Assay Detail
Binding
CHEMBL5330548
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Inhibition of EGFR L858R/T790M/C797S triple mutant in mouse BaF3 cells assessed as cell growth inhibition measured after 72 hrs by CellTiter-Glo assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | BaF3 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of EGFR kinase inhibitors that spans the orthosteric and allosteric sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.23 | 5.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 5.66 |
| CHEMBL5424516 | — | — | 1 | 5.43 |
| CHEMBL5422597 | — | — | 1 | 5.26 |
| CHEMBL5394643 | — | — | 1 | 5.23 |
| CHEMBL4565609 | — | — | 1 | 5.21 |
| CHEMBL5427645 | — | — | 1 | 5.11 |
| CHEMBL5427654 | — | — | 1 | 5.07 |
| CHEMBL5400243 | — | — | 1 | 5.05 |
| CHEMBL5440904 | — | — | 1 | 5.04 |
| CHEMBL5440459 | — | — | 1 | - |
| CHEMBL5397284 | — | — | 1 | - |
| CHEMBL5422464 | — | — | 1 | - |
| CHEMBL5416664 | — | — | 1 | - |
| CHEMBL5394899 | — | — | 1 | - |
| CHEMBL4284413 | — | — | 1 | - |
| CHEMBL5409028 | — | — | 1 | - |
| CHEMBL5397063 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 2190.0 | nM | 5.66 |
| CHEMBL5424516 | — | IC50 | = | 3670.0 | nM | 5.43 |
| CHEMBL5422597 | — | IC50 | = | 5470.0 | nM | 5.26 |
| CHEMBL5394643 | — | IC50 | = | 5850.0 | nM | 5.23 |
| CHEMBL4565609 | — | IC50 | = | 6160.0 | nM | 5.21 |
| CHEMBL5427645 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL5427654 | — | IC50 | = | 8450.0 | nM | 5.07 |
| CHEMBL5400243 | — | IC50 | = | 8830.0 | nM | 5.05 |
| CHEMBL5440904 | — | IC50 | = | 9060.0 | nM | 5.04 |
| CHEMBL5440459 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5397284 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5422464 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5416664 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5394899 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4284413 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5409028 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5397063 | — | IC50 | > | 20000.0 | nM | - |