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Assay Detail

CHEMBL663301

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 7.09 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267849 1 9.22
CHEMBL433647 1 8.31
CHEMBL421471 1 7.66
CHEMBL436199 1 6.44
CHEMBL338056 1 5.92
CHEMBL124719 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267849 IC50 = 0.6 nM 9.22
CHEMBL433647 IC50 = 4.9 nM 8.31
CHEMBL421471 IC50 = 22.0 nM 7.66
CHEMBL436199 IC50 = 360.0 nM 6.44
CHEMBL338056 IC50 = 1200.0 nM 5.92
CHEMBL124719 IC50 = 10000.0 nM 5.00