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Assay Detail

CHEMBL3398877

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

Binding
Antagonist activity against rat recombinant TRPA1 expressed in HEK293 cells assessed as inhibition of AITC-induced Ca2+ influx pre-treated 5 mins before capsaicin addition by Fluo-4 dye based assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery of non-electrophilic capsaicinoid-type TRPA1 ligands.
Del Prete D, Caprioglio D, Appendino G, Minassi A, Schiano-Moriello A, Di Marzo V, De Petrocellis L.
Bioorg Med Chem Lett (2015) 25 : 1009 -1011
PubMed 25666822 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.27 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3398239 1 6.00
CHEMBL3398238 1 5.77
CHEMBL3398241 1 5.54
CHEMBL3398240 1 4.95
CHEMBL233248 ALLYL ISOTHIOCYANATE 1.0 1 4.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3398239 IC50 = 1000.0 nM 6.00
CHEMBL3398238 IC50 = 1710.0 nM 5.77
CHEMBL3398241 IC50 = 2900.0 nM 5.54
CHEMBL3398240 IC50 = 11200.0 nM 4.95
CHEMBL233248 ALLYL ISOTHIOCYANATE IC50 = 85900.0 nM 4.07