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. 2018 Jun 11;9(7):1093–1104. doi: 10.1039/c8md00140e

Table 4. SAR examples of reported inhibitors.

Entry Active Inactive Assay Mode of inhibition
1 Inline graphic C1 Inline graphic UM-C1 Ubiquitylation Block phospho-p27 binding to Skp2–Cks1
Inline graphic Neg-3
Inline graphic Neg-5
2 Inline graphic C2 Inline graphic UM-C2a Ubiquitylation Block phospho-p27 binding to Skp2–Cks1
Inline graphic UM-C2b
3 Inline graphic 25 Inline graphic 25-12 Ubiquitylation Block Skp2–Skp1 association
Inline graphic 25-5 Inline graphic 25-1
4 Inline graphic 22d Inline graphic 23a Cks1–Skp2 interaction Block Skp2–Cks1 interaction
Inline graphic 22c Inline graphic 4
Inline graphic 1
5 Inline graphic Compound A Inline graphic 3h HeLa cell proliferation Block Skp2–Skp1 interaction
8 Inline graphic Q857 Inline graphic 3h AlphaScreen PPI assay Block Skp2–Cks1 interaction
Inline graphic NSC689857
Inline graphic MHQ