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Assay Detail

CHEMBL662397

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

Binding
Inhibition of [3H]propanoyl binding to cholecystokinin type A receptor was determined in fresh rat pancreatic tissue membranes
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Carboxylic acids and tetrazoles as isosteric replacements for sulfate in cholecystokinin analogues.
Tilley JW, Danho W, Lovey K, Wagner R, Swistok J, Makofske R, Michalewsky J, Triscari J, Nelson D, Weatherford S.
J Med Chem (1991) 34 : 1125 -1136
PubMed 2002454 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.56 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL430906 1 9.60
CHEMBL2370122 1 9.22
CHEMBL2079549 1 8.59
CHEMBL2079606 1 8.52
CHEMBL2079603 1 7.68
CHEMBL2370119 1 7.64
CHEMBL273344 1 7.58
CHEMBL2079548 1 7.52
CHEMBL275167 1 7.46
CHEMBL2079551 1 7.17
CHEMBL2079547 1 6.92
CHEMBL2079550 1 6.85
CHEMBL2079602 1 6.77
CHEMBL2079604 1 6.68
CHEMBL2079601 1 6.42
CHEMBL2370120 1 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430906 IC50 = 0.25 nM 9.60
CHEMBL2370122 IC50 = 0.6 nM 9.22
CHEMBL2079549 IC50 = 2.6 nM 8.59
CHEMBL2079606 IC50 = 3.0 nM 8.52
CHEMBL2079603 IC50 = 21.0 nM 7.68
CHEMBL2370119 IC50 = 23.0 nM 7.64
CHEMBL273344 IC50 = 26.0 nM 7.58
CHEMBL2079548 IC50 = 30.0 nM 7.52
CHEMBL275167 IC50 = 35.0 nM 7.46
CHEMBL2079551 IC50 = 67.0 nM 7.17
CHEMBL2079547 IC50 = 120.0 nM 6.92
CHEMBL2079550 IC50 = 140.0 nM 6.85
CHEMBL2079602 IC50 = 170.0 nM 6.77
CHEMBL2079604 IC50 = 210.0 nM 6.68
CHEMBL2079601 IC50 = 380.0 nM 6.42
CHEMBL2370120 IC50 = 390.0 nM 6.41