Table 1 Emax values of S1P derivatives at S1P receptors.

From: Ligand chain length drives activation of lipid G protein-coupled receptors

 

C16

C17

S1P

C19

C20

S1P1 (n = 4)

78 ± 6

107 ± 8

100

117 ± 12

n.r.

S1P2 1 (n = 4)

70 ± 6

87 ± 3

100

113 ± 1

113 ± 5

S1P2 2 (n = 3)

54 ± 7

78 ± 1

100

112 ± 6

121 ± 4

S1P4 (n = 4)

206 ± 32

151 ± 12

100

76 ± 3

79 ± 4

S1P5 (n = 2)

32 ± 5

79 ± 6

100

178 ± 45

n.r.

  1. The maximal efficacy for each compound at each S1P subtype was determined from the dose-response curves of the aequorin-based functional assay. Mean values on 2 to 4 independent experiments are normalized on S1P maximal response and expressed in %, along with the corresponding S.E.M. values.
  2. 1S1P5 cells, 2CHO-Aeq cells, n.r. = not reliable.
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