Assay Detail
ADMET
CHEMBL4830970
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type EGFR (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate incubated for 1 hr by TR-FRET assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A sulfonyl fluoride derivative inhibits EGFR<sup>L858R/T790M/C797S</sup> by covalent modification of the catalytic lysine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.21 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 9.49 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 8.47 |
| CHEMBL4866162 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4866162 | — | IC50 | = | 210.0 | nM | 6.68 |