Assay Detail
Binding
CHEMBL3293164
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA
27
Total Activities
27
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 | 27 | 7.16 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3286826 | — | — | 1 | 9.12 |
| CHEMBL3286823 | — | — | 1 | 8.85 |
| CHEMBL3286828 | — | — | 1 | 8.72 |
| CHEMBL3286825 | — | — | 1 | 8.68 |
| CHEMBL3286829 | — | — | 1 | 8.24 |
| CHEMBL3128069 | — | — | 1 | 8.18 |
| CHEMBL3286820 | — | — | 1 | 7.85 |
| CHEMBL3286818 | — | — | 1 | 7.70 |
| CHEMBL3286830 | LORLATINIB | 4.0 | 1 | 7.68 |
| CHEMBL3286827 | — | — | 1 | 7.68 |
| CHEMBL3286819 | — | — | 1 | 7.68 |
| CHEMBL3286832 | — | — | 1 | 7.35 |
| CHEMBL3286811 | — | — | 1 | 7.28 |
| CHEMBL3286813 | — | — | 1 | 7.27 |
| CHEMBL3286822 | — | — | 1 | 7.01 |
| CHEMBL3286814 | — | — | 1 | 7.00 |
| CHEMBL3286815 | — | — | 1 | 6.95 |
| CHEMBL3128075 | — | — | 1 | 6.75 |
| CHEMBL3286812 | — | — | 1 | 6.51 |
| CHEMBL3286831 | — | — | 1 | 6.44 |
| CHEMBL3286816 | — | — | 1 | 6.18 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.07 |
| CHEMBL3286824 | — | — | 1 | 5.91 |
| CHEMBL3286809 | — | — | 1 | 5.78 |
| CHEMBL3128060 | — | — | 1 | 5.58 |
| CHEMBL3286808 | — | — | 1 | 5.50 |
| CHEMBL3286817 | — | — | 1 | 5.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3286826 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL3286823 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3286828 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3286825 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3286829 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3128069 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3286820 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3286818 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3286830 | LORLATINIB | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3286827 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3286819 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3286832 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3286811 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3286813 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3286822 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL3286814 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL3286815 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL3128075 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL3286812 | — | IC50 | = | 312.0 | nM | 6.51 |
| CHEMBL3286831 | — | IC50 | = | 365.0 | nM | 6.44 |
| CHEMBL3286816 | — | IC50 | = | 654.0 | nM | 6.18 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 843.0 | nM | 6.07 |
| CHEMBL3286824 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL3286809 | — | IC50 | = | 1665.0 | nM | 5.78 |
| CHEMBL3128060 | — | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL3286808 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL3286817 | — | IC50 | = | 3655.0 | nM | 5.44 |