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Assay Detail

CHEMBL662391

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 rat pancreas Cholecystokinin type A receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cholecystokinin receptor type A (CHEMBL2871)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 5.90 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL341460 1 6.10
CHEMBL2112693 1 6.06
CHEMBL335914 1 6.02
CHEMBL341281 1 5.96
CHEMBL2112694 1 5.89
CHEMBL2062154 CI-988 1.0 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL341460 IC50 = 790.0 nM 6.10
CHEMBL2112693 IC50 = 870.0 nM 6.06
CHEMBL335914 IC50 = 950.0 nM 6.02
CHEMBL341281 IC50 = 1100.0 nM 5.96
CHEMBL2112694 IC50 = 1300.0 nM 5.89
CHEMBL2062154 CI-988 IC50 = 4300.0 nM 5.37