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

In Model Organisms: (0 reviews)
Selectivity
In Vivo
Control Compounds

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
AR
      --

      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

      Orthogonal Probes def

      BAVDEGALUTAMIDE
      ARCC-4
      AKR1C3-PROTAC-5

      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 4.1378000000000075
      HBond acceptors 12
      HBond donors 5
      Atoms 122

      Vendors

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      Expert Reviews


      (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.
      (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....
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