Assay Detail
Binding
CHEMBL3293161
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type human recombinant ALK kinase domain (amino acids 1093 to 1141) expressed in baculovirus system using 5'FAM-KKSRGDYMTMQIG-CONH2 as substrate incubated for 15 mins prior to ATP addition measured after 1 hr by microfluidic mobility shift assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| Ki | 26 | 8.60 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3286815 | — | — | 1 | 9.66 |
| CHEMBL3286814 | — | — | 1 | 9.44 |
| CHEMBL3286816 | — | — | 1 | 9.42 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 9.13 |
| CHEMBL3286812 | — | — | 1 | 9.07 |
| CHEMBL3286809 | — | — | 1 | 8.55 |
| CHEMBL3286808 | — | — | 1 | 8.40 |
| CHEMBL3286817 | — | — | 1 | 8.30 |
| CHEMBL3128060 | — | — | 1 | 8.05 |
| CHEMBL3286821 | — | — | 1 | 7.77 |
| CHEMBL3286824 | — | — | 1 | 7.77 |
| CHEMBL3286810 | — | — | 1 | 7.66 |
| CHEMBL3128069 | — | — | 1 | - |
| CHEMBL3128075 | — | — | 1 | - |
| CHEMBL3286811 | — | — | 1 | - |
| CHEMBL3286813 | — | — | 1 | - |
| CHEMBL3286818 | — | — | 1 | - |
| CHEMBL3286819 | — | — | 1 | - |
| CHEMBL3286820 | — | — | 1 | - |
| CHEMBL3286822 | — | — | 1 | - |
| CHEMBL3286830 | LORLATINIB | 4.0 | 1 | - |
| CHEMBL3286823 | — | — | 1 | - |
| CHEMBL3286828 | — | — | 1 | - |
| CHEMBL3286825 | — | — | 1 | - |
| CHEMBL3286827 | — | — | 1 | - |
| CHEMBL3286826 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3286815 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL3286814 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL3286816 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL601719 | CRIZOTINIB | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL3286812 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL3286809 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL3286808 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3286817 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3128060 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3286821 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3286824 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3286810 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL3128069 | — | Ki | < | 0.1 | nM | - |
| CHEMBL3128075 | — | Ki | < | 0.2 | nM | - |
| CHEMBL3286811 | — | Ki | < | 0.2 | nM | - |
| CHEMBL3286813 | — | Ki | < | 0.2 | nM | - |
| CHEMBL3286818 | — | Ki | < | 0.1 | nM | - |
| CHEMBL3286819 | — | Ki | < | 0.1 | nM | - |
| CHEMBL3286820 | — | Ki | < | 0.2 | nM | - |
| CHEMBL3286822 | — | Ki | < | 0.2 | nM | - |
| CHEMBL3286830 | LORLATINIB | Ki | < | 0.07 | nM | - |
| CHEMBL3286823 | — | Ki | < | 0.2 | nM | - |
| CHEMBL3286828 | — | Ki | < | 0.1 | nM | - |
| CHEMBL3286825 | — | Ki | < | 0.2 | nM | - |
| CHEMBL3286827 | — | Ki | < | 0.07 | nM | - |
| CHEMBL3286826 | — | Ki | < | 0.08 | nM | - |