Assay Detail
Binding
CHEMBL1935855
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR phosphorylation in EGF-stimulated human A431 after 2 hrs by Western blot analysis
3
Total Activities
3
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 novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.67 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 9.00 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 9.00 |
| CHEMBL1201179 | LAPATINIB DITOSYLATE | 4.0 | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL553 | ERLOTINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL939 | GEFITINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1201179 | LAPATINIB DITOSYLATE | IC50 | = | 10.0 | nM | 8.00 |