Assay Detail
Binding
CHEMBL4256643
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human full length N-terminal GST-tagged Aurora B (1 to 344 end residues)/His-tagged INCENP (803 to 918 end residues) expressed in baculovirus expression system using fluorescence-labeled FL-Peptide 21 as substrate after 60 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 | 7 — Homologous single protein target |
| Curated By | Intermediate |
Target
Aurora kinase B/Inner centromere protein (CHEMBL3430907) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 | 4.61 | 5.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4288628 | — | — | 1 | 5.50 |
| CHEMBL4291472 | — | — | 1 | 5.44 |
| CHEMBL4286130 | — | — | 1 | 5.26 |
| CHEMBL1765097 | — | — | 1 | 5.13 |
| CHEMBL4282263 | — | — | 1 | 4.92 |
| CHEMBL4280041 | — | — | 1 | 4.89 |
| CHEMBL4292538 | — | — | 1 | 4.82 |
| CHEMBL4295011 | — | — | 1 | 4.73 |
| CHEMBL302219 | — | — | 1 | 4.59 |
| CHEMBL4292942 | — | — | 1 | 4.48 |
| CHEMBL1738828 | — | — | 1 | 4.39 |
| CHEMBL4280308 | — | — | 1 | 4.38 |
| CHEMBL12856 | INAMRINONE | 4.0 | 1 | 4.23 |
| CHEMBL4291350 | — | — | 1 | 4.19 |
| CHEMBL1605269 | — | — | 1 | 4.15 |
| CHEMBL1201292 | — | — | 1 | 4.01 |
| CHEMBL4282410 | — | — | 1 | 3.99 |
| CHEMBL4286709 | — | — | 1 | 3.80 |
| CHEMBL4281678 | — | — | 1 | - |
| CHEMBL4279867 | — | — | 1 | - |
| CHEMBL4278218 | — | — | 1 | - |
| CHEMBL4285109 | — | — | 1 | - |
| CHEMBL4278538 | — | — | 1 | - |
| CHEMBL189 | MILRINONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4288628 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL4291472 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL4286130 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL1765097 | — | Ki | = | 7400.0 | nM | 5.13 |
| CHEMBL4282263 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL4280041 | — | Ki | = | 12900.0 | nM | 4.89 |
| CHEMBL4292538 | — | Ki | = | 15100.0 | nM | 4.82 |
| CHEMBL4295011 | — | Ki | = | 18700.0 | nM | 4.73 |
| CHEMBL302219 | — | Ki | = | 25700.0 | nM | 4.59 |
| CHEMBL4292942 | — | Ki | = | 32900.0 | nM | 4.48 |
| CHEMBL1738828 | — | Ki | = | 41000.0 | nM | 4.39 |
| CHEMBL4280308 | — | Ki | = | 41700.0 | nM | 4.38 |
| CHEMBL12856 | INAMRINONE | Ki | = | 59300.0 | nM | 4.23 |
| CHEMBL4291350 | — | Ki | = | 63900.0 | nM | 4.19 |
| CHEMBL1605269 | — | Ki | = | 70300.0 | nM | 4.15 |
| CHEMBL1201292 | — | Ki | = | 97200.0 | nM | 4.01 |
| CHEMBL4282410 | — | Ki | = | 102700.0 | nM | 3.99 |
| CHEMBL4286709 | — | Ki | = | 159700.0 | nM | 3.80 |
| CHEMBL4281678 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4279867 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4278218 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4285109 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4278538 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL189 | MILRINONE | Ki | > | 100000.0 | nM | - |