Table 3.
Inhibitor Class | Compound | IC50 Values (μM) a |
Reference | ||
---|---|---|---|---|---|
A3G | RNase H | Integrase b | |||
Human A3G | MN8 | 0.59 | >25 | >25 | This study |
MN13 | 0.70 | >25 | >25 | This study | |
MN2 | 1.3 | >25 | >25 | This study | |
MN35 | 1.3 | 2.2 | >25 | This study | |
MN16 | 1.7 | >25 | >25 | This study | |
MN32 | 1.8 | <0.39 | >25 | This study | |
MN24 | 2.0 | 5.0 | >25 | This study | |
MN30 | 9.1 | >25 | >25 | This study | |
MN28 | 13 | >25 | >25 | This study | |
MN12 | 19 | >25 | >25 | This study | |
MN15 | 27 | >25 | >25 | This study | |
HIV RNase H | BHMP-07 | 13 | 0.10 | ND c | (47) |
KMMP-02 (THBNH) | >100 | 0.20 | ND | M. Parniak, unpublished | |
β-Thujaplicinol | >100 | 0.21 | ND | (48) | |
9 | >100 | 0.24 | ND | (48) | |
6 | >100 | 0.38 | ND | (48) | |
3 | >100 | 0.50 | ND | (48) | |
KMMP-05 (DHBNH) | >100 | 0.50 | ND | (43) | |
11 | >100 | 0.51 | ND | (48) | |
BHMP-03 | >100 | 0.60 | ND | (47) | |
Manicol | >100 | 0.60 | ND | (48) | |
13 | >100 | 0.68 | ND | (48) | |
1 | >100 | 0.82 | ND | (48) | |
7 | >100 | 0.93 | ND | (48) | |
14 | >100 | 0.96 | ND | (48) | |
4 | >100 | 1.2 | ND | (48) | |
5 | >100 | 1.2 | ND | (48) | |
10 | 98 | 1.3 | ND | (48) | |
8 | >100 | 1.3 | ND | (48) | |
2 | >100 | 1.9 | ND | (48) | |
12 | 26 | 1.9 | ND | (48) | |
HIV Integrase | L-Chicoric Acid | 2.8 | ND | 0.06 | Cmpd D in (44) |
GMII 107B | >100 | ND | 0.18 | Cmpd F in (44) | |
CGI-109 | 2.5 | ND | 0.21 | Cmpd 14 in (46) | |
CGI-83D | 1.0 | ND | 0.44 | Cmpd 13 in (46) | |
CAPE | >100 | ND | 18.9 | (44, 45) | |
L-Tartaric Acid | >100 | ND | >25 | (49) | |
Quinic Acid | >100 | ND | >25 | (51) | |
Chlorogenic acid | >100 | ND | >50 | Cmpd E in (44) |
IC50 values are ranked from lowest to highest for each inhibitor class.
Concerted integration assays were done to determine IC50 values for A3G inhibitors, whereas a variety of in vitro integrase assays were used for the published inhibitors.
Not determined.