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. 2011 Sep 15;21(18):5460–5464. doi: 10.1016/j.bmcl.2011.06.123

Table 1.

Structures of fragments that bind solely H4R (1–3), solely 5-HT3AR (4–6) and both H4R and 5-HT3AR (7–11)

# H4R/5-HT3AR Structure Affinity (pKi)
H4Ra 5-HT3ARc
1 graphic file with name fx2.gif graphic file with name fx3.gif 7.0 ± 0.1 n.a.
2 graphic file with name fx2.gif graphic file with name fx4.gif 6.2 ± 0.1 n.a.
3 graphic file with name fx2.gif graphic file with name fx5.gif 6.7 ± 0.0 n.a.
4 graphic file with name fx6.gif graphic file with name fx7.gif n.a. 6.1 ± 0.2
5 graphic file with name fx6.gif graphic file with name fx8.gif n.a. 6.0 ± 0.0
6 graphic file with name fx6.gif graphic file with name fx9.gif n.a. 6.1 ± 0.1
7 graphic file with name fx10.gif graphic file with name fx11.gif 6.2 ± 0.0 6.6 ± 0.3
8 graphic file with name fx10.gif graphic file with name fx12.gif 7.2 ± 0.0 7.9 ± 0.3
9 graphic file with name fx10.gif graphic file with name fx13.gif 6.1 ± 0.1b 8.8 ± 0.1
10 graphic file with name fx10.gif graphic file with name fx14.gif 8.2 ± 0.1 5.9 ± 0.1
11 graphic file with name fx10.gif graphic file with name fx15.gif 6.2 ± 0.1b 5.9 ± 0.3

n.a.: Non active.

a

Measured by displacement of [3H]histamine binding using membranes of HEK293 cells transiently expressing the human H4R. pKi’s are calculated from at least three independent measurements as the mean ± SEM.

b

Determined using membranes of SK-N-MC cells transiently expressing the human H4R. pKi’s are calculated from at least three independent measurements as the mean ± SEM.

c

pKi: Measured by displacement of [3H]granisetron binding using membranes of HEK293 cells expressing the human 5-HT3AR. pKi’s are calculated from at least two independent measurements as the mean ± SEM.