Assay Detail
Binding
CHEMBL4426453
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ERK in human A375SM cells harboring BRAF V600E mutant assessed as inhibition of RSK phosphorylation measured after 4 hrs by mesoscale electrochemiluminescent sandwich assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.56 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2408789 | — | — | 1 | 7.16 |
| CHEMBL3663084 | — | — | 1 | 7.01 |
| CHEMBL3654680 | — | — | 1 | 6.96 |
| CHEMBL3654682 | — | — | 1 | 6.89 |
| CHEMBL2408788 | — | — | 1 | 6.66 |
| CHEMBL3663099 | — | — | 1 | 6.52 |
| CHEMBL3654673 | — | — | 1 | 6.46 |
| CHEMBL3654681 | — | — | 1 | 6.44 |
| CHEMBL3654676 | — | — | 1 | 6.26 |
| CHEMBL3654729 | — | — | 1 | 6.12 |
| CHEMBL3663095 | — | — | 1 | 6.09 |
| CHEMBL3654742 | — | — | 1 | 6.09 |
| CHEMBL3654712 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2408789 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3663084 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL3654680 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3654682 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2408788 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3663099 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3654673 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3654681 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3654676 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL3654729 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3663095 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL3654742 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL3654712 | — | IC50 | > | 10000.0 | nM | - |