Assay Detail
Binding
CHEMBL3299554
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPV1 expressed in CHOK1 cells assessed as inhibition of capsaicin-induced calcium flux incubated 10 mins prior to capsaicin 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 | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL4794) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 |
|---|---|---|---|
| Inhibition | 6 | - | - |
| IC50 | 6 | 5.03 | 5.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3298923 | — | — | 2 | 5.29 |
| CHEMBL3299022 | — | — | 2 | 5.09 |
| CHEMBL3299024 | — | — | 2 | 4.94 |
| CHEMBL3298922 | — | — | 2 | 4.78 |
| CHEMBL3298242 | — | — | 2 | - |
| CHEMBL3299019 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3298923 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL3299022 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL3299024 | — | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL3298922 | — | IC50 | = | 16700.0 | nM | 4.78 |
| CHEMBL3298242 | — | Inhibition | = | 34.0 | % | - |
| CHEMBL3298242 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3298922 | — | Inhibition | = | 70.0 | % | - |
| CHEMBL3298923 | — | Inhibition | = | 87.0 | % | - |
| CHEMBL3299019 | — | Inhibition | = | 35.0 | % | - |
| CHEMBL3299019 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3299022 | — | Inhibition | = | 99.0 | % | - |
| CHEMBL3299024 | — | Inhibition | = | 78.0 | % | - |