Assay Detail
Functional
CHEMBL5577191
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Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H1975 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Exploring the structural activity relationship of the Osimertinib: A covalent inhibitor of double mutant EGFR<sup>L858R/T790M</sup> tyrosine kinase for the treatment of Non-Small Cell Lung Cancer (NSCLC).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.28 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353408 | — | — | 1 | 9.70 |
| CHEMBL3353404 | — | — | 1 | 9.22 |
| CHEMBL3353406 | — | — | 1 | 9.05 |
| CHEMBL3353409 | — | — | 1 | 9.00 |
| CHEMBL3353403 | — | — | 1 | 8.70 |
| CHEMBL3353407 | — | — | 1 | 8.70 |
| CHEMBL3353411 | — | — | 1 | 8.70 |
| CHEMBL3353405 | — | — | 1 | 8.40 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 7.82 |
| CHEMBL3353395 | — | — | 1 | 7.80 |
| CHEMBL3353396 | — | — | 1 | 7.72 |
| CHEMBL3353399 | — | — | 1 | 7.18 |
| CHEMBL3353400 | — | — | 1 | 7.12 |
| CHEMBL3353402 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353408 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3353404 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3353406 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3353409 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3353403 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3353407 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3353411 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3353405 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3353395 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3353396 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3353399 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3353400 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3353402 | — | IC50 | = | 177.0 | nM | 6.75 |