Assay Detail
Binding
CHEMBL4256641
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Inhibition of full length human Mps1 using fluorescence-labeled H236 peptide as substrate after 60 to 90 mins in presence of ATP by fluorescence assay based Cheng-Prusoff equation analysis
24
Total Activities
24
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
Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 4.44 | 5.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1765097 | — | — | 1 | 5.54 |
| CHEMBL4291472 | — | — | 1 | 5.50 |
| CHEMBL4286130 | — | — | 1 | 5.32 |
| CHEMBL1738828 | — | — | 1 | 5.27 |
| CHEMBL4282263 | — | — | 1 | 4.96 |
| CHEMBL4285109 | — | — | 1 | 4.61 |
| CHEMBL4292538 | — | — | 1 | 4.59 |
| CHEMBL4280308 | — | — | 1 | 4.52 |
| CHEMBL4292942 | — | — | 1 | 4.52 |
| CHEMBL12856 | INAMRINONE | 4.0 | 1 | 4.09 |
| CHEMBL4291350 | — | — | 1 | 4.04 |
| CHEMBL4288628 | — | — | 1 | 4.02 |
| CHEMBL1201292 | — | — | 1 | 4.01 |
| CHEMBL1605269 | — | — | 1 | 3.89 |
| CHEMBL4282410 | — | — | 1 | 3.63 |
| CHEMBL4295011 | — | — | 1 | 3.57 |
| CHEMBL4280041 | — | — | 1 | 3.44 |
| CHEMBL189 | MILRINONE | 4.0 | 1 | - |
| CHEMBL4278538 | — | — | 1 | - |
| CHEMBL302219 | — | — | 1 | - |
| CHEMBL4281678 | — | — | 1 | - |
| CHEMBL4279867 | — | — | 1 | - |
| CHEMBL4278218 | — | — | 1 | - |
| CHEMBL4286709 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1765097 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL4291472 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL4286130 | — | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL1738828 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL4282263 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL4285109 | — | Ki | = | 24800.0 | nM | 4.61 |
| CHEMBL4292538 | — | Ki | = | 25600.0 | nM | 4.59 |
| CHEMBL4280308 | — | Ki | = | 30200.0 | nM | 4.52 |
| CHEMBL4292942 | — | Ki | = | 30100.0 | nM | 4.52 |
| CHEMBL12856 | INAMRINONE | Ki | = | 80800.0 | nM | 4.09 |
| CHEMBL4291350 | — | Ki | = | 91200.0 | nM | 4.04 |
| CHEMBL4288628 | — | Ki | = | 94700.0 | nM | 4.02 |
| CHEMBL1201292 | — | Ki | = | 98100.0 | nM | 4.01 |
| CHEMBL1605269 | — | Ki | = | 128200.0 | nM | 3.89 |
| CHEMBL4282410 | — | Ki | = | 236400.0 | nM | 3.63 |
| CHEMBL4295011 | — | Ki | = | 269300.0 | nM | 3.57 |
| CHEMBL4280041 | — | Ki | = | 367300.0 | nM | 3.44 |
| CHEMBL189 | MILRINONE | Ki | > | 100000.0 | nM | - |
| CHEMBL4278538 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL302219 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4281678 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4279867 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4278218 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4286709 | — | Ki | > | 1000000.0 | nM | - |