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Table 1 On and off target profile of novel 1-derivative ligands

From: Identification of novel RHPS4-derivative ligands with improved toxicological profiles and telomere-targeting activities

Compound ID

Off target receptor profile

DNA Affinity & Selectivity (Measured by SPR)

Cancer cell activity

”Normal” Cell activity

 

Muscarinic (M2) % inh @1μM

β2 adrenergic %inh @1 μM

hERG % inh @10 μM

Quadruplex DNA affinity Kx106M-1

Duplex DNA affinity Kx106M-1

Quadruplex/duplex ratio

HT-29 (GI50/μm)

WI-38 (GI50/μM)

Ratio PMX WI38 /HT29

1

98

100

100

9.0

0.6

16.3

0.62

7.2

11,6

2

98

11

41

4.2

0,2

21

0.10

3.11

31,1

3

98,0

13

74,0

22,0

0,1

244,4

0,70

13,04

18,5

4

65

1

15

7.4

1,1

6,7

1,63

17.3

10,6

5

93

10

16

23

<0,1

>230

1,83

>30

ND

6

77

8

35

14,7

0,7

21

0,26

22,3

85,7

7

92

0

37

29,3

0,9

32,6

0,28

9.36

33,4

8

99

2

40

14,2

0,9

15,8

0,75

25,12

33,5

9

24

NE

86

1,5

<0,1

>15

0,21

5,11

24,3

10

49

NE

95

1,0

<0,1

>10

0,13

6,17

47,5