Assay Detail
Binding
CHEMBL4721173
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST tagged EGFR L858R/T790M double mutant (669 to 1210 residues) expressed in insect expression system using peptide as substrate incubated for 2 hrs followed by substrate addition and measured after 30 mins by TR-FRET assay
5
Total Activities
5
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
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 8.41 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1229592 | — | — | 1 | 10.40 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 8.96 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 8.90 |
| CHEMBL4750196 | — | — | 1 | 5.37 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1229592 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL31965 | CANERTINIB | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL4750196 | — | IC50 | = | 4223.0 | nM | 5.37 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.002 | nM | - |