Assay Detail
Binding
CHEMBL4382298
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type GST-tagged human EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a potent dual ALK and EGFR T790M inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.68 | 7.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4448107 | — | — | 1 | 7.34 |
| CHEMBL4581316 | — | — | 1 | 7.27 |
| CHEMBL4520341 | — | — | 1 | 7.19 |
| CHEMBL4558227 | — | — | 1 | 6.97 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.94 |
| CHEMBL1229592 | — | — | 1 | 6.92 |
| CHEMBL4465103 | — | — | 1 | 6.83 |
| CHEMBL4473365 | — | — | 1 | 6.82 |
| CHEMBL4565984 | — | — | 1 | 6.76 |
| CHEMBL4449391 | — | — | 1 | 6.69 |
| CHEMBL4467561 | — | — | 1 | 6.61 |
| CHEMBL4540442 | — | — | 1 | 6.51 |
| CHEMBL4531697 | — | — | 1 | 6.06 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 5.67 |
| CHEMBL4516287 | — | — | 1 | 5.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4448107 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4581316 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4520341 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4558227 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL1229592 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4465103 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL4473365 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL4565984 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL4449391 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL4467561 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL4540442 | — | IC50 | = | 307.0 | nM | 6.51 |
| CHEMBL4531697 | — | IC50 | = | 865.0 | nM | 6.06 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 2156.0 | nM | 5.67 |
| CHEMBL4516287 | — | IC50 | = | 2480.0 | nM | 5.61 |