Table 1. Dissociation constants (Kd, nM) of the compounds for 12 human CA isoforms.
No | CA I | CA II | CA III | CA IV | CA VA | CA VB | CA VI | CA VII | CA IX | CA XII | CA XIII | CA XIV |
---|---|---|---|---|---|---|---|---|---|---|---|---|
1. | 270 | 560; 1125[10] | >200000 | 1200 | 320 | 470 | 2600 | 400 | 860 | 420 | 570 | 430 |
2. | 480; 1200 [22] | 3.2; 38 [22] | 550; 680000[22] | 6.3; 15000[22] | 25; 630[22] | 0.25; 21[22] | 15; 79[22] | 0.46; 26[22] | 3.1; 50[22] | 3.4; 50[22] | 4.5; 23m[22] | 0.92; 345[22] |
3. | 23000 | 370; 372 [23] | 15000 | 310 | 830 | 48 | 620 | 70 | 130 | 180 | 39 | 250 |
4. | 23000; 328[22] | 2600; 7190 [23] 290[22] | 200000; 790000[22] | 1600; 427[22] | 2000; 4225[22] | 200; 603[22] | 830; 3655[22] | 870; 5010[22] | 350; 367[22] | 570; 355[22] | 530; 3885m[22] | 620; 4105[22] |
5. | 6200; 345 [24] | 1700; 2600[23]; 91 [24] | >200000; 560000 [24] | 1000; 449 [24] | 3300; 763 [24] | 1500; 134 [24] | 1500; 2459 [24] | 710; 7.9 [24] | 260; 87 [24] | 420; 312 [24] | 940; 645m [24] | 590; 3450 [24] |
6. | 940 | 1200 | 270000 | 270 | 1100 | 140 | 430 | 500 | 150 | 170 | 430 | 360 |
7. | 250 | 500 | >200000 | 330 | 5000 | 280 | 580 | 100 | 100 | 1600 | 190 | 230 |
8. | 4300 | 6.4; 16.7 [23] | 4500 | 43 | 90 | 6.6 | 500 | 15 | 26 | 18 | 0.64 | 36 |
9. | 1600 | 790 | 51000 | 330 | 1500 | 61 | 490 | 250 | 120 | 120 | 150 | 51 |
10. | 50000; 2840 [22] | 17000; 435 [22] | >200000; 870000 [22] | 24000; 4780 [22] | 40000; 10200 [22] | 910; 429 [22] | 29000; 8250 [22] | 17000; 433 [22] | 1600; 412 [22] | 31000; 305 [22] | 470; 15400m [22] | 3600; 360 [22] |
11. | 5800 | 1700 | >200000 | 1600 | 32000 | 360 | 5300 | 440 | 210 | 480 | 910 | 130 |
12. | 2800; 51900 [24] | 130; 1420 [23] 2520 [24] | 11000; 230000 [24] | 47; 213 [24] | 280; 890 [24] | 13; 274 [24] | 130; 1606 [24] | 42; 0.23 [24] | 140; 36 [24] | 150; 10 [24] | 41; 13m [24] | 88; 4950 [24] |
13. | 4900 | 370; 14600[23] | >200000 | 360 | 440 | 660 | 470 | 250 | 330 | 760 | 170 | 200 |
14. | 56000 | 10000 | >200000 | 1400 | >200000 | 61000 | 36000 | 93000 | 15000 | 26000 | 680 | 15000 |
15. | 830; 62 [24] | 630; 3140 [23] 65 [24] | >200000; 3200000 [24] | 920; 564 [24] | >200000; 499 [24] | 120000; 322 [24] | 49000; 245 [24] | 620; 513 [24] | 200; 420 [24] | 120; 261 [24] | 230; 550m [24] | 420; 52 [24] |
16. | 310; 348 [24] | 35; 11.9 [23]; 138 [24] | 17000; 11000 [24] | 16; 196 [24] | 4800; 917 [24] | 470; 9 [24] | 110; 1347[24] | 43; 2.8 [24] | 33; 23 [24] | 12; 4.5 [24] | 30; 15m [24] | 19; 4130[24] |
17. | 1600 | 76 | >200000 | 250 | 42000 | 500 | 420 | 100 | 42 | 89 | 51 | 58 |
18. | 51000; 35000 [22] | 14000; 1260 [22] | 180000 | 2100 | 7100 | 15000 | 3900 | 36000 | 2300 | 20000 | 1100 | 4700 |
19. | 13000 | 15000 | >200000 | 4400 | 11000 | 19000 | 5300 | 27000 | 2700 | 28000 | 930 | 5700 |
20. | 130000; 54000 [22] | 2800; 2000 [22] | >200000; 610000 [22] | 91; 216 [22] | 5800; 750 [22] | 1400; 312 [22] | 990; 1714 [22] | 8300; 2.1 [22] | 800; 320 [22] | 15000; 5.4 [22] | 180; 15m [22] | 1300; 5432 [22] |
The Kd values in the top rows were determined in this study by FTSA and are the averages of at least two measurements. The second and the following rows in the cell (if provided) show the literature values of inhibition constants of CA enzymatic activity, Ki (nM), or the dissociation constants Kd (nM) (listed together with the citation).
m murine protein.