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Assay Detail

CHEMBL653018

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

Binding
Inhibition of [3H]pCCK-8 binding to cholecystokinin type B receptor of rat cerebral cortex
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Confidence 9 — Direct single protein target
Curated By Expert

Target

Gastrin/cholecystokinin type B receptor (CHEMBL3508)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structure-activity relationship studies on the central 1,3-dioxoperhydropyrido[1,2-c]pyrimidine scaffold.
Bartolomé-Nebreda JM, García-López MT, González-Muñiz R, Cenarruzabeitia E, Latorre M, Del Río J, Herranz R.
J Med Chem (2001) 44 : 4196 -4206
PubMed 11708921 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.73 8.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1121 SINCALIDE 4.0 1 8.25
CHEMBL116127 1 5.21
CHEMBL3350851 1 -
CHEMBL3350854 1 -
CHEMBL3350855 1 -
CHEMBL3350857 1 -
CHEMBL3350852 1 -
CHEMBL3350858 1 -
CHEMBL3350853 1 -
CHEMBL3350849 1 -
CHEMBL3350850 1 -
CHEMBL3350859 1 -
CHEMBL3350856 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1121 SINCALIDE IC50 = 5.6 nM 8.25
CHEMBL116127 IC50 = 6153.0 nM 5.21
CHEMBL3350851 IC50 > 10000.0 nM -
CHEMBL3350854 IC50 > 10000.0 nM -
CHEMBL3350855 IC50 > 10000.0 nM -
CHEMBL3350857 IC50 > 10000.0 nM -
CHEMBL3350852 IC50 > 10000.0 nM -
CHEMBL3350858 IC50 > 10000.0 nM -
CHEMBL3350853 IC50 > 10000.0 nM -
CHEMBL3350849 IC50 > 10000.0 nM -
CHEMBL3350850 IC50 > 10000.0 nM -
CHEMBL3350859 IC50 > 10000.0 nM -
CHEMBL3350856 IC50 > 10000.0 nM -