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Assay Detail

CHEMBL663300

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

Binding
The compound was tested in vitro for inhibition of specific [3H]propionyl-CCK-8 binding to Cholecystokinin type A receptor in rat pancreatic membranes
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Analogs of Ac-CCK-7 incorporating dipeptide mimics in place of Met28-Gly29.
Tilley JW, Danho W, Shiuey SJ, Kulesha I, Swistok J, Makofske R, Michalewsky J, Triscari J, Nelson D, Weatherford S.
J Med Chem (1992) 35 : 3774 -3783
PubMed 1433191 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.13 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL331408 1 8.68
CHEMBL122438 1 7.60
CHEMBL405805 1 7.14
CHEMBL2112635 1 6.79
CHEMBL2111823 1 6.78
CHEMBL126008 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL331408 IC50 = 2.1 nM 8.68
CHEMBL122438 IC50 = 25.0 nM 7.60
CHEMBL405805 IC50 = 73.0 nM 7.14
CHEMBL2112635 IC50 = 161.0 nM 6.79
CHEMBL2111823 IC50 = 165.0 nM 6.78
CHEMBL126008 IC50 = 1600.0 nM 5.80