Assay Detail
Binding
CHEMBL3811380
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Inhibition of wild type Myc-ectopic MPS1 (unknown origin) expressed in human HCT116 cells assessed as autophosphorylation at Thr33/Ser37 after 2 hrs by electrochemiluminescence assay in presence of MG132
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.18 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3109945 | — | — | 1 | 7.37 |
| CHEMBL3809829 | — | — | 1 | 7.23 |
| CHEMBL3809252 | — | — | 1 | 6.85 |
| CHEMBL3809210 | — | — | 1 | 6.72 |
| CHEMBL3808500 | — | — | 1 | 6.66 |
| CHEMBL3809925 | — | — | 1 | 6.37 |
| CHEMBL3809186 | — | — | 1 | 6.32 |
| CHEMBL3809656 | — | — | 1 | 6.22 |
| CHEMBL3809287 | — | — | 1 | 6.19 |
| CHEMBL3809219 | — | — | 1 | 5.66 |
| CHEMBL3808838 | — | — | 1 | 5.59 |
| CHEMBL3808471 | — | — | 1 | 5.58 |
| CHEMBL3809446 | — | — | 1 | 5.56 |
| CHEMBL3810175 | — | — | 1 | 5.32 |
| CHEMBL3808564 | — | — | 1 | 5.11 |
| CHEMBL3809531 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3109945 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3809829 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3809252 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3809210 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3808500 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3809925 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL3809186 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3809656 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3809287 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL3809219 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3808838 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL3808471 | — | IC50 | = | 2640.0 | nM | 5.58 |
| CHEMBL3809446 | — | IC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL3810175 | — | IC50 | = | 4840.0 | nM | 5.32 |
| CHEMBL3808564 | — | IC50 | = | 7810.0 | nM | 5.11 |
| CHEMBL3809531 | — | IC50 | > | 10000.0 | nM | - |