Assay Detail
Binding
CHEMBL4382299
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged human EGFR T790M mutant 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 | 8.39 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4449391 | — | — | 1 | 8.70 |
| CHEMBL4565984 | — | — | 1 | 8.70 |
| CHEMBL4581316 | — | — | 1 | 8.70 |
| CHEMBL4520341 | — | — | 1 | 8.70 |
| CHEMBL4558227 | — | — | 1 | 8.70 |
| CHEMBL4473365 | — | — | 1 | 8.70 |
| CHEMBL4448107 | — | — | 1 | 8.70 |
| CHEMBL4467561 | — | — | 1 | 8.52 |
| CHEMBL4540442 | — | — | 1 | 8.40 |
| CHEMBL1229592 | — | — | 1 | 8.30 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 8.30 |
| CHEMBL4465103 | — | — | 1 | 8.30 |
| CHEMBL4531697 | — | — | 1 | 8.05 |
| CHEMBL4516287 | — | — | 1 | 7.58 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 7.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4449391 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4565984 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4581316 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4520341 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4558227 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4473365 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4448107 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4467561 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4540442 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1229592 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4465103 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4531697 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4516287 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 28.0 | nM | 7.55 |