Assay Detail
Binding
CHEMBL5587332
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin)
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
Targeting Solvent-Front Mutations for Kinase Drug Discovery: From Structural Basis to Design Strategies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.45 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5195904 | — | — | 1 | 10.05 |
| CHEMBL5169450 | — | — | 1 | 9.34 |
| CHEMBL5596876 | — | — | 1 | 8.68 |
| CHEMBL4294743 | — | — | 1 | 8.26 |
| CHEMBL5597916 | — | — | 1 | 7.82 |
| CHEMBL4474196 | — | — | 1 | 7.56 |
| CHEMBL3545311 | BRIGATINIB | 4.0 | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5195904 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL5169450 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL5596876 | — | IC50 | = | 2.09 | nM | 8.68 |
| CHEMBL4294743 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL5597916 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4474196 | — | IC50 | = | 27.5 | nM | 7.56 |
| CHEMBL3545311 | BRIGATINIB | IC50 | = | 38.0 | nM | 7.42 |