TABLE 5 .
Selectivity of inhibition of TbCet1 versus other TTM triphosphatases
| Compound | IC50, µM (IC50/IC50 TbCet1) |
||||
|---|---|---|---|---|---|
| TbCet1 | MimiCE | SceCet1 | CthTTM | Lef4 | |
| 1A | 0.013 | 1.4 (108) | 7.1 (546) | 11 (846) | 5.7 (438) |
| 1C | 0.11 | >500 | >500 | >500 | 75 (682) |
| 1D | 0.15 | 16 (107) | 10 (67) | 160 (1,067) | 7.2 (48) |
| 1E | 0.19 | 8.4 (44) | 29 (153) | 33 (174) | 5.6 (29) |
| 1F | 0.22 | 3.4 (15) | >500 | 21 (95) | 33 (150) |
| 1G | 0.34 | 3.7 (11) | >500 | 55 (162) | 22 (65) |
| 1H | 1.3 | 52 (40) | >500 | >500 | 140 (108) |
| 1I | 1.6 | 17 (11) | >500 | 17 (11) | 6 (4) |
| 1J | 2.4 | >500 | >500 | >500 | >500 |
| 1K | 5.8 | 20 (3) | >500 | 72 (12) | 46 (8) |
| 1L | 12 | >500 | >500 | >500 | >500 |
| 1M | 24 | >500 | >500 | >500 | >500 |
| 1N | 25 | >500 | >500 | >500 | >500 |
| 1O | 125 | >500 | 10 (0.08) | >500 | >500 |
| 2A | 0.046 | 5.1 (111) | 3.2 (70) | 1.4 (30) | 59 (1,283) |
| 2B | 0.66 | 120 (182) | 41 (62) | 29 (44) | 150 (227) |
| 3A | 0.12 | 4.3 (36) | 3.3 (28) | 1.5 (13) | 3.2 (27) |
| 3B | 29 | >500 | >500 | 310 (11) | 75 (3) |
| 4A | 0.18 | 19 (106) | 43 (239) | 24 (133) | 29 (161) |
| 4B | 0.36 | 20 (56) | 26 (72) | 6.5 (18) | 160 (444) |
| 4C | 0.25 | 10 (40) | 8.7 (35) | 26 (104) | 34 (136) |
| 5 | 0.64 | 84 (131) | >500 | 9.2 (14) | 160 (250) |
| 6A | 0.12 | 2 (17) | 2 (17) | 6.4 (53) | 2.6 (22) |
| 6B | 1.5 | 19 (13) | >500 | 150 (100) | 10 (7) |
| 6C | 3.6 | 15 (4) | 14 (4) | 46 (13) | 21 (6) |