Assay Detail
Binding
CHEMBL4715073
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CRAF Y340D/Y341D mutant (unknown origin) assessed as using inactive phosphorylated MAP2K1 substrate preincubated for 30 mins measured after 90 mins by DELFIA assay
8
Total Activities
8
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
RAF proto-oncogene serine/threonine-protein kinase (CHEMBL1906) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 10.19 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4776565 | — | — | 1 | 10.22 |
| CHEMBL4780060 | — | — | 1 | 10.21 |
| CHEMBL3577124 | LY-3009120 | 1.0 | 1 | 10.21 |
| CHEMBL4778419 | — | — | 1 | 10.21 |
| CHEMBL4740241 | — | — | 1 | 10.09 |
| CHEMBL4775998 | — | — | 1 | - |
| CHEMBL4778772 | — | — | 1 | - |
| CHEMBL4758903 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4776565 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL4780060 | — | Ki | = | 0.061 | nM | 10.21 |
| CHEMBL3577124 | LY-3009120 | Ki | = | 0.061 | nM | 10.21 |
| CHEMBL4778419 | — | Ki | = | 0.062 | nM | 10.21 |
| CHEMBL4740241 | — | Ki | = | 0.081 | nM | 10.09 |
| CHEMBL4775998 | — | Ki | < | 0.05 | nM | - |
| CHEMBL4778772 | — | Ki | < | 0.05 | nM | - |
| CHEMBL4758903 | — | Ki | < | 0.05 | nM | - |