Assay Detail
Binding
CHEMBL5166090
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Inhibition of ERK5 phosphorylation in human HeLa cells incubated for 1 hr by Western blot densitometry analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.04 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5197199 | — | — | 1 | 7.70 |
| CHEMBL5186248 | — | — | 1 | 7.51 |
| CHEMBL5173346 | — | — | 1 | 7.37 |
| CHEMBL5175760 | — | — | 1 | 7.24 |
| CHEMBL5172952 | — | — | 1 | 7.22 |
| CHEMBL5188920 | — | — | 1 | 7.16 |
| CHEMBL5193786 | — | — | 1 | 6.85 |
| CHEMBL5198962 | — | — | 1 | 6.17 |
| CHEMBL5180089 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5197199 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5186248 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5173346 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5175760 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5172952 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5188920 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5193786 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL5198962 | — | IC50 | = | 671.0 | nM | 6.17 |
| CHEMBL5180089 | — | IC50 | = | 787.0 | nM | 6.10 |