Assay Detail
Binding
CHEMBL2014114
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Inhibition of human N-terminal GST-tagged DYRK2 expressed in baculovirus using DYRKtide-F as substrate assessed as inhibition of [33P] incorporation into substrate using [gamma33P]ATP after 10 mins by liquid scintillation counting
18
Total Activities
18
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 2 (CHEMBL4376) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.13 | 5.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2012570 | — | — | 1 | 5.32 |
| CHEMBL2012568 | — | — | 1 | 5.31 |
| CHEMBL2012567 | — | — | 1 | 5.16 |
| CHEMBL2012571 | — | — | 1 | 5.10 |
| CHEMBL2012575 | — | — | 1 | 5.07 |
| CHEMBL2012574 | — | — | 1 | 4.82 |
| CHEMBL2012558 | — | — | 1 | - |
| CHEMBL2012573 | — | — | 1 | - |
| CHEMBL2012572 | — | — | 1 | - |
| CHEMBL2012559 | — | — | 1 | - |
| CHEMBL2012560 | — | — | 1 | - |
| CHEMBL2012569 | — | — | 1 | - |
| CHEMBL2012561 | — | — | 1 | - |
| CHEMBL2012562 | — | — | 1 | - |
| CHEMBL2012566 | — | — | 1 | - |
| CHEMBL2012565 | — | — | 1 | - |
| CHEMBL2012564 | — | — | 1 | - |
| CHEMBL2012563 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2012570 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL2012568 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL2012567 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL2012571 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL2012575 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL2012574 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2012558 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2012573 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2012572 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2012559 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2012560 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2012569 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2012561 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2012562 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2012566 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2012565 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2012564 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2012563 | — | IC50 | > | 10000.0 | nM | - |