Assay Detail
Binding
CHEMBL5255138
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Inhibition of EGFR D770-N771 ins NPG mutant (unknown origin)
27
Total Activities
27
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
Structure optimization and discovery of novel compound for the treatment of insertion mutations within exon 20 of EGFR and HER2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 8.68 | 10.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5288888 | — | — | 1 | 10.57 |
| CHEMBL5282641 | — | — | 1 | 10.28 |
| CHEMBL3545154 | POZIOTINIB | 3.0 | 1 | 10.21 |
| CHEMBL5274692 | — | — | 1 | 9.81 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 9.78 |
| CHEMBL5280967 | — | — | 1 | 9.62 |
| CHEMBL5268781 | — | — | 1 | 9.47 |
| CHEMBL5271930 | — | — | 1 | 9.39 |
| CHEMBL5281167 | — | — | 1 | 9.26 |
| CHEMBL5277739 | — | — | 1 | 9.09 |
| CHEMBL5281741 | — | — | 1 | 9.09 |
| CHEMBL5280664 | — | — | 1 | 8.98 |
| CHEMBL5270938 | — | — | 1 | 8.92 |
| CHEMBL5281140 | — | — | 1 | 8.92 |
| CHEMBL5283507 | — | — | 1 | 8.81 |
| CHEMBL5266649 | — | — | 1 | 8.78 |
| CHEMBL5281205 | — | — | 1 | 8.78 |
| CHEMBL5286007 | — | — | 1 | 8.75 |
| CHEMBL5266601 | — | — | 1 | 7.97 |
| CHEMBL5288249 | — | — | 1 | 7.97 |
| CHEMBL5281748 | — | — | 1 | 7.89 |
| CHEMBL5284701 | — | — | 1 | 7.72 |
| CHEMBL5272004 | — | — | 1 | 7.41 |
| CHEMBL5273261 | — | — | 1 | 7.08 |
| CHEMBL5290971 | — | — | 1 | 6.64 |
| CHEMBL5290095 | — | — | 1 | 6.64 |
| CHEMBL5270309 | — | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5288888 | — | IC50 | = | 0.027 | nM | 10.57 |
| CHEMBL5282641 | — | IC50 | = | 0.053 | nM | 10.28 |
| CHEMBL3545154 | POZIOTINIB | IC50 | = | 0.061 | nM | 10.21 |
| CHEMBL5274692 | — | IC50 | = | 0.153 | nM | 9.81 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 0.166 | nM | 9.78 |
| CHEMBL5280967 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL5268781 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL5271930 | — | IC50 | = | 0.403 | nM | 9.39 |
| CHEMBL5281167 | — | IC50 | = | 0.551 | nM | 9.26 |
| CHEMBL5277739 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL5281741 | — | IC50 | = | 0.817 | nM | 9.09 |
| CHEMBL5280664 | — | IC50 | = | 1.04 | nM | 8.98 |
| CHEMBL5270938 | — | IC50 | = | 1.21 | nM | 8.92 |
| CHEMBL5281140 | — | IC50 | = | 1.21 | nM | 8.92 |
| CHEMBL5283507 | — | IC50 | = | 1.53 | nM | 8.81 |
| CHEMBL5266649 | — | IC50 | = | 1.67 | nM | 8.78 |
| CHEMBL5281205 | — | IC50 | = | 1.67 | nM | 8.78 |
| CHEMBL5286007 | — | IC50 | = | 1.79 | nM | 8.75 |
| CHEMBL5266601 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL5288249 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL5281748 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL5284701 | — | IC50 | = | 18.9 | nM | 7.72 |
| CHEMBL5272004 | — | IC50 | = | 38.9 | nM | 7.41 |
| CHEMBL5273261 | — | IC50 | = | 83.5 | nM | 7.08 |
| CHEMBL5290971 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL5290095 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL5270309 | — | IC50 | = | 272.0 | nM | 6.57 |