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Assay Detail

CHEMBL1944174

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

Functional
Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of N-methyl-maleimide-induced current by patch clamp assay
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Tricyclic 3,4-dihydropyrimidine-2-thione derivatives as potent TRPA1 antagonists.
Gijsen HJ, Berthelot D, De Cleyn MA, Geuens I, Brône B, Mercken M.
Bioorg Med Chem Lett (2012) 22 : 797 -800
PubMed 22222037 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 2 - -
EC50 2 6.46 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1939828 2 8.00
CHEMBL1939829 2 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1939828 EC50 = 10.0 nM 8.00
CHEMBL1939829 EC50 = 12000.0 nM 4.92
CHEMBL1939828 Inhibition = 100.0 % -
CHEMBL1939829 Inhibition = 40.0 % -