Assay Detail
Binding
CHEMBL1044057
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Inhibition of Her1 T790M mutant by fluorescence polarization assay
4
Total Activities
4
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 a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.79 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL569880 | — | — | 1 | 7.96 |
| CHEMBL571040 | — | — | 1 | 7.62 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL569880 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL571040 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL553 | ERLOTINIB | IC50 | > | 1000.0 | nM | - |
| CHEMBL554 | LAPATINIB | IC50 | > | 1000.0 | nM | - |