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Assay Detail

CHEMBL4134894

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Binding
Inhibition of human FLAG-tagged TRPM2 expressed in HEK293 cells assessed as reduction in H2O2-induced intracellular calcium flux pretreated for 30 secs followed by H2O2 addition measured for 120 secs by Fluo4-AM dye based fluorescence assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Scalaradial Is a Potent Inhibitor of Transient Receptor Potential Melastatin 2 (TRPM2) Ion Channels.
Starkus JG, Poerzgen P, Layugan K, Kawabata KG, Goto JI, Suzuki S, Myers G, Kelly M, Penner R, Fleig A, Horgen FD.
J Nat Prod (2017) 80 : 2741 -2750
PubMed 29019677 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.91 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4161122 1 7.60
CHEMBL127336 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4161122 IC50 = 25.0 nM 7.60
CHEMBL127336 IC50 = 600.0 nM 6.22