Assay Detail
Functional
CHEMBL1944173
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at rat TRPA1 expressed in HEK293 cells assessed as inhibition of BITC-induced increase in intracellular calcium concentration by Fluo4-AM based fluorometric assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| 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
Tricyclic 3,4-dihydropyrimidine-2-thione derivatives as potent TRPA1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.55 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1939822 | — | — | 1 | 8.52 |
| CHEMBL1939826 | — | — | 1 | 8.40 |
| CHEMBL1939833 | — | — | 1 | 8.00 |
| CHEMBL1939972 | — | — | 1 | 7.96 |
| CHEMBL1939828 | — | — | 1 | 7.92 |
| CHEMBL1939978 | — | — | 1 | 7.70 |
| CHEMBL1939977 | — | — | 1 | 7.36 |
| CHEMBL1939832 | — | — | 1 | 7.33 |
| CHEMBL1939836 | — | — | 1 | 7.16 |
| CHEMBL1939980 | — | — | 1 | 7.15 |
| CHEMBL1939831 | — | — | 1 | 6.80 |
| CHEMBL1939976 | — | — | 1 | 6.64 |
| CHEMBL1939984 | — | — | 1 | 6.51 |
| CHEMBL1939982 | — | — | 1 | 6.41 |
| CHEMBL1939823 | — | — | 1 | 6.30 |
| CHEMBL1939835 | — | — | 1 | 6.10 |
| CHEMBL1939824 | — | — | 1 | 6.01 |
| CHEMBL1939990 | — | — | 1 | 5.72 |
| CHEMBL1939974 | — | — | 1 | 5.57 |
| CHEMBL1939981 | — | — | 1 | 5.47 |
| CHEMBL1939979 | — | — | 1 | 5.46 |
| CHEMBL1939825 | — | — | 1 | 5.33 |
| CHEMBL1086310 | — | — | 1 | 5.25 |
| CHEMBL1939834 | — | — | 1 | 5.05 |
| CHEMBL1939983 | — | — | 1 | 5.03 |
| CHEMBL1939991 | — | — | 1 | 5.02 |
| CHEMBL1939829 | — | — | 1 | - |
| CHEMBL1939830 | — | — | 1 | - |
| CHEMBL1939975 | — | — | 1 | - |
| CHEMBL1939827 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1939822 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1939826 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1939833 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1939972 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1939828 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1939978 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1939977 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL1939832 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL1939836 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1939980 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL1939831 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1939976 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1939984 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1939982 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL1939823 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1939835 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL1939824 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL1939990 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1939974 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1939981 | — | IC50 | = | 3390.0 | nM | 5.47 |
| CHEMBL1939979 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL1939825 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL1086310 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL1939834 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL1939983 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL1939991 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL1939829 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939830 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939975 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939827 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939973 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939985 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1567258 | — | IC50 | > | 10000.0 | nM | - |