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. 2017 Jul 14;2(7):3616–3631. doi: 10.1021/acsomega.7b00451

Table 1. Binding Data at NPY Receptor Subtypes.

  Y1R Y2R Y4R Y5R
compd Ki [nM]a Ki [nM]b Ki [nM]c Ki [nM]d
hPP 440e >5000e 0.65f 17e
(2R,7R)-1 440f 830f 0.45f 1500f
2 720f 1700f 3.5f 280f
3 >5000 >5000 337 ± 110 >5000
4 24g 920g 660f >5000g
(2R,7R)-26 1840 ± 380 >5000 30.8 ± 7.5 >5000
27 574 ± 49 >5000 134 ± 20 2700 ± 490
28 n.d. n.d. 130 ± 39 n.d.
29 3730 ± 350 >5000 52.7 ± 7.1 3560 ± 440
30 n.d. n.d. 385 ± 127 n.d.
31 53 ± 12 3270 ± 870 113 ± 14 2100 ± 240
33 589 ± 120 >5000 56.9 ± 5.3 3440 ± 210
34 >5000 >5000 19.5 ± 2.6 >5000
35 4830 ± 1400 >5000 2.87 ± 0.78 >5000
36 1180 ± 380 >5000 3.43 ± 1.3 >5000
37 1120 ± 270 >5000 501 ± 200 >5000
38 >5000 >5000 724 ± 140 >5000
39 >5000 >5000 568 ± 76 >5000
40 >5000 >5000 248 ± 23 >5000
41 >5000 >5000 10.4 ± 3.3 >5000
42 >5000 >5000 40.5± 15 >5000
43 >5000 >5000 >5000 >5000
44 >5000 >5000 1650 ± 290 >5000
a

Radioligand competition binding assay with 46(22) (Kd = 6.2 nM, c = 4 nM) using MCF-7-hY1 cells.23

b

Radioligand competition binding assay with [3H]propionyl-pNPY24 (Kd = 1.4 nM, c = 1 nM) using CHO-hY2-Gqi5-mtAEQ cells.25

c

Radioligand competition binding assay with 45(11) (Kd = 0.67 nM, c = 0.6 nM) using CHO-hY4R-Gqi5-mtAEQ cells.26

d

Radioligand competition binding assay with [3H]propionyl-pNPY (Kd = 4.83 nM, c = 4 nM) using HEC-1b hY5R cells.27

e

Ki value reported by Berlicki et al.6

f

Ki value reported by Kuhn et al.11

g

Ki value reported by Keller et al.5 Presented are mean values ± SEM from at least three independent experiments (performed in triplicate). n.d.: not determined.