822 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 117633 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 117633 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 63931 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 63931 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 64137 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 64137 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 14367 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 14367 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 14367 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 202677 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 202677 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 112831 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 112831 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 69411 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 69411 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 208330 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 208330 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 113490 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 113490 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 141798 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 141798 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 112556 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 112556 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 112873 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 112873 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 142454 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 142454 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 95808 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 95808 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 114793 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 114793 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 71788 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 71788 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 139830 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 139830 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 28109 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 28109 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 113373 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 113373 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 102028 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 102028 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 114773 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 114773 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 100283 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 100283 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 208303 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 208303 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 113334 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 113334 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 72476 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 72476 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 212316 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 212316 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 108542 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 108542 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 196935 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 196935 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 197530 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 197530 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 197590 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 197590 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 198868 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 198868 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 108542 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 108542 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 207634 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 207634 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 72507 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 72507 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 94600 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 94600 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 102036 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 102036 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 102036 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 4372 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 4372 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 102036 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 102036 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 102036 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 12949 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 12949 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 98745 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 98745 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 141754 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 141754 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 85450 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 85450 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 11801 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 11801 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 11801 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 12261 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 12261 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 12261 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 12280 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 12280 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 12280 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 211229 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 211541 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 822 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
864 822 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 822 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 822 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 822 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 107282 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 107282 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 207275 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 207275 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 211533 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 13878 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 13878 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 143582 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 143582 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 102022 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 102022 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 114113 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 114113 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 110773 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 110773 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 4275 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 4275 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 114802 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 114802 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 141791 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 141791 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 64146 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 64146 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 101935 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 101935 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 114131 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 114131 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 158237 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 158237 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 102036 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 102036 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 102036 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 14002 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 14002 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 14002 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 15297 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 15297 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 211583 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 140739 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 140739 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 194677 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 194677 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 208584 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 209199 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 4619 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 4619 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 207270 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 207270 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 212698 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 73648 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 73648 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 101690 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 101690 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 115231 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 115231 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 4295 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 4295 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 116570 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 116570 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 64156 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 64156 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 212875 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 12472 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 12472 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 113339 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 113339 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 69410 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 69410 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 212293 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 211539 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 203485 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 203485 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 203260 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 203260 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 215953 0 None - 58 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 22789 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 22789 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 2349 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 2349 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 2349 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 2349 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 815 0 None 3 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 6256771
860 815 0 None 3 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 6256771
91898395 815 0 None 3 2 Rat 9.3 pKd = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 6256771
3476 1400 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 1400 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 1400 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 1400 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 822 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
864 822 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 822 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 822 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 822 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 166911 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 166911 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 166911 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 822 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
864 822 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 822 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 822 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 822 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 822 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
864 822 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 822 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 822 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 822 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
859 472 0 None 7943 2 Rat 10.5 pKi None 10.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476993
3074331 925 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
872 925 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 2240 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 2240 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 2240 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 3025 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 3025 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 3025 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 3025 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 4115 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 4115 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 4115 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 1403 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 1403 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 1403 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 1403 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 1403 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 2136 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 2136 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 2136 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 3848 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 3848 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