Assay Detail
Functional
CHEMBL2406362
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity against human KARPAS299 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 | Functional |
| Organism | Homo sapiens |
| Cell Type | KARPAS-299 |
| Confidence | 1 — Organism |
| 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 | 7.64 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL509032 | TAE-684 | — | 1 | 8.62 |
| CHEMBL2403845 | — | — | 1 | 8.11 |
| CHEMBL2403841 | — | — | 1 | 8.10 |
| CHEMBL2403836 | — | — | 1 | 8.09 |
| CHEMBL2403827 | — | — | 1 | 7.98 |
| CHEMBL2403834 | — | — | 1 | 7.96 |
| CHEMBL2403849 | — | — | 1 | 7.95 |
| CHEMBL2403846 | — | — | 1 | 7.88 |
| CHEMBL2403848 | — | — | 1 | 7.88 |
| CHEMBL2403847 | — | — | 1 | 7.87 |
| CHEMBL2403833 | — | — | 1 | 7.84 |
| CHEMBL2403835 | — | — | 1 | 7.84 |
| CHEMBL2403840 | — | — | 1 | 7.82 |
| CHEMBL2403843 | — | — | 1 | 7.81 |
| CHEMBL2403837 | — | — | 1 | 7.79 |
| CHEMBL2403842 | — | — | 1 | 7.66 |
| CHEMBL2403829 | — | — | 1 | 7.65 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 7.64 |
| CHEMBL2403828 | — | — | 1 | 7.62 |
| CHEMBL2403844 | — | — | 1 | 7.59 |
| CHEMBL2403831 | — | — | 1 | 7.48 |
| CHEMBL2403830 | — | — | 1 | 7.42 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.19 |
| CHEMBL2403838 | — | — | 1 | 7.00 |
| CHEMBL2403839 | — | — | 1 | 6.53 |
| CHEMBL2403832 | — | — | 1 | 5.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL509032 | TAE-684 | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2403845 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL2403841 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL2403836 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL2403827 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL2403834 | — | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL2403849 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL2403846 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL2403848 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL2403847 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL2403833 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL2403835 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL2403840 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL2403843 | — | IC50 | = | 15.6 | nM | 7.81 |
| CHEMBL2403837 | — | IC50 | = | 16.1 | nM | 7.79 |
| CHEMBL2403842 | — | IC50 | = | 21.7 | nM | 7.66 |
| CHEMBL2403829 | — | IC50 | = | 22.4 | nM | 7.65 |
| CHEMBL2403108 | CERITINIB | IC50 | = | 22.8 | nM | 7.64 |
| CHEMBL2403828 | — | IC50 | = | 23.8 | nM | 7.62 |
| CHEMBL2403844 | — | IC50 | = | 25.5 | nM | 7.59 |
| CHEMBL2403831 | — | IC50 | = | 33.3 | nM | 7.48 |
| CHEMBL2403830 | — | IC50 | = | 38.4 | nM | 7.42 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 64.2 | nM | 7.19 |
| CHEMBL2403838 | — | IC50 | = | 100.3 | nM | 7.00 |
| CHEMBL2403839 | — | IC50 | = | 293.5 | nM | 6.53 |
| CHEMBL2403832 | — | IC50 | = | 5510.0 | nM | 5.26 |