TABLE 2

Kiapp values for the inhibition of hiCE, hCE1, rCE, hAChE, or hBChE after preincubation of the enzymes with the TFK analogs for 5 min

Data were analyzed using Eq. 1 and are presented ± S.E.


ID

Ki
hiCE
hCE1
rCE
hAChE
HBChE
nM
1 15.0 ± 2.0a 71.0 ± 7.0b 160 ± 20b >100,000 1200 ± 300c
2 54.0 ± 6.0c 1900 ± 300b 1100 ± 200b >100,000 >100,000
3 32.0 ± 2.0c 740 ± 100b 150 ± 20a >100,000 >100,000
4 150 ± 20b 130 ± 20b 160 ± 30b 710 ± 110c 10,800 ± 1500b
5 1900 ± 300b 5300 ± 100b 2500 ± 200b >100,000 >100,000
6 80.0 ± 5.0a 800 ± 130b 220 ± 20a >100,000 >100,000
7 22 ± 1c 150 ± 20b 140 ± 10b >100,000 3800 ± 440c
8 220 ± 40b 190 ± 40b 150 ± 30b 1750 ± 220c 11,500 ± 1100b
9 2400 ± 700b 14,700 ± 2900b 4900 ± 1400b >100,000 >100,000
10 4700 ± 5000b 1500 ± 300b 4800 ± 800b >100,000 >100,000
11 560 ± 110b 330 ± 80b 250 ± 50b >100,000 18,400 ± 2900c
12 67,900 ± 35,900b 79,500 ± 3200b 22,800 ± 12,400b >100,000 >100,000
13 27,500 ± 5800b 9800 ± 1400b 15,300 ± 1800b >100,000 >100,000
14 9100 ± 1600b 3300 ± 1000b 2700 ± 800b >100,000 >100,000
15 >100,000 >100,000 >100,000 >100,000 >100,000
16 >100,000 >100,000 >100,000 >100,000 >100,000
17 >100,000 >100,000 >100,000 >100,000 >100,000
18 1700 ± 300b 800 ± 100b 420 ± 50b 2500 ± 100c >100,000
19 >100,000 >100,000 >100,000 >100,000 >100,000
20 750 ± 90b 120 ± 20c 410 ± 110b 72,000 ± 37,000b 65,600 ± 8000b
21
50,700 ± 13,600b
13,800 ± 3000b
13,600 ± 2300b
>100,000
>100,000
  • Modes of enzyme inhibition are:

  • a Competitive

  • b Partially noncompetitive.

  • c Partially competitive.