Assay Detail
Binding
CHEMBL5115840
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R/T790M mutant (unknown origin) incubated for 35 mins by HTRF KinEASE-TK 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 |
Publication
Design and synthesis of proteolysis targeting chimeras (PROTACs) as an EGFR degrader based on CO-1686.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.29 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 8.38 |
| CHEMBL5201794 | — | — | 1 | 7.69 |
| CHEMBL5206775 | — | — | 1 | 7.62 |
| CHEMBL5196498 | — | — | 1 | 7.48 |
| CHEMBL5175891 | — | — | 1 | 7.37 |
| CHEMBL5200495 | — | — | 1 | 6.92 |
| CHEMBL5204954 | — | — | 1 | 6.87 |
| CHEMBL5179538 | — | — | 1 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545308 | ROCILETINIB | IC50 | = | 4.19 | nM | 8.38 |
| CHEMBL5201794 | — | IC50 | = | 20.33 | nM | 7.69 |
| CHEMBL5206775 | — | IC50 | = | 24.12 | nM | 7.62 |
| CHEMBL5196498 | — | IC50 | = | 33.03 | nM | 7.48 |
| CHEMBL5175891 | — | IC50 | = | 43.12 | nM | 7.37 |
| CHEMBL5200495 | — | IC50 | = | 121.3 | nM | 6.92 |
| CHEMBL5204954 | — | IC50 | = | 133.7 | nM | 6.87 |
| CHEMBL5179538 | — | IC50 | = | 965.3 | nM | 6.01 |