Assay Detail
Binding
CHEMBL3241596
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R mutant (unknown origin) after 1.5 hr by FRET-based Z-lyte assay
11
Total Activities
11
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
Synthesis and evaluation of 2-anilinopyrimidines bearing 3-aminopropamides as potential epidermal growth factor receptor inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.43 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 9.70 |
| CHEMBL1229592 | — | — | 1 | 8.32 |
| CHEMBL3237937 | — | — | 1 | 6.58 |
| CHEMBL3237931 | — | — | 1 | 6.37 |
| CHEMBL3237929 | — | — | 1 | 6.09 |
| CHEMBL3237930 | — | — | 1 | 6.09 |
| CHEMBL3237935 | — | — | 1 | 5.62 |
| CHEMBL3237932 | — | — | 1 | 5.34 |
| CHEMBL3237936 | — | — | 1 | 5.23 |
| CHEMBL3237934 | — | — | 1 | 5.00 |
| CHEMBL3237933 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1229592 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3237937 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL3237931 | — | IC50 | = | 427.0 | nM | 6.37 |
| CHEMBL3237929 | — | IC50 | = | 804.0 | nM | 6.09 |
| CHEMBL3237930 | — | IC50 | = | 818.0 | nM | 6.09 |
| CHEMBL3237935 | — | IC50 | = | 2385.0 | nM | 5.62 |
| CHEMBL3237932 | — | IC50 | = | 4527.0 | nM | 5.34 |
| CHEMBL3237936 | — | IC50 | = | 5866.0 | nM | 5.23 |
| CHEMBL3237934 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3237933 | — | IC50 | > | 10000.0 | nM | - |