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Literature summary for 3.4.23.16 extracted from

  • Tossi, A.; Benedetti, F.; Norbedo, S.; Skrbec, D.; Berti, F.; Romeo, D.
    Small hydroxyethylene-based peptidomimetics inhibiting both HIV-1 and C. albicans aspartic proteases (2003), Bioorg. Med. Chem., 11, 4719-4727.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2,6-dimethylphenoxyacetyl-Phe-PSI(S,R,S)[OH]-Phe-2,6-dimethylphenoxyacetyl IC50: 25 nM Human immunodeficiency virus 1
2,6-dimethylphenoxyacetyl-Phe-PSI(S,S,S)[OH]-Phe-2,6-dimethylphenoxyacetyl IC50: 28 nM Human immunodeficiency virus 1
2-hydroxyphenoxyacetyl-Phe-PSI(S,R,S)[OH]-Phe-2-hydroxyphenoxyacetyl IC50: 0.009 mM Human immunodeficiency virus 1
2-hydroxyphenoxyacetyl-Phe-PSI(S,S,S)[OH]-Phe-2-hydroxyphenoxyacetyl IC50: 0.007 mM Human immunodeficiency virus 1
4-acetylphenoxyacetyl-Phe-PSI(S,R,S)[OH]-Phe-4-acetylphenoxyacetyl IC50: 0.023 mM Human immunodeficiency virus 1
4-acetylphenoxyacetyl-Phe-PSI(S,S,S)[OH]-Phe-4-acetylphenoxyacetyl IC50: 0.019 mM Human immunodeficiency virus 1
4-formylphenoxyacetyl-Phe-PSI(S,R,S)[OH]-Phe-4-acetylphenoxyacetyl IC50: 0.08 mM Human immunodeficiency virus 1
4-formylphenoxyacetyl-Phe-PSI(S,S,S)[OH]-Phe-4-acetylphenoxyacetyl IC50: 0.068 mM Human immunodeficiency virus 1
indinavir IC50: 1.3 nM Human immunodeficiency virus 1
Kyn-(D-alpha-(2-thienyl)glycine)-Phe-PSI(S,R,S)[OH]-Phe-2,6-dimethylphenoxyacetyl IC50: 3 nM Human immunodeficiency virus 1
Kyn-Thr-Phe-PSI(S,R,S)[OH]-Phe-2,6-dimethylphenoxyacetyl IC50: 4 nM Human immunodeficiency virus 1
Kyn-Val-Phe-PSI(S,R,S)[OH]-Phe-2,6-dimethylphenoxyacetyl IC50: 3 nM Human immunodeficiency virus 1
Kyn-Val-Phe-PSI(S,R,S)[OH]-Phe-Val-Kyn IC50: 4 nM Human immunodeficiency virus 1
Kyn-Val-Phe-PSI(S,S,S)[OH]-Phe-2,6-dimethylphenoxyacetyl IC50: 3 nM Human immunodeficiency virus 1
nelfinavir IC50: 1.9 nM Human immunodeficiency virus 1
phenoxyacetyl-Phe-PSI(S,R,S)[OH]-Phe-phenoxyacetyl IC50: 0.017 mM Human immunodeficiency virus 1
phenoxyacetyl-Phe-PSI(S,S,S)[OH]-Phe-phenoxyacetyl IC50: 0.005 mM Human immunodeficiency virus 1
ritonavir IC50: 3 nM Human immunodeficiency virus 1

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Abz-Thr-Nle-Phe(NO2)-QR-NH2 + H2O
-
Human immunodeficiency virus 1 Abz-Thr-Ile-Nle + Phe(NO2)-Gln-Arg-NH2
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000013
-
IC50: 1.3 nM Human immunodeficiency virus 1 indinavir
0.0000019
-
IC50: 1.9 nM Human immunodeficiency virus 1 nelfinavir
0.000003
-
IC50: 3 nM Human immunodeficiency virus 1 ritonavir
0.000003
-
IC50: 3 nM Human immunodeficiency virus 1 Kyn-(D-alpha-(2-thienyl)glycine)-Phe-PSI(S,R,S)[OH]-Phe-2,6-dimethylphenoxyacetyl
0.000003
-
IC50: 3 nM Human immunodeficiency virus 1 Kyn-Val-Phe-PSI(S,R,S)[OH]-Phe-2,6-dimethylphenoxyacetyl
0.000003
-
IC50: 3 nM Human immunodeficiency virus 1 Kyn-Val-Phe-PSI(S,S,S)[OH]-Phe-2,6-dimethylphenoxyacetyl
0.000004
-
IC50: 4 nM Human immunodeficiency virus 1 Kyn-Thr-Phe-PSI(S,R,S)[OH]-Phe-2,6-dimethylphenoxyacetyl
0.000004
-
IC50: 4 nM Human immunodeficiency virus 1 Kyn-Val-Phe-PSI(S,R,S)[OH]-Phe-Val-Kyn
0.000025
-
IC50: 25 nM Human immunodeficiency virus 1 2,6-dimethylphenoxyacetyl-Phe-PSI(S,R,S)[OH]-Phe-2,6-dimethylphenoxyacetyl
0.000028
-
IC50: 28 nM Human immunodeficiency virus 1 2,6-dimethylphenoxyacetyl-Phe-PSI(S,S,S)[OH]-Phe-2,6-dimethylphenoxyacetyl
0.005
-
IC50: 0.005 mM Human immunodeficiency virus 1 phenoxyacetyl-Phe-PSI(S,S,S)[OH]-Phe-phenoxyacetyl
0.007
-
IC50: 0.007 mM Human immunodeficiency virus 1 2-hydroxyphenoxyacetyl-Phe-PSI(S,S,S)[OH]-Phe-2-hydroxyphenoxyacetyl
0.009
-
IC50: 0.009 mM Human immunodeficiency virus 1 2-hydroxyphenoxyacetyl-Phe-PSI(S,R,S)[OH]-Phe-2-hydroxyphenoxyacetyl
0.017
-
IC50: 0.017 mM Human immunodeficiency virus 1 phenoxyacetyl-Phe-PSI(S,R,S)[OH]-Phe-phenoxyacetyl
0.019
-
IC50: 0.019 mM Human immunodeficiency virus 1 4-acetylphenoxyacetyl-Phe-PSI(S,S,S)[OH]-Phe-4-acetylphenoxyacetyl
0.023
-
IC50: 0.023 mM Human immunodeficiency virus 1 4-acetylphenoxyacetyl-Phe-PSI(S,R,S)[OH]-Phe-4-acetylphenoxyacetyl
0.068
-
IC50: 0.068 mM Human immunodeficiency virus 1 4-formylphenoxyacetyl-Phe-PSI(S,S,S)[OH]-Phe-4-acetylphenoxyacetyl
0.08
-
IC50: 0.08 mM Human immunodeficiency virus 1 4-formylphenoxyacetyl-Phe-PSI(S,R,S)[OH]-Phe-4-acetylphenoxyacetyl