Assay Detail
Binding
CHEMBL2328802
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human EGFR T790M/L858R mutant expressed in Sf9 cells using [gamma32P]-ATP after 10 mins by scintillation counting
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Based Approach for the Discovery of Pyrrolo[3,2-d]pyrimidine-Based EGFR T790M/L858R Mutant Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.27 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2322330 | — | — | 1 | 7.72 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 7.18 |
| CHEMBL2322329 | — | — | 1 | 5.09 |
| CHEMBL1614725 | TAK-285 | 1.0 | 1 | 5.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2322330 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL180022 | NERATINIB | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2322329 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL1614725 | TAK-285 | IC50 | = | 8400.0 | nM | 5.08 |