Assay Detail
Binding
CHEMBL3578340
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of KDR (unknown origin)
11
Total Activities
11
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
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| 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 | 11 | 6.91 | 9.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3577114 | — | — | 1 | 9.34 |
| CHEMBL3577115 | — | — | 1 | 8.72 |
| CHEMBL3577116 | — | — | 1 | 7.60 |
| CHEMBL3577120 | — | — | 1 | 7.48 |
| CHEMBL3577121 | — | — | 1 | 6.77 |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | 6.44 |
| CHEMBL3577122 | — | — | 1 | 6.27 |
| CHEMBL3577119 | — | — | 1 | 6.12 |
| CHEMBL3577117 | — | — | 1 | 6.12 |
| CHEMBL3577123 | — | — | 1 | 5.72 |
| CHEMBL3577124 | LY-3009120 | 1.0 | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3577114 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL3577115 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3577116 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3577120 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3577121 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1229517 | VEMURAFENIB | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3577122 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL3577119 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3577117 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3577123 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3577124 | LY-3009120 | IC50 | = | 3900.0 | nM | 5.41 |