Assay Detail
Binding
CHEMBL4050074
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild-type BRAF (unknown origin) using human His6-tagged MEK1 K97R mutant as substrate pretreated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter binding method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase B-raf (CHEMBL5145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and evaluation of derivatives based on pyrimidine scaffold as potent Pan-Raf inhibitors to overcome resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.54 | 8.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | 8.16 |
| CHEMBL4080362 | — | — | 1 | 7.98 |
| CHEMBL4066939 | — | — | 1 | 7.85 |
| CHEMBL4060057 | — | — | 1 | 7.76 |
| CHEMBL4104590 | — | — | 1 | 7.67 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.65 |
| CHEMBL4075036 | — | — | 1 | 7.53 |
| CHEMBL4087837 | — | — | 1 | 7.47 |
| CHEMBL4085294 | — | — | 1 | 7.40 |
| CHEMBL4082425 | — | — | 1 | 7.28 |
| CHEMBL4060531 | — | — | 1 | 7.22 |
| CHEMBL4101882 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1229517 | VEMURAFENIB | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4080362 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL4066939 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL4060057 | — | IC50 | = | 17.2 | nM | 7.76 |
| CHEMBL4104590 | — | IC50 | = | 21.2 | nM | 7.67 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL4075036 | — | IC50 | = | 29.7 | nM | 7.53 |
| CHEMBL4087837 | — | IC50 | = | 33.8 | nM | 7.47 |
| CHEMBL4085294 | — | IC50 | = | 39.8 | nM | 7.40 |
| CHEMBL4082425 | — | IC50 | = | 52.1 | nM | 7.28 |
| CHEMBL4060531 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4101882 | — | IC50 | = | 287.0 | nM | 6.54 |