Table 4 Quantification of inhibition of mycolate containing products by GSK3011724A.
From: Identification of KasA as the cellular target of an anti-tubercular scaffold
Inhibitor | Inhibitor concentration (μM) | FAMEs | α-MAMEs | k-MAMEs | TDM | TMM | |||||
---|---|---|---|---|---|---|---|---|---|---|---|
c.p.m. | % Relative to control | c.p.m. | % Relative to control | c.p.m. | % Relative to control | c.p.m. | % Relative to control | c.p.m. | % Relative to control | ||
Control | 0 | 9,796 | 100 | 4,029 | 100 | 7,641 | 100 | 3,149 | 100 | 1,425 | 100 |
GSK3011724A | 0.25 | 16,207 | 165 | 3,438 | 85 | 7,147 | 94 | ND | ND | ND | ND |
0.5 | 17,780 | 182 | 3,026 | 75 | 6,651 | 87 | 864 | 27 | 911 | 64 | |
1 | 16,478 | 168 | 2,488 | 62 | 4,925 | 64 | 874 | 28 | 893 | 63 | |
2 | 18,268 | 186 | 1,806 | 45 | 4,407 | 58 | ND | ND | ND | ND | |
4 | ND | ND | ND | ND | ND | ND | 652 | 21 | 951 | 67 | |
Control | 0 | 10,231 | 100 | 4,156 | 100 | 6,722 | 100 | —* | —* | —* | —* |
TLM | 95 | 15,334 | 150 | 2,721 | 65 | 3,727 | 55 | 817 | 26 | 704 | 49 |
INH | 1.5 | 16,926 | 165 | 1,426 | 34 | 1,808 | 27 | 642 | 20 | 552 | 39 |