Assay Detail
Binding
CHEMBL4707739
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type N-terminal GST-tagged human EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus infected Sf21 cells using biotin-labeled TK substrate preincubated for 30 mins followed by substrate and ATP addition at Km concentration and further incubated for 20 mins by HTRF assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.20 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 8.19 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.85 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 7.47 |
| CHEMBL4558324 | LAZERTINIB | 4.0 | 1 | 7.46 |
| CHEMBL4798177 | — | — | 1 | 7.05 |
| CHEMBL4798480 | — | — | 1 | 6.81 |
| CHEMBL4778502 | — | — | 1 | 6.75 |
| CHEMBL4788364 | — | — | 1 | 6.71 |
| CHEMBL4786701 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL939 | GEFITINIB | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 33.7 | nM | 7.47 |
| CHEMBL4558324 | LAZERTINIB | IC50 | = | 34.6 | nM | 7.46 |
| CHEMBL4798177 | — | IC50 | = | 89.3 | nM | 7.05 |
| CHEMBL4798480 | — | IC50 | = | 156.4 | nM | 6.81 |
| CHEMBL4778502 | — | IC50 | = | 178.8 | nM | 6.75 |
| CHEMBL4788364 | — | IC50 | = | 195.8 | nM | 6.71 |
| CHEMBL4786701 | — | IC50 | = | 333.0 | nM | 6.48 |