Assay Detail
Binding
CHEMBL2412779
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R mutant (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET based Z'-lyte assay
10
Total Activities
10
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
Nitric oxide donating anilinopyrimidines: synthesis and biological evaluation as EGFR inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.76 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 9.70 |
| CHEMBL1229592 | — | — | 1 | 8.27 |
| CHEMBL2408828 | — | — | 1 | 6.82 |
| CHEMBL2408830 | — | — | 1 | 6.43 |
| CHEMBL2408829 | — | — | 1 | 6.31 |
| CHEMBL2408825 | — | — | 1 | 5.82 |
| CHEMBL2408826 | — | — | 1 | 5.49 |
| CHEMBL2408824 | — | — | 1 | 5.27 |
| CHEMBL2408827 | — | — | 1 | - |
| CHEMBL2408823 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1229592 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL2408828 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2408830 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL2408829 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL2408825 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL2408826 | — | IC50 | = | 3220.0 | nM | 5.49 |
| CHEMBL2408824 | — | IC50 | = | 5360.0 | nM | 5.27 |
| CHEMBL2408827 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2408823 | — | IC50 | > | 10000.0 | nM | - |