Table 1 Characterization of newly developed Ko143 analogs

From: Inhibition of ABCG2 prevents phototoxicity in a mouse model of erythropoietic protoporphyria

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Cpd

R

IC50 (μM)

CC50 (μM)

Stability in HLM (% remaining)

30 min

60 min

Ko143

0.18 ± 0.08

22.3 ± 0.6

6 ± 0.8

2 ± 1

K16

-OBzl

0.12 ± 0.01

49.6 ± 2.8

22 ± 4

9 ± 2

K17

-OH

15% @ 1 μM

N.D.

N.D.

N.D.

K3

0.18 ± 0.12

58.9 ± 5.3

74 ± 25

60 ± 3

K23

0.13 ± 0.07

46.6 ± 0.9

45 ± 2

26 ± 2

K25

3.14 ± 1.42

26.5 ± 2.5

N.D.

N.D.

K31

0.27 ± 0.04

> 100

65 ± 3

49 ± 9

K33

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0.25 ± 0.06

31.1 ± 3.7

37 ± 3

18 ± 1

  1. All data are expressed as mean ± SD (n ≥ 3). Source data are provided as a Source Data file.
  2. IC50 half-maximal inhibitory concentration on ABCG2, CC50 half-cytotoxic concentration, HLM human liver microsomes, N.D. not determined.
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