Assay Detail
Binding
CHEMBL4416111
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged human EGFR D770_N771insNPG mutant using poly(Glu, Tyr) 4:1 substrate incubated for 120 mins by kinase-Glo plus luminescent kinase 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
Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 9.06 | 9.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4521381 | — | — | 1 | 9.88 |
| CHEMBL3545154 | POZIOTINIB | 3.0 | 1 | 9.66 |
| CHEMBL4559807 | — | — | 1 | 9.20 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 9.02 |
| CHEMBL4514452 | — | — | 1 | 8.83 |
| CHEMBL4534719 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4521381 | — | IC50 | = | 0.133 | nM | 9.88 |
| CHEMBL3545154 | POZIOTINIB | IC50 | = | 0.218 | nM | 9.66 |
| CHEMBL4559807 | — | IC50 | = | 0.636 | nM | 9.20 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL4514452 | — | IC50 | = | 1.48 | nM | 8.83 |
| CHEMBL4534719 | — | IC50 | = | 17.8 | nM | 7.75 |