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Assay Detail

CHEMBL657477

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

Binding
Ability to inhibit the binding of [125I]CCK-8 to Cholecystokinin type B receptor in guinea pig cortex.
20
Total Activities
20
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

Benzolactams as non-peptide cholecystokinin receptor ligands
Bock MG, DiPardo RM, Veber DF, Chang RS, Lotti VJ, Freedman SB, Freidinger RM
Bioorg Med Chem Lett (1993) 3 : 871 -874
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.58 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445095 1 9.55
CHEMBL38404 1 9.00
CHEMBL342640 1 8.10
CHEMBL354442 1 6.99
CHEMBL354040 1 6.96
CHEMBL34335 1 6.96
CHEMBL355319 1 6.82
CHEMBL170293 1 6.80
CHEMBL424211 1 6.75
CHEMBL9506 DEVAZEPIDE 2.0 1 6.61
CHEMBL423278 1 6.57
CHEMBL168386 1 6.19
CHEMBL352939 1 6.06
CHEMBL170777 1 5.92
CHEMBL171722 1 5.66
CHEMBL169807 1 5.30
CHEMBL169931 1 5.07
CHEMBL169794 1 4.89
CHEMBL170068 1 4.77
CHEMBL297534 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445095 IC50 = 0.28 nM 9.55
CHEMBL38404 IC50 = 1.0 nM 9.00
CHEMBL342640 IC50 = 8.0 nM 8.10
CHEMBL354442 IC50 = 103.0 nM 6.99
CHEMBL354040 IC50 = 109.0 nM 6.96
CHEMBL34335 IC50 = 110.0 nM 6.96
CHEMBL355319 IC50 = 150.0 nM 6.82
CHEMBL170293 IC50 = 160.0 nM 6.80
CHEMBL424211 IC50 = 180.0 nM 6.75
CHEMBL9506 DEVAZEPIDE IC50 = 245.0 nM 6.61
CHEMBL423278 IC50 = 270.0 nM 6.57
CHEMBL168386 IC50 = 650.0 nM 6.19
CHEMBL352939 IC50 = 878.0 nM 6.06
CHEMBL170777 IC50 = 1190.0 nM 5.92
CHEMBL171722 IC50 = 2200.0 nM 5.66
CHEMBL169807 IC50 = 5000.0 nM 5.30
CHEMBL169931 IC50 = 8600.0 nM 5.07
CHEMBL169794 IC50 = 13000.0 nM 4.89
CHEMBL170068 IC50 = 17000.0 nM 4.77
CHEMBL297534 IC50 > 10000.0 nM -