Table 2 Structure-activity relationship of UM171 analogues in the degradation of CoREST1 and LSD1 in HEK 293 cells

From: Structural mimicry of UM171 and neomorphic cancer mutants co-opts E3 ligase KBTBD4 for HDAC1/2 recruitment

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No

R1

R2

R3

R4

LSD1 rel level* / %

CoREST1 rel level* / %

1 (UM171)

H

28 ± 2

22 ± 5

2

H

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>100

>100

3

H

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>100

>100

4

H

17 ± 6

5 ± 0.1

5

H

>100

95 ± 10

6

H

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>100

>100

7

H

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92 ± 25

>100

8

H

H

41 ± 11

45 ± 18

9

H

29 ± 4

21 ± 6

10

H

98 ± 23

90 ± 24

11

H

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31 ± 3

14 ± 6

12

H

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46 ± 12

36 ± 9

13(S234984)

H

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15 ± 5

5 ± 0.3

14

H

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27 ± 9

4 ± 1

15

N/A

N/A

N/A

N/A

>100

>100

  1. *The immunoblots of corresponding proteins were quantified and normalised to the GAPDH loading controls. The relative protein levels were calculated in relation to the DMSO controls on the same blot (n = 3; errors represent S.E.M.). Source data are provided in the Source Data file.
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