Assay Detail
Binding
CHEMBL4384432
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human wild type GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus expression system after 1 hr by kinase tracer 199 based TR-FRET assay
7
Total Activities
7
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
Balancing reactivity and antitumor activity: heteroarylthioacetamide derivatives as potent and time-dependent inhibitors of EGFR.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 9.27 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4449681 | — | — | 1 | 9.47 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 9.33 |
| CHEMBL4530170 | — | — | 1 | 9.28 |
| CHEMBL4439974 | — | — | 1 | 9.28 |
| CHEMBL4526992 | — | — | 1 | 9.21 |
| CHEMBL4440618 | — | — | 1 | 9.06 |
| CHEMBL4572315 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4449681 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL939 | GEFITINIB | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL4530170 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL4439974 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL4526992 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL4440618 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL4572315 | — | IC50 | - | — | - |