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. Author manuscript; available in PMC: 2021 Aug 10.
Published in final edited form as: Angew Chem Int Ed Engl. 2020 Jun 3;59(33):13865–13870. doi: 10.1002/anie.202004087

Table 3.

Chemical structures and CDKs inhibitory activities of degraders.

graphic file with name nihms-1637531-t0009.jpg
Compound TMX-2138 TMX-2172 ZXH-7035 TMX-2174
CDK1/cyclin B
IC50 (nM)		 8.7 20.3 8.9 8.9
CDK2/cyclin A
IC50 (nM)		 10.9 6.5 2.2 8.1
CDK5/p25
IC50 (nM)		 7.0 6.8 2.6 7.1
CDK4/cyclin D1
IC50 (nM)		 901.0 7390.0 ND[a] 2880.0
CDK6/cyclin D1
IC50 (nM)		 465.0 2220.0 ND 1130.0
CDK7/cyclin H
IC50 (nM)		 286.0 2620.0 ND 343.0
CDK9/cyclin T1
IC50 (nM)		 25.7 2640.0 ND 116.0
[a]

Not determined. All the IC50 values were tested in duplicate, value ranges are shown in Table S2 in the Supporting Information.