Assay Detail
Binding
CHEMBL3757749
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Antagonist activity at rat TRPA1 expressed in HEK293 cells assessed as inhibition of allyl isothiocyanate-induced increase 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 |
Target
Transient receptor potential cation channel subfamily A member 1 (CHEMBL5160) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
TRPA1 channels as targets for resveratrol and related stilbenoids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 5.14 | 5.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2387062 | — | — | 1 | 5.77 |
| CHEMBL2387060 | — | — | 1 | 5.66 |
| CHEMBL3753921 | — | — | 1 | 5.64 |
| CHEMBL215583 | — | — | 1 | 5.54 |
| CHEMBL296411 | TRISMETHOXYRESVERATROL | — | 1 | 5.52 |
| CHEMBL2387061 | (E)-3-STILBENOL | — | 1 | 5.47 |
| CHEMBL188181 | 3,5-O-DIMETHYLPINOSYLVIN | — | 1 | 5.47 |
| CHEMBL195624 | (E)-4-STYRYLPHENOL | — | 1 | 5.26 |
| CHEMBL186366 | PINOSYLVIN METHYL ETHER | — | 1 | 5.16 |
| CHEMBL83527 | PTEROSTILBENE | 2.0 | 1 | 5.12 |
| CHEMBL3751954 | — | — | 1 | 5.07 |
| CHEMBL3736424 | — | — | 1 | 5.00 |
| CHEMBL476678 | (E)-5-METHOXY-4'-STILBENOL | — | 1 | 5.00 |
| CHEMBL310102 | — | — | 1 | 4.97 |
| CHEMBL597744 | TRIACETYLRESVERATROL | — | 1 | 4.93 |
| CHEMBL101506 | PINOSYLVIN | — | 1 | 4.92 |
| CHEMBL2230272 | (E)-3,4'-STILBENDIOL | — | 1 | 4.78 |
| CHEMBL2387063 | — | — | 1 | 4.75 |
| CHEMBL165 | RESVERATROL | 3.0 | 1 | 4.70 |
| CHEMBL196731 | TRANS-4,4'-DIHYDROXYSTILBENE | — | 1 | 4.60 |
| CHEMBL3753259 | — | — | 1 | 4.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2387062 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2387060 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3753921 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL215583 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL296411 | TRISMETHOXYRESVERATROL | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL2387061 | (E)-3-STILBENOL | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL188181 | 3,5-O-DIMETHYLPINOSYLVIN | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL195624 | (E)-4-STYRYLPHENOL | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL186366 | PINOSYLVIN METHYL ETHER | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL83527 | PTEROSTILBENE | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL3751954 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL3736424 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL476678 | (E)-5-METHOXY-4'-STILBENOL | IC50 | = | 10100.0 | nM | 5.00 |
| CHEMBL310102 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL597744 | TRIACETYLRESVERATROL | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL101506 | PINOSYLVIN | IC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL2230272 | (E)-3,4'-STILBENDIOL | IC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL2387063 | — | IC50 | = | 17800.0 | nM | 4.75 |
| CHEMBL165 | RESVERATROL | IC50 | = | 19900.0 | nM | 4.70 |
| CHEMBL196731 | TRANS-4,4'-DIHYDROXYSTILBENE | IC50 | = | 25200.0 | nM | 4.60 |
| CHEMBL3753259 | — | IC50 | = | 29400.0 | nM | 4.53 |