Assay Detail
Binding
CHEMBL2428558
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Inhibition of wild type human EGFR tyrosine kinase assessed as Ulight-CAGAGAIETDKEYYTVKD phosphorylation after 15 mins by time-resolved fluorometry
5
Total Activities
5
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
Long-lasting inhibition of EGFR autophosphorylation in A549 tumor cells by intracellular accumulation of non-covalent inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 8.63 | 9.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2425736 | — | — | 1 | 9.39 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 9.22 |
| CHEMBL2425735 | — | — | 1 | 9.20 |
| CHEMBL2425737 | — | — | 1 | 7.72 |
| CHEMBL597402 | — | — | 1 | 7.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2425736 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL939 | GEFITINIB | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL2425735 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL2425737 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL597402 | — | IC50 | = | 23.6 | nM | 7.63 |