Assay Detail
Binding
CHEMBL4178362
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of EGFR L858R mutant phosphorylation in human H3255 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 |
Target
Receptor tyrosine-protein kinase erbB-3 (CHEMBL5838) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 8.15 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3883534 | — | — | 1 | 9.00 |
| CHEMBL3608429 | — | — | 1 | 8.70 |
| CHEMBL4216679 | — | — | 1 | 8.70 |
| CHEMBL3989970 | MAVELERTINIB | 2.0 | 1 | 8.40 |
| CHEMBL3608432 | — | — | 1 | 8.05 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 8.00 |
| CHEMBL3786098 | PF-06459988 | 2.0 | 1 | 7.68 |
| CHEMBL4206501 | — | — | 1 | 7.44 |
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 7.34 |
| CHEMBL4218154 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3883534 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3608429 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4216679 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3989970 | MAVELERTINIB | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3608432 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3786098 | PF-06459988 | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4206501 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3545308 | ROCILETINIB | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4218154 | — | IC50 | - | — | - |