Assay Detail
Binding
CHEMBL3293163
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type human EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | NIH3T3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.19 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3286826 | — | — | 1 | 9.96 |
| CHEMBL3286825 | — | — | 1 | 9.74 |
| CHEMBL3286823 | — | — | 1 | 9.68 |
| CHEMBL3286828 | — | — | 1 | 9.47 |
| CHEMBL3286820 | — | — | 1 | 9.15 |
| CHEMBL3128069 | — | — | 1 | 9.12 |
| CHEMBL3286819 | — | — | 1 | 9.05 |
| CHEMBL3286818 | — | — | 1 | 9.00 |
| CHEMBL3286830 | LORLATINIB | 4.0 | 1 | 8.89 |
| CHEMBL3286827 | — | — | 1 | 8.89 |
| CHEMBL3286813 | — | — | 1 | 8.34 |
| CHEMBL3286822 | — | — | 1 | 8.19 |
| CHEMBL3286811 | — | — | 1 | 8.01 |
| CHEMBL3128075 | — | — | 1 | 7.85 |
| CHEMBL3286815 | — | — | 1 | 7.82 |
| CHEMBL3286812 | — | — | 1 | 7.80 |
| CHEMBL3286814 | — | — | 1 | 7.66 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.10 |
| CHEMBL3286816 | — | — | 1 | 7.07 |
| CHEMBL3286808 | — | — | 1 | 7.02 |
| CHEMBL3286809 | — | — | 1 | 6.94 |
| CHEMBL3286824 | — | — | 1 | 6.81 |
| CHEMBL3128060 | — | — | 1 | 6.60 |
| CHEMBL3286817 | — | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3286826 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL3286825 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL3286823 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL3286828 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL3286820 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3128069 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL3286819 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3286818 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3286830 | LORLATINIB | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3286827 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3286813 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3286822 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL3286811 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL3128075 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3286815 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3286812 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3286814 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3286816 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL3286808 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL3286809 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL3286824 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL3128060 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL3286817 | — | IC50 | = | 524.0 | nM | 6.28 |