Assay Detail
ADMET
CHEMBL4013166
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal GST-fused EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin incubated for 2 to 90 mins by HTFR assay
8
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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 |
|---|---|---|---|
| Ki | 4 | 9.07 | 10.15 |
| Kinact | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4100860 | — | — | 2 | 10.15 |
| CHEMBL4098072 | — | — | 2 | 9.46 |
| CHEMBL4071012 | — | — | 2 | 8.80 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 2 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4100860 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL4098072 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL4071012 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL3353410 | OSIMERTINIB | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4071012 | — | Kinact | = | 0.09 | /min | - |
| CHEMBL3353410 | OSIMERTINIB | Kinact | = | 0.43 | /min | - |
| CHEMBL4098072 | — | Kinact | = | 0.16 | /min | - |
| CHEMBL4100860 | — | Kinact | = | 0.16 | /min | - |