Assay Detail
Binding
CHEMBL3578335
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant BRAF V600E mutant (unknown origin) assessed as ADP formation measured for 5 hrs by pyruvate kinase/lactate dehydrogenase coupled assay in presence of ATP, MEK1, NADH
12
Total Activities
12
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
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 | 8.37 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3577114 | — | — | 1 | 9.00 |
| CHEMBL3577115 | — | — | 1 | 8.92 |
| CHEMBL3577123 | — | — | 1 | 8.70 |
| CHEMBL3577120 | — | — | 1 | 8.52 |
| CHEMBL3577116 | — | — | 1 | 8.38 |
| CHEMBL3577118 | — | — | 1 | 8.37 |
| CHEMBL3577124 | LY-3009120 | 1.0 | 1 | 8.24 |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | 8.21 |
| CHEMBL3577119 | — | — | 1 | 8.12 |
| CHEMBL3577117 | — | — | 1 | 8.11 |
| CHEMBL3577122 | — | — | 1 | 8.10 |
| CHEMBL3577121 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3577114 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3577115 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3577123 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3577120 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3577116 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3577118 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3577124 | LY-3009120 | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL1229517 | VEMURAFENIB | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL3577119 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL3577117 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL3577122 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL3577121 | — | IC50 | = | 18.0 | nM | 7.75 |