Assay Detail
Binding
CHEMBL4417018
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay
14
Total Activities
14
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
Discovery of an Oleanolic Acid/Hederagenin-Nitric Oxide Donor Hybrid as an EGFR Tyrosine Kinase Inhibitor for Non-Small-Cell Lung Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.45 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 9.00 |
| CHEMBL4588786 | — | — | 1 | 8.00 |
| CHEMBL4452906 | — | — | 1 | 7.70 |
| CHEMBL4437863 | — | — | 1 | 7.52 |
| CHEMBL4537422 | — | — | 1 | 7.40 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 7.05 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.50 |
| CHEMBL168 | OLEANOLIC_ACID | — | 1 | - |
| CHEMBL486400 | HEDERAGENIN | — | 1 | - |
| CHEMBL4554092 | — | — | 1 | - |
| CHEMBL4456487 | — | — | 1 | - |
| CHEMBL4470692 | — | — | 1 | - |
| CHEMBL4454172 | — | — | 1 | - |
| CHEMBL4460981 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545311 | BRIGATINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4588786 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4452906 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4437863 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4537422 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL939 | GEFITINIB | IC50 | = | 3170.0 | nM | 5.50 |
| CHEMBL168 | OLEANOLIC_ACID | IC50 | > | 20000.0 | nM | - |
| CHEMBL486400 | HEDERAGENIN | IC50 | > | 20000.0 | nM | - |
| CHEMBL4554092 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4456487 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4470692 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4454172 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4460981 | — | IC50 | > | 20000.0 | nM | - |