Assay Detail
Binding
CHEMBL5534724
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to EGFR L858R mutant (unknown origin) assessed as apparent inhibition constant in presence of ATP by TR-FRET assay
3
Total Activities
3
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
Pitfalls and Considerations in Determining the Potency and Mutant Selectivity of Covalent Epidermal Growth Factor Receptor Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 8.53 | 8.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4098072 | — | — | 1 | 8.90 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 8.35 |
| CHEMBL4558324 | LAZERTINIB | 4.0 | 1 | 8.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4098072 | — | Ki | = | 1.27 | nM | 8.90 |
| CHEMBL3353410 | OSIMERTINIB | Ki | = | 4.47 | nM | 8.35 |
| CHEMBL4558324 | LAZERTINIB | Ki | = | 4.68 | nM | 8.33 |