Assay Detail
Binding
CHEMBL5046854
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR T790M/C797S double mutant (unknown origin) using flurogenic substrate in presence of ATP by HTRF assay
22
Total Activities
22
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
Discovery of highly potent and selective EGFR<sup>T790M/L858R</sup> TKIs against NSCLC based on molecular dynamic simulation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.87 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 9.38 |
| CHEMBL5093402 | — | — | 1 | 8.70 |
| CHEMBL5072451 | — | — | 1 | 8.40 |
| CHEMBL5089161 | — | — | 1 | 8.36 |
| CHEMBL5080676 | — | — | 1 | 8.25 |
| CHEMBL5083034 | — | — | 1 | 8.24 |
| CHEMBL5085816 | — | — | 1 | 8.24 |
| CHEMBL5088907 | — | — | 1 | 8.21 |
| CHEMBL5094406 | — | — | 1 | 8.10 |
| CHEMBL5082074 | — | — | 1 | 8.09 |
| CHEMBL5070579 | — | — | 1 | 8.07 |
| CHEMBL5084983 | — | — | 1 | 7.91 |
| CHEMBL5087139 | — | — | 1 | 7.90 |
| CHEMBL5071181 | — | — | 1 | 7.67 |
| CHEMBL5094237 | — | — | 1 | 7.56 |
| CHEMBL5089336 | — | — | 1 | 7.44 |
| CHEMBL5093625 | — | — | 1 | 7.40 |
| CHEMBL5089912 | — | — | 1 | 7.37 |
| CHEMBL5076881 | — | — | 1 | 7.24 |
| CHEMBL5087994 | — | — | 1 | 6.40 |
| CHEMBL5093794 | — | — | 1 | 6.30 |
| CHEMBL5090133 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.414 | nM | 9.38 |
| CHEMBL5093402 | — | IC50 | = | 2.003 | nM | 8.70 |
| CHEMBL5072451 | — | IC50 | = | 4.014 | nM | 8.40 |
| CHEMBL5089161 | — | IC50 | = | 4.363 | nM | 8.36 |
| CHEMBL5080676 | — | IC50 | = | 5.654 | nM | 8.25 |
| CHEMBL5083034 | — | IC50 | = | 5.751 | nM | 8.24 |
| CHEMBL5085816 | — | IC50 | = | 5.751 | nM | 8.24 |
| CHEMBL5088907 | — | IC50 | = | 6.198 | nM | 8.21 |
| CHEMBL5094406 | — | IC50 | = | 8.023 | nM | 8.10 |
| CHEMBL5082074 | — | IC50 | = | 8.131 | nM | 8.09 |
| CHEMBL5070579 | — | IC50 | = | 8.58 | nM | 8.07 |
| CHEMBL5084983 | — | IC50 | = | 12.34 | nM | 7.91 |
| CHEMBL5087139 | — | IC50 | = | 12.54 | nM | 7.90 |
| CHEMBL5071181 | — | IC50 | = | 21.43 | nM | 7.67 |
| CHEMBL5094237 | — | IC50 | = | 27.34 | nM | 7.56 |
| CHEMBL5089336 | — | IC50 | = | 36.61 | nM | 7.44 |
| CHEMBL5093625 | — | IC50 | = | 39.62 | nM | 7.40 |
| CHEMBL5089912 | — | IC50 | = | 42.38 | nM | 7.37 |
| CHEMBL5076881 | — | IC50 | = | 57.97 | nM | 7.24 |
| CHEMBL5087994 | — | IC50 | = | 397.0 | nM | 6.40 |
| CHEMBL5093794 | — | IC50 | = | 501.5 | nM | 6.30 |
| CHEMBL5090133 | — | IC50 | > | 1000.0 | nM | - |