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Assay Detail

CHEMBL653980

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

Binding
Inhibition of [125I]BH-CCK- binding to cholecystokinin type B receptor from guinea pig brain membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Gastrin/cholecystokinin type B receptor (CHEMBL298)
Type SINGLE PROTEIN
Organism Homo sapiens

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Synthesis and biological evaluation of cholecystokinin analogs in which the Asp-Phe-NH2 moiety has been replaced by a 3-amino-7-phenylheptanoic acid or a 3-amino-6-(phenyloxy)hexanoic acid.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 12 7.01 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL384035 1 9.54
CHEMBL274661 1 8.70
CHEMBL441165 1 8.00
CHEMBL216079 1 7.50
CHEMBL262155 1 7.24
CHEMBL217424 1 6.70
CHEMBL217234 1 6.69
CHEMBL386811 1 6.30
CHEMBL263876 1 5.94
CHEMBL444113 1 5.92
CHEMBL385918 1 5.78
CHEMBL414180 1 5.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL384035 IC50 = 0.29 nM 9.54
CHEMBL274661 IC50 = 2.0 nM 8.70
CHEMBL441165 IC50 = 10.0 nM 8.00
CHEMBL216079 IC50 = 32.0 nM 7.50
CHEMBL262155 IC50 = 57.0 nM 7.24
CHEMBL217424 IC50 = 200.0 nM 6.70
CHEMBL217234 IC50 = 205.0 nM 6.69
CHEMBL386811 IC50 = 500.0 nM 6.30
CHEMBL263876 IC50 = 1150.0 nM 5.94
CHEMBL444113 IC50 = 1200.0 nM 5.92
CHEMBL385918 IC50 = 1650.0 nM 5.78
CHEMBL414180 IC50 = 1750.0 nM 5.76