Assay Detail
Binding
CHEMBL5540864
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Inhibition of ERK phosphorylation in human A-375 cells harboring class-I BRAF mutant incubated for 1 hr by HTRF analysis
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A-375 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 6.65 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5590216 | — | — | 1 | 7.38 |
| CHEMBL5594839 | — | — | 1 | 7.35 |
| CHEMBL5575362 | — | — | 1 | 7.32 |
| CHEMBL5095099 | EXARAFENIB | 2.0 | 1 | 7.21 |
| CHEMBL5570335 | — | — | 1 | 6.81 |
| CHEMBL5572440 | — | — | 1 | 6.52 |
| CHEMBL5575696 | — | — | 1 | 6.38 |
| CHEMBL5542253 | — | — | 1 | 6.18 |
| CHEMBL5563313 | — | — | 1 | 6.16 |
| CHEMBL5565399 | — | — | 1 | 6.07 |
| CHEMBL5572210 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5590216 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5594839 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5575362 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5095099 | EXARAFENIB | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL5570335 | — | EC50 | = | 154.0 | nM | 6.81 |
| CHEMBL5572440 | — | EC50 | = | 302.0 | nM | 6.52 |
| CHEMBL5575696 | — | EC50 | = | 415.0 | nM | 6.38 |
| CHEMBL5542253 | — | EC50 | = | 654.0 | nM | 6.18 |
| CHEMBL5563313 | — | EC50 | = | 699.0 | nM | 6.16 |
| CHEMBL5565399 | — | EC50 | = | 845.0 | nM | 6.07 |
| CHEMBL5572210 | — | EC50 | = | 1620.0 | nM | 5.79 |