Assay Detail
Binding
CHEMBL3636899
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 phosphorylation of ERK
11
Total Activities
11
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 RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.70 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3632721 | — | — | 1 | 7.38 |
| CHEMBL3335371 | — | — | 1 | 7.36 |
| CHEMBL3632719 | — | — | 1 | 6.92 |
| CHEMBL3632720 | — | — | 1 | 6.89 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 6.85 |
| CHEMBL3632723 | — | — | 1 | 6.68 |
| CHEMBL470808 | — | — | 1 | 6.55 |
| CHEMBL3632717 | — | — | 1 | 6.41 |
| CHEMBL3632718 | — | — | 1 | 6.32 |
| CHEMBL3632724 | — | — | 1 | 6.21 |
| CHEMBL3632722 | — | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3632721 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3335371 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3632719 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3632720 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL558752 | RAF-265 | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3632723 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL470808 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3632717 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3632718 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3632724 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL3632722 | — | IC50 | = | 780.0 | nM | 6.11 |