CCT400028

CCT400028 : Degrader (PROTAC) of AURKA

Structure

SERP Rating

Probe CCT400028 is in the process of SERP review.

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Information

AURKA

Degrader (PROTAC)

up to 1 uM

In Vitro Validations

Uniprot ID: O14965

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency Value: ECmax 620 nM

Potency Assay: Aurora A/PROTAC/CRBN ternary complexes was assessed in the TR- FRET assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Aurora kinase A, STK6, STK15, IAK1, BTAK, AYK1, AU ...

DOI Reference: 10.1021/acs.jmedchem.5c03024

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay, off target (cells): Proteomics profiling of CCT400028 in Kelly human pediatric neuroblastoma cells treated with 1 μM of compound for 4 h shows only degradation for AURKA.

Potency assay (off target): CCT400028 was profiled in the Eurofins scanEDGE kinase binding assay, which contains 97 kinases distributed across the kinome.

Probe Selectivity in Vitro:

CCT400028 showed excellent binding selectivity against the 97 kinase panel with Aurora A the only kinase that CCT400028 bound to potently (<35% control binding remaining) at 1 μM. Within the Aurora kinase family, CCT400028 showed high selectivity for Aurora A with no measurable affinity for Aurora C and a 28-fold selectivity over Aurora B. CCT400028 would therefore not be expected to affect Aurora B activity in cells due to its weak affinity for Aurora B (2100 nM).

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