Assay Detail
Binding
CHEMBL5554345
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 6-His tagged BRAF V600E mutant (445 to 723 residues) (unknown origin)
23
Total Activities
23
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
Identification of the Clinical Candidate <b>PF-07284890</b> (<b>ARRY-461</b>), a Highly Potent and Brain Penetrant BRAF Inhibitor for the Treatment of Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.42 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5564820 | — | — | 1 | 8.68 |
| CHEMBL5571735 | — | — | 1 | 8.44 |
| CHEMBL5573455 | — | — | 1 | 8.41 |
| CHEMBL5579698 | — | — | 1 | 7.93 |
| CHEMBL3236198 | — | — | 1 | 7.86 |
| CHEMBL5572318 | — | — | 1 | 7.84 |
| CHEMBL5572855 | — | — | 1 | 7.76 |
| CHEMBL5591583 | — | — | 1 | 7.70 |
| CHEMBL3233047 | — | — | 1 | 7.55 |
| CHEMBL5572717 | — | — | 1 | 7.43 |
| CHEMBL5564932 | — | — | 1 | 7.34 |
| CHEMBL5564615 | — | — | 1 | 7.29 |
| CHEMBL5095256 | TINLORAFENIB | 2.0 | 1 | 7.28 |
| CHEMBL3236467 | — | — | 1 | 7.26 |
| CHEMBL3236462 | — | — | 1 | 7.22 |
| CHEMBL3236466 | — | — | 1 | 7.16 |
| CHEMBL5592701 | — | — | 1 | 7.11 |
| CHEMBL3236461 | — | — | 1 | 7.06 |
| CHEMBL5570852 | — | — | 1 | 6.80 |
| CHEMBL5569261 | — | — | 1 | 6.74 |
| CHEMBL3236468 | — | — | 1 | 6.71 |
| CHEMBL5563407 | — | — | 1 | 6.60 |
| CHEMBL5572505 | — | — | 1 | 6.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5564820 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5571735 | — | IC50 | = | 3.61 | nM | 8.44 |
| CHEMBL5573455 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5579698 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL3236198 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL5572318 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL5572855 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL5591583 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3233047 | — | IC50 | = | 28.4 | nM | 7.55 |
| CHEMBL5572717 | — | IC50 | = | 36.9 | nM | 7.43 |
| CHEMBL5564932 | — | IC50 | = | 46.1 | nM | 7.34 |
| CHEMBL5564615 | — | IC50 | = | 50.81 | nM | 7.29 |
| CHEMBL5095256 | TINLORAFENIB | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3236467 | — | IC50 | = | 54.9 | nM | 7.26 |
| CHEMBL3236462 | — | IC50 | = | 60.3 | nM | 7.22 |
| CHEMBL3236466 | — | IC50 | = | 69.2 | nM | 7.16 |
| CHEMBL5592701 | — | IC50 | = | 77.4 | nM | 7.11 |
| CHEMBL3236461 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5570852 | — | IC50 | = | 156.7 | nM | 6.80 |
| CHEMBL5569261 | — | IC50 | = | 181.9 | nM | 6.74 |
| CHEMBL3236468 | — | IC50 | = | 197.3 | nM | 6.71 |
| CHEMBL5563407 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5572505 | — | IC50 | = | 255.7 | nM | 6.59 |