Table 4. Top characterized OASS chemical inhibitors.
Inhibitor | Enzyme | IC50 (µM)* | KD (µM)* | Citation |
---|---|---|---|---|
Cyclopropyl derivative 7 (UPAR40) | HiCysK | 700 ± 53 | 1.46 ± 0.25 | [114] |
Cyclopropyl derivative 17 | ND | 1.45† | [117] | |
Cyclopropane carboxylic acid 14b (UPAR415) | StCysK | ND | 0.028 ± 0.005 | [117] |
StCysM | ND | 0.49 ± 0.05 | [117] | |
Cyclopropane carboxylic acid 15b | StCysK | 0.099 ± 0.004 | 0.054 ± 0.008 | [117] |
StCysM | 0.50 ± 0.03 | 0.42 ± 0.06 | [117] | |
8a | StCysK | ND | – | [123] |
StCysM | ND | – | [123] | |
9e | StCysK | ND | 0.035 ± 0.003 | [123] |
StCysM | ND | 0.61 ± 0.08 | [123] | |
9f | StCysK | ND | 0.051 ± 0.004 | [123] |
StCysM | ND | 1.45 ± 0.31 | [123] | |
12h | StCysK | ND | – | [123] |
StCysM | ND | – | [123] | |
13h | StCysK | ND | 0.066 ± 0.005 | [123] |
StCysM | ND | 3.37 ± 0.72 | [123] | |
21i | StCysK | ND | 0.45 ± 0.09 | [123] |
StCysM | ND | 83.8 ± 16.1 | [123] | |
21j | StCysK | ND | 0.25 ± 0.06 | [123] |
StCysM | ND | 23.6 ± 4.5 | [123] | |
Trifluoroalanine | StCysK | 130 ± 10 | ND | [122] |
StCysM | 1290 ± 230 | ND | [122] | |
Benzoic acid 87 | MtbCysK1 | 0.019 ± 0.0011 | ND | [121] |
Benzoic acid 1 | MtbCysM | ND | 0.32 ± 0.01 | [7] |
Benzoic acid 2 | MtbCysK2 | ND | 22.6 ± 2.4 | [7] |
ND = not determined.
Error reported as standard error.
No error reported.