Assay Detail
Binding
CHEMBL5534726
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to EGFR L858R/T790M double mutant (unknown origin) assessed as apparent inhibition constant in presence of ATP by TR-FRET assay
6
Total Activities
6
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 | 6 | 7.43 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 8.35 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 8.15 |
| CHEMBL4558324 | LAZERTINIB | 4.0 | 1 | 7.47 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 7.34 |
| CHEMBL4098072 | — | — | 1 | 6.65 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL180022 | NERATINIB | Ki | = | 4.51 | nM | 8.35 |
| CHEMBL31965 | CANERTINIB | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL4558324 | LAZERTINIB | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL1173655 | AFATINIB | Ki | = | 45.3 | nM | 7.34 |
| CHEMBL4098072 | — | Ki | = | 224.0 | nM | 6.65 |
| CHEMBL3353410 | OSIMERTINIB | Ki | = | 256.0 | nM | 6.59 |