Assay Detail
Binding
CHEMBL2406363
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BaF3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.30 | 7.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL509032 | TAE-684 | — | 1 | 7.36 |
| CHEMBL2403847 | — | — | 1 | 6.71 |
| CHEMBL2403835 | — | — | 1 | 6.62 |
| CHEMBL2403845 | — | — | 1 | 6.55 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 6.50 |
| CHEMBL2403836 | — | — | 1 | 6.49 |
| CHEMBL2403833 | — | — | 1 | 6.47 |
| CHEMBL2403834 | — | — | 1 | 6.46 |
| CHEMBL2403837 | — | — | 1 | 6.46 |
| CHEMBL2403841 | — | — | 1 | 6.44 |
| CHEMBL2403843 | — | — | 1 | 6.43 |
| CHEMBL2403827 | — | — | 1 | 6.40 |
| CHEMBL2403842 | — | — | 1 | 6.38 |
| CHEMBL2403829 | — | — | 1 | 6.38 |
| CHEMBL2403844 | — | — | 1 | 6.38 |
| CHEMBL2403849 | — | — | 1 | 6.33 |
| CHEMBL2403848 | — | — | 1 | 6.29 |
| CHEMBL2403846 | — | — | 1 | 6.27 |
| CHEMBL2403831 | — | — | 1 | 6.25 |
| CHEMBL2403830 | — | — | 1 | 6.11 |
| CHEMBL2403840 | — | — | 1 | 6.05 |
| CHEMBL2403838 | — | — | 1 | 5.93 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 5.78 |
| CHEMBL2403828 | — | — | 1 | 5.78 |
| CHEMBL2403832 | — | — | 1 | 5.72 |
| CHEMBL2403839 | — | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL509032 | TAE-684 | IC50 | = | 43.7 | nM | 7.36 |
| CHEMBL2403847 | — | IC50 | = | 197.2 | nM | 6.71 |
| CHEMBL2403835 | — | IC50 | = | 240.1 | nM | 6.62 |
| CHEMBL2403845 | — | IC50 | = | 281.8 | nM | 6.55 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 319.5 | nM | 6.50 |
| CHEMBL2403836 | — | IC50 | = | 326.5 | nM | 6.49 |
| CHEMBL2403833 | — | IC50 | = | 339.0 | nM | 6.47 |
| CHEMBL2403834 | — | IC50 | = | 344.5 | nM | 6.46 |
| CHEMBL2403837 | — | IC50 | = | 349.0 | nM | 6.46 |
| CHEMBL2403841 | — | IC50 | = | 361.1 | nM | 6.44 |
| CHEMBL2403843 | — | IC50 | = | 375.3 | nM | 6.43 |
| CHEMBL2403827 | — | IC50 | = | 401.0 | nM | 6.40 |
| CHEMBL2403842 | — | IC50 | = | 416.0 | nM | 6.38 |
| CHEMBL2403829 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL2403844 | — | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL2403849 | — | IC50 | = | 464.0 | nM | 6.33 |
| CHEMBL2403848 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL2403846 | — | IC50 | = | 541.5 | nM | 6.27 |
| CHEMBL2403831 | — | IC50 | = | 564.0 | nM | 6.25 |
| CHEMBL2403830 | — | IC50 | = | 784.0 | nM | 6.11 |
| CHEMBL2403840 | — | IC50 | = | 891.5 | nM | 6.05 |
| CHEMBL2403838 | — | IC50 | = | 1186.0 | nM | 5.93 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 1643.0 | nM | 5.78 |
| CHEMBL2403828 | — | IC50 | = | 1643.0 | nM | 5.78 |
| CHEMBL2403832 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL2403839 | — | IC50 | = | 4874.0 | nM | 5.31 |