Assay Detail
Binding
CHEMBL3593137
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ERK1/2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-RSK level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A-375 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Mitogen-activated protein kinase; ERK1/ERK2 (CHEMBL1907606) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.39 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3590107 | — | — | 1 | 7.70 |
| CHEMBL3590120 | — | — | 1 | 7.55 |
| CHEMBL3590121 | — | — | 1 | 7.19 |
| CHEMBL3590118 | — | — | 1 | 7.16 |
| CHEMBL3590123 | — | — | 1 | 6.92 |
| CHEMBL3590106 | ULIXERTINIB | 2.0 | 1 | 6.85 |
| CHEMBL3590124 | — | — | 1 | 6.70 |
| CHEMBL3590125 | — | — | 1 | 6.55 |
| CHEMBL3590117 | — | — | 1 | 6.40 |
| CHEMBL3590110 | — | — | 1 | 6.33 |
| CHEMBL3590122 | — | — | 1 | 6.13 |
| CHEMBL3590111 | — | — | 1 | 6.00 |
| CHEMBL3590109 | — | — | 1 | 5.96 |
| CHEMBL3590116 | — | — | 1 | 5.62 |
| CHEMBL3590114 | — | — | 1 | 5.29 |
| CHEMBL3590108 | — | — | 1 | 5.24 |
| CHEMBL3590115 | — | — | 1 | 5.00 |
| CHEMBL3590113 | — | — | 1 | - |
| CHEMBL3590119 | — | — | 1 | - |
| CHEMBL3590112 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3590107 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3590120 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3590121 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3590118 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3590123 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3590106 | ULIXERTINIB | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3590124 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3590125 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3590117 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3590110 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3590122 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL3590111 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3590109 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3590116 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3590114 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL3590108 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL3590115 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3590113 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3590119 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3590112 | — | IC50 | > | 30000.0 | nM | - |