Assay Detail
Binding
CHEMBL4625061
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Inhibition of recombinant human partial length EGFR L858R mutant (669 to 1011 residues) expressed in bacterial expression system by competitive binding assay
2
Total Activities
2
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
Potent dual EGFR/Her4 tyrosine kinase inhibitors containing novel (1,2-dithiolan-4-yl)acetamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 2 | 8.30 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 8.55 |
| CHEMBL4646030 | — | — | 1 | 8.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL554 | LAPATINIB | Kd | = | 2.8 | nM | 8.55 |
| CHEMBL4646030 | — | Kd | = | 9.2 | nM | 8.04 |