Assay Detail
Binding
CHEMBL5540230
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Inhibition of PKCalpha (unknown origin) incubated for 15 mins in presence of 33P-ATP by Topcount scintillation counting method
21
Total Activities
21
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 |
Publication
Discovery of Darovasertib (NVP-LXS196), a Pan-PKC Inhibitor for the Treatment of Metastatic Uveal Melanoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.77 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3946659 | — | — | 1 | 9.70 |
| CHEMBL3957149 | — | — | 1 | 9.70 |
| CHEMBL5592487 | — | — | 1 | 9.70 |
| CHEMBL3965722 | — | — | 1 | 9.52 |
| CHEMBL3950697 | — | — | 1 | 9.52 |
| CHEMBL5566264 | — | — | 1 | 9.40 |
| CHEMBL565612 | SOTRASTAURIN | 2.0 | 1 | 9.10 |
| CHEMBL3924825 | — | — | 1 | 9.08 |
| CHEMBL3890986 | — | — | 1 | 8.70 |
| CHEMBL3982723 | DAROVASERTIB | 2.0 | 1 | 8.52 |
| CHEMBL3915489 | — | — | 1 | 8.52 |
| CHEMBL5564760 | — | — | 1 | 8.00 |
| CHEMBL5565713 | — | — | 1 | 7.96 |
| CHEMBL5571382 | — | — | 1 | 7.37 |
| CHEMBL5591535 | — | — | 1 | 6.75 |
| CHEMBL3943147 | — | — | 1 | - |
| CHEMBL3966643 | — | — | 1 | - |
| CHEMBL3982497 | — | — | 1 | - |
| CHEMBL3957715 | — | — | 1 | - |
| CHEMBL3966595 | — | — | 1 | - |
| CHEMBL5573642 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3946659 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3957149 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5592487 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3965722 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3950697 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5566264 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL565612 | SOTRASTAURIN | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3924825 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL3890986 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3982723 | DAROVASERTIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3915489 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5564760 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5565713 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5571382 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5591535 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3943147 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL3966643 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL3982497 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL3957715 | — | IC50 | < | 0.1 | nM | - |
| CHEMBL3966595 | — | IC50 | < | 0.13 | nM | - |
| CHEMBL5573642 | — | IC50 | < | 0.1 | nM | - |