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. 2011 Dec 15;3(3):186–192. doi: 10.1021/cn200103n

Table 3. Mutations at Tyr102, Tyr198, Tyr241, and Tyr247a.

  Y102
Y198
Y241
Y247
residues EC50 (μM) nH EC50 (μM) nH EC50 (μM) nH EC50 (μM) nH
Y(wild type) 1.4 ± 0.2 1.6 ± 0.3 1.4 ± 0.2 1.6 ± 0.3 1.4 ± 0.2 1.6 ± 0.3 1.4 ± 0.2 1.6 ± 0.3
F 1.9 ± 0.6 1.1 ± 0.3 12 ± 1b 1.6 ± 0.1 21 ± 1b 1.3 ± 0.1 42 ± 4b 1.5 ± 0.2
A 110 ± 20b 1.2 ± 0.2 2000 ± 200b 1.1 ± 0.1 4900 ± 480b 1.1 ± 0.1 NR  
S 135 ± 25b 1.3 ± 0.3 5600 ± 600b 1.6 ± 0.2 1500 ± 96b 1.2 ± 0.1 NR  
W 860 ± 60b 1.4 ± 0.1 250 ± 30b 1.1 ± 0.1 8.2 ± 1.4b 1.3 ± 0.3 99 ± 8b 1.3 ± 0.1
4-F-Phe 3.1 ± 0.3 1.5 ± 0.2 34 ± 7c 1.9 ± 0.3 1100 ± 370b 0.6 ± 0.1b 90 ± 3b 1.9 ± 0.1
3,5-F2–Phe 6.1 ± 0.9b 1.6 ± 0.3 1700 ± 400c 1.4 ± 0.2 490 ± 190b 1.5 ± 0.3 NR  
3,4,5-F3-Phe 3.4 ± 0.5 1.3 ± 0.2 8400 ± 1000c 1.5 ± 0.1 950 ± 140b 1.3 ± 0.3 NR  
4-Br-Phe 1.6 ± 0.8 1.3 ± 0.4     620 ± 30b 1.8 ± 0.2 2900 ± 170b 1.1 ± 0.1
4-Me-Phe 4.6 ± 2.1 1.4 ± 0.3     140 ± 100b 1.4 ± 0.4 NR  
4-MeO-Phe 180 ± 20b 1.4 ± 0.2 6.6 ± 2c 1.6 ± 0.2 530 ± 50b 1.7 ± 0.2 NR  
3-OH-Phe 66 ± 9b 1.7 ± 0.3     350 ± 70b 1.5 ± 0.4 NR  
a

Data = mean ± SEM, n ≥ 3.

b

Significantly different to wild type, p < 0.05.

c

Previously published (ref (11)).