Assay Detail
Binding
CHEMBL4384426
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Inhibition of wild type EGFR autophosphorylation in human A549 cells by Western blot analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Balancing reactivity and antitumor activity: heteroarylthioacetamide derivatives as potent and time-dependent inhibitors of EGFR.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.68 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4562352 | — | — | 1 | 9.22 |
| CHEMBL4530170 | — | — | 1 | 8.30 |
| CHEMBL4440618 | — | — | 1 | 8.15 |
| CHEMBL4572315 | — | — | 1 | 7.96 |
| CHEMBL4556799 | — | — | 1 | 7.92 |
| CHEMBL4530987 | — | — | 1 | 7.85 |
| CHEMBL4435699 | — | — | 1 | 7.82 |
| CHEMBL4437599 | — | — | 1 | 7.60 |
| CHEMBL4558356 | — | — | 1 | 7.57 |
| CHEMBL4449681 | — | — | 1 | 7.57 |
| CHEMBL4526992 | — | — | 1 | 7.57 |
| CHEMBL4439974 | — | — | 1 | 7.47 |
| CHEMBL4538707 | — | — | 1 | 7.36 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.22 |
| CHEMBL4521214 | — | — | 1 | 7.16 |
| CHEMBL4473375 | — | — | 1 | 7.08 |
| CHEMBL4559217 | — | — | 1 | 6.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4562352 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4530170 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4440618 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4572315 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4556799 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4530987 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4435699 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4437599 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4558356 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4449681 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4526992 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4439974 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4538707 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL939 | GEFITINIB | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4521214 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4473375 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4559217 | — | IC50 | = | 197.0 | nM | 6.71 |