Assay Detail
Binding
CHEMBL4721174
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST tagged EGFR d746-750 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 | 8.04 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 10.40 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 10.00 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 9.70 |
| CHEMBL1229592 | — | — | 1 | 9.52 |
| CHEMBL4792426 | — | — | 1 | 9.22 |
| CHEMBL4750196 | — | — | 1 | 8.89 |
| CHEMBL4753193 | — | — | 1 | 8.77 |
| CHEMBL4745521 | — | — | 1 | 8.51 |
| CHEMBL4757724 | — | — | 1 | 8.41 |
| CHEMBL4793852 | — | — | 1 | 8.28 |
| CHEMBL4796407 | — | — | 1 | 8.04 |
| CHEMBL4763967 | — | — | 1 | 7.96 |
| CHEMBL4790583 | — | — | 1 | 7.96 |
| CHEMBL4743173 | — | — | 1 | 7.46 |
| CHEMBL4777554 | — | — | 1 | 7.15 |
| CHEMBL4763697 | — | — | 1 | 6.96 |
| CHEMBL4747893 | — | — | 1 | 6.90 |
| CHEMBL4755444 | — | — | 1 | 6.89 |
| CHEMBL4790485 | — | — | 1 | 6.68 |
| CHEMBL4757531 | — | — | 1 | 6.57 |
| CHEMBL4756049 | — | — | 1 | 6.38 |
| CHEMBL4784185 | — | — | 1 | 6.32 |
| CHEMBL4777353 | — | — | 1 | - |
| CHEMBL4749765 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL31965 | CANERTINIB | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1229592 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4792426 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4750196 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4753193 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4745521 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4757724 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4793852 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4796407 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4763967 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4790583 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4743173 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4777554 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4763697 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4747893 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4755444 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL4790485 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4757531 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL4756049 | — | IC50 | = | 419.0 | nM | 6.38 |
| CHEMBL4784185 | — | IC50 | = | 474.0 | nM | 6.32 |
| CHEMBL4777353 | — | IC50 | - | — | - | |
| CHEMBL4749765 | — | IC50 | > | 200.0 | nM | - |