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Assay Detail

CHEMBL4835359

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Binding
Inhibition of mouse TRPM1 expressed in HEK293T cells assessed as blocked of capsaicin-activated current at 10 uM by whole cell patch clamp electrophysiology relative to control
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.
Zhang H, Yu P, Lin H, Jin Z, Zhao S, Zhang Y, Xu Q, Jin H, Liu Z, Yang W, Zhang L.
J Med Chem (2021) 64 : 3976 -3996
PubMed 33784097 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 2 - -
IC50 1 8.22 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122413 1 8.22
CHEMBL4863549 1 -
CHEMBL4863360 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122413 IC50 = 6.0 nM 8.22
CHEMBL4863549 Inhibition = 12.7 % -
CHEMBL4863360 Inhibition = 5.4 % -