Assay Detail
Binding
CHEMBL964130
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Inhibition of EGFR L858R mutant by time resolved fluorescence assay
10
Total Activities
10
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
Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.27 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL446250 | — | — | 1 | 8.52 |
| CHEMBL448628 | — | — | 1 | 7.60 |
| CHEMBL455208 | — | — | 1 | 7.52 |
| CHEMBL503638 | — | — | 1 | 7.52 |
| CHEMBL437584 | — | — | 1 | 7.24 |
| CHEMBL443098 | — | — | 1 | 7.24 |
| CHEMBL251732 | — | — | 1 | 7.19 |
| CHEMBL452717 | — | — | 1 | 6.89 |
| CHEMBL249496 | — | — | 1 | 6.57 |
| CHEMBL248877 | — | — | 1 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL446250 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL448628 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL455208 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL503638 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL437584 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL443098 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL251732 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL452717 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL249496 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL248877 | — | IC50 | = | 361.0 | nM | 6.44 |