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Assay Detail

CHEMBL828686

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

Binding
Inhibition of 71 pM [125I]BH-(Thr,Nle)CCK-9 binding to rat cholecystokinin 1 receptor
5
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cholecystokinin receptor type A (CHEMBL2871)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Combination of molecular modeling, site-directed mutagenesis, and SAR studies to delineate the binding site of pyridopyrimidine antagonists on the human CCK1 receptor.
Martín-Martínez M, Marty A, Jourdan M, Escrieut C, Archer E, González-Muñiz R, García-López MT, Maigret B, Herranz R, Fourmy D.
J Med Chem (2005) 48 : 4842 -4850
PubMed 16033264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.89 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL363916 2 10.05
CHEMBL366344 2 9.23
CHEMBL113718 IQM-95333 1 8.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL363916 IC50 = 0.09 nM 10.05
CHEMBL366344 IC50 = 0.59 nM 9.23
CHEMBL113718 IQM-95333 IC50 = 1.59 nM 8.80
CHEMBL363916 IC50 = 2.83 nM 8.55
CHEMBL366344 IC50 = 15.4 nM 7.81