Assay Detail
Binding
CHEMBL1105218
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR Leu858Arg and Thr790Met mutant by HTRF 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
Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.61 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1090840 | — | — | 1 | 8.49 |
| CHEMBL1089524 | — | — | 1 | 6.89 |
| CHEMBL304929 | — | — | 1 | 6.85 |
| CHEMBL1088901 | — | — | 1 | 6.72 |
| CHEMBL1092382 | — | — | 1 | 6.28 |
| CHEMBL188762 | — | — | 1 | 6.00 |
| CHEMBL1092250 | — | — | 1 | 5.82 |
| CHEMBL1089203 | — | — | 1 | 5.82 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL285063 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1090840 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1089524 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL304929 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1088901 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1092382 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL188762 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1092250 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1089203 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 1000.0 | nM | - |
| CHEMBL285063 | — | IC50 | < | 1.0 | nM | - |