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Assay Detail

CHEMBL661733

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

Binding
Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-8
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents.
Henke BR, Willson TM, Sugg EE, Croom DK, Dougherty RW, Queen KL, Birkemo LS, Ervin GN, Grizzle MK, Johnson MF, James MK.
J Med Chem (1996) 39 : 2655 -2658
PubMed 8709093 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.49 8.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1121 SINCALIDE 4.0 1 8.88
CHEMBL316164 1 8.08
CHEMBL88602 1 7.96
CHEMBL293226 1 7.64
CHEMBL310466 1 7.37
CHEMBL88545 1 7.06
CHEMBL431212 1 6.97
CHEMBL430451 1 6.92
CHEMBL89953 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1121 SINCALIDE IC50 = 1.318 nM 8.88
CHEMBL316164 IC50 = 8.318 nM 8.08
CHEMBL88602 IC50 = 10.96 nM 7.96
CHEMBL293226 IC50 = 22.91 nM 7.64
CHEMBL310466 IC50 = 42.66 nM 7.37
CHEMBL88545 IC50 = 87.1 nM 7.06
CHEMBL431212 IC50 = 107.15 nM 6.97
CHEMBL430451 IC50 = 120.23 nM 6.92
CHEMBL89953 IC50 = 309.03 nM 6.51