Assay Detail
Functional
CHEMBL3578342
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Antiproliferative activity against human HCT116 cells after 67 hrs by resazurin assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 1 — Organism |
| 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 | 6.77 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3577114 | — | — | 1 | 7.50 |
| CHEMBL3577123 | — | — | 1 | 6.96 |
| CHEMBL3577116 | — | — | 1 | 6.89 |
| CHEMBL3577120 | — | — | 1 | 6.80 |
| CHEMBL3577115 | — | — | 1 | 6.80 |
| CHEMBL3577117 | — | — | 1 | 6.76 |
| CHEMBL3577122 | — | — | 1 | 6.72 |
| CHEMBL3577124 | LY-3009120 | 1.0 | 1 | 6.66 |
| CHEMBL3577119 | — | — | 1 | 6.55 |
| CHEMBL3577121 | — | — | 1 | 6.50 |
| CHEMBL3577118 | — | — | 1 | 6.29 |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3577114 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3577123 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3577116 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3577120 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3577115 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3577117 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL3577122 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3577124 | LY-3009120 | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3577119 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3577121 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3577118 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL1229517 | VEMURAFENIB | IC50 | > | 10000.0 | nM | - |