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Assay Detail

CHEMBL662559

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

Binding
Binding affinity towards Cholecystokinin type B receptor was measured by displacement of [125I]CCK from guinea pig cortical membranes
10
Total Activities
10
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

Potent, selective, water-soluble benzodiazepine-based CCKB receptor antagonists that contain lipophilic carboxylate surrogates
Chambers MS, Hobbs SC, Graham MI, Watt AP, Fletcher SR, Baker R, Freedman SB, Patel S, Smith AJ, Matassa VG
Bioorg Med Chem Lett (1995) 5 : 2303 -2308
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 9.33 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75490 1 9.62
CHEMBL305649 1 9.57
CHEMBL58699 1 9.55
CHEMBL75536 1 9.52
CHEMBL441989 1 9.44
CHEMBL75892 1 9.24
CHEMBL306944 1 9.23
CHEMBL311154 1 9.14
CHEMBL75019 1 9.11
CHEMBL306803 1 8.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75490 IC50 = 0.24 nM 9.62
CHEMBL305649 IC50 = 0.27 nM 9.57
CHEMBL58699 IC50 = 0.28 nM 9.55
CHEMBL75536 IC50 = 0.3 nM 9.52
CHEMBL441989 IC50 = 0.36 nM 9.44
CHEMBL75892 IC50 = 0.58 nM 9.24
CHEMBL306944 IC50 = 0.59 nM 9.23
CHEMBL311154 IC50 = 0.73 nM 9.14
CHEMBL75019 IC50 = 0.78 nM 9.11
CHEMBL306803 IC50 = 1.4 nM 8.85