Assay Detail
Toxicity
CHEMBL5160033
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Inhibition of human Haspin kinase domain using histone H3 biotin peptide as substrate preincubated with enzyme for 30 mins followed by substrate and ATP addition for 90 mins by luminescence based analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Toxicity |
| 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
Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.47 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5201780 | — | — | 1 | 8.52 |
| CHEMBL5201904 | — | — | 1 | 8.30 |
| CHEMBL5179988 | — | — | 1 | 7.96 |
| CHEMBL5187817 | — | — | 1 | 7.50 |
| CHEMBL5192443 | — | — | 1 | 7.35 |
| CHEMBL5187610 | — | — | 1 | 7.11 |
| CHEMBL5170360 | — | — | 1 | 6.85 |
| CHEMBL5195201 | — | — | 1 | 6.70 |
| CHEMBL5207627 | — | — | 1 | 6.16 |
| CHEMBL5204715 | — | — | 1 | 6.11 |
| CHEMBL5200247 | — | — | 1 | 5.89 |
| CHEMBL5181699 | — | — | 1 | 5.88 |
| CHEMBL5189523 | — | — | 1 | 5.76 |
| CHEMBL5189235 | — | — | 1 | 5.39 |
| CHEMBL5173325 | — | — | 1 | 5.30 |
| CHEMBL5196893 | — | — | 1 | 5.28 |
| CHEMBL5173264 | INE-963 | 2.0 | 1 | 5.26 |
| CHEMBL5191906 | — | — | 1 | 5.09 |
| CHEMBL5176864 | — | — | 1 | - |
| CHEMBL5199414 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5201780 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5201904 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5179988 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5187817 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5192443 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5187610 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5170360 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5195201 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5207627 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL5204715 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL5200247 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL5181699 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL5189523 | — | IC50 | = | 1740.0 | nM | 5.76 |
| CHEMBL5189235 | — | IC50 | = | 4040.0 | nM | 5.39 |
| CHEMBL5173325 | — | IC50 | = | 4960.0 | nM | 5.30 |
| CHEMBL5196893 | — | IC50 | = | 5310.0 | nM | 5.28 |
| CHEMBL5173264 | INE-963 | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL5191906 | — | IC50 | = | 8070.0 | nM | 5.09 |
| CHEMBL5176864 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5199414 | — | IC50 | > | 30000.0 | nM | - |