Assay Detail
Binding
CHEMBL5318375
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat TRPA1 channel expressed in CHO-K1 cells tagged with GCaMP6 by measuring calcium flux measured after 10 mins by FLIPR tetra analysis
39
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO-K1 |
| 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
Discovery of <b>BAY-390</b>, a Selective CNS Penetrant Chemical Probe as Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 5.79 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5428371 | — | — | 1 | 7.62 |
| CHEMBL4514203 | BAY-390 | — | 1 | 7.20 |
| CHEMBL5394758 | — | — | 1 | 6.93 |
| CHEMBL5439762 | — | — | 1 | 6.92 |
| CHEMBL5428179 | — | — | 1 | 6.89 |
| CHEMBL5419744 | — | — | 1 | 6.70 |
| CHEMBL5413437 | — | — | 1 | 6.21 |
| CHEMBL5422541 | — | — | 1 | 6.19 |
| CHEMBL5423752 | — | — | 1 | 6.17 |
| CHEMBL5437183 | — | — | 3 | 6.07 |
| CHEMBL5413993 | — | — | 1 | 6.02 |
| CHEMBL5440996 | — | — | 1 | 5.92 |
| CHEMBL5394738 | — | — | 1 | 5.89 |
| CHEMBL5398163 | — | — | 1 | 5.86 |
| CHEMBL5426246 | — | — | 1 | 5.64 |
| CHEMBL5440987 | — | — | 1 | 5.62 |
| CHEMBL5408516 | — | — | 1 | 5.42 |
| CHEMBL5411635 | — | — | 1 | 5.42 |
| CHEMBL5424148 | — | — | 1 | 5.28 |
| CHEMBL5419942 | — | — | 1 | 5.20 |
| CHEMBL5436178 | — | — | 1 | 5.12 |
| CHEMBL5419147 | — | — | 1 | 5.00 |
| CHEMBL5431800 | — | — | 1 | 4.94 |
| CHEMBL5401746 | — | — | 1 | 4.89 |
| CHEMBL5407661 | — | — | 1 | 4.82 |
| CHEMBL5398623 | — | — | 1 | 4.80 |
| CHEMBL5397630 | — | — | 1 | 4.68 |
| CHEMBL5431088 | — | — | 1 | 4.60 |
| CHEMBL5436224 | — | — | 1 | - |
| CHEMBL5397294 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5428371 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4514203 | BAY-390 | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5394758 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL5439762 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5428179 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5419744 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5413437 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL5422541 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5423752 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL5437183 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL5413993 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL5440996 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5394738 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5398163 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL5437183 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL5426246 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5440987 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5408516 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL5411635 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL5424148 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL5419942 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL5436178 | — | IC50 | = | 7570.0 | nM | 5.12 |
| CHEMBL5419147 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5431800 | — | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL5401746 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL5407661 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL5398623 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL5397630 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL5431088 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL5437183 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5394183 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5428534 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4555711 | BAY-9897 | IC50 | > | 25000.0 | nM | - |
| CHEMBL5419068 | — | IC50 | > | 12500.0 | nM | - |
| CHEMBL5438649 | — | IC50 | > | 12500.0 | nM | - |
| CHEMBL5436224 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5396560 | — | IC50 | > | 12500.0 | nM | - |
| CHEMBL5397294 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5424431 | — | IC50 | > | 25000.0 | nM | - |