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Assay Detail

CHEMBL3757750

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Binding
Agonist activity at rat TRPA1 expressed in HEK293 cells assessed as induction of intracellular calcium level
21
Total Activities
21
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

TRPA1 channels as targets for resveratrol and related stilbenoids.
Nalli M, Ortar G, Moriello AS, Morera E, Di Marzo V, De Petrocellis L.
Bioorg Med Chem Lett (2016) 26 : 899 -902
PubMed 26750258 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 5.43 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2387060 1 6.24
CHEMBL2387062 1 6.06
CHEMBL215583 1 5.82
CHEMBL3753921 1 5.77
CHEMBL296411 TRISMETHOXYRESVERATROL 1 5.77
CHEMBL188181 3,5-O-DIMETHYLPINOSYLVIN 1 5.77
CHEMBL2387061 (E)-3-STILBENOL 1 5.75
CHEMBL2387063 1 5.62
CHEMBL186366 PINOSYLVIN METHYL ETHER 1 5.46
CHEMBL83527 PTEROSTILBENE 2.0 1 5.44
CHEMBL310102 1 5.38
CHEMBL476678 (E)-5-METHOXY-4'-STILBENOL 1 5.18
CHEMBL3751954 1 5.14
CHEMBL597744 TRIACETYLRESVERATROL 1 5.12
CHEMBL195624 (E)-4-STYRYLPHENOL 1 5.08
CHEMBL3736424 1 5.00
CHEMBL196731 TRANS-4,4'-DIHYDROXYSTILBENE 1 4.96
CHEMBL2230272 (E)-3,4'-STILBENDIOL 1 4.87
CHEMBL3753259 1 4.79
CHEMBL165 RESVERATROL 3.0 1 -
CHEMBL101506 PINOSYLVIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2387060 EC50 = 580.0 nM 6.24
CHEMBL2387062 EC50 = 880.0 nM 6.06
CHEMBL215583 EC50 = 1500.0 nM 5.82
CHEMBL3753921 EC50 = 1700.0 nM 5.77
CHEMBL296411 TRISMETHOXYRESVERATROL EC50 = 1700.0 nM 5.77
CHEMBL188181 3,5-O-DIMETHYLPINOSYLVIN EC50 = 1700.0 nM 5.77
CHEMBL2387061 (E)-3-STILBENOL EC50 = 1800.0 nM 5.75
CHEMBL2387063 EC50 = 2400.0 nM 5.62
CHEMBL186366 PINOSYLVIN METHYL ETHER EC50 = 3500.0 nM 5.46
CHEMBL83527 PTEROSTILBENE EC50 = 3600.0 nM 5.44
CHEMBL310102 EC50 = 4200.0 nM 5.38
CHEMBL476678 (E)-5-METHOXY-4'-STILBENOL EC50 = 6600.0 nM 5.18
CHEMBL3751954 EC50 = 7200.0 nM 5.14
CHEMBL597744 TRIACETYLRESVERATROL EC50 = 7500.0 nM 5.12
CHEMBL195624 (E)-4-STYRYLPHENOL EC50 = 8400.0 nM 5.08
CHEMBL3736424 EC50 = 10100.0 nM 5.00
CHEMBL196731 TRANS-4,4'-DIHYDROXYSTILBENE EC50 = 11000.0 nM 4.96
CHEMBL2230272 (E)-3,4'-STILBENDIOL EC50 = 13500.0 nM 4.87
CHEMBL3753259 EC50 = 16300.0 nM 4.79
CHEMBL165 RESVERATROL EC50 - -
CHEMBL101506 PINOSYLVIN EC50 - -