Assay Detail
Binding
CHEMBL3363074
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Antagonist activity at human TRPA1 assessed as inhibition of AITC-induced calcium uptake by [45Ca2+] fluorimetry assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
Development of novel azabenzofuran TRPA1 antagonists as in vivo tools.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.54 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1939826 | — | — | 1 | 7.58 |
| CHEMBL1939972 | — | — | 1 | 7.52 |
| CHEMBL3314489 | — | — | 1 | 6.77 |
| CHEMBL3314488 | — | — | 1 | 6.70 |
| CHEMBL3314486 | — | — | 1 | 6.52 |
| CHEMBL3314487 | — | — | 1 | 6.23 |
| CHEMBL3314485 | — | — | 1 | 6.15 |
| CHEMBL3314490 | — | — | 1 | 6.03 |
| CHEMBL3314484 | — | — | 1 | 6.01 |
| CHEMBL3314482 | — | — | 1 | 5.92 |
| CHEMBL3314491 | — | — | 1 | - |
| CHEMBL3314483 | — | — | 1 | - |
| CHEMBL3314481 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1939826 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1939972 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3314489 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3314488 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3314486 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3314487 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL3314485 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL3314490 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL3314484 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL3314482 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3314491 | — | IC50 | > | 40000000.0 | nM | - |
| CHEMBL3314483 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL3314481 | — | IC50 | > | 2000.0 | nM | - |