Assay Detail
Binding
CHEMBL4122824
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human TRPC6 expressed in HEK293 cells assessed as decrease in intracellular calcium level after 24 hrs by Fluo-4 dye-based FLIPR assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Short transient receptor potential channel 6 (CHEMBL2417347) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a bicyclo[4.3.0]nonane derivative DS88790512 as a potent, selective, and orally bioavailable blocker of transient receptor potential canonical 6 (TRPC6).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.13 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4129456 | — | — | 1 | 8.52 |
| CHEMBL4129805 | — | — | 1 | 8.10 |
| CHEMBL4129809 | — | — | 1 | 8.02 |
| CHEMBL4127600 | — | — | 1 | 7.96 |
| CHEMBL4126041 | — | — | 1 | 7.66 |
| CHEMBL4128079 | — | — | 1 | 7.52 |
| CHEMBL4128782 | — | — | 1 | 7.48 |
| CHEMBL4127190 | — | — | 1 | 7.43 |
| CHEMBL4125756 | — | — | 1 | 7.31 |
| CHEMBL4126989 | — | — | 1 | 7.28 |
| CHEMBL4130214 | — | — | 1 | 6.80 |
| CHEMBL4129002 | — | — | 1 | 6.70 |
| CHEMBL4126938 | — | — | 1 | 6.68 |
| CHEMBL4126435 | — | — | 1 | 6.55 |
| CHEMBL4126528 | — | — | 1 | 6.41 |
| CHEMBL4127992 | — | — | 1 | 6.36 |
| CHEMBL4129133 | — | — | 1 | 6.30 |
| CHEMBL4129913 | — | — | 1 | 6.25 |
| CHEMBL4125839 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4129456 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4129805 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4129809 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL4127600 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4126041 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4128079 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4128782 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4127190 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4125756 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4126989 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4130214 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4129002 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4126938 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4126435 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4126528 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4127992 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4129133 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4129913 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4125839 | — | IC50 | = | 660.0 | nM | 6.18 |