Assay Detail
Binding
CHEMBL2345977
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of B-Raf V600E mutant in human SK-MEL-28 cells assessed as decrease in ERK phosphorylation incubated for 1 hr by immunoassay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-MEL-28 |
| 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 | 7.58 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 8.40 |
| CHEMBL2337915 | — | — | 1 | 8.40 |
| CHEMBL2337916 | — | — | 1 | 8.15 |
| CHEMBL2337910 | — | — | 1 | 8.15 |
| CHEMBL2337917 | — | — | 1 | 7.96 |
| CHEMBL1808262 | — | — | 1 | 7.64 |
| CHEMBL2337913 | — | — | 1 | 7.58 |
| CHEMBL2337912 | — | — | 1 | 7.55 |
| CHEMBL2331621 | — | — | 1 | 7.29 |
| CHEMBL2337914 | — | — | 1 | 7.14 |
| CHEMBL2337909 | — | — | 1 | 7.11 |
| CHEMBL2337911 | — | — | 1 | 5.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2028663 | DABRAFENIB | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2337915 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2337916 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2337910 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2337917 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1808262 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2337913 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2337912 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2331621 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2337914 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2337909 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL2337911 | — | IC50 | = | 2555.0 | nM | 5.59 |