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. Author manuscript; available in PMC: 2012 May 26.
Published in final edited form as: J Med Chem. 2011 May 2;54(10):3524–3548. doi: 10.1021/jm2001053

Table 4.

KI values for head group modifications.

Compound Structure KI (μM)a SphK1 Selectivityb
SphK1 SphK2
1 graphic file with name nihms293508t23.jpg 0.2 0.5 5
33 graphic file with name nihms293508t24.jpg 1.6 5 6.3
36a graphic file with name nihms293508t25.jpg 0.13 1.5 24
36b graphic file with name nihms293508t26.jpg 16 5 0.6
38 graphic file with name nihms293508t27.jpg 0.075 3 80
47 graphic file with name nihms293508t28.jpg 0.099 5.3 110
40 graphic file with name nihms293508t29.jpg 0.13 8 130
a

KI = [I]/(K’M/KM - 1); KM of Sphingosine at SphK1 = 10 μM; KM of Sphingosine at SphK2 = 5 μM

b

Selectivity = (KI/KM)SphK2/(KI/KM)SphK1