Assay Detail
Binding
CHEMBL4052484
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R/T790M double mutant (unknown origin)
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 | Autocuration |
Publication
Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.50 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4101719 | — | — | 1 | 8.19 |
| CHEMBL4082764 | — | — | 1 | 6.80 |
| CHEMBL1229592 | — | — | 1 | - |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4101719 | — | IC50 | = | 6.47 | nM | 8.19 |
| CHEMBL4082764 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1229592 | — | IC50 | < | 0.5 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | IC50 | < | 0.5 | nM | - |