Assay Detail
Binding
CHEMBL4178356
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR T790M/L858R double mutant (unknown origin)
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.66 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4216749 | — | — | 1 | 8.70 |
| CHEMBL3608429 | — | — | 1 | 8.70 |
| CHEMBL4211367 | — | — | 1 | 8.52 |
| CHEMBL4211782 | — | — | 1 | 8.52 |
| CHEMBL4206481 | — | — | 1 | 8.40 |
| CHEMBL4205392 | — | — | 1 | 8.22 |
| CHEMBL4216679 | — | — | 1 | 8.10 |
| CHEMBL4208811 | — | — | 1 | 8.05 |
| CHEMBL3989970 | MAVELERTINIB | 2.0 | 1 | 7.89 |
| CHEMBL3608432 | — | — | 1 | 7.77 |
| CHEMBL4208829 | — | — | 1 | 7.75 |
| CHEMBL4218154 | — | — | 1 | 7.72 |
| CHEMBL4206312 | — | — | 1 | 7.50 |
| CHEMBL4212326 | — | — | 1 | 7.44 |
| CHEMBL4204498 | — | — | 1 | 7.25 |
| CHEMBL4207951 | — | — | 1 | 7.07 |
| CHEMBL4209368 | — | — | 1 | 6.98 |
| CHEMBL4204566 | — | — | 1 | 6.82 |
| CHEMBL4207425 | — | — | 1 | 6.79 |
| CHEMBL4213741 | — | — | 1 | 6.79 |
| CHEMBL4206604 | — | — | 1 | 6.79 |
| CHEMBL4203072 | — | — | 1 | 6.74 |
| CHEMBL4213609 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4216749 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3608429 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4211367 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4211782 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4206481 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4205392 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4216679 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4208811 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3989970 | MAVELERTINIB | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL3608432 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4208829 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4218154 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4206312 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL4212326 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL4204498 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL4207951 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL4209368 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL4204566 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL4207425 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL4213741 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL4206604 | — | Ki | = | 161.0 | nM | 6.79 |
| CHEMBL4203072 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL4213609 | — | Ki | - | — | - |