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Assay Detail

CHEMBL1259377

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Functional
Agonist activity at human TRPA1 expressed in T-REx-HEK293 cells assessed as time point of maximal current amplitude by patch-clamp electrophysiology
4
Total Activities
4
Compounds Tested
1
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

Analogues of morphanthridine and the tear gas dibenz[b,f][1,4]oxazepine (CR) as extremely potent activators of the human transient receptor potential ankyrin 1 (TRPA1) channel.
Gijsen HJ, Berthelot D, Zaja M, Brône B, Geuens I, Mercken M.
J Med Chem (2010) 53 : 7011 -7020
PubMed 20806939 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.67 8.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1085102 1 8.36
CHEMBL1084637 1 8.13
CHEMBL233248 ALLYL ISOTHIOCYANATE 1.0 1 5.24
CHEMBL55285 BENZYL ISOTHIOCYANATE 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1085102 EC50 = 4.365 nM 8.36
CHEMBL1084637 EC50 = 7.413 nM 8.13
CHEMBL233248 ALLYL ISOTHIOCYANATE EC50 = 5754.4 nM 5.24
CHEMBL55285 BENZYL ISOTHIOCYANATE EC50 = 10964.78 nM 4.96