Assay Detail
Binding
CHEMBL3293162
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant ALK L1196M mutant 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
29
Total Activities
29
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 | 29 | 8.55 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3286823 | — | — | 1 | 10.00 |
| CHEMBL3286825 | — | — | 1 | 10.00 |
| CHEMBL3286828 | — | — | 1 | 9.92 |
| CHEMBL3128069 | — | — | 1 | 9.70 |
| CHEMBL3286820 | — | — | 1 | 9.54 |
| CHEMBL3286827 | — | — | 1 | 9.40 |
| CHEMBL3286832 | — | — | 1 | 9.25 |
| CHEMBL3286818 | — | — | 1 | 9.24 |
| CHEMBL3286819 | — | — | 1 | 9.21 |
| CHEMBL3286811 | — | — | 1 | 9.15 |
| CHEMBL3286830 | LORLATINIB | 4.0 | 1 | 9.15 |
| CHEMBL3286813 | — | — | 1 | 8.85 |
| CHEMBL3286814 | — | — | 1 | 8.80 |
| CHEMBL3286822 | — | — | 1 | 8.72 |
| CHEMBL3286831 | — | — | 1 | 8.70 |
| CHEMBL3128075 | — | — | 1 | 8.59 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 8.09 |
| CHEMBL3286812 | — | — | 1 | 8.09 |
| CHEMBL3286816 | — | — | 1 | 7.54 |
| CHEMBL3286809 | — | — | 1 | 7.46 |
| CHEMBL3286817 | — | — | 1 | 7.44 |
| CHEMBL3286808 | — | — | 1 | 7.42 |
| CHEMBL3286821 | — | — | 1 | 7.21 |
| CHEMBL3286824 | — | — | 1 | 7.21 |
| CHEMBL3128060 | — | — | 1 | 7.16 |
| CHEMBL3286810 | — | — | 1 | 6.51 |
| CHEMBL3286826 | — | — | 1 | - |
| CHEMBL3286829 | — | — | 1 | - |
| CHEMBL3286815 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3286823 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3286825 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3286828 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL3128069 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3286820 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL3286827 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3286832 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL3286818 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL3286819 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL3286811 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3286830 | LORLATINIB | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3286813 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3286814 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL3286822 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL3286831 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3128075 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL601719 | CRIZOTINIB | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL3286812 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL3286816 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL3286809 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL3286817 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL3286808 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL3286821 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL3286824 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL3128060 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL3286810 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL3286826 | — | Ki | < | 0.02 | nM | - |
| CHEMBL3286829 | — | Ki | < | 0.1 | nM | - |
| CHEMBL3286815 | — | Ki | < | 0.1 | nM | - |