Assay Detail
Binding
CHEMBL3578339
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 6.73 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3577123 | — | — | 1 | 7.80 |
| CHEMBL3577120 | — | — | 1 | 7.34 |
| CHEMBL3577119 | — | — | 1 | 7.32 |
| CHEMBL3577114 | — | — | 1 | 7.24 |
| CHEMBL3577115 | — | — | 1 | 7.04 |
| CHEMBL3577116 | — | — | 1 | 6.92 |
| CHEMBL3577121 | — | — | 1 | 6.92 |
| CHEMBL3577124 | LY-3009120 | 1.0 | 1 | 6.82 |
| CHEMBL3577117 | — | — | 1 | 6.80 |
| CHEMBL3577118 | — | — | 1 | 6.57 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 5.23 |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | 4.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3577123 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3577120 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3577119 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3577114 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3577115 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL3577116 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3577121 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3577124 | LY-3009120 | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3577117 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3577118 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2028663 | DABRAFENIB | IC50 | = | 5880.0 | nM | 5.23 |
| CHEMBL1229517 | VEMURAFENIB | IC50 | = | 16600.0 | nM | 4.78 |