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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 2.

KI values for the tail modified compounds.

graphic file with name nihms293508u1.jpg
Compound Tail Group (R) KI (μM)a
 SphK1 Selectivityb
SphK1 SphK2
2 graphic file with name nihms293508t4.jpg 0.3 6 40
4a graphic file with name nihms293508t5.jpg 6 7.5 2.5
4b graphic file with name nihms293508t6.jpg 5.4 >100 >37
4c graphic file with name nihms293508t7.jpg 9 >100 >22
9a graphic file with name nihms293508t8.jpg 5 38 15
14a graphic file with name nihms293508t9.jpg 0.50 >10 >40
14b graphic file with name nihms293508t10.jpg 1.3 >10 15
9b graphic file with name nihms293508t11.jpg 0.39 12 61
9c graphic file with name nihms293508t12.jpg 0.24 7 58
9d graphic file with name nihms293508t13.jpg 0.80 >20 >50
9e graphic file with name nihms293508t14.jpg 1.5 4.6 6.1
19a graphic file with name nihms293508t15.jpg 0.11 26 470
19b graphic file with name nihms293508t16.jpg 0.45 25 110
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