Assay Detail
Binding
CHEMBL5042245
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Displacement of tracer K9 from NanoLuc-fused MPS1 (unknown origin) expressed in HEK293T cells measured after 2 hrs by NanoBRET assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| 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 | 7.46 | 8.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4449557 | — | — | 1 | 8.33 |
| CHEMBL5094006 | — | — | 1 | 7.65 |
| CHEMBL5077230 | — | — | 1 | 7.49 |
| CHEMBL2140523 | — | — | 1 | 6.37 |
| CHEMBL4456085 | BAY-1217389 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4449557 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5094006 | — | IC50 | = | 22.4 | nM | 7.65 |
| CHEMBL5077230 | — | IC50 | = | 32.7 | nM | 7.49 |
| CHEMBL2140523 | — | IC50 | = | 429.0 | nM | 6.37 |
| CHEMBL4456085 | BAY-1217389 | IC50 | < | 1.0 | nM | - |