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Assay Detail

CHEMBL657476

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

Binding
The compound was tested for its activity to inhibit the binding of [125I]CCK-8 to Cholecystokinin type B receptor in guinea pig brain at a pH of 6.5
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Diphenylpyrazolidinone and benzodiazepine cholecystokinin antagonists: A case of convergent evolution in medicinal chemistry
Howbert J, Lobb KL, Britton TC, Mason NR, Bruns RF
Bioorg Med Chem Lett (1993) 3 : 875 -880
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.34 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9387 L-365260 1 8.70
CHEMBL70380 1 6.82
CHEMBL9506 DEVAZEPIDE 2.0 1 6.57
CHEMBL168852 1 5.54
CHEMBL419764 1 5.43
CHEMBL169438 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9387 L-365260 IC50 = 2.0 nM 8.70
CHEMBL70380 IC50 = 150.0 nM 6.82
CHEMBL9506 DEVAZEPIDE IC50 = 270.0 nM 6.57
CHEMBL168852 IC50 = 2900.0 nM 5.54
CHEMBL419764 IC50 = 3700.0 nM 5.43
CHEMBL169438 IC50 = 11000.0 nM 4.96