Assay Detail
Binding
CHEMBL892951
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human EGFR in presence of 1 uM ATP
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.47 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 10.10 |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | 9.22 |
| CHEMBL29197 | — | — | 1 | 8.59 |
| CHEMBL428741 | — | — | 1 | 8.39 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 8.27 |
| CHEMBL243837 | — | — | 1 | 7.91 |
| CHEMBL243629 | — | — | 1 | 7.73 |
| CHEMBL241919 | — | — | 1 | 7.60 |
| CHEMBL243839 | — | — | 1 | 7.32 |
| CHEMBL398154 | — | — | 1 | 7.04 |
| CHEMBL241918 | — | — | 1 | 6.97 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.95 |
| CHEMBL243628 | — | — | 1 | 6.78 |
| CHEMBL243410 | — | — | 1 | 6.55 |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | 6.34 |
| CHEMBL428039 | — | — | 1 | 6.10 |
| CHEMBL242349 | — | — | 1 | 5.11 |
| CHEMBL242131 | — | — | 1 | - |
| CHEMBL242555 | — | — | 1 | - |
| CHEMBL396472 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL180022 | NERATINIB | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL607707 | PELITINIB | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL29197 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL428741 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL939 | GEFITINIB | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL243837 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL243629 | — | IC50 | = | 18.7 | nM | 7.73 |
| CHEMBL241919 | — | IC50 | = | 24.9 | nM | 7.60 |
| CHEMBL243839 | — | IC50 | = | 47.5 | nM | 7.32 |
| CHEMBL398154 | — | IC50 | = | 90.8 | nM | 7.04 |
| CHEMBL241918 | — | IC50 | = | 107.3 | nM | 6.97 |
| CHEMBL24828 | VANDETANIB | IC50 | = | 112.4 | nM | 6.95 |
| CHEMBL243628 | — | IC50 | = | 166.7 | nM | 6.78 |
| CHEMBL243410 | — | IC50 | = | 283.3 | nM | 6.55 |
| CHEMBL101253 | VATALANIB | IC50 | = | 457.7 | nM | 6.34 |
| CHEMBL428039 | — | IC50 | = | 799.3 | nM | 6.10 |
| CHEMBL242349 | — | IC50 | = | 7710.0 | nM | 5.11 |
| CHEMBL242131 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL242555 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL396472 | — | IC50 | > | 10000.0 | nM | - |