Assay Detail
Binding
CHEMBL3240202
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of B-Raf V600E mutant in human Malme-3M cells assessed as basal ERK phosphorylation
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Malme-3M |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase B-raf (CHEMBL5145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.08 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3236471 | — | — | 1 | 8.52 |
| CHEMBL3236464 | — | — | 1 | 8.22 |
| CHEMBL3236472 | — | — | 1 | 8.15 |
| CHEMBL3236470 | — | — | 1 | 7.82 |
| CHEMBL3236463 | — | — | 1 | 7.80 |
| CHEMBL3236459 | — | — | 1 | 7.75 |
| CHEMBL3236198 | — | — | 1 | 7.58 |
| CHEMBL2144069 | — | — | 1 | 7.57 |
| CHEMBL3236193 | — | — | 1 | 7.36 |
| CHEMBL3236461 | — | — | 1 | 7.26 |
| CHEMBL3236466 | — | — | 1 | 7.21 |
| CHEMBL3233047 | — | — | 1 | 7.08 |
| CHEMBL3236468 | — | — | 1 | 6.96 |
| CHEMBL3236462 | — | — | 1 | 6.94 |
| CHEMBL3236467 | — | — | 1 | 6.94 |
| CHEMBL3236192 | — | — | 1 | 6.93 |
| CHEMBL3236196 | — | — | 1 | 6.88 |
| CHEMBL3236460 | — | — | 1 | 6.24 |
| CHEMBL3236469 | — | — | 1 | 6.22 |
| CHEMBL3236195 | — | — | 1 | 6.13 |
| CHEMBL3236194 | — | — | 1 | 6.09 |
| CHEMBL3236197 | — | — | 1 | 6.06 |
| CHEMBL3236191 | — | — | 1 | 5.20 |
| CHEMBL3236465 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3236471 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3236464 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3236472 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3236470 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3236463 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3236459 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3236198 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2144069 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3236193 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3236461 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3236466 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3233047 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL3236468 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3236462 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL3236467 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL3236192 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL3236196 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL3236460 | — | IC50 | = | 581.0 | nM | 6.24 |
| CHEMBL3236469 | — | IC50 | = | 603.0 | nM | 6.22 |
| CHEMBL3236195 | — | IC50 | = | 733.0 | nM | 6.13 |
| CHEMBL3236194 | — | IC50 | = | 814.0 | nM | 6.09 |
| CHEMBL3236197 | — | IC50 | = | 878.0 | nM | 6.06 |
| CHEMBL3236191 | — | IC50 | = | 6251.0 | nM | 5.20 |
| CHEMBL3236465 | — | IC50 | - | — | - |