Inhibitors | Comment | Organism | Structure |
---|---|---|---|
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-3-aminobenzamide | highly effective against the malaria parasites, IC50 values of 233 nM; highly effective against the malaria parasites, IC50 values of 233 nM | Plasmodium falciparum | |
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-4-aminobenzamide | highly effective against the malaria parasites, IC50 values of 283 nM; highly effective against the malaria parasites, IC50 values of 283 nM | Plasmodium falciparum | |
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-pivalamide | most effective inhibitor of isoform M1 and one of the more potent inhibitors of isoform M17 tested, the most effective compound against 3D7 malaria parasites, with an IC50 of 227 nM; most effective inhibitor of isoform M1 and one of the more potent inhibitors of isoform M17 tested, the most effective compound against 3D7 malaria parasites, with an IC50 of 227 nM | Plasmodium falciparum | |
tert-butyl (1-(4-(1H-Pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)carbamate | compound shows good in vitro inhibitory properties, but IC50 for parasite growth is only 783 nM, suggesting that compounds substituted with the N-Boc group are either less capable of cellular penetration or less stable than the corresponding N-acyl derivatives; compound shows good in vitro inhibitory properties, but IC50 for parasite growth is only 783 nM, suggesting that compounds substituted with the N-Boc group are either less capable of cellular penetration or less stable than the corresponding N-acyl derivatives | Plasmodium falciparum |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Plasmodium falciparum | O96935 | - |
- |
Plasmodium falciparum | Q8IL11 | - |
- |
Plasmodium falciparum isolate FcB1/Columbia | O96935 | - |
- |
Synonyms | Comment | Organism |
---|---|---|
M1 aminopeptidase | - |
Plasmodium falciparum |
M17 aminopeptidase | - |
Plasmodium falciparum |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000011 | - |
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-4-aminobenzamide | pH 8.0, 37°C | Plasmodium falciparum | |
0.000014 | - |
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-3-aminobenzamide | pH 8.0, 37°C | Plasmodium falciparum | |
0.000028 | - |
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-pivalamide | pH 8.0, 37°C | Plasmodium falciparum | |
0.00003 | - |
tert-butyl (1-(4-(1H-Pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)carbamate | pH 8.0, 37°C | Plasmodium falciparum | |
0.0007 | - |
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-pivalamide | pH 8.0, 37°C | Plasmodium falciparum | |
0.0008 | - |
tert-butyl (1-(4-(1H-Pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)carbamate | pH 8.0, 37°C | Plasmodium falciparum | |
0.0055 | - |
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-3-aminobenzamide | pH 8.0, 37°C | Plasmodium falciparum | |
0.0074 | - |
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-4-aminobenzamide | pH 8.0, 37°C | Plasmodium falciparum |