Assay Detail
Binding
CHEMBL4013164
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Inhibition of human EGFR T790M/C797S/L858R triple mutant preincubated for 20 mins followed by [33P]ATP addition measured after 2 hrs
10
Total Activities
10
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 Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.14 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4090686 | — | — | 1 | 8.15 |
| CHEMBL4100860 | — | — | 1 | 8.10 |
| CHEMBL4071368 | — | — | 1 | 7.96 |
| CHEMBL4060003 | — | — | 1 | 7.28 |
| CHEMBL4098072 | — | — | 1 | 7.05 |
| CHEMBL4094927 | — | — | 1 | 6.78 |
| CHEMBL4102577 | — | — | 1 | 6.65 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.56 |
| CHEMBL1229592 | — | — | 1 | 5.69 |
| CHEMBL4087268 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4090686 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4100860 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4071368 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4060003 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4098072 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4094927 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL4102577 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 278.0 | nM | 6.56 |
| CHEMBL1229592 | — | IC50 | = | 2053.0 | nM | 5.69 |
| CHEMBL4087268 | — | IC50 | - | — | - |