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PROTAC-AR-Degrader-4 | Degrader (PROTAC) of AR
RATINGS:
Cellular Use: (2 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
AR
      Degrader (PROTAC)
      --

      Selectivity

      Potency
      Cellular
      In Vitro

      AR

      Mode of Action: Degrader (PROTAC)

      Structure-Activity-Relationship data available? Yes

      DOI Reference: 10.1016/j.bmc.2011.09.041

      Chemical Information

      Molecular Formula C43H67N3O9
      SMILEs CC(C)C[C@H](NC(=O)[C@@H](O)[C@H](N)Cc1ccccc1)C(=O)NCCOCCOCCOCC(=O)O[C@H]1CC[C@H]2[C@@H]3CC[C@H]4CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C
      InChI InChI=1S/C43H67N3O9/c1-28(2)24-36(46-41(51)39(49)35(44)25-29-8-6-5-7-9-29)40(50)45-18-19-52-20-21-53-22-23-54-27-38(48)55-37-13-12-33-32-11-10-30-26-31(47)14-16-42(30,3)34(32)15-17-43(33,37)4/h5-9,28,30,32-37,39,49H,10-27,44H2,1-4H3,(H,45,50)(H,46,51)/t30-,32-,33-,34-,35+,36-,37-,39-,42-,43-/m0/s1
      Molecular weight 769.49 Da
      AlogP 4.1378
      HBond acceptors 12
      HBond donors 5
      Atoms 122

      References

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      Expert Reviews

      by SERP
      (on 8 Jul 2022)
      Cellular Use Rating
      This PROTAC was reported to induce partial AR depletion at a relatively high 30 µM compound concentration. More potent AR degraders have been recently reported.
      by SERP+
      (on 31 Oct 2024)
      Cellular Use Rating
      This compound 13 was tested only at one concentration 30uM and it was a partial degradation and looked only at one time point 24hrs. No selectivity or related control or phenotypic control experiment done....
      Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria