Assay Detail
Binding
CHEMBL4273762
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His6-tagged recombinant EGFR cytoplasmic domain (645 to 1186 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells preincubated for 10 mins followed by ATP-MgCl2 addition and measured after 1 hr by DELFIA/time-resolved fluorometric analysis
7
Total Activities
7
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
Synthesis, anticancer activity and molecular modeling studies of 1,2,4-triazole derivatives as EGFR inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.67 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1079742 | ERLOTINIB HYDROCHLORIDE | 4.0 | 1 | 7.16 |
| CHEMBL4279008 | — | — | 1 | 5.82 |
| CHEMBL4289274 | — | — | 1 | 5.77 |
| CHEMBL4286943 | — | — | 1 | 5.55 |
| CHEMBL4290355 | — | — | 1 | 5.25 |
| CHEMBL4282482 | — | — | 1 | 5.14 |
| CHEMBL4286998 | — | — | 1 | 5.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1079742 | ERLOTINIB HYDROCHLORIDE | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4279008 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4289274 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4286943 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4290355 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4282482 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4286998 | — | IC50 | = | 9800.0 | nM | 5.01 |