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Literature summary for 3.4.23.16 extracted from

  • Waibel, M.; Pitrat, D.; Hasserodt, J.
    On the inhibition of HIV-1 protease by hydrazino-ureas displaying the N-->C=O interaction (2009), Bioorg. Med. Chem., 17, 3671-3679.
    View publication on PubMed
Search for more literature for 3.4.23.16

Cloned(Commentary)

Cloned (Comment) Organism
-
 Human immunodeficiency virus 1

Inhibitors

Inhibitors Comment Organism Structure
(R)-1-benzyl-3-(1-benzyl-2-oxo-ethyl)-1-piperidin-1-yl-urea
-
 Human immunodeficiency virus 1
(S)-1-benzyl-3-(1-benzyl-2-oxo-ethyl)-1-piperidin-1-yl-urea
-
 Human immunodeficiency virus 1
(S,S)-1-[1-benzyl-3-(1-benzyl-2-oxo-ethyl)-ureido]-pyrrolidine-2-carboxylic acid tert-butylamide
-
 Human immunodeficiency virus 1
(S,S,S,S)-1-[1-benzyl-3-(1-benzyl-2-oxo-ethyl)-ureido]-pyrrolidine-2-carboxylic acid [1-(1-tert-butylcarbamoyl-2-methyl-propylcarbamoyl)-2-methyl-butyl]-amide
-
 Human immunodeficiency virus 1
1-(benzyl[[(2S)-1-oxo-3-phenylpropan-2-yl]carbamoyl]amino)-L-prolyl-N-tert-butyl-L-valinamide
-
 Human immunodeficiency virus 1
1-[(3R)-3-benzyl-3-([N-[(benzyloxy)carbonyl]-L-valyl]amino)-4-oxobutyl]-L-prolyl-N-tert-butyl-L-valinamide
-
 Human immunodeficiency virus 1
1-[(3R)-3-benzyl-3-([N-[(benzyloxy)carbonyl]-L-valyl]amino)-4-oxobutyl]-N-tert-butyl-L-prolinamide
-
 Human immunodeficiency virus 1
pepstatin
-
 Human immunodeficiency virus 1

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.025
-
 Arg-Glu(EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg
-
 Human immunodeficiency virus 1

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
-
-
-

Purification (Commentary)

Purification (Comment) Organism
commercial preparation Human immunodeficiency virus 1

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Arg-Glu(EDANS)-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg + H2O
-
 Human immunodeficiency virus 1 ?
-
 ?

Synonyms

Synonyms Comment Organism
HIV-1 protease
-
 Human immunodeficiency virus 1

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000038
-
 pepstatin
-
 Human immunodeficiency virus 1
0.0262
-
 (S)-1-benzyl-3-(1-benzyl-2-oxo-ethyl)-1-piperidin-1-yl-urea
-
 Human immunodeficiency virus 1
0.0343
-
 (S,S)-1-[1-benzyl-3-(1-benzyl-2-oxo-ethyl)-ureido]-pyrrolidine-2-carboxylic acid tert-butylamide
-
 Human immunodeficiency virus 1
0.099
-
 1-[(3R)-3-benzyl-3-([N-[(benzyloxy)carbonyl]-L-valyl]amino)-4-oxobutyl]-L-prolyl-N-tert-butyl-L-valinamide
-
 Human immunodeficiency virus 1
0.1486
-
 (S,S,S,S)-1-[1-benzyl-3-(1-benzyl-2-oxo-ethyl)-ureido]-pyrrolidine-2-carboxylic acid [1-(1-tert-butylcarbamoyl-2-methyl-propylcarbamoyl)-2-methyl-butyl]-amide
-
 Human immunodeficiency virus 1
0.292
-
 1-(benzyl[[(2S)-1-oxo-3-phenylpropan-2-yl]carbamoyl]amino)-L-prolyl-N-tert-butyl-L-valinamide
-
 Human immunodeficiency virus 1
0.461
-
 (R)-1-benzyl-3-(1-benzyl-2-oxo-ethyl)-1-piperidin-1-yl-urea
-
 Human immunodeficiency virus 1
0.574
-
 1-[(3R)-3-benzyl-3-([N-[(benzyloxy)carbonyl]-L-valyl]amino)-4-oxobutyl]-N-tert-butyl-L-prolinamide
-
 Human immunodeficiency virus 1

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000041
-
-
 Human immunodeficiency virus 1 pepstatin
0.0372
-
-
 Human immunodeficiency virus 1 (S)-1-benzyl-3-(1-benzyl-2-oxo-ethyl)-1-piperidin-1-yl-urea
0.0445
-
-
 Human immunodeficiency virus 1 (S,S)-1-[1-benzyl-3-(1-benzyl-2-oxo-ethyl)-ureido]-pyrrolidine-2-carboxylic acid tert-butylamide
0.169
-
-
 Human immunodeficiency virus 1 (S,S,S,S)-1-[1-benzyl-3-(1-benzyl-2-oxo-ethyl)-ureido]-pyrrolidine-2-carboxylic acid [1-(1-tert-butylcarbamoyl-2-methyl-propylcarbamoyl)-2-methyl-butyl]-amide
0.204
-
-
 Human immunodeficiency virus 1 1-[(3R)-3-benzyl-3-([N-[(benzyloxy)carbonyl]-L-valyl]amino)-4-oxobutyl]-L-prolyl-N-tert-butyl-L-valinamide
0.341
-
-
 Human immunodeficiency virus 1 1-(benzyl[[(2S)-1-oxo-3-phenylpropan-2-yl]carbamoyl]amino)-L-prolyl-N-tert-butyl-L-valinamide
0.543
-
-
 Human immunodeficiency virus 1 (R)-1-benzyl-3-(1-benzyl-2-oxo-ethyl)-1-piperidin-1-yl-urea
0.545
-
-
 Human immunodeficiency virus 1 1-[(3R)-3-benzyl-3-([N-[(benzyloxy)carbonyl]-L-valyl]amino)-4-oxobutyl]-N-tert-butyl-L-prolinamide