Assay Detail
Binding
CHEMBL4331432
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GST-tagged BRAF V600E mutant (416 to 766 residues) using human full length 6His-tagged MEK1 (K97R) as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by filter binding method
18
Total Activities
18
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
Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.08 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4438001 | — | — | 1 | 9.70 |
| CHEMBL4545914 | — | — | 1 | 8.92 |
| CHEMBL4559599 | — | — | 1 | 8.68 |
| CHEMBL4518581 | — | — | 1 | 8.64 |
| CHEMBL4438236 | — | — | 1 | 8.46 |
| CHEMBL3577124 | LY-3009120 | 1.0 | 1 | 8.26 |
| CHEMBL4457131 | — | — | 1 | 8.21 |
| CHEMBL4439157 | — | — | 1 | 8.13 |
| CHEMBL4471370 | — | — | 1 | 7.91 |
| CHEMBL4555839 | — | — | 1 | 7.87 |
| CHEMBL4436132 | — | — | 1 | 7.87 |
| CHEMBL4586402 | — | — | 1 | 7.80 |
| CHEMBL4588013 | — | — | 1 | 7.77 |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | 7.50 |
| CHEMBL4538140 | — | — | 1 | 7.47 |
| CHEMBL4473290 | — | — | 1 | 7.46 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.42 |
| CHEMBL4518466 | — | — | 1 | 7.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4438001 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4545914 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4559599 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4518581 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4438236 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3577124 | LY-3009120 | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4457131 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL4439157 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4471370 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL4555839 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL4436132 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL4586402 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL4588013 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1229517 | VEMURAFENIB | IC50 | = | 31.6 | nM | 7.50 |
| CHEMBL4538140 | — | IC50 | = | 34.1 | nM | 7.47 |
| CHEMBL4473290 | — | IC50 | = | 34.5 | nM | 7.46 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 38.1 | nM | 7.42 |
| CHEMBL4518466 | — | IC50 | = | 43.7 | nM | 7.36 |