TABLE 3

Kiapp values for the inhibition of hiCE, hCE1, rCE, hAChE, or hBChE after preincubation of the enzymes with the TFK analogs for 24 h

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


ID

Kiapp
hiCE
hCE1
rCE
hAChE
hBChE
nM
1 64.9 ± 22.2a 24.7 ± 5.0a 46.7 ± 12.9a >100,000 2550 ± 310b
2 4.50 ± 1.10a 0.44 ± 0.08b 1.10 ± 0.11b >100,000 >100,000
3 0.84 ± 0.17b 0.36 ± 0.05c 0.66 ± 0.06b >100,000 >100,000
4 59.2 ± 17.5a 11.3 ± 3.0a 29.0 ± 4.0a 16,200 ± 3300a 95,000 ± 6700a
5 6.60 ± 0.87a 0.49 ± 0.08c 16.1 ± 1.4a >100,000 >100,000
6 0.75 ± 0.17b 0.86 ± 0.20a 1.35 ± 0.10b >100,000 >100,000
7 25,200 ± 2100a 6.50 ± 0.64d 20,500 ± 3800a >100,000 >100,000
8 3.60 ± 0.64b 4.24 ± 0.81b 42.6 ± 5.2a 1630 ± 500b 40,400 ± 5100a
9 4.90 ± 0.89a 1.22 ± 0.10b 4.70 ± 0.54b >100,000 >100,000
10 33.0 ± 7.5a 0.59 ± 0.10c 22.8 ± 3.4a >100,000 >100,000
11 67.7 ± 10.1a 14.1 ± 2.8d 10.1 ± 1.1c >100,000 >100,000
12 0.79 ± 0.05b 3.50 ± 0.30b 89.8 ± 11.8a >100,000 >100,000
13 3.0 ± 0.3b 2.36 ± 0.26a 19.5 ± 3.1b >100,000 >100,000
14 1.20 ± 0.16b 2.65 ± 0.45a 11.3 ± 0.8da >100,000 >100,000
15 >100,000 >100,000 >100,000 >100,000 >100,000
16 450 ± 100b 3610 ± 1600a 18,300 ± 3900a >100,000 >100,000
17 >100,000 >100,000 >100,000 >100,000 >100,000
18 17.0 ± 2.0b 13.5 ± 2.2a 45.8 ± 8.8a 31,400 ± 7500a >100,000
19 0.20 ± 0.09b 32.9 ± 8.0a 268 ± 30a >100,000 >100,000
20 62.1 ± 10.4a 16.9 ± 4.2d 42.4 ± 7.7a 360 ± 35b >100,000
21
376 ± 77a
4.70 ± 0.37a
29.9 ± 10.7a
>100,000
>100,000
  • Modes of enzyme inhibition are:

  • a Partially noncompetitive.

  • b Partially competitive.

  • c Competitive.

  • d Noncompetitive.