Assay Detail
Functional
CHEMBL5114498
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human PC-9 cells harboring EGFR del19/T790M/C797S mutant assessed as inhibition of cell proliferation
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PC-9 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFR<sup>del19/T790M/C797S</sup> and EGFR<sup>L858R/T790M/C797S</sup>).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.95 | 7.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5206715 | — | — | 1 | 7.18 |
| CHEMBL5189768 | — | — | 1 | 7.17 |
| CHEMBL5200379 | — | — | 1 | 6.90 |
| CHEMBL5194613 | — | — | 1 | 6.83 |
| CHEMBL5192879 | — | — | 1 | 6.66 |
| CHEMBL5184348 | — | — | 1 | - |
| CHEMBL5197088 | — | — | 1 | - |
| CHEMBL5203896 | — | — | 1 | - |
| CHEMBL5178352 | — | — | 1 | - |
| CHEMBL5198787 | — | — | 1 | - |
| CHEMBL5179412 | — | — | 1 | - |
| CHEMBL5183388 | — | — | 1 | - |
| CHEMBL5199289 | — | — | 1 | - |
| CHEMBL5172169 | — | — | 1 | - |
| CHEMBL5190420 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5206715 | — | IC50 | = | 66.7 | nM | 7.18 |
| CHEMBL5189768 | — | IC50 | = | 67.4 | nM | 7.17 |
| CHEMBL5200379 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL5194613 | — | IC50 | = | 148.1 | nM | 6.83 |
| CHEMBL5192879 | — | IC50 | = | 216.9 | nM | 6.66 |
| CHEMBL5184348 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5197088 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5203896 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5178352 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5198787 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5179412 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5183388 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5199289 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5172169 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5190420 | — | IC50 | > | 1000.0 | nM | - |