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Assay Detail

CHEMBL3795243

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

Binding
Inhibition of pig gastric H+/K+-ATPase in stomach ion leaky membrane vesicle assessed as reduction in monophosphate production after 30 mins by microplate reader analysis in presence of valinomycin
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Tissue Stomach
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, synthesis and biological evaluation of bisabolangelone oxime derivatives as potassium-competitive acid blockers (P-CABs).
Huang NY, Wang WB, Chen L, Luo HJ, Wang JZ, Deng WQ, Zou K.
Bioorg Med Chem Lett (2016) 26 : 2268 -2272
PubMed 27013393 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.94 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3793140 1 6.36
CHEMBL3792909 1 6.25
CHEMBL3792908 1 6.07
CHEMBL1618279 REVAPRAZAN 2.0 1 6.02
CHEMBL3793211 1 6.00
CHEMBL3793451 1 5.94
CHEMBL3792708 1 5.54
CHEMBL3793888 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3793140 IC50 = 436.52 nM 6.36
CHEMBL3792909 IC50 = 562.34 nM 6.25
CHEMBL3792908 IC50 = 851.14 nM 6.07
CHEMBL1618279 REVAPRAZAN IC50 = 950.0 nM 6.02
CHEMBL3793211 IC50 = 1000.0 nM 6.00
CHEMBL3793451 IC50 = 1148.15 nM 5.94
CHEMBL3792708 IC50 = 2884.03 nM 5.54
CHEMBL3793888 IC50 = 5011.87 nM 5.30