Assay Detail
Binding
CHEMBL4883005
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Inhibition of Protein Serine/Threonine Kinase, PRKCA (PKCα) at 10 µM in the Eurofins-Panlabs enzyme assay (Eurofins_assay_180010)
12
Total Activities
3
Compounds Tested
2
Activity Types
8
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Profiling data from Eurofins-Panlabs
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 10 | - | - |
| IC50 | 2 | 4.04 | 4.04 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Assay protocol publication | Assay protocol publication | - | — | PMID: 3457562 |
| Detection method | Detection method | - | — | Quantitation of [32]PHistone H1 |
| Incubation temperature | Incubation temperature | - | — | 25 °C |
| Incubation time | Incubation time | - | — | 10 min |
| Reference compound | Reference compound | - | — | Staurosporine |
| reference compound EC50 | reference compound EC50 | 0.0017 | uM | — |
| Source of protein | Source of protein | - | — | Human recombinant insect Sf21 cells |
| Substrate with concentration | Substrate with concentration | - | — | Histone |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1800285 | MSD-M1PAM | — | 10 | 4.04 |
| CHEMBL1800685 | PPTN | — | 1 | - |
| CHEMBL4594444 | PECAVAPTAN | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1800285 | MSD-M1PAM | IC50 | = | 91500.0 | nM | 4.04 |
| CHEMBL1800285 | MSD-M1PAM | IC50 | = | 91500.0 | nM | 4.04 |
| CHEMBL1800685 | PPTN | Inhibition | = | 29.0 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | 52.0 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | 11.0 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | -3.0 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | -9.0 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | 52.0 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | 11.0 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | -3.0 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | -9.0 | % | - |
| CHEMBL4594444 | PECAVAPTAN | Inhibition | = | -2.0 | % | - |