Assay Detail
Binding
CHEMBL5160887
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Protac activity at VHL/EGFR L858R/T790M mutant (unknown origin) assessed as inhibition of EGFR incubated for 40 mins in presence of ATP by Kinase Glo luminescence assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
von Hippel-Lindau disease tumor suppressor/EGFR (CHEMBL4523998) ↗| Type | PROTEIN-PROTEIN INTERACTION |
| Organism | Homo sapiens |
Publication
Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.41 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 8.52 |
| CHEMBL5202214 | — | — | 1 | 7.64 |
| CHEMBL5185820 | — | — | 1 | 7.42 |
| CHEMBL5202759 | — | — | 1 | 6.07 |
| CHEMBL5181560 | — | — | 1 | - |
| CHEMBL5201463 | — | — | 1 | - |
| CHEMBL5176927 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5202214 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5185820 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5202759 | — | IC50 | = | 857.0 | nM | 6.07 |
| CHEMBL5181560 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5201463 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5176927 | — | IC50 | > | 10000.0 | nM | - |