Assay Detail
Binding
CHEMBL3389022
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Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LoVo |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 4.72 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2426279 | — | — | 1 | 5.92 |
| CHEMBL3353408 | — | — | 1 | 4.96 |
| CHEMBL2426277 | — | — | 1 | 4.92 |
| CHEMBL3353411 | — | — | 1 | 4.48 |
| CHEMBL3353406 | — | — | 1 | 4.34 |
| CHEMBL3353407 | — | — | 1 | 4.24 |
| CHEMBL3353409 | — | — | 1 | 4.15 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | - |
| CHEMBL3353395 | — | — | 1 | - |
| CHEMBL3353396 | — | — | 1 | - |
| CHEMBL3353397 | — | — | 1 | - |
| CHEMBL3353398 | — | — | 1 | - |
| CHEMBL3353399 | — | — | 1 | - |
| CHEMBL3353400 | — | — | 1 | - |
| CHEMBL2426288 | — | — | 1 | - |
| CHEMBL3353402 | — | — | 1 | - |
| CHEMBL3353403 | — | — | 1 | - |
| CHEMBL3353404 | — | — | 1 | - |
| CHEMBL3353405 | — | — | 1 | - |
| CHEMBL3353412 | — | — | 1 | - |
| CHEMBL3353401 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2426279 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3353408 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2426277 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3353411 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3353406 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL3353407 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL3353409 | — | IC50 | = | 71000.0 | nM | 4.15 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 480000.0 | nM | - |
| CHEMBL3353395 | — | IC50 | = | 10000000.0 | nM | - |
| CHEMBL3353396 | — | IC50 | = | 1600000.0 | nM | - |
| CHEMBL3353397 | — | IC50 | = | 6060000.0 | nM | - |
| CHEMBL3353398 | — | IC50 | = | 5600000.0 | nM | - |
| CHEMBL3353399 | — | IC50 | = | 7500000.0 | nM | - |
| CHEMBL3353400 | — | IC50 | = | 11000000.0 | nM | - |
| CHEMBL2426288 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3353402 | — | IC50 | = | 9000000.0 | nM | - |
| CHEMBL3353403 | — | IC50 | = | 357000.0 | nM | - |
| CHEMBL3353404 | — | IC50 | = | 145000.0 | nM | - |
| CHEMBL3353405 | — | IC50 | = | 938000.0 | nM | - |
| CHEMBL3353412 | — | IC50 | = | 786000.0 | nM | - |
| CHEMBL3353401 | — | IC50 | = | 10300000.0 | nM | - |