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Assay Detail

CHEMBL682555

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

Binding
Inhibitory activity against gastrin receptor.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and pharmacological evaluation of highly potent dual histamine H2 and gastrin receptor antagonists
Kawanishi Y, Ishihara S, Tsushima T, Seno K, Miyagoshi M, Hagishita S, Ishikawa M, Shima N, Shimamura M, Ishihara Y
Bioorg Med Chem Lett (1996) 6 : 1427 -1430
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.69 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432671 1 8.40
CHEMBL9387 L-365260 1 8.40
CHEMBL33412 1 8.15
CHEMBL285719 1 8.05
CHEMBL284976 1 7.96
CHEMBL282175 1 7.77
CHEMBL33398 1 7.72
CHEMBL290122 1 7.64
CHEMBL33698 1 7.58
CHEMBL284975 1 7.57
CHEMBL406844 1 7.44
CHEMBL285995 1 7.43
CHEMBL33743 1 6.87
CHEMBL287295 1 6.66
CHEMBL286835 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432671 IC50 = 4.0 nM 8.40
CHEMBL9387 L-365260 IC50 = 4.0 nM 8.40
CHEMBL33412 IC50 = 7.0 nM 8.15
CHEMBL285719 IC50 = 9.0 nM 8.05
CHEMBL284976 IC50 = 11.0 nM 7.96
CHEMBL282175 IC50 = 17.0 nM 7.77
CHEMBL33398 IC50 = 19.0 nM 7.72
CHEMBL290122 IC50 = 23.0 nM 7.64
CHEMBL33698 IC50 = 26.0 nM 7.58
CHEMBL284975 IC50 = 27.0 nM 7.57
CHEMBL406844 IC50 = 36.0 nM 7.44
CHEMBL285995 IC50 = 37.0 nM 7.43
CHEMBL33743 IC50 = 135.0 nM 6.87
CHEMBL287295 IC50 = 220.0 nM 6.66
CHEMBL286835 IC50 > 1000.0 nM -