Assay Detail
Binding
CHEMBL5318377
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human 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 | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transient receptor potential cation channel subfamily A member 1 (CHEMBL6007) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 6.67 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5428371 | — | — | 1 | 8.40 |
| CHEMBL5428179 | — | — | 1 | 8.30 |
| CHEMBL5398163 | — | — | 1 | 7.85 |
| CHEMBL4514203 | BAY-390 | — | 1 | 7.80 |
| CHEMBL5394758 | — | — | 1 | 7.77 |
| CHEMBL5439762 | — | — | 1 | 7.70 |
| CHEMBL5419744 | — | — | 1 | 7.68 |
| CHEMBL5437183 | — | — | 3 | 7.48 |
| CHEMBL5422541 | — | — | 1 | 7.39 |
| CHEMBL5413437 | — | — | 1 | 7.37 |
| CHEMBL5419147 | — | — | 1 | 7.35 |
| CHEMBL5423752 | — | — | 1 | 7.26 |
| CHEMBL5413993 | — | — | 1 | 7.20 |
| CHEMBL5440987 | — | — | 1 | 7.00 |
| CHEMBL5394738 | — | — | 1 | 6.99 |
| CHEMBL5431800 | — | — | 1 | 6.47 |
| CHEMBL5436178 | — | — | 1 | 6.41 |
| CHEMBL5426246 | — | — | 1 | 6.37 |
| CHEMBL5397630 | — | — | 1 | 6.37 |
| CHEMBL5419942 | — | — | 1 | 6.36 |
| CHEMBL5440996 | — | — | 1 | 6.33 |
| CHEMBL5424148 | — | — | 1 | 6.14 |
| CHEMBL5408516 | — | — | 1 | 6.12 |
| CHEMBL5394183 | — | — | 1 | 6.09 |
| CHEMBL5436224 | — | — | 1 | 6.00 |
| CHEMBL5411635 | — | — | 1 | 5.92 |
| CHEMBL5419068 | — | — | 1 | 5.90 |
| CHEMBL5424431 | — | — | 1 | 5.80 |
| CHEMBL5398623 | — | — | 1 | 5.50 |
| CHEMBL5407661 | — | — | 1 | 5.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5428371 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5428179 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5398163 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4514203 | BAY-390 | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5394758 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5439762 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5419744 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5437183 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5437183 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5422541 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5413437 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5419147 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5423752 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5413993 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5440987 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5394738 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL5431800 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5436178 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL5397630 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5426246 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5419942 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5440996 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5424148 | — | IC50 | = | 722.0 | nM | 6.14 |
| CHEMBL5408516 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL5394183 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL5436224 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5411635 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5419068 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL5424431 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5398623 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5407661 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL5401746 | — | IC50 | = | 5550.0 | nM | 5.26 |
| CHEMBL5428534 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL5431088 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL5397294 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL5396560 | — | IC50 | > | 12500.0 | nM | - |
| CHEMBL5438649 | — | IC50 | > | 12500.0 | nM | - |
| CHEMBL4555711 | BAY-9897 | IC50 | > | 25000.0 | nM | - |
| CHEMBL5437183 | — | IC50 | > | 25000.0 | nM | - |