Assay Detail
Binding
CHEMBL4256642
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length N-terminal His-tagged Aurora A (unknown origin) 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 | 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 | 4.38 | 5.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1765097 | — | — | 1 | 5.58 |
| CHEMBL1738828 | — | — | 1 | 5.48 |
| CHEMBL4288628 | — | — | 1 | 5.12 |
| CHEMBL4286130 | — | — | 1 | 4.83 |
| CHEMBL4291472 | — | — | 1 | 4.76 |
| CHEMBL4292538 | — | — | 1 | 4.67 |
| CHEMBL4282263 | — | — | 1 | 4.52 |
| CHEMBL1605269 | — | — | 1 | 4.17 |
| CHEMBL4280308 | — | — | 1 | 4.12 |
| CHEMBL4295011 | — | — | 1 | 4.05 |
| CHEMBL4282410 | — | — | 1 | 4.00 |
| CHEMBL1201292 | — | — | 1 | 3.90 |
| CHEMBL4291350 | — | — | 1 | 3.73 |
| CHEMBL4286709 | — | — | 1 | 3.44 |
| CHEMBL12856 | INAMRINONE | 4.0 | 1 | 3.40 |
| CHEMBL302219 | — | — | 1 | - |
| CHEMBL4278538 | — | — | 1 | - |
| CHEMBL4285109 | — | — | 1 | - |
| CHEMBL4292942 | — | — | 1 | - |
| CHEMBL4281678 | — | — | 1 | - |
| CHEMBL4279867 | — | — | 1 | - |
| CHEMBL4278218 | — | — | 1 | - |
| CHEMBL189 | MILRINONE | 4.0 | 1 | - |
| CHEMBL4280041 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1765097 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL1738828 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL4288628 | — | Ki | = | 7500.0 | nM | 5.12 |
| CHEMBL4286130 | — | Ki | = | 14900.0 | nM | 4.83 |
| CHEMBL4291472 | — | Ki | = | 17300.0 | nM | 4.76 |
| CHEMBL4292538 | — | Ki | = | 21300.0 | nM | 4.67 |
| CHEMBL4282263 | — | Ki | = | 30200.0 | nM | 4.52 |
| CHEMBL1605269 | — | Ki | = | 66900.0 | nM | 4.17 |
| CHEMBL4280308 | — | Ki | = | 76300.0 | nM | 4.12 |
| CHEMBL4295011 | — | Ki | = | 89600.0 | nM | 4.05 |
| CHEMBL4282410 | — | Ki | = | 99500.0 | nM | 4.00 |
| CHEMBL1201292 | — | Ki | = | 125200.0 | nM | 3.90 |
| CHEMBL4291350 | — | Ki | = | 184700.0 | nM | 3.73 |
| CHEMBL4286709 | — | Ki | = | 361000.0 | nM | 3.44 |
| CHEMBL12856 | INAMRINONE | Ki | = | 393900.0 | nM | 3.40 |
| CHEMBL302219 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4278538 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4285109 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4292942 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4281678 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4279867 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4278218 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL189 | MILRINONE | Ki | > | 100000.0 | nM | - |
| CHEMBL4280041 | — | Ki | > | 100000.0 | nM | - |