Assay Detail
Functional
CHEMBL5260461
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Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A-431 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Addressing the Osimertinib Resistance Mutation EGFR-L858R/C797S with Reversible Aminopyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 5.61 | 6.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.08 |
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 6.03 |
| CHEMBL5285052 | — | — | 1 | 5.85 |
| CHEMBL4650319 | MOBOCERTINIB | 4.0 | 1 | 5.78 |
| CHEMBL5270693 | — | — | 1 | 5.74 |
| CHEMBL5284924 | — | — | 1 | 5.58 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 5.55 |
| CHEMBL5280082 | — | — | 1 | 5.43 |
| CHEMBL5288276 | — | — | 1 | 5.41 |
| CHEMBL5289859 | — | — | 1 | 5.41 |
| CHEMBL5287229 | — | — | 1 | 5.40 |
| CHEMBL5275642 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | EC50 | = | 830.0 | nM | 6.08 |
| CHEMBL3545311 | BRIGATINIB | EC50 | = | 936.0 | nM | 6.03 |
| CHEMBL5285052 | — | EC50 | = | 1414.0 | nM | 5.85 |
| CHEMBL4650319 | MOBOCERTINIB | EC50 | = | 1676.0 | nM | 5.78 |
| CHEMBL5270693 | — | EC50 | = | 1837.0 | nM | 5.74 |
| CHEMBL5284924 | — | EC50 | = | 2607.0 | nM | 5.58 |
| CHEMBL553 | ERLOTINIB | EC50 | = | 2805.0 | nM | 5.55 |
| CHEMBL5280082 | — | EC50 | = | 3669.0 | nM | 5.43 |
| CHEMBL5288276 | — | EC50 | = | 3915.0 | nM | 5.41 |
| CHEMBL5289859 | — | EC50 | = | 3887.0 | nM | 5.41 |
| CHEMBL5287229 | — | EC50 | = | 4016.0 | nM | 5.40 |
| CHEMBL5275642 | — | EC50 | = | 7956.0 | nM | 5.10 |