Assay Detail
Binding
CHEMBL973503
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Inhibition of Aurora A in human HCT116 cells assessed as complete loss of phospho-Aurora A staining in centrosomes by immunofluorescence assay
6
Total Activities
6
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
A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.75 | 6.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | 6.51 |
| CHEMBL508307 | — | — | 1 | 5.60 |
| CHEMBL502124 | — | — | 1 | 5.60 |
| CHEMBL521949 | — | — | 1 | 5.30 |
| CHEMBL507170 | — | — | 1 | - |
| CHEMBL523991 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL259084 | MLN-8054 | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL508307 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL502124 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL521949 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL507170 | — | IC50 | - | — | - | |
| CHEMBL523991 | — | IC50 | - | — | - |