Assay Detail
Binding
CHEMBL3578338
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A-375 |
| 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 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.36 | 8.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3577114 | — | — | 1 | 8.17 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 7.96 |
| CHEMBL3577117 | — | — | 1 | 7.66 |
| CHEMBL3577123 | — | — | 1 | 7.57 |
| CHEMBL3577124 | LY-3009120 | 1.0 | 1 | 7.43 |
| CHEMBL3577116 | — | — | 1 | 7.40 |
| CHEMBL3577121 | — | — | 1 | 7.33 |
| CHEMBL3577120 | — | — | 1 | 7.09 |
| CHEMBL3577115 | — | — | 1 | 7.02 |
| CHEMBL3577119 | — | — | 1 | 6.96 |
| CHEMBL3577118 | — | — | 1 | 6.85 |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3577114 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL2028663 | DABRAFENIB | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3577117 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3577123 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3577124 | LY-3009120 | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3577116 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3577121 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3577120 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3577115 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL3577119 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3577118 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1229517 | VEMURAFENIB | IC50 | = | 150.0 | nM | 6.82 |