Assay Detail
Binding
CHEMBL5042273
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Inhibition of recombinant human full length N-terminal GST-fused MPS1 (1 to 857 residues) using histone H3 as substrate by TR-FRET assay
6
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.98 | 8.04 |
| Ki | 1 | 9.08 | 9.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5094006 | — | — | 2 | 9.08 |
| CHEMBL5077230 | — | — | 1 | 8.04 |
| CHEMBL2140523 | — | — | 1 | 8.01 |
| CHEMBL4449557 | — | — | 1 | - |
| CHEMBL4456085 | BAY-1217389 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5094006 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL5077230 | — | IC50 | = | 9.06 | nM | 8.04 |
| CHEMBL2140523 | — | IC50 | = | 9.79 | nM | 8.01 |
| CHEMBL5094006 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4449557 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL4456085 | BAY-1217389 | IC50 | < | 1.0 | nM | - |