Assay Detail
Binding
CHEMBL4274201
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Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.61 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.94 |
| CHEMBL4282506 | — | — | 1 | 7.47 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 7.42 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL939 | GEFITINIB | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL4282506 | — | IC50 | = | 33.8 | nM | 7.47 |
| CHEMBL554 | LAPATINIB | IC50 | = | 37.55 | nM | 7.42 |
| CHEMBL553 | ERLOTINIB | IC50 | - | — | - |