Table 3
Inhibition of human mast-cell tryptase by APC-1390 and phenylguanidine. The values of apparent inhibition constants Kj were calculated for each inhibitor concentration by using equation (4). The bottom row in the table lists the iteratively re-weighted averages computed by using equation (5). The iterations were terminated when two consecutive values of K agreed within six significant digits.
j |
APC-1390 ([E] = 0.29 nM) |
phenylguanidine ([E] = 2.50 nM) |
|
[I]j (nM) |
vj (106 a.u./sec) |
K (pM) |
[I]j(µM) |
vj (106 a.u./sec) |
K (µM) |
|
0 |
0.000 |
78.55 |
- |
0.00 |
702.80 |
- (a) |
|
1 |
0.234 |
31.89 |
42.20 |
0.46 |
715.60 |
- (a) |
|
2 |
0.351 |
21.58 |
53.27 |
1.37 |
722.10 |
- (a) |
|
3 |
0.526 |
13.89 |
61.70 |
4.12 |
662.10 |
66.94 |
|
4 |
0.790 |
9.55 |
74.12 |
12.35 |
587.20 |
62.73 |
|
5 |
1.185 |
8.42 |
111.26 |
37.04 |
454.50 |
67.80 |
|
6 |
1.770 |
4.05 |
81.23 |
111.10 |
241.80 |
58.27 |
|
7 |
4.000 |
3.17 |
156.69 |
333.30 |
103.30 |
57.43 |
|
8 |
- |
- |
- |
1000.00 |
38.19 |
57.46 |
|
|
K = 66.3 pM |
K = 62.0 µM |
(a) Velocities greater than control are automatically excluded from the analysis.
|
