Assay Detail
Binding
CHEMBL2433972
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Antagonist activity at rat recombinant TRPA1 overexpressed in HEK293 cells assessed as inhibition of allyl isothiocyanate-induced intracellular calcium influx preincubated for 5 mins followed by allyl isothiocyanate challenge by Fluo-4-AM dye-based spectrofluorimetric analysis
17
Total Activities
17
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
3-Ylidenephthalides as a new class of transient receptor potential channel TRPA1 and TRPM8 modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.21 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2430154 | — | — | 1 | 6.10 |
| CHEMBL304786 | — | — | 1 | 5.82 |
| CHEMBL67100 | — | — | 1 | 5.66 |
| CHEMBL1377580 | — | — | 1 | 5.62 |
| CHEMBL67365 | — | — | 1 | 5.54 |
| CHEMBL2430155 | — | — | 1 | 5.50 |
| CHEMBL2430153 | — | — | 1 | 5.48 |
| CHEMBL2430158 | — | — | 1 | 4.47 |
| CHEMBL2430152 | — | — | 1 | 4.44 |
| CHEMBL249592 | Z-butylidenephthalide | — | 1 | 4.35 |
| CHEMBL2430161 | — | — | 1 | 4.33 |
| CHEMBL2430162 | — | — | 1 | - |
| CHEMBL2430160 | — | — | 1 | - |
| CHEMBL2430159 | — | — | 1 | - |
| CHEMBL2430157 | — | — | 1 | - |
| CHEMBL2429871 | — | — | 1 | - |
| CHEMBL2430156 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2430154 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL304786 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL67100 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1377580 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL67365 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL2430155 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL2430153 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL2430158 | — | IC50 | = | 33950.0 | nM | 4.47 |
| CHEMBL2430152 | — | IC50 | = | 36300.0 | nM | 4.44 |
| CHEMBL249592 | Z-butylidenephthalide | IC50 | = | 44500.0 | nM | 4.35 |
| CHEMBL2430161 | — | IC50 | = | 46700.0 | nM | 4.33 |
| CHEMBL2430162 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2430160 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2430159 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2430157 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2429871 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2430156 | — | IC50 | > | 100000.0 | nM | - |