Assay Detail
Binding
CHEMBL3790965
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PC-9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.29 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.96 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 7.25 |
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 7.10 |
| CHEMBL3786098 | PF-06459988 | 2.0 | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3545308 | ROCILETINIB | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3786098 | PF-06459988 | IC50 | = | 140.0 | nM | 6.85 |