Assay Detail
Binding
CHEMBL5638807
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type N-terminal GST-tagged EGFR (669 to 1210 residues) (unknown origin) using poly(Glu, Tyr) 4:1 as substrate preincubated with compound for 15 mins followed by substrate addition and measured after 50 mins in presence of ATP by ADP-glo kinase assay
12
Total Activities
12
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
Vinylpyridine as a Tunable Covalent Warhead Targeting C797 in EGFR.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 9.33 | 9.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5647479 | — | — | 1 | 9.50 |
| CHEMBL3545154 | POZIOTINIB | 3.0 | 1 | 9.40 |
| CHEMBL5639556 | — | — | 1 | 9.40 |
| CHEMBL5641648 | — | — | 1 | 9.40 |
| CHEMBL5641888 | — | — | 1 | 9.40 |
| CHEMBL5646965 | — | — | 1 | 9.40 |
| CHEMBL5647150 | — | — | 1 | 9.30 |
| CHEMBL5647083 | — | — | 1 | 9.30 |
| CHEMBL5646414 | — | — | 1 | 9.30 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 9.20 |
| CHEMBL5647295 | — | — | 1 | 9.20 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 9.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5647479 | — | IC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL3545154 | POZIOTINIB | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL5639556 | — | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL5641648 | — | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL5641888 | — | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL5646965 | — | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL5647150 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL5647083 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL5646414 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL939 | GEFITINIB | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL5647295 | — | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 0.7943 | nM | 9.10 |