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Assay Detail

CHEMBL684568

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

Binding
Displacement of [125I]gastrin from guinea pig gastric glands
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Stomach
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

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 5.84 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53907 1 8.15
CHEMBL50986 1 7.19
CHEMBL53234 1 6.42
CHEMBL298705 1 6.42
CHEMBL298948 1 5.62
CHEMBL301172 1 5.52
CHEMBL416483 1 5.32
CHEMBL51569 1 4.92
CHEMBL299538 1 4.60
CHEMBL300926 1 4.22
CHEMBL301331 1 -
CHEMBL51280 1 -
CHEMBL661 ALPRAZOLAM 4.0 1 -
CHEMBL646 TRIAZOLAM 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53907 IC50 = 7.0 nM 8.15
CHEMBL50986 IC50 = 65.0 nM 7.19
CHEMBL53234 IC50 = 380.0 nM 6.42
CHEMBL298705 IC50 = 380.0 nM 6.42
CHEMBL298948 IC50 = 2400.0 nM 5.62
CHEMBL301172 IC50 = 3000.0 nM 5.52
CHEMBL416483 IC50 = 4800.0 nM 5.32
CHEMBL51569 IC50 = 12000.0 nM 4.92
CHEMBL299538 IC50 = 25000.0 nM 4.60
CHEMBL300926 IC50 = 60000.0 nM 4.22
CHEMBL301331 IC50 > 100000.0 nM -
CHEMBL51280 IC50 > 100000.0 nM -
CHEMBL661 ALPRAZOLAM IC50 > 100000.0 nM -
CHEMBL646 TRIAZOLAM IC50 > 100000.0 nM -