Assay Detail
Binding
CHEMBL5362954
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Inhibition of Mps1 (unknown origin) pretreated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-glo kinase assay
20
Total Activities
19
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 |
Publication
Discovery of pyrazolo[3,4-b]pyridine derivatives as novel and potent Mps1 inhibitors for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 8.12 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5410634 | — | — | 1 | 8.59 |
| CHEMBL5410080 | — | — | 1 | 8.47 |
| CHEMBL5417870 | — | — | 1 | 8.42 |
| CHEMBL5410578 | — | — | 1 | 8.39 |
| CHEMBL5397510 | — | — | 1 | 8.31 |
| CHEMBL4456085 | BAY-1217389 | 1.0 | 2 | 8.31 |
| CHEMBL5428851 | — | — | 1 | 8.21 |
| CHEMBL5429411 | — | — | 1 | 8.07 |
| CHEMBL2140523 | — | — | 1 | 7.46 |
| CHEMBL5440897 | — | — | 1 | - |
| CHEMBL5420207 | — | — | 1 | - |
| CHEMBL5399816 | — | — | 1 | - |
| CHEMBL5413129 | — | — | 1 | - |
| CHEMBL5436525 | — | — | 1 | - |
| CHEMBL5413333 | — | — | 1 | - |
| CHEMBL5414333 | — | — | 1 | - |
| CHEMBL5434037 | — | — | 1 | - |
| CHEMBL5396072 | — | — | 1 | - |
| CHEMBL5434294 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5410634 | — | IC50 | = | 2.596 | nM | 8.59 |
| CHEMBL5410080 | — | IC50 | = | 3.371 | nM | 8.47 |
| CHEMBL5417870 | — | IC50 | = | 3.808 | nM | 8.42 |
| CHEMBL5410578 | — | IC50 | = | 4.026 | nM | 8.39 |
| CHEMBL5397510 | — | IC50 | = | 4.842 | nM | 8.31 |
| CHEMBL4456085 | BAY-1217389 | IC50 | = | 4.842 | nM | 8.31 |
| CHEMBL5428851 | — | IC50 | = | 6.14 | nM | 8.21 |
| CHEMBL5429411 | — | IC50 | = | 8.516 | nM | 8.07 |
| CHEMBL2140523 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4456085 | BAY-1217389 | IC50 | = | 121.1 | nM | 6.92 |
| CHEMBL5440897 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5420207 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5399816 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5413129 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5436525 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5413333 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5414333 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5434037 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5396072 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5434294 | — | IC50 | > | 1000.0 | nM | - |