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Assay Detail

CHEMBL663482

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

Binding
Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Cholecystokinin antagonists. Synthesis and biological evaluation of 4-substituted 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines.
Bock MG, DiPardo RM, Evans BE, Rittle KE, Veber DF, Freidinger RM, Chang RS, Lotti VJ.
J Med Chem (1988) 31 : 176 -181
PubMed 3336017 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.48 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53907 1 9.70
CHEMBL50986 1 9.05
CHEMBL298948 1 8.36
CHEMBL298705 1 7.09
CHEMBL416483 1 7.00
CHEMBL53234 1 6.92
CHEMBL299538 1 6.70
CHEMBL301172 1 6.66
CHEMBL51569 1 6.52
CHEMBL300926 1 4.85
CHEMBL301331 1 4.66
CHEMBL51280 1 4.60
CHEMBL646 TRIAZOLAM 4.0 1 4.41
CHEMBL661 ALPRAZOLAM 4.0 1 4.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53907 IC50 = 0.2 nM 9.70
CHEMBL50986 IC50 = 0.9 nM 9.05
CHEMBL298948 IC50 = 4.4 nM 8.36
CHEMBL298705 IC50 = 82.0 nM 7.09
CHEMBL416483 IC50 = 100.0 nM 7.00
CHEMBL53234 IC50 = 120.0 nM 6.92
CHEMBL299538 IC50 = 200.0 nM 6.70
CHEMBL301172 IC50 = 220.0 nM 6.66
CHEMBL51569 IC50 = 300.0 nM 6.52
CHEMBL300926 IC50 = 14000.0 nM 4.85
CHEMBL301331 IC50 = 22000.0 nM 4.66
CHEMBL51280 IC50 = 25000.0 nM 4.60
CHEMBL646 TRIAZOLAM IC50 = 39000.0 nM 4.41
CHEMBL661 ALPRAZOLAM IC50 = 64000.0 nM 4.19