Table 12 Examples of cereblon-based PROTACs from non-classic synthetic approaches

From: Synthesis, biological evaluation and clinical trials of Cereblon-based PROTACs

No.

Chemical structure

Target

Biological activity

Ref.

121

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Sirt

HeLa cells

Dmax > 40%

IC50 = 0.25 µM (enzymatic assay)

169

122

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GSK-3

PC12 cells

Dmax = 65.8%

IC50 = 83.1 nM (enzymatic assay)

175

123

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PD-L1

A375 cells

IC50 = 8.07 µM

Dmax > 50%

176

124

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BRD4

HiBiT-BRD4 HEK293 CRISPR cells

DC50 = 0.3 nM

177

  1. Note:View full size image
  2. BRD4 Bromodomain-containing protein 4, GSK-3 glycogen synthase kinase 3, PD-L1 programmed death-ligand 1, SIRT sirtuin, IC₅₀ half-maximal inhibitory concentration, DC₅₀ half-maximal degradation concentration, Dmax half-maximal achievable degradation.