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Assay Detail

CHEMBL857783

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

Binding
Binding affinity was measured by its ability to displace [3H]CCK-8S from CCK-A receptor in rat pancreas
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1,5-Benzodiazepines as CCK-B antagonists. Effect of halogen substitution at the benzo-fused ring on potency and selectivity
Curotto G, Donati D, Pentassuglia G, Ursini A
Bioorg Med Chem Lett (1995) 5 : 3011 -3016
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.15 8.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL103750 1 8.81
CHEMBL319795 1 8.34
CHEMBL103968 1 8.31
CHEMBL317081 1 8.05
CHEMBL102867 1 8.01
CHEMBL101125 1 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL103750 Ki = 1.549 nM 8.81
CHEMBL319795 Ki = 4.571 nM 8.34
CHEMBL103968 Ki = 4.898 nM 8.31
CHEMBL317081 Ki = 8.913 nM 8.05
CHEMBL102867 Ki = 9.772 nM 8.01
CHEMBL101125 Ki = 41.69 nM 7.38