Assay Detail
Binding
CHEMBL3299553
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at mouse TRPA1 expressed in CHO-TREX cells assessed as inhibition of cinnamaldehyde-induced calcium flux incubated 10 mins prior to cinnamaldehyde addition by FLIPR assay relative to control
12
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | CHO-TREX |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transient receptor potential cation channel subfamily A member 1 (CHEMBL1075310) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Discovery, optimization, and biological evaluation of 5-(2-(trifluoromethyl)phenyl)indazoles as a novel class of transient receptor potential A1 (TRPA1) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.88 | 7.28 |
| Inhibition | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3298923 | — | — | 2 | 7.28 |
| CHEMBL3298922 | — | — | 2 | 7.03 |
| CHEMBL3299022 | — | — | 2 | 6.98 |
| CHEMBL3299019 | — | — | 2 | 6.79 |
| CHEMBL3298242 | — | — | 2 | 6.60 |
| CHEMBL3299024 | — | — | 2 | 6.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3298923 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3298922 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL3299022 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL3299019 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL3298242 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL3299024 | — | IC50 | = | 254.0 | nM | 6.59 |
| CHEMBL3298242 | — | Inhibition | = | 100.0 | % | - |
| CHEMBL3298922 | — | Inhibition | = | 100.0 | % | - |
| CHEMBL3298923 | — | Inhibition | = | 100.0 | % | - |
| CHEMBL3299019 | — | Inhibition | = | 100.0 | % | - |
| CHEMBL3299022 | — | Inhibition | = | 100.0 | % | - |
| CHEMBL3299024 | — | Inhibition | = | 100.0 | % | - |