Activating Compound | Comment | Organism | Structure |
---|---|---|---|
Pep4AK | cofactor, peptide spanning the central hydrophobic core of the NS4A protein, with a three-lysine tag at the N-terminus | Hepacivirus C |
Protein Variants | Comment | Organism |
---|---|---|
K136M | IC50 for CO1a is 2-[1-[1-(1-carbamoyl-3-methyl-butylcarbamoyl)-2-carboxy-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl]-cyclohexanecarboxylic acid of that of the wild-type enzyme | Hepacivirus C |
K136R | IC50 for 2-[1-[1-(1-carbamoyl-3-methyl-butylcarbamoyl)-2-carboxy-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl]-cyclohexanecarboxylic acid is 53% of that of the wild-type enzyme | Hepacivirus C |
K136S | IC50 for 2-[1-[1-(1-carbamoyl-3-methyl-butylcarbamoyl)-2-carboxy-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl]-cyclohexanecarboxylic acid is 1.6fold higher than that of the wild-type enzyme | Hepacivirus C |
R109Q | IC50 for 2-[1-[1-(1-carbamoyl-3-methyl-butylcarbamoyl)-2-carboxy-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl]-cyclohexanecarboxylic acid is more than 9fold higher than that of the wild-type enzyme | Hepacivirus C |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-[1-[1-(1-Carbamoyl-3-methyl-butylcarbamoyl)-2-carboxy-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl]-cyclohexanecarboxylic acid | IC50: 0.015 mM, wild-type enzyme, IC50: 0.017 mM, mutant enzyme K136R, IC50: 0.027 mM, mutant enzyme K136M, IC50: 0.05 mM, mutant enzyme K136S, IC50: above 0.3 mM, mutant enzyme R109Q | Hepacivirus C | |
2-[1-[2-Carboxy-1-(1-ethylcarbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl]-cyclohexanecarboxylic acid | IC50: 0.032 mM | Hepacivirus C |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Hepacivirus C | - |
- |
- |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.032 | - |
IC50: 0.032 mM | Hepacivirus C | 2-[1-[2-Carboxy-1-(1-ethylcarbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl]-cyclohexanecarboxylic acid | |
0.3 | - |
IC50: 0.015 mM, wild-type enzyme, IC50: 0.017 mM, mutant enzyme K136R, IC50: 0.027 mM, mutant enzyme K136M, IC50: 0.05 mM, mutant enzyme K136S, IC50: above 0.3 mM, mutant enzyme R109Q | Hepacivirus C | 2-[1-[1-(1-Carbamoyl-3-methyl-butylcarbamoyl)-2-carboxy-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl]-cyclohexanecarboxylic acid |