Assay Detail
Functional
CHEMBL5165820
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
19
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | BaF3 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.48 | 7.80 |
| Activity | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5205581 | — | — | 1 | 7.80 |
| CHEMBL5193609 | — | — | 1 | 7.44 |
| CHEMBL5197952 | — | — | 1 | 7.18 |
| CHEMBL5181684 | — | — | 1 | 6.85 |
| CHEMBL5170653 | — | — | 1 | 6.85 |
| CHEMBL5188272 | — | — | 1 | 6.78 |
| CHEMBL5201250 | — | — | 1 | 6.75 |
| CHEMBL5179214 | — | — | 1 | 6.58 |
| CHEMBL5180778 | — | — | 1 | 6.39 |
| CHEMBL5181437 | — | — | 1 | 6.35 |
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 6.21 |
| CHEMBL5176897 | — | — | 1 | 5.58 |
| CHEMBL5209545 | — | — | 1 | 5.56 |
| CHEMBL5206683 | — | — | 1 | 5.50 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 5.37 |
| CHEMBL5185999 | — | — | 1 | - |
| CHEMBL5201287 | — | — | 1 | - |
| CHEMBL5170303 | — | — | 1 | - |
| CHEMBL5169943 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5205581 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5193609 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5197952 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5181684 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL5170653 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5188272 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL5201250 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5179214 | — | IC50 | = | 263.0 | nM | 6.58 |
| CHEMBL5180778 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5181437 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL3545311 | BRIGATINIB | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL5176897 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL5209545 | — | IC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL5206683 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 4270.0 | nM | 5.37 |
| CHEMBL5185999 | — | Activity | - | — | - | |
| CHEMBL5201287 | — | Activity | - | — | - | |
| CHEMBL5170303 | — | Activity | - | — | - | |
| CHEMBL5169943 | — | Activity | - | — | - |