Assay Detail
Binding
CHEMBL4880888
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Inhibition of Protein Serine/Threonine Kinase, MAPK3 (ERK1) at 10 µM in the Eurofins-Panlabs enzyme assay (Eurofins_assay_171000)
8
Total Activities
7
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 | 7 | - | - |
| IC50 | 1 | 5.31 | 5.31 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Assay protocol publication | Assay protocol publication | - | — | PMID: 7644477/PMID: 12471242 |
| Detection method | Detection method | - | — | Quantitation of [32P]MBP |
| Incubation temperature | Incubation temperature | - | — | 37 °C |
| Incubation time | Incubation time | - | — | 30 min |
| Reference compound | Reference compound | - | — | Staurosporine |
| reference compound EC50 | reference compound EC50 | 1.6 | uM | — |
| Source of protein | Source of protein | - | — | Human recombinant E. coli |
| Substrate with concentration | Substrate with concentration | - | — | 50 µg/mL Myelin Basic Protein (MBP) |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4537788 | BAY-784 | — | 2 | 5.31 |
| CHEMBL4098877 | MLi-2 | — | 1 | - |
| CHEMBL1800685 | PPTN | — | 1 | - |
| CHEMBL2204538 | THPP-1 | — | 1 | - |
| CHEMBL1800285 | MSD-M1PAM | — | 1 | - |
| CHEMBL2048623 | — | — | 1 | - |
| CHEMBL4594444 | PECAVAPTAN | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4537788 | BAY-784 | IC50 | = | 4870.0 | nM | 5.31 |
| CHEMBL4537788 | BAY-784 | Inhibition | = | 87.0 | % | - |
| CHEMBL4098877 | MLi-2 | Inhibition | = | 33.0 | % | - |
| CHEMBL1800685 | PPTN | Inhibition | = | -5.0 | % | - |
| CHEMBL2204538 | THPP-1 | Inhibition | = | 6.0 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | -21.0 | % | - |
| CHEMBL2048623 | — | Inhibition | = | 30.0 | % | - |
| CHEMBL4594444 | PECAVAPTAN | Inhibition | = | -7.0 | % | - |