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Assay Detail

CHEMBL5167556

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

Binding
Inhibition of N-terminal Flag-GFP-TEV site-Met48 recombinant pig gastric H(+)/K(+) ATPase alpha/beta subunit in HEK293 cells by colorimetric microplate reader
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump.
Tanaka S, Morita M, Yamagishi T, Madapally HV, Hayashida K, Khandelia H, Gerle C, Shigematsu H, Oshima A, Abe K.
J Med Chem (2022) 65 : 7843 -7853
PubMed 35604136 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.25 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2079130 VONOPRAZAN 4.0 1 8.82
CHEMBL2105502 SORAPRAZAN 2.0 1 6.52
CHEMBL47529 1 5.68
CHEMBL4297583 TEGOPRAZAN 3.0 1 5.64
CHEMBL1618279 REVAPRAZAN 2.0 1 5.64
CHEMBL5208003 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2079130 VONOPRAZAN IC50 = 1.5 nM 8.82
CHEMBL2105502 SORAPRAZAN IC50 = 300.0 nM 6.52
CHEMBL47529 IC50 = 2100.0 nM 5.68
CHEMBL4297583 TEGOPRAZAN IC50 = 2300.0 nM 5.64
CHEMBL1618279 REVAPRAZAN IC50 = 2300.0 nM 5.64
CHEMBL5208003 IC50 = 6500.0 nM 5.19