Cpd. | Inhibitor | Ki sGC α1β1 ± S.E. | pKi sGC α1β1 | pKi Bovine sGC | pKi mAC1 | pKi mAC2 | pKi mAC5 | pKi VC1:IIC2 |
---|---|---|---|---|---|---|---|---|
nM | ||||||||
1 | MANT-ATP | 170 ± 10 | 6.77 | 6.37a | 6.82c | 6.48c | 7.00c | 7.80c |
2 | MANT-ITP | 500 ± 30 | 6.31 | 8.55c | 7.85c | 8.92c | 9.15c | |
3 | MANT-GTP | 860 ± 50 | 6.06 | 6.15b | 7.05c | 6.21c | 7.28c | 7.74c |
4 | MANT-XTP | 110 ± 10 | 6.95 | 5.96c | 5.52c | 5.89c | 5.92c | |
5 | MANT-CTP | 520 ± 40 | 6.28 | 6.82c | 6.16c | 6.82c | 8.04c | |
6 | MANT-UTP | 500 ± 50 | 6.30 | 7.34c | 6.34c | 7.49c | 8.21c | |
7 | 2-MANT-3′-dATP | 17 ± 1 | 7.78 | 6.33c | 6.27c | 7.19c | 7.05c | |
8 | 3′-MANT-2-dATP | 740 ± 80 | 6.13 | 5.44a | 6.49c | 5.32c | 6.44c | 6.72c |
9 | MANT-ATPγS | 130 ± 7 | 6.88 | 6.80d | 6.42d | 7.11d | ||
10 | MANT-ITPγS | 930 ± 80 | 6.03 | 5.3b | 7.39b | 6.92b | 7.51b | 7.72c |
11 | MANT-GTPγS | 470 ± 40 | 6.33 | 5.96b | 7.21b | 6.44b | 7.46b | 7.62c |
12 | ANT-ATP | 240 ± 20 | 6.63 | 6.89c | 6.19c | 6.92c | 7.77c | |
13 | Cl-ANT-ATP | 47 ± 4 | 7.33 | 7.10e | 6.31e | 7.35e | ||
14 | Cl-ANT-ITP | 1200 ± 100 | 5.92 | 8.48e | 8.10e | 8.70e | ||
15 | Br-ANT-ITP | 600 ± 50 | 6.22 | 8.15e | 7.66e | 8.34e | ||
16 | Pr-ANT-ATP | 160 ± 10 | 6.80 | 6.36e | 5.96e | 6.44e | ||
17 | Pr-ANT-ITP | 390 ± 50 | 6.41 | 7.66e | 7.17e | 8.00e | ||
18 | AcNH-ANT-ATP | 780 ± 70 | 6.11 | 5.17e | 4.96e | 5.47e | ||
19 | AcNH-ANT-ITP | 600 ± 50 | 6.22 | 6.85e | 6.41e | 7.43e | ||
20 | MANT-AppNHp | 170 ± 20 | 6.77 | 6.64b | 6.80b | 6.31b | 6.92b | 7.70b |
21 | MANT-GppNHp | 2800 ± 400 | 5.56 | 5.82b | 6.96b | 6.18b | 7.01b | 7.47b |
22 | TNP-ATP | 21 ± 2 | 7.67 | 8.14a | 8.05a | 7.00a | 8.43a | 7.09f |
23 | TNP-GTP | 11 ± 1 | 7.97 | 8.07a | 7.64a | 6.66a | 7.57a | 7.08f |
24 | TNP-CTP | 98 ± 5 | 7.01 | 7.57a | 7.62a | 6.96a | 7.51a | 6.51f |
25 | TNP-UTP | 51 ± 4 | 7.29 | 7.48a | 8.15a | 7.62a | 7.82a | 7.04f |
26 | Bis-MANT-ATP | 580 ± 70 | 6.23 | 6.15e | 5.68e | 6.37e | ||
27 | Bis-MANT-ITP | 350 ± 20 | 6.46 | 6.51e | 5.96e | 6.85e | ||
28 | Bis-MANT-CTP | 790 ± 80 | 6.10 | 6.21e | 5.11e | 6.12e | ||
29 | Bis-MANT-IDP | 1900 ± 100 | 5.72 | 6.00e | 5.85e | 6.15e | ||
30 | Bis-MANT-IMP | >100,000 | < 3 | <3e | < 3e | < 3e | ||
31 | Bis-Cl-ANT-ATP | 520 ± 50 | 6.28 | 5.77e | 5.62e | 5.80e | ||
32 | Bis-Cl-ANT-ITP | 840 ± 60 | 6.08 | 7.18e | 6.70e | 7.19e | ||
33 | Bis-Br-ANT-ATP | 430 ± 50 | 6.37 | |||||
34 | Bis-Br-ANT-ITP | 630 ± 50 | 6.20 | 7.68e | 7.15e | 7.82e | ||
35 | Bis-Pr-ANT-ATP | 3600 ± 300 | 5.44 | 4.74e | 4.44e | 4.74e | ||
36 | Bis-Pr-ANT-ITP | 1200 ± 70 | 5.91 | 6.36e | 5.85e | 6.60e | ||
37 | Bis-AcNH-ANT-ATP | 3900 ± 600 | 5.41 | 4.66e | 5.15e | 5.21e | ||
38 | Bis-AcNH-ANT-ITP | 1100 ± 80 | 5.97 | 5.77e | 5.25e | 6.32e |