Assay Detail
ADMET
CHEMBL3790960
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | A549 |
| 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 | 19 | 6.86 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3787662 | — | — | 1 | 9.10 |
| CHEMBL3786962 | — | — | 1 | 8.80 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 8.22 |
| CHEMBL3786453 | — | — | 1 | 8.12 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.96 |
| CHEMBL3787386 | — | — | 1 | 7.82 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.82 |
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 5.80 |
| CHEMBL3786802 | — | — | 1 | 5.46 |
| CHEMBL3787220 | — | — | 1 | 5.38 |
| CHEMBL3786812 | — | — | 1 | 5.38 |
| CHEMBL3786098 | PF-06459988 | 2.0 | 1 | 5.29 |
| CHEMBL3786523 | — | — | 1 | 5.04 |
| CHEMBL3786220 | — | — | 1 | - |
| CHEMBL3786647 | — | — | 1 | - |
| CHEMBL3787132 | — | — | 1 | - |
| CHEMBL3786858 | — | — | 1 | - |
| CHEMBL3785393 | — | — | 1 | - |
| CHEMBL3787327 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3787662 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL3786962 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL31965 | CANERTINIB | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3786453 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3787386 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3545308 | ROCILETINIB | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3786802 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3787220 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL3786812 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL3786098 | PF-06459988 | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL3786523 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL3786220 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3786647 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3787132 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3786858 | — | IC50 | > | 3300.0 | nM | - |
| CHEMBL3785393 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3787327 | — | IC50 | - | — | - |