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JB170 | JB170 : Degrader (PROTAC) of AURKA
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
AURKA
  • Kd:99 nM
  • Kd:183 ± 22 nM
  • Activity:28 ± 4 nM
  • Dmax:300 nM
Degrader (PROTAC)
300 nM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
Kinobead selectivity profiling in MV4–11 cell lysates. JB170 bound AURORA-A with the lowest Kd (Kdap ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
MV4–11 cells were treated with JB170 (0.1 µM) for 6 h, and the proteins were analyzed by triple-SIL ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
In cell BRET assay shows that JB170 preferentially binds AURORA-A over AURORA-B (AURORA-A EC50 = 193 ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Potency and specificity of JB170 was further evaluated via quantitative MS. On IMR5 cells, JB170 ind ...

Potency
Cellular
In Vitro

AURKA

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/s41589-020-00652-y

Negative Control Compounds

JB211
Notes: JB211 (Cpd 6) did not deplete AURORA-A, but enhanced AURORA-A protein levels
SMILES: O=C(C1=CC=C(NC2=NC(C(C=CC(Cl)=C3)=C3C(C4=C(OC)C=CC=C4F)=NC5)=C5C=N2)C=C1OC)NCCOCCOCCNC(COC(C=CC=C67)=C7C(N(C6=O)C8CCC(N(C)C8=O)=O)=O)=O

Chemical Information

Molecular Formula C48H44ClFN8O11
SMILEs COc1cc(Nc2ncc3c(n2)-c2ccc(Cl)cc2C(c2c(F)cccc2OC)=NC3)ccc1C(=O)NCCOCCOCCNC(=O)COc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O
InChI InChI=1S/C48H44ClFN8O11/c1-65-35-7-4-6-33(50)41(35)43-32-21-27(49)9-11-29(32)42-26(23-53-43)24-54-48(57-42)55-28-10-12-30(37(22-28)66-2)44(61)52-16-18-68-20-19-67-17-15-51-39(60)25-69-36-8-3-5-31-40(36)47(64)58(46(31)63)34-13-14-38(59)56-45(34)62/h3-12,21-22,24,34H,13-20,23,25H2,1-2H3,(H,51,60)(H,52,61)(H,54,55,57)(H,56,59,62)
Molecular weight 962.28 Da
AlogP 0.0
HBond acceptors 19
HBond donors 4
Atoms 113

References

Publications

Cross References

canSARChEMBLBindingDB

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Expert Reviews

by SERP
(on 6 Apr 2025 )
Cellular Use Rating
Good specificity Aurora A degrader (only protein significantly degraded out of ~4K quantified by proteomics). Degradation is however incomplete and there are some emerging newer degraders available that...
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