Assay Detail
Binding
CHEMBL4707740
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human EGFR cytoplasmic domain L858R/T790M mutant (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 40 mins by HTRF assay
10
Total Activities
10
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 | 10 | 7.20 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 9.22 |
| CHEMBL4558324 | LAZERTINIB | 4.0 | 1 | 8.57 |
| CHEMBL4798177 | — | — | 1 | 7.37 |
| CHEMBL4753387 | — | — | 1 | 6.95 |
| CHEMBL4788364 | — | — | 1 | 6.84 |
| CHEMBL4778502 | — | — | 1 | 6.83 |
| CHEMBL4786701 | — | — | 1 | 6.81 |
| CHEMBL4798480 | — | — | 1 | 6.67 |
| CHEMBL4787536 | — | — | 1 | 6.63 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4558324 | LAZERTINIB | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4798177 | — | IC50 | = | 43.1 | nM | 7.37 |
| CHEMBL4753387 | — | IC50 | = | 111.6 | nM | 6.95 |
| CHEMBL4788364 | — | IC50 | = | 143.4 | nM | 6.84 |
| CHEMBL4778502 | — | IC50 | = | 146.9 | nM | 6.83 |
| CHEMBL4786701 | — | IC50 | = | 155.7 | nM | 6.81 |
| CHEMBL4798480 | — | IC50 | = | 212.7 | nM | 6.67 |
| CHEMBL4787536 | — | IC50 | = | 234.4 | nM | 6.63 |
| CHEMBL939 | GEFITINIB | IC50 | = | 777.1 | nM | 6.11 |