Assay Detail
Binding
CHEMBL5046853
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR del19 (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 | 7.19 | 8.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 8.97 |
| CHEMBL5072451 | — | — | 1 | 8.02 |
| CHEMBL5089161 | — | — | 1 | 7.95 |
| CHEMBL5080676 | — | — | 1 | 7.93 |
| CHEMBL5088907 | — | — | 1 | 7.90 |
| CHEMBL5093402 | — | — | 1 | 7.88 |
| CHEMBL5094406 | — | — | 1 | 7.73 |
| CHEMBL5070579 | — | — | 1 | 7.65 |
| CHEMBL5083034 | — | — | 1 | 7.33 |
| CHEMBL5071181 | — | — | 1 | 7.26 |
| CHEMBL5085816 | — | — | 1 | 7.19 |
| CHEMBL5089912 | — | — | 1 | 6.97 |
| CHEMBL5082074 | — | — | 1 | 6.84 |
| CHEMBL5084983 | — | — | 1 | 6.67 |
| CHEMBL5093794 | — | — | 1 | 6.54 |
| CHEMBL5087139 | — | — | 1 | 6.52 |
| CHEMBL5087994 | — | — | 1 | 6.20 |
| CHEMBL5089336 | — | — | 1 | 6.14 |
| CHEMBL5094237 | — | — | 1 | 6.04 |
| CHEMBL5076881 | — | — | 1 | 6.02 |
| CHEMBL5093625 | — | — | 1 | - |
| CHEMBL5090133 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 1.065 | nM | 8.97 |
| CHEMBL5072451 | — | IC50 | = | 9.574 | nM | 8.02 |
| CHEMBL5089161 | — | IC50 | = | 11.23 | nM | 7.95 |
| CHEMBL5080676 | — | IC50 | = | 11.61 | nM | 7.93 |
| CHEMBL5088907 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL5093402 | — | IC50 | = | 13.11 | nM | 7.88 |
| CHEMBL5094406 | — | IC50 | = | 18.7 | nM | 7.73 |
| CHEMBL5070579 | — | IC50 | = | 22.34 | nM | 7.65 |
| CHEMBL5083034 | — | IC50 | = | 46.36 | nM | 7.33 |
| CHEMBL5071181 | — | IC50 | = | 54.35 | nM | 7.26 |
| CHEMBL5085816 | — | IC50 | = | 63.98 | nM | 7.19 |
| CHEMBL5089912 | — | IC50 | = | 106.2 | nM | 6.97 |
| CHEMBL5082074 | — | IC50 | = | 142.8 | nM | 6.84 |
| CHEMBL5084983 | — | IC50 | = | 212.7 | nM | 6.67 |
| CHEMBL5093794 | — | IC50 | = | 287.7 | nM | 6.54 |
| CHEMBL5087139 | — | IC50 | = | 300.5 | nM | 6.52 |
| CHEMBL5087994 | — | IC50 | = | 625.4 | nM | 6.20 |
| CHEMBL5089336 | — | IC50 | = | 723.5 | nM | 6.14 |
| CHEMBL5094237 | — | IC50 | = | 902.4 | nM | 6.04 |
| CHEMBL5076881 | — | IC50 | = | 948.8 | nM | 6.02 |
| CHEMBL5093625 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5090133 | — | IC50 | > | 1000.0 | nM | - |