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. 2014 Mar 25;5(6):634–638. doi: 10.1021/ml4004759

Table 2. Activity of Bivalent Ligands against CB1, OX1, and Coexpressed Receptors.

  Ke (nM) ± SEM
No. linker length (atoms) CB1 vs CP55,940 CB1-OX1 vs CP55,940 CB1-OX1 vs Orexin-A OX1 vs Orexin-A
1   1.1 ± 0.1 1.0 ± 0.6 >10000 >10000
SB334867   >10000 >10000 32 ± 20 45 ± 12
18 15 2100 ± 140 1200 ± 270 >10000 8800 ± 2300
19 15 1800 ± 710 610 ± 16 >10000 8460 ± 680
20 18 1800 ± 1300 110 ± 45 5900 ± 1300 >10000
21 20 1100 ± 500 410 ± 46 >10000 >10000
22 19 1800 ± 680 420 ± 280 4500 ± 2200 3500 ± 1300
24 19 8000 ± 2800 580 ± 260 >10000 8600 ± 1200
26 15 3000 ± 1100 230 ± 11 >10000 5500 ± 1300