Assay Detail
Binding
CHEMBL4178351
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR T790M/L858R double mutant phosphorylation in human H1975 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISA
22
Total Activities
22
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 |
|---|---|---|---|
| IC50 | 22 | 7.43 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4216679 | — | — | 1 | 8.30 |
| CHEMBL3883534 | — | — | 1 | 8.15 |
| CHEMBL4218154 | — | — | 1 | 8.15 |
| CHEMBL3608429 | — | — | 1 | 8.15 |
| CHEMBL4205392 | — | — | 1 | 8.10 |
| CHEMBL3989970 | MAVELERTINIB | 2.0 | 1 | 7.92 |
| CHEMBL3786098 | PF-06459988 | 2.0 | 1 | 7.89 |
| CHEMBL4206501 | — | — | 1 | 7.82 |
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 7.80 |
| CHEMBL4208829 | — | — | 1 | 7.77 |
| CHEMBL4208811 | — | — | 1 | 7.72 |
| CHEMBL3608432 | — | — | 1 | 7.58 |
| CHEMBL4206312 | — | — | 1 | 7.54 |
| CHEMBL4207951 | — | — | 1 | 7.31 |
| CHEMBL4212326 | — | — | 1 | 7.28 |
| CHEMBL4213400 | — | — | 1 | 7.11 |
| CHEMBL4213741 | — | — | 1 | 6.55 |
| CHEMBL4213609 | — | — | 1 | 6.17 |
| CHEMBL4204566 | — | — | 1 | 6.15 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 5.05 |
| CHEMBL4203072 | — | — | 1 | - |
| CHEMBL4207425 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4216679 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3883534 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4218154 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3608429 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4205392 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3989970 | MAVELERTINIB | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3786098 | PF-06459988 | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4206501 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3545308 | ROCILETINIB | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4208829 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4208811 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3608432 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4206312 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4207951 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4212326 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4213400 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4213741 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4213609 | — | IC50 | = | 675.0 | nM | 6.17 |
| CHEMBL4204566 | — | IC50 | = | 713.0 | nM | 6.15 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 9003.0 | nM | 5.05 |
| CHEMBL4203072 | — | IC50 | - | — | - | |
| CHEMBL4207425 | — | IC50 | - | — | - |