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Assay Detail

CHEMBL657482

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

Binding
In vitro binding affinity against Cholecystokinin type B receptor in guinea pig brain membranes
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

On the significance of the C-terminal primary amide in cholecystokinin
Rolland M, Lignon M, Galas M, Bernad N, Rodriguez M, Fulcrand P, Martinez J
Bioorg Med Chem Lett (1993) 3 : 851 -854
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.02 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL384035 1 9.54
CHEMBL384505 2 8.00
CHEMBL265147 1 7.28
CHEMBL436690 1 7.14
CHEMBL268337 1 6.22
CHEMBL414523 1 6.16
CHEMBL216527 1 6.00
CHEMBL413186 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL384035 IC50 = 0.29 nM 9.54
CHEMBL384505 IC50 = 10.0 nM 8.00
CHEMBL265147 IC50 = 53.0 nM 7.28
CHEMBL436690 IC50 = 72.0 nM 7.14
CHEMBL384505 IC50 = 80.0 nM 7.10
CHEMBL268337 IC50 = 600.0 nM 6.22
CHEMBL414523 IC50 = 700.0 nM 6.16
CHEMBL216527 IC50 = 1000.0 nM 6.00
CHEMBL413186 IC50 = 1800.0 nM 5.75