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Assay Detail

CHEMBL2019603

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [125I]-CCK-2 from human CCK1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholecystokinin receptor type A (CHEMBL1901)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists.
Cameron KO, Beretta EE, Chen Y, Chu-Moyer M, Fernando D, Gao H, Kohrt J, Lavergne S, Jardine Pda S, Guzman-Perez A, Hoth C, Perry DA, Hadcock JR, Gautreau D, Makowski M, Perez S, Polivkova J, Rogers L, Scott DO, Swick AG, Thiede L, Trebino CE, Trilles RV, Wilmowski J, Zhang Y.
Bioorg Med Chem Lett (2012) 22 : 2943 -2947
PubMed 22424974 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.25 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2017828 1 8.37
CHEMBL2017832 1 8.00
CHEMBL2017835 1 7.69
CHEMBL1269258 CE-326597 2.0 1 7.63
CHEMBL2017833 1 7.44
CHEMBL2017691 1 7.43
CHEMBL2017831 1 7.42
CHEMBL2017827 1 7.35
CHEMBL2017690 1 7.31
CHEMBL2017692 1 7.16
CHEMBL2017826 1 7.10
CHEMBL2017834 1 7.06
CHEMBL2017829 1 7.03
CHEMBL2017825 1 6.78
CHEMBL2017824 1 6.61
CHEMBL2017830 1 6.47
CHEMBL2017823 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2017828 IC50 = 4.24 nM 8.37
CHEMBL2017832 IC50 = 9.9 nM 8.00
CHEMBL2017835 IC50 = 20.3 nM 7.69
CHEMBL1269258 CE-326597 IC50 = 23.6 nM 7.63
CHEMBL2017833 IC50 = 36.0 nM 7.44
CHEMBL2017691 IC50 = 36.9 nM 7.43
CHEMBL2017831 IC50 = 38.1 nM 7.42
CHEMBL2017827 IC50 = 44.7 nM 7.35
CHEMBL2017690 IC50 = 49.3 nM 7.31
CHEMBL2017692 IC50 = 68.6 nM 7.16
CHEMBL2017826 IC50 = 80.1 nM 7.10
CHEMBL2017834 IC50 = 87.6 nM 7.06
CHEMBL2017829 IC50 = 93.3 nM 7.03
CHEMBL2017825 IC50 = 168.0 nM 6.78
CHEMBL2017824 IC50 = 248.0 nM 6.61
CHEMBL2017830 IC50 = 340.0 nM 6.47
CHEMBL2017823 IC50 = 373.0 nM 6.43