Assay Detail
Binding
CHEMBL5224781
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R/T790M double mutant (unknown origin)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of novel macrocyclic derivatives bearing aniline pyrimidine scaffolds as EGFR-TKIs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 8.15 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 9.60 |
| CHEMBL5287438 | — | — | 1 | 8.54 |
| CHEMBL5274514 | — | — | 1 | 8.46 |
| CHEMBL5290583 | — | — | 1 | 8.19 |
| CHEMBL5269317 | — | — | 1 | 8.08 |
| CHEMBL5289304 | — | — | 1 | 8.00 |
| CHEMBL5286636 | — | — | 1 | 7.98 |
| CHEMBL5273197 | — | — | 1 | 7.88 |
| CHEMBL5286055 | — | — | 1 | 7.70 |
| CHEMBL5272747 | — | — | 1 | 7.60 |
| CHEMBL5266919 | — | — | 1 | 7.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL5287438 | — | IC50 | = | 2.92 | nM | 8.54 |
| CHEMBL5274514 | — | IC50 | = | 3.45 | nM | 8.46 |
| CHEMBL5290583 | — | IC50 | = | 6.49 | nM | 8.19 |
| CHEMBL5269317 | — | IC50 | = | 8.31 | nM | 8.08 |
| CHEMBL5289304 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5286636 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL5273197 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL5286055 | — | IC50 | = | 20.1 | nM | 7.70 |
| CHEMBL5272747 | — | IC50 | = | 25.2 | nM | 7.60 |
| CHEMBL5266919 | — | IC50 | = | 25.7 | nM | 7.59 |