Assay Detail
Binding
CHEMBL3129555
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BRAF V600E mutant in human HT-29 cells assessed as phosphorylation of MEK
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HT-29 |
| 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 | 7.12 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3125885 | — | — | 1 | 7.66 |
| CHEMBL3125893 | — | — | 1 | 7.62 |
| CHEMBL3125892 | — | — | 1 | 7.54 |
| CHEMBL3125891 | — | — | 1 | 7.47 |
| CHEMBL3125890 | — | — | 1 | 7.12 |
| CHEMBL3125883 | — | — | 1 | 7.12 |
| CHEMBL3125886 | — | — | 1 | 7.09 |
| CHEMBL3125884 | — | — | 1 | 6.96 |
| CHEMBL3125881 | — | — | 1 | 6.77 |
| CHEMBL3125889 | — | — | 1 | 6.50 |
| CHEMBL3125888 | — | — | 1 | 6.44 |
| CHEMBL3125887 | — | — | 1 | - |
| CHEMBL3125882 | — | — | 1 | - |
| CHEMBL3124950 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3125885 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3125893 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3125892 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3125891 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3125890 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3125883 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3125886 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL3125884 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3125881 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3125889 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3125888 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3125887 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL3125882 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL3124950 | — | IC50 | - | — | - |