Assay Detail
Binding
CHEMBL4190120
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ERK1/2 in human A375 cells harboring BRAF V600E mutant assessed as suppression of RSK phosphorylation after 4 hrs by MSD assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Intermediate |
Target
Mitogen-activated protein kinase; ERK1/ERK2 (CHEMBL1907606) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 7.33 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4212211 | — | — | 1 | 8.46 |
| CHEMBL4210682 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4212211 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4210682 | — | IC50 | = | 630.0 | nM | 6.20 |