Assay Detail
Binding
CHEMBL2014113
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Inhibition of human recombinant N-terminal MBP-tagged haspin kinase expressed in Escherichia coli DE3 after 10 mins by TR-FRET assay
20
Total Activities
20
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
Serine/threonine-protein kinase haspin (CHEMBL1075163) ↗| 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 | 20 | 6.31 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2012574 | — | — | 1 | 7.00 |
| CHEMBL2012563 | — | — | 1 | 6.80 |
| CHEMBL2012559 | — | — | 1 | 6.77 |
| CHEMBL2012562 | — | — | 1 | 6.72 |
| CHEMBL2012575 | — | — | 1 | 6.66 |
| CHEMBL2012569 | — | — | 1 | 6.66 |
| CHEMBL2012560 | — | — | 1 | 6.52 |
| CHEMBL2012572 | — | — | 1 | 6.47 |
| CHEMBL2012558 | — | — | 1 | 6.34 |
| CHEMBL2012561 | — | — | 1 | 6.34 |
| CHEMBL2012573 | — | — | 1 | 6.33 |
| CHEMBL2012570 | — | — | 1 | 6.30 |
| CHEMBL2012564 | — | — | 1 | 6.24 |
| CHEMBL269538 | HARMINE | 1.0 | 1 | 6.23 |
| CHEMBL2012565 | — | — | 1 | 6.16 |
| CHEMBL486817 | HARMOL | — | 1 | 6.11 |
| CHEMBL2012571 | — | — | 1 | 6.08 |
| CHEMBL2012568 | — | — | 1 | 5.62 |
| CHEMBL2012567 | — | — | 1 | 5.57 |
| CHEMBL2012566 | — | — | 1 | 5.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2012574 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2012563 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2012559 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2012562 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2012575 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2012569 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2012560 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2012572 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL2012558 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL2012561 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL2012573 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL2012570 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2012564 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL269538 | HARMINE | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL2012565 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL486817 | HARMOL | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL2012571 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL2012568 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2012567 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL2012566 | — | IC50 | = | 4600.0 | nM | 5.34 |