Assay Detail
Binding
CHEMBL2188996
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant GST-fused DYRK1A expressed in Escherichia coli using KKISGRLSPIMTEQ as substrate and [gamma-33P]-ATP after 30 mins by scintillation counting
28
Total Activities
28
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 |
Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A (CHEMBL2292) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel tetrahydropyrido[1,2-a]isoindolone derivatives (valmerins): potent cyclin-dependent kinase/glycogen synthase kinase 3 inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 5.39 | 5.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2180844 | — | — | 1 | 5.75 |
| CHEMBL2180868 | — | — | 1 | 5.62 |
| CHEMBL2180852 | — | — | 1 | 5.47 |
| CHEMBL2180855 | — | — | 1 | 5.46 |
| CHEMBL2180851 | — | — | 1 | 5.25 |
| CHEMBL2180854 | — | — | 1 | 5.12 |
| CHEMBL2180858 | — | — | 1 | 5.09 |
| CHEMBL2180846 | — | — | 1 | - |
| CHEMBL2180843 | — | — | 1 | - |
| CHEMBL2180847 | — | — | 1 | - |
| CHEMBL2180848 | — | — | 1 | - |
| CHEMBL2180849 | — | — | 1 | - |
| CHEMBL2180850 | — | — | 1 | - |
| CHEMBL2180853 | — | — | 1 | - |
| CHEMBL2180856 | — | — | 1 | - |
| CHEMBL2180857 | — | — | 1 | - |
| CHEMBL2180859 | — | — | 1 | - |
| CHEMBL2180870 | — | — | 1 | - |
| CHEMBL2180869 | — | — | 1 | - |
| CHEMBL2180845 | — | — | 1 | - |
| CHEMBL2180867 | — | — | 1 | - |
| CHEMBL2180866 | — | — | 1 | - |
| CHEMBL2180865 | — | — | 1 | - |
| CHEMBL2180861 | — | — | 1 | - |
| CHEMBL2180864 | — | — | 1 | - |
| CHEMBL2180860 | — | — | 1 | - |
| CHEMBL2180862 | — | — | 1 | - |
| CHEMBL2180863 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2180844 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL2180868 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2180852 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL2180855 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL2180851 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL2180854 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL2180858 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL2180846 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180843 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180847 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180848 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180849 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180850 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180853 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180856 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180857 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180859 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180870 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180869 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180845 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180867 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180866 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180865 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180861 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180864 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180860 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180862 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180863 | — | IC50 | > | 10000.0 | nM | - |