Assay Detail
Binding
CHEMBL3862723
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged human Aurora A kinase (122 to 40 residues) expressed in Escherichia coli BL21 (DE3) Rosetta cells using biotinylated STK2 substrate incubated for 30 mins by HTRF assay
50
Total Activities
50
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 a Selective Aurora A Kinase Inhibitor by Virtual Screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 50 | 6.27 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL483158 | ALISERTIB | 3.0 | 1 | 10.40 |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | 10.19 |
| CHEMBL3921246 | — | — | 1 | 8.70 |
| CHEMBL3915550 | — | — | 1 | 8.40 |
| CHEMBL3932394 | — | — | 1 | 8.22 |
| CHEMBL3904239 | — | — | 1 | 8.21 |
| CHEMBL3985313 | — | — | 1 | 8.21 |
| CHEMBL3896597 | — | — | 1 | 7.62 |
| CHEMBL3903187 | — | — | 1 | 7.60 |
| CHEMBL3975102 | — | — | 1 | 6.89 |
| CHEMBL3941377 | — | — | 1 | 6.72 |
| CHEMBL3924918 | — | — | 1 | 6.72 |
| CHEMBL3913242 | — | — | 1 | 6.66 |
| CHEMBL3951166 | — | — | 1 | 6.52 |
| CHEMBL3939478 | — | — | 1 | 6.43 |
| CHEMBL3935395 | — | — | 1 | 6.42 |
| CHEMBL3984254 | — | — | 1 | 6.41 |
| CHEMBL3923442 | — | — | 1 | 6.37 |
| CHEMBL3941909 | — | — | 1 | 6.32 |
| CHEMBL3983087 | — | — | 1 | 6.22 |
| CHEMBL3938394 | — | — | 1 | 6.11 |
| CHEMBL3924626 | — | — | 1 | 5.89 |
| CHEMBL3911508 | — | — | 1 | 5.80 |
| CHEMBL3956916 | — | — | 1 | 5.72 |
| CHEMBL3914435 | — | — | 1 | 5.70 |
| CHEMBL3949078 | — | — | 1 | 5.64 |
| CHEMBL3967949 | — | — | 1 | 5.48 |
| CHEMBL3921919 | — | — | 1 | 5.46 |
| CHEMBL3974813 | — | — | 1 | 5.46 |
| CHEMBL3984529 | — | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL483158 | ALISERTIB | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL3600873 | MK-5108 | IC50 | = | 0.064 | nM | 10.19 |
| CHEMBL3921246 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3915550 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3932394 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3904239 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3985313 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3896597 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3903187 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3975102 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3941377 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3924918 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3913242 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3951166 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3939478 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3935395 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3984254 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3923442 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL3941909 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3983087 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3938394 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL3924626 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL3911508 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3956916 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3914435 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3949078 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3967949 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3921919 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3974813 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3984529 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL3976213 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL3920194 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL3955906 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL3905664 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL3982818 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3915966 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3981269 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3902875 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL3966317 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL3930861 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL3929346 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL3915641 | — | IC50 | = | 76000.0 | nM | 4.12 |
| CHEMBL3903930 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3912939 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL3894995 | — | IC50 | - | — | - | |
| CHEMBL3947173 | — | IC50 | - | — | - | |
| CHEMBL3962294 | — | IC50 | - | — | - | |
| CHEMBL3893267 | — | IC50 | > | 70000.0 | nM | - |
| CHEMBL3970952 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL3985380 | — | IC50 | > | 200000.0 | nM | - |