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Assay Detail

CHEMBL663168

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

Binding
Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to mouse cerebral cortex Cholecystokinin type B receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Gastrin/cholecystokinin type B receptor (CHEMBL2854)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
Horwell DC, Hughes J, Hunter JC, Pritchard MC, Richardson RS, Roberts E, Woodruff GN.
J Med Chem (1991) 34 : 404 -414
PubMed 1671419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.60 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL341460 1 9.15
CHEMBL2112693 1 9.10
CHEMBL2062154 CI-988 1.0 1 8.77
CHEMBL335914 1 8.38
CHEMBL341281 1 8.34
CHEMBL2112694 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL341460 IC50 = 0.7 nM 9.15
CHEMBL2112693 IC50 = 0.8 nM 9.10
CHEMBL2062154 CI-988 IC50 = 1.7 nM 8.77
CHEMBL335914 IC50 = 4.2 nM 8.38
CHEMBL341281 IC50 = 4.6 nM 8.34
CHEMBL2112694 IC50 = 14.0 nM 7.85