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Assay Detail

CHEMBL661164

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

Binding
In vitro inhibition of [125I]CCK-8 binding to guinea pig pancreas
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Cholecystokinin receptor (CHEMBL2095185)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

CCK-A-selective tetrapeptides containing lys(N epsilon)-amide residues: favorable in vivo and in vitro effects of N-methylation at the aspartyl residue.
Bennett MJ, Nikkel AL, Bianchi BR, Miller TR, Bednarz L, Witte DG, Stashko M, Wang SS, Gore PA, Asin KE.
J Med Chem (1994) 37 : 1569 -1571
PubMed 8201591 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.84 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL156559 1 8.43
CHEMBL411466 1 8.38
CHEMBL290936 1 8.30
CHEMBL432293 1 8.05
CHEMBL290143 1 7.75
CHEMBL290034 1 7.50
CHEMBL290142 1 7.46
CHEMBL289744 1 7.39
CHEMBL289284 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL156559 IC50 = 3.7 nM 8.43
CHEMBL411466 IC50 = 4.2 nM 8.38
CHEMBL290936 IC50 = 5.0 nM 8.30
CHEMBL432293 IC50 = 9.0 nM 8.05
CHEMBL290143 IC50 = 18.0 nM 7.75
CHEMBL290034 IC50 = 32.0 nM 7.50
CHEMBL290142 IC50 = 35.0 nM 7.46
CHEMBL289744 IC50 = 41.0 nM 7.39
CHEMBL289284 IC50 = 50.0 nM 7.30