. 2010 Dec 29;2(2):107–112. doi: 10.1021/ml100306h

Table 1. SAR of Thiazolopyridine Analogues^a.

graphic file with name ml-2010-00306h_0005.jpg

compd	X	Y	Z	hS1P₁ RI EC₅₀, μM (% efficacy)	hS1P₃ Ca²⁺ EC₅₀, μM (% efficacy)
3a	CH	CH	CH	0.041 (102)	1.21 (24)
3b	N	CH	CH	0.144 (106)	10.1 (63)
3c	CH	N	CH	0.429 (115)	>25
3d	CH	CH	N	0.138 (125)	2.89 (36)
4a	CH	CH	CH	0.221 (84)	3.47 (50)
4b	N	CH	CH	1.60 (75)	>25
4c	CH	N	CH	3.98 (77)	5.46 (64)
4d	CH	CH	N	0.199 (92)	0.478 (94)

Data represents an average of at least two determinations. % efficacy is reported relative to 1.00 μM 1-(4-(6-benzylbenzofuran-2-yl)-3-fluorobenzyl)azetidine-3-carboxylic acid and 0.200 μM S1P for hS1P₁ RI and hS1P₃ Ca²⁺ assays, respectively; >[highest concentration tested] is reported for compounds that do not achieve >10% of control activity. For statistical analysis, see the Supporting Information.

Table 1. SAR of Thiazolopyridine Analoguesa.

Table 1. SAR of Thiazolopyridine Analogues^a.