Assay Detail
Binding
CHEMBL4417511
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus using FAM-labelled peptide as substrate pre-incubated for 10 mins followed by substrate addition by mobility shift 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 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.11 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 7.96 |
| CHEMBL4548481 | — | — | 1 | 7.41 |
| CHEMBL4537004 | — | — | 1 | 6.76 |
| CHEMBL4439933 | — | — | 1 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1173655 | AFATINIB | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL4548481 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4537004 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL4439933 | — | IC50 | = | 490.0 | nM | 6.31 |