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. Author manuscript; available in PMC: 2019 Mar 13.
Published in final edited form as: Biochem Pharmacol. 2016 Jan 28;110-111:1–15. doi: 10.1016/j.bcp.2016.01.021

Table 3.

Structures and relative FFA4 versus FFA1 potencies of synthetic FFA4 agonists expressed as nanomolar potency and (pEC50 ± S.D). Values are for human receptors and for FFA4-S unless noted. N.R. denotes data that are not reported.

Agonist Ca+2 mobilization β-arrestin BRET References
FFA1
nM / (pEC50 ± SD)		 FFA4
nM / (pEC50 ± SD)		 FFA1
nM / (pEC50 ± SD)		 FFA4
nM / (pEC50 ± SD)
graphic file with name nihms-1004808-t0013.jpg
GW9508 		48 / (7.32 ± 0.03) 3467 / (5.46 ± 0.09) [75]
1950 / (5.71 ± 0.02) 912 / (6.04 ± 0.04) [14]
851 / (6.07 ± 0.08) 48 / (7.32 ± 0.20) 933 / (6.03 ± 0.03) [17]
28 / (7.55 ± 0.15) 1412 / (5.85 ± 0.05) [77]
graphic file with name nihms-1004808-t0014.jpg
NCG21 		19,054 / (4.72)* 1260 / (5.9)* [76]
74,131 / (4.13 ± 0.13) 9120 / (5.04 ± 0.10) 23,442 / (4.63 ± 0.15) 1905 / (5.72 ± 0.08) [17]
9772 / (5.01 ± 0.23) 2398 / (5.62 ± 0.10) [77]
graphic file with name nihms-1004808-t0015.jpg
TUG-891 		537 / ( 6.27 ± 0.02) 72 / (7.14 ± 0.04) [14]
64,565 / (4.19 ± 0.97) 44 / (7.36 ± 0.15) [77]
5011 / (5.30 ± 0.04) 93 / (7.02 ± 0.09) 65 / (7.19 ± 0.07) [17]
graphic file with name nihms-1004808-t0016.jpg
GSK137647A 		< 32,000 / (< 4.5) 501 / (6.3 ± 0.2) N.R. N.R. [78]
graphic file with name nihms-1004808-t0017.jpg
cpdA 		Negligible effect 24 / (7.62 ± 0.11) N.R. 347 / (6.46) [9]
*

Utilized Gα16 fused receptor construct, putatively FFA4-L