Assay Detail
Binding
CHEMBL4178361
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR exon 19 deletion mutant phosphorylation in human PC9 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISA
10
Total Activities
10
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 | 10 | 7.89 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3883534 | — | — | 1 | 9.00 |
| CHEMBL4216679 | — | — | 1 | 8.70 |
| CHEMBL3989970 | MAVELERTINIB | 2.0 | 1 | 8.30 |
| CHEMBL3608429 | — | — | 1 | 8.05 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.96 |
| CHEMBL3608432 | — | — | 1 | 7.80 |
| CHEMBL4206501 | — | — | 1 | 7.25 |
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 7.10 |
| CHEMBL3786098 | PF-06459988 | 2.0 | 1 | 6.85 |
| CHEMBL4218154 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3883534 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4216679 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3989970 | MAVELERTINIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3608429 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3608432 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4206501 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3545308 | ROCILETINIB | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3786098 | PF-06459988 | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4218154 | — | IC50 | - | — | - |