Assay Detail
Binding
CHEMBL4013157
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal GST-fused EGFR T790M/L858R double mutant (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubated for 30 mins followed by substrate addition measured after 20 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 | 7.21 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4096980 | — | — | 1 | 8.96 |
| CHEMBL4079393 | — | — | 1 | 8.60 |
| CHEMBL4100777 | — | — | 1 | 8.51 |
| CHEMBL4087268 | — | — | 1 | 8.48 |
| CHEMBL4082362 | — | — | 1 | 8.35 |
| CHEMBL4094927 | — | — | 1 | 8.30 |
| CHEMBL4100377 | — | — | 1 | 8.17 |
| CHEMBL4105526 | — | — | 1 | 8.13 |
| CHEMBL4076854 | — | — | 1 | 8.07 |
| CHEMBL4098412 | — | — | 1 | 7.92 |
| CHEMBL4071180 | — | — | 1 | 7.75 |
| CHEMBL4062543 | — | — | 1 | 7.54 |
| CHEMBL4081860 | — | — | 1 | 7.54 |
| CHEMBL4086878 | — | — | 1 | 7.48 |
| CHEMBL4071012 | — | — | 1 | 7.42 |
| CHEMBL4102224 | — | — | 1 | 7.28 |
| CHEMBL4070707 | — | — | 1 | 7.18 |
| CHEMBL4061473 | — | — | 1 | 7.12 |
| CHEMBL4064942 | — | — | 1 | 7.09 |
| CHEMBL4091569 | — | — | 1 | 7.08 |
| CHEMBL4089279 | — | — | 1 | 7.05 |
| CHEMBL4102577 | — | — | 1 | 7.03 |
| CHEMBL321494 | — | — | 1 | 6.89 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 6.73 |
| CHEMBL4076363 | — | — | 1 | 6.62 |
| CHEMBL4089601 | — | — | 1 | 6.49 |
| CHEMBL4086078 | — | — | 1 | 6.38 |
| CHEMBL4082884 | — | — | 1 | 6.31 |
| CHEMBL4062722 | — | — | 1 | 6.23 |
| CHEMBL4068092 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4096980 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4079393 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4100777 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4087268 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4082362 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4094927 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4100377 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4105526 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4076854 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4098412 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4071180 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4081860 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4062543 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4086878 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4071012 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4102224 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4070707 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4061473 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4064942 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4091569 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4089279 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4102577 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL321494 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL939 | GEFITINIB | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL4076363 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4089601 | — | IC50 | = | 321.0 | nM | 6.49 |
| CHEMBL4086078 | — | IC50 | = | 417.0 | nM | 6.38 |
| CHEMBL4082884 | — | IC50 | = | 485.0 | nM | 6.31 |
| CHEMBL4062722 | — | IC50 | = | 586.0 | nM | 6.23 |
| CHEMBL4068092 | — | IC50 | = | 597.0 | nM | 6.22 |
| CHEMBL4084248 | — | IC50 | = | 646.0 | nM | 6.19 |
| CHEMBL4081732 | — | IC50 | = | 746.0 | nM | 6.13 |
| CHEMBL4067255 | — | IC50 | = | 1246.0 | nM | 5.90 |
| CHEMBL4092003 | — | IC50 | = | 1328.0 | nM | 5.88 |
| CHEMBL4101193 | — | IC50 | = | 3511.0 | nM | 5.46 |
| CHEMBL4060003 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL1173655 | AFATINIB | IC50 | < | 1.0 | nM | - |
| CHEMBL4098072 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | IC50 | < | 1.0 | nM | - |
| CHEMBL1229592 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4071368 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4090686 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4100860 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4078963 | — | IC50 | < | 1.0 | nM | - |