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Assay Detail

CHEMBL661735

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

Binding
Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-KI
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cholecystokinin receptor type A (CHEMBL1901)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
Hirst GC, Aquino C, Birkemo L, Croom DK, Dezube M, Dougherty RW, Ervin GN, Grizzle MK, Henke B, James MK, Johnson MF, Momtahen T, Queen KL, Sherrill RG, Szewczyk J, Willson TM, Sugg EE.
J Med Chem (1996) 39 : 5236 -5245
PubMed 8978852 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.84 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1121 SINCALIDE 4.0 1 9.20
CHEMBL358778 1 8.00
CHEMBL356408 1 7.80
CHEMBL321761 1 7.30
CHEMBL147186 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1121 SINCALIDE IC50 = 0.631 nM 9.20
CHEMBL358778 IC50 = 10.0 nM 8.00
CHEMBL356408 IC50 = 15.85 nM 7.80
CHEMBL321761 IC50 = 50.12 nM 7.30
CHEMBL147186 IC50 = 125.89 nM 6.90