Assay Detail
Binding
CHEMBL4009508
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal GST-tagged EGFR L858R/T790M double mutant cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression system using TK peptide substrate preincubated with enzyme for 30 mins followed by substrate addition measured after 20 mins by HTRF assay
22
Total Activities
22
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
Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.58 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4089863 | — | — | 1 | 8.96 |
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 8.59 |
| CHEMBL4079566 | — | — | 1 | 8.57 |
| CHEMBL4060039 | — | — | 1 | 8.37 |
| CHEMBL4098444 | — | — | 1 | 8.32 |
| CHEMBL4071463 | — | — | 1 | 8.30 |
| CHEMBL4079501 | — | — | 1 | 8.30 |
| CHEMBL4088277 | — | — | 1 | 8.22 |
| CHEMBL4060103 | — | — | 1 | 8.00 |
| CHEMBL4080424 | — | — | 1 | 7.82 |
| CHEMBL4103757 | — | — | 1 | 7.66 |
| CHEMBL4082000 | — | — | 1 | 7.42 |
| CHEMBL4098500 | — | — | 1 | 7.14 |
| CHEMBL4061043 | — | — | 1 | 7.07 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 6.73 |
| CHEMBL4074766 | — | — | 1 | 6.33 |
| CHEMBL4090330 | — | — | 1 | 5.58 |
| CHEMBL4069284 | — | — | 1 | 5.01 |
| CHEMBL4097594 | — | — | 1 | - |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | - |
| CHEMBL4068763 | — | — | 1 | - |
| CHEMBL4065517 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4089863 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3545308 | ROCILETINIB | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4079566 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4060039 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4098444 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4071463 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4079501 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4088277 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4060103 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4080424 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4103757 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4082000 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4098500 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4061043 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL939 | GEFITINIB | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL4074766 | — | IC50 | = | 462.0 | nM | 6.33 |
| CHEMBL4090330 | — | IC50 | = | 2626.0 | nM | 5.58 |
| CHEMBL4069284 | — | IC50 | = | 9726.0 | nM | 5.01 |
| CHEMBL4097594 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | IC50 | < | 1.0 | nM | - |
| CHEMBL4068763 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4065517 | — | IC50 | > | 10000.0 | nM | - |