Assay Detail
Binding
CHEMBL4222846
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R/T790M double mutant (unknown origin) using poly (Glu, Tyr) as substrate after 40 mins by kinase-glo plus luminescence assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.48 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 8.74 |
| CHEMBL4226676 | — | — | 1 | 6.98 |
| CHEMBL4228518 | — | — | 1 | 6.72 |
| CHEMBL4227084 | — | — | 1 | - |
| CHEMBL4225951 | — | — | 1 | - |
| CHEMBL4226937 | — | — | 1 | - |
| CHEMBL4225777 | — | — | 1 | - |
| CHEMBL4225565 | — | — | 1 | - |
| CHEMBL4226151 | — | — | 1 | - |
| CHEMBL4225306 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4226676 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4228518 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL4227084 | — | IC50 | - | — | - | |
| CHEMBL4225951 | — | IC50 | - | — | - | |
| CHEMBL4226937 | — | IC50 | - | — | - | |
| CHEMBL4225777 | — | IC50 | - | — | - | |
| CHEMBL4225565 | — | IC50 | - | — | - | |
| CHEMBL4226151 | — | IC50 | - | — | - | |
| CHEMBL4225306 | — | IC50 | - | — | - |