Assay Detail
Binding
CHEMBL4013155
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal GST-fused EGFR L858R mutant (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubated for 30 mins followed by substrate addition measured after 15 mins by HTFR assay
44
Total Activities
44
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 | 44 | 8.04 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4064942 | — | — | 1 | 9.00 |
| CHEMBL4091569 | — | — | 1 | 8.96 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 8.89 |
| CHEMBL4062543 | — | — | 1 | 8.77 |
| CHEMBL4071180 | — | — | 1 | 8.72 |
| CHEMBL4070707 | — | — | 1 | 8.72 |
| CHEMBL4071012 | — | — | 1 | 8.66 |
| CHEMBL321494 | — | — | 1 | 8.60 |
| CHEMBL4081860 | — | — | 1 | 8.59 |
| CHEMBL4061473 | — | — | 1 | 8.51 |
| CHEMBL4102224 | — | — | 1 | 8.49 |
| CHEMBL4089279 | — | — | 1 | 8.31 |
| CHEMBL4076854 | — | — | 1 | 8.25 |
| CHEMBL4102577 | — | — | 1 | 8.17 |
| CHEMBL4086878 | — | — | 1 | 8.00 |
| CHEMBL4076363 | — | — | 1 | 7.92 |
| CHEMBL4082884 | — | — | 1 | 7.80 |
| CHEMBL4089601 | — | — | 1 | 7.66 |
| CHEMBL4086078 | — | — | 1 | 7.60 |
| CHEMBL4081732 | — | — | 1 | 7.40 |
| CHEMBL4068092 | — | — | 1 | 7.34 |
| CHEMBL4062722 | — | — | 1 | 7.26 |
| CHEMBL4067255 | — | — | 1 | 7.12 |
| CHEMBL4092003 | — | — | 1 | 7.12 |
| CHEMBL4084248 | — | — | 1 | 6.84 |
| CHEMBL4101193 | — | — | 1 | 6.44 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | - |
| CHEMBL4087268 | — | — | 1 | - |
| CHEMBL4079393 | — | — | 1 | - |
| CHEMBL4098072 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4064942 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4091569 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4062543 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4071180 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4070707 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4071012 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL321494 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4081860 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4061473 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4102224 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4089279 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4076854 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4102577 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4086878 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4076363 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4082884 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4089601 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4086078 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4081732 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4068092 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4062722 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4067255 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4092003 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4084248 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL4101193 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL1229592 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4060003 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4071368 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4098412 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4090686 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4100860 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4082362 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4100377 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL939 | GEFITINIB | IC50 | < | 1.0 | nM | - |
| CHEMBL4105526 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4078963 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4096980 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4100777 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4094927 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4098072 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4079393 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4087268 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL1173655 | AFATINIB | IC50 | < | 1.0 | nM | - |