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Assay Detail

CHEMBL662415

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

Binding
Inhibition of [125I]Cholecystokinin-8 (125I-CCK-8) binding to Cholecystokinin type A receptor of rat pancreatic membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Dual CCK-A and -B receptor antagonists (I) C9-methyl-1,4-benzodiazepines
Tabuchi S, Ito H, Sogabe H, Kuno M, Katsumi I, Yamamoto N, Mitsui H, Satoh Y
Bioorg Med Chem Lett (1997) 7 : 169 -174
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.09 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9506 DEVAZEPIDE 2.0 1 10.10
CHEMBL300072 PRANAZEPIDE 2.0 1 9.17
CHEMBL299523 1 8.29
CHEMBL50216 1 8.14
CHEMBL48563 1 8.13
CHEMBL50215 1 7.89
CHEMBL285921 1 7.85
CHEMBL299800 1 7.77
CHEMBL413267 1 7.68
CHEMBL49085 1 7.21
CHEMBL50926 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9506 DEVAZEPIDE IC50 = 0.08 nM 10.10
CHEMBL300072 PRANAZEPIDE IC50 = 0.67 nM 9.17
CHEMBL299523 IC50 = 5.1 nM 8.29
CHEMBL50216 IC50 = 7.3 nM 8.14
CHEMBL48563 IC50 = 7.4 nM 8.13
CHEMBL50215 IC50 = 13.0 nM 7.89
CHEMBL285921 IC50 = 14.0 nM 7.85
CHEMBL299800 IC50 = 17.0 nM 7.77
CHEMBL413267 IC50 = 21.0 nM 7.68
CHEMBL49085 IC50 = 62.0 nM 7.21
CHEMBL50926 IC50 = 160.0 nM 6.80