Assay Detail
Functional
CHEMBL1944172
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of 5H-dibenzo[b,e]azepine-10-carboxylic acid methyl ester-induced increase in intracellular calcium by Fluo4-AM based fluorometric assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Tricyclic 3,4-dihydropyrimidine-2-thione derivatives as potent TRPA1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 6.28 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1939826 | — | — | 1 | 7.89 |
| CHEMBL1939972 | — | — | 1 | 7.30 |
| CHEMBL1939833 | — | — | 1 | 7.16 |
| CHEMBL1939828 | — | — | 1 | 7.12 |
| CHEMBL1939822 | — | — | 1 | 7.07 |
| CHEMBL1939978 | — | — | 1 | 6.89 |
| CHEMBL1939832 | — | — | 1 | 6.68 |
| CHEMBL1939836 | — | — | 1 | 6.51 |
| CHEMBL1939980 | — | — | 1 | 6.30 |
| CHEMBL1939976 | — | — | 1 | 6.19 |
| CHEMBL1939977 | — | — | 1 | 6.15 |
| CHEMBL1939984 | — | — | 1 | 6.11 |
| CHEMBL1939982 | — | — | 1 | 5.96 |
| CHEMBL1939831 | — | — | 1 | 5.82 |
| CHEMBL1939823 | — | — | 1 | 5.77 |
| CHEMBL1939990 | — | — | 1 | 5.75 |
| CHEMBL1939981 | — | — | 1 | 5.68 |
| CHEMBL1939835 | — | — | 1 | 5.56 |
| CHEMBL1939979 | — | — | 1 | 5.51 |
| CHEMBL1939825 | — | — | 1 | 5.41 |
| CHEMBL1939985 | — | — | 1 | 5.09 |
| CHEMBL1939834 | — | — | 1 | - |
| CHEMBL1939991 | — | — | 1 | - |
| CHEMBL1939830 | — | — | 1 | - |
| CHEMBL1388908 | — | — | 1 | - |
| CHEMBL1939829 | — | — | 1 | - |
| CHEMBL1086310 | — | — | 1 | - |
| CHEMBL1939827 | — | — | 1 | - |
| CHEMBL1939824 | — | — | 1 | - |
| CHEMBL1939987 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1939826 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1939972 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1939833 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1939828 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL1939822 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL1939978 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1939832 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1939836 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1939980 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1939976 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL1939977 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL1939984 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL1939982 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1939831 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1939823 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1939990 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1939981 | — | IC50 | = | 2070.0 | nM | 5.68 |
| CHEMBL1939835 | — | IC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL1939979 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL1939825 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL1939985 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL1939988 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1567258 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939983 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1364775 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939986 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939973 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939974 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939975 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939989 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1469047 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939834 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1492420 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939987 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939824 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939827 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1086310 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939829 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1388908 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939830 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1939991 | — | IC50 | > | 10000.0 | nM | - |