Assay Detail
Binding
CHEMBL4009534
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Reversible inhibition of human N-terminal GST-tagged EGFR L858R mutant cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression system using TK peptide substrate preincubated for 2 to 90 mins followed by 6-fold dilution
7
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 8.03 | 8.80 |
| Inhibition | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 8.80 |
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 8.74 |
| CHEMBL4068763 | — | — | 1 | 8.41 |
| CHEMBL4098444 | — | — | 1 | 7.24 |
| CHEMBL4089863 | — | — | 1 | 6.98 |
| CHEMBL4079501 | — | — | 1 | - |
| CHEMBL4097594 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353410 | OSIMERTINIB | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL3545308 | ROCILETINIB | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL4068763 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL4098444 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL4089863 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL4079501 | — | Inhibition | - | % | - | |
| CHEMBL4097594 | — | Inhibition | - | % | - |