Assay Detail
Binding
CHEMBL4721175
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST tagged EGFR L858R 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
24
Total Activities
24
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 | 24 | 7.69 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 10.00 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 9.70 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 9.30 |
| CHEMBL1229592 | — | — | 1 | 9.10 |
| CHEMBL4792426 | — | — | 1 | 8.72 |
| CHEMBL4750196 | — | — | 1 | 8.57 |
| CHEMBL4777353 | — | — | 1 | 8.42 |
| CHEMBL4745521 | — | — | 1 | 8.42 |
| CHEMBL4757724 | — | — | 1 | 8.42 |
| CHEMBL4753193 | — | — | 1 | 7.92 |
| CHEMBL4793852 | — | — | 1 | 7.85 |
| CHEMBL4790583 | — | — | 1 | 7.77 |
| CHEMBL4796407 | — | — | 1 | 7.75 |
| CHEMBL4763967 | — | — | 1 | 7.50 |
| CHEMBL4743173 | — | — | 1 | 7.13 |
| CHEMBL4747893 | — | — | 1 | 6.71 |
| CHEMBL4755444 | — | — | 1 | 6.57 |
| CHEMBL4763697 | — | — | 1 | 6.37 |
| CHEMBL4790485 | — | — | 1 | 6.33 |
| CHEMBL4757531 | — | — | 1 | 6.32 |
| CHEMBL4756049 | — | — | 1 | 6.18 |
| CHEMBL4777554 | — | — | 1 | 6.13 |
| CHEMBL4784185 | — | — | 1 | 5.65 |
| CHEMBL4749765 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL31965 | CANERTINIB | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1229592 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4792426 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4750196 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4777353 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4745521 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4757724 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4753193 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4793852 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4790583 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4796407 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4763967 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4743173 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4747893 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL4755444 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4763697 | — | IC50 | = | 427.0 | nM | 6.37 |
| CHEMBL4790485 | — | IC50 | = | 463.0 | nM | 6.33 |
| CHEMBL4757531 | — | IC50 | = | 475.0 | nM | 6.32 |
| CHEMBL4756049 | — | IC50 | = | 666.0 | nM | 6.18 |
| CHEMBL4777554 | — | IC50 | = | 735.0 | nM | 6.13 |
| CHEMBL4784185 | — | IC50 | = | 2245.0 | nM | 5.65 |
| CHEMBL4749765 | — | IC50 | > | 200.0 | nM | - |