Assay Detail
Binding
CHEMBL5260456
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R mutant (unknown origin) using TK-substrate preincubated with enzyme for 30 mins followed by substrate and ATP addition for 15 mins by HTRF 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
Addressing the Osimertinib Resistance Mutation EGFR-L858R/C797S with Reversible Aminopyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 9.50 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4650319 | MOBOCERTINIB | 4.0 | 1 | 11.00 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 10.30 |
| CHEMBL5275642 | — | — | 1 | 9.77 |
| CHEMBL5278657 | — | — | 1 | 9.17 |
| CHEMBL5269375 | — | — | 1 | 8.47 |
| CHEMBL5285308 | — | — | 1 | 8.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4650319 | MOBOCERTINIB | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL5275642 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL5278657 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL5269375 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5285308 | — | IC50 | = | 5.4 | nM | 8.27 |