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Assay Detail

CHEMBL662414

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Binding
Compound was evaluated for the inhibition of 124 I-CCK-8 binding at Cholecystokinin type A receptor in rat pancreatic membranes
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cholecystokinin receptor type A (CHEMBL2871)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Relationship between dihedral angles of N1 and C9 substituents in 1,4-benzodiazepines and dual cholecystokinin-A and -B antagonistic activities.
Tabuchi S, Nakanishi I, Satoh Y.
Bioorg Med Chem Lett (1998) 8 : 1449 -1454
PubMed 9873368 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.68 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL32492 1 7.89
CHEMBL285921 1 7.85
CHEMBL285850 1 7.75
CHEMBL432266 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL32492 IC50 = 13.0 nM 7.89
CHEMBL285921 IC50 = 14.0 nM 7.85
CHEMBL285850 IC50 = 18.0 nM 7.75
CHEMBL432266 IC50 = 62.0 nM 7.21