Assay Detail
Binding
CHEMBL4012725
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CRAF Y340E/Y341E mutant (unknown origin) using human MEK1 K97R mutant as substrate pretreated for 30 mins followed by substrate addition measured after 40 mins by alphascreen assay
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
RAF proto-oncogene serine/threonine-protein kinase (CHEMBL1906) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 9.33 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3956654 | — | — | 1 | 10.00 |
| CHEMBL3912148 | — | — | 1 | 9.70 |
| CHEMBL3945337 | — | — | 1 | 9.52 |
| CHEMBL3936445 | — | — | 1 | 9.40 |
| CHEMBL3978705 | — | — | 1 | 9.40 |
| CHEMBL4081025 | — | — | 1 | 9.30 |
| CHEMBL3984244 | — | — | 1 | 9.30 |
| CHEMBL3962812 | — | — | 1 | 9.30 |
| CHEMBL3902816 | — | — | 1 | 9.22 |
| CHEMBL3986273 | — | — | 1 | 9.10 |
| CHEMBL4062317 | — | — | 1 | 9.00 |
| CHEMBL4105276 | — | — | 1 | 8.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3956654 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3912148 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3945337 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3936445 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3978705 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4081025 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3984244 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3962812 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3902816 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3986273 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4062317 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4105276 | — | IC50 | = | 2.0 | nM | 8.70 |