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Assay Detail

CHEMBL663085

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

Binding
Binding affinity against Cholecystokinin type B receptor using [3H](MeNLE28,31)-CCK-8 as radioligand in guinea pig cerebral cortex.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Cerebral cortex
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Gastrin/cholecystokinin type B receptor (CHEMBL298)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors.
Cappelli A, Anzini M, Vomero S, Menziani MC, De Benedetti PG, Sbacchi M, Clarke GD, Mennuni L.
J Med Chem (1996) 39 : 860 -872
PubMed 8632410 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.03 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9506 DEVAZEPIDE 2.0 1 8.43
CHEMBL127969 1 4.89
CHEMBL124015 1 4.77
CHEMBL169703 TIFLUADOM 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9506 DEVAZEPIDE Ki = 3.69 nM 8.43
CHEMBL127969 Ki = 13000.0 nM 4.89
CHEMBL124015 Ki = 17000.0 nM 4.77
CHEMBL169703 TIFLUADOM Ki > 100000.0 nM -