Assay Detail
Binding
CHEMBL5553826
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human haspin preincubated for 30 mins followed by ATP and ULight-histone H3 peptide/ULight-eIF4E binding protein addition and measured after 2 hrs by LANCE Ultra TR-FRET assay
31
Total Activities
31
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
A Comprehensive <i>In Vitro</i> Characterization of a New Class of Indole-Based Compounds Developed as Selective Haspin Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.66 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5563528 | — | — | 1 | 8.52 |
| CHEMBL5178368 | — | — | 1 | 8.40 |
| CHEMBL5575484 | — | — | 1 | 8.30 |
| CHEMBL4446681 | — | — | 1 | 8.22 |
| CHEMBL5566424 | — | — | 1 | 8.15 |
| CHEMBL5566041 | — | — | 1 | 7.19 |
| CHEMBL5595605 | — | — | 1 | 6.98 |
| CHEMBL5572441 | — | — | 1 | 6.80 |
| CHEMBL5571554 | — | — | 1 | 6.45 |
| CHEMBL5570156 | — | — | 1 | 6.42 |
| CHEMBL5565688 | — | — | 1 | 6.18 |
| CHEMBL5568999 | — | — | 1 | 6.04 |
| CHEMBL5591651 | — | — | 1 | 6.01 |
| CHEMBL5574750 | — | — | 1 | 6.00 |
| CHEMBL5595763 | — | — | 1 | 5.95 |
| CHEMBL5564624 | — | — | 1 | 5.94 |
| CHEMBL5593072 | — | — | 1 | 5.93 |
| CHEMBL5591618 | — | — | 1 | 5.83 |
| CHEMBL5583809 | — | — | 1 | 4.94 |
| CHEMBL5564324 | — | — | 1 | 4.88 |
| CHEMBL5571240 | — | — | 1 | - |
| CHEMBL5564931 | — | — | 1 | - |
| CHEMBL5571306 | — | — | 1 | - |
| CHEMBL5591602 | — | — | 1 | - |
| CHEMBL5574302 | — | — | 1 | - |
| CHEMBL5575275 | — | — | 1 | - |
| CHEMBL5576026 | — | — | 1 | - |
| CHEMBL5563118 | — | — | 1 | - |
| CHEMBL5575835 | — | — | 1 | - |
| CHEMBL5569783 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5563528 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5178368 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5575484 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4446681 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5566424 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5566041 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5595605 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL5572441 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5571554 | — | IC50 | = | 353.0 | nM | 6.45 |
| CHEMBL5570156 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5565688 | — | IC50 | = | 666.0 | nM | 6.18 |
| CHEMBL5568999 | — | IC50 | = | 922.0 | nM | 6.04 |
| CHEMBL5591651 | — | IC50 | = | 975.0 | nM | 6.01 |
| CHEMBL5574750 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5595763 | — | IC50 | = | 1135.0 | nM | 5.95 |
| CHEMBL5564624 | — | IC50 | = | 1148.0 | nM | 5.94 |
| CHEMBL5593072 | — | IC50 | = | 1168.0 | nM | 5.93 |
| CHEMBL5591618 | — | IC50 | = | 1463.0 | nM | 5.83 |
| CHEMBL5583809 | — | IC50 | = | 11590.0 | nM | 4.94 |
| CHEMBL5564324 | — | IC50 | = | 13150.0 | nM | 4.88 |
| CHEMBL5571240 | — | IC50 | - | — | - | |
| CHEMBL5564931 | — | IC50 | - | — | - | |
| CHEMBL5571306 | — | IC50 | - | — | - | |
| CHEMBL5591602 | — | IC50 | - | — | - | |
| CHEMBL5574302 | — | IC50 | = | 0.035 | 10^-4microM | - |
| CHEMBL5575275 | — | IC50 | - | — | - | |
| CHEMBL5576026 | — | IC50 | = | 0.084 | 10^-4microM | - |
| CHEMBL5563118 | — | IC50 | = | 0.002 | 10^-4microM | - |
| CHEMBL5575835 | — | IC50 | = | 1.0 | 10^-5 uM | - |
| CHEMBL5569783 | — | IC50 | - | — | - | |
| CHEMBL5567189 | — | IC50 | - | — | - |