Assay Detail
Binding
CHEMBL2345978
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His tagged B-Raf V600E mutant (unknown origin) expressed in baculovirus infected insect cells co-expressing CDC37 assessed as decrease in biotinylated-MEK protein phosphorylation by AlphaScreen assay
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
Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.05 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2337916 | — | — | 1 | 9.52 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 9.15 |
| CHEMBL2337915 | — | — | 1 | 9.00 |
| CHEMBL1808262 | — | — | 1 | 8.42 |
| CHEMBL2337910 | — | — | 1 | 8.10 |
| CHEMBL2337913 | — | — | 1 | 7.96 |
| CHEMBL2337917 | — | — | 1 | 7.89 |
| CHEMBL2331621 | — | — | 1 | 7.89 |
| CHEMBL2337914 | — | — | 1 | 7.55 |
| CHEMBL2337912 | — | — | 1 | 7.50 |
| CHEMBL2337909 | — | — | 1 | 7.40 |
| CHEMBL2337911 | — | — | 1 | 6.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2337916 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL2028663 | DABRAFENIB | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL2337915 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1808262 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL2337910 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2337913 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2337917 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2331621 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2337914 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2337912 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2337909 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2337911 | — | IC50 | = | 536.0 | nM | 6.27 |