Assay Detail
Binding
CHEMBL3130306
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal FLAG-tagged recombinant BRAF V600E mutant (unknown origin) expressed in baculovirus system preincubated for 10 mins before substrate addition measured after 20 mins by scintillation counting
14
Total Activities
14
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 a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.79 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3125888 | — | — | 1 | 8.89 |
| CHEMBL3125890 | — | — | 1 | 8.62 |
| CHEMBL3125889 | — | — | 1 | 8.02 |
| CHEMBL3125893 | — | — | 1 | 7.92 |
| CHEMBL3125891 | — | — | 1 | 7.89 |
| CHEMBL3125887 | — | — | 1 | 7.85 |
| CHEMBL3125884 | — | — | 1 | 7.75 |
| CHEMBL3125883 | — | — | 1 | 7.75 |
| CHEMBL3125882 | — | — | 1 | 7.72 |
| CHEMBL3125881 | — | — | 1 | 7.62 |
| CHEMBL3125892 | — | — | 1 | 7.60 |
| CHEMBL3125886 | — | — | 1 | 7.58 |
| CHEMBL3125885 | — | — | 1 | 7.31 |
| CHEMBL3124950 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3125888 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3125890 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3125889 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL3125893 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3125891 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3125887 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3125884 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3125883 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3125882 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3125881 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3125892 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3125886 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3125885 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3124950 | — | IC50 | = | 290.0 | nM | 6.54 |