CCT400028 |
CCT400028 : Degrader (PROTAC) of AURKA
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| AURKA |
|
Degrader (PROTAC)
up to 1 uM
Selectivity
In Cell Selectivity Assessment
Potency Assay Off-Target:
Proteomics profiling of CCT400028 in Kelly human pediatric neuroblastoma cells treated with 1 μM of ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
CCT400028 was profiled in the Eurofins scanEDGE kinase binding assay, which contains 97 kinases dist ...
Selectivity Assessment Description:
CCT400028 showed excellent binding selectivity against the 97 kinase panel with Aurora A the only ki ...
Potency Cellular
In Vitro
AURKA
Mode of Action: Degrader (PROTAC)
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.5c03024
Negative Control Compounds
cpd 57
Notes: CRBN-inactive N-methylated version of CCT400028 (57) was unable to reduce Aurora A protein levels at concentrations up to 10 μM in Kelly neuroblastoma cells.
SMILES:
CN1C(=O)CCN(C2=CC=C(C=C2)OCCCCCOCCCCCNC(=O)C3=CC=C(C=C3OC)NC4=NC5=C(CN=C(C6=CC(=CC=C65)Cl)C7=C(C=CC=C7OC)F)C=N4)C1=O
Chemical Information
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