Table 1 Summary of EN inhibitor IC50, Kd, and retrotransposition efficiency values

From: Identification and characterization of small molecule inhibitors of the LINE-1 retrotransposon endonuclease

Name

IC50 (μM)

Kd (μM)

Retrotransposition efficiency (%)

AD2

104.0 ± 8.8

82.9 ± 34.5

50 µM: 98.0 ± 22.9

AD3

114.4 ± 22.7

11.9 ± 7.9

20 µM: 59.0 ± 22.4

AD5

16.1 ± 5.4

1.4 ± 0.2

10 µM: 89.7 ± 14.0

AD7

866.4 ± 249.3

230.4 ± 60.2

20 µM: 42.2 ± 23.9

AD9

468.2 ± 117.8

5.9 ± 2.5

50 µM: 21.9 ± 10.9

AD11

4.0 ± 1.2

11.3 ± 7.4

50 µM: 52.2 ± 14.4

AD12

671.2 ± 139.6

755.7 ± 398.7

50 µM: 17.7 ± 1.9

AD13

25.0 ± 4.9

22.5 ± 11.2

20 µM: 75.4 ± 30.7

AD14

6.0 ± 1.7

23.0 ± 9.5

25 µM: 71.6 ± 10.4

AD16

5.8 ± 1.0

9.6 ± 1.8

25 µM: 59.2 ± 21.7

AD17

46.6 ± 7.3

41.4 ± 13.0

5 µM: 94.8 ± 15.8

AD18

76.3 ± 8.5

6.8 ± 2.8

10 µM: 92.2 ± 16.4

AD28

420.7 ± 30.9

14.7 ± 3.7

Toxicity at 2.5 μM

AD29

28.8 ± 3.2

139.5 ± 42.2

50 µM: 85.8 ± 7.9

AD32

458.7 ± 82.6

N.D.

25 µM: 35.1 ± 16.5

AD34

12.5 ± 4.2

1.8 ± 0.4

25 µM: 104.3 ± 7.8

AD36

865.7 ± 300.1

242.9 ± 36.9

25 µM: 42.9 ± 22.2

AD41

514.2 ± 156.1

N.D.

25 µM: 129.4 ± 12.0

AD43

722.2 ± 135.3

516.4 ± 44.0

50 µM: 57.3 ± 9.0

AD50

290.6 ± 13.0

207.6 ± 42.7

25 µM: 100.5 ± 15.0

  1. IC50 values were calculated from at least 3 independent experiments of the fluorescent oligonucleotide nicking assay and are shown as mean ± s.d. Kd values were calculated from at least 3 independent spectral shift experiments and are shown as mean ± s.d. N.D., binding not detected. Retrotransposition efficiencies calculated as percent of the no inhibitor control were obtained from at least 3 independent experiments and are shown as mean ± s.d. Individual values used to calculate mean ± s.d values shown here can be found in the Source Data file.
Back to article page