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Assay Detail

CHEMBL661736

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

Binding
Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Expert

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. 1. Optimization of the agonist "trigger".
Aquino CJ, Armour DR, Berman JM, Birkemo LS, Carr RA, Croom DK, Dezube M, Dougherty RW, Ervin GN, Grizzle MK, Head JE, Hirst GC, James MK, Johnson MF, Miller LJ, Queen KL, Rimele TJ, Smith DN, Sugg EE.
J Med Chem (1996) 39 : 562 -569
PubMed 8558528 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.06 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1121 SINCALIDE 4.0 1 9.20
CHEMBL443825 1 7.40
CHEMBL321761 1 7.30
CHEMBL345869 1 7.20
CHEMBL108130 1 7.10
CHEMBL345786 1 7.00
CHEMBL154615 1 5.70
CHEMBL346179 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1121 SINCALIDE IC50 = 0.631 nM 9.20
CHEMBL443825 IC50 = 39.81 nM 7.40
CHEMBL321761 IC50 = 50.12 nM 7.30
CHEMBL345869 IC50 = 63.1 nM 7.20
CHEMBL108130 IC50 = 79.43 nM 7.10
CHEMBL345786 IC50 = 100.0 nM 7.00
CHEMBL154615 IC50 = 1995.26 nM 5.70
CHEMBL346179 IC50 = 2511.89 nM 5.60