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Assay Detail

CHEMBL662474

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

Binding
Inhibition of [125I]BH-CCK- binding to peripheral cholecystokinin type B receptor from rat pancreatic acini
11
Total Activities
11
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

Gastrin/cholecystokinin type B receptor (CHEMBL3508)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological evaluation of cholecystokinin analogs in which the Asp-Phe-NH2 moiety has been replaced by a 3-amino-7-phenylheptanoic acid or a 3-amino-6-(phenyloxy)hexanoic acid.
Amblard M, Rodriguez M, Lignon MF, Galas MC, Bernad N, Artis-Noël AM, Hauad L, Laur J, Califano JC, Aumelas A.
J Med Chem (1993) 36 : 3021 -3028
PubMed 7692048 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.88 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL384035 1 8.64
CHEMBL274661 1 8.52
CHEMBL216079 1 7.92
CHEMBL262155 1 7.89
CHEMBL263876 1 7.85
CHEMBL217234 1 7.82
CHEMBL217424 1 7.80
CHEMBL414180 1 7.75
CHEMBL444113 1 7.64
CHEMBL441165 1 7.52
CHEMBL385918 1 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL384035 IC50 = 2.3 nM 8.64
CHEMBL274661 IC50 = 3.0 nM 8.52
CHEMBL216079 IC50 = 12.0 nM 7.92
CHEMBL262155 IC50 = 13.0 nM 7.89
CHEMBL263876 IC50 = 14.0 nM 7.85
CHEMBL217234 IC50 = 15.0 nM 7.82
CHEMBL217424 IC50 = 16.0 nM 7.80
CHEMBL414180 IC50 = 18.0 nM 7.75
CHEMBL444113 IC50 = 23.0 nM 7.64
CHEMBL441165 IC50 = 30.0 nM 7.52
CHEMBL385918 IC50 = 42.0 nM 7.38