Assay Detail
Binding
CHEMBL2383987
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R mutant (unknown origin) after 1.5 hrs by FRET-based Z'Lyte assay
13
Total Activities
13
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 hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.34 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 9.70 |
| CHEMBL1229592 | — | — | 1 | 8.27 |
| CHEMBL2381516 | — | — | 1 | 7.40 |
| CHEMBL2381514 | — | — | 1 | 7.20 |
| CHEMBL2381509 | — | — | 1 | 7.19 |
| CHEMBL2381504 | — | — | 1 | 7.18 |
| CHEMBL2381515 | — | — | 1 | 7.17 |
| CHEMBL2381506 | — | — | 1 | 7.08 |
| CHEMBL2381507 | — | — | 1 | 7.01 |
| CHEMBL2381505 | — | — | 1 | 7.00 |
| CHEMBL2381510 | — | — | 1 | 6.95 |
| CHEMBL2381508 | — | — | 1 | 6.72 |
| CHEMBL2381511 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1229592 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL2381516 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2381514 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL2381509 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2381504 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2381515 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL2381506 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL2381507 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL2381505 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL2381510 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL2381508 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL2381511 | — | IC50 | = | 305.0 | nM | 6.52 |