Literature summary for 3.4.23.16 extracted from

Jones, K.L.; Holloway, M.K.; Su, H.P.; Carroll, S.S.; Burlein, C.; Touch, S.; DiStefano, D.J.; Sanchez, R.I.; Williams, T.M.; Vacca, J.P.; Coburn, C.A.
Epsilon substituted lysinol derivatives as HIV-1 protease inhibitors (2010), Bioorg. Med. Chem. Lett., 20, 4065-4068.

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Inhibitors

Inhibitors	Comment	Organism	Structure
N-[(2R,6S)-6-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-7-hydroxyheptan-2-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide	-	Human immunodeficiency virus 1
N-[(2S,6S)-6-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-7-hydroxyheptan-2-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide	-	Human immunodeficiency virus 1
N-[(3S,7S)-7-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-1,8-dihydroxyoctan-3-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide	-	Human immunodeficiency virus 1
N-[(3S,7S)-7-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-8-hydroxy-2-methyloctan-3-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide	-	Human immunodeficiency virus 1
N-[(3S,7S)-7-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-8-hydroxyoctan-3-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide	-	Human immunodeficiency virus 1
N-[(4S,8S)-8-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-9-hydroxynonan-4-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide	-	Human immunodeficiency virus 1
N-[(5S)-5-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-6-hydroxyhexyl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide	-	Human immunodeficiency virus 1
N-[(5S)-5-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-6-hydroxyhexyl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide	-	Human immunodeficiency virus 1

Organism

Organism	UniProt	Comment	Textmining
Human immunodeficiency virus 1	-	-	-
Human immunodeficiency virus 1 IIIb	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining

Synonyms

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

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000000007	-	pH and temperature not specified in the publication	Human immunodeficiency virus 1	N-[(2S,6S)-6-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-7-hydroxyheptan-2-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide
0.000000013	-	pH and temperature not specified in the publication	Human immunodeficiency virus 1	N-[(3S,7S)-7-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-1,8-dihydroxyoctan-3-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide
0.000000016	-	pH and temperature not specified in the publication	Human immunodeficiency virus 1	N-[(3S,7S)-7-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-8-hydroxyoctan-3-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide
0.00000003	-	pH and temperature not specified in the publication	Human immunodeficiency virus 1	N-[(5S)-5-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-6-hydroxyhexyl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide
0.0000001	-	pH and temperature not specified in the publication	Human immunodeficiency virus 1	N-[(4S,8S)-8-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-9-hydroxynonan-4-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide
0.0000001	-	pH and temperature not specified in the publication	Human immunodeficiency virus 1	N-[(3S,7S)-7-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-8-hydroxy-2-methyloctan-3-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide
0.0000004	-	pH and temperature not specified in the publication	Human immunodeficiency virus 1	N-[(2R,6S)-6-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-7-hydroxyheptan-2-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide
0.0000005	-	pH and temperature not specified in the publication	Human immunodeficiency virus 1	N-[(5S)-5-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-6-hydroxyhexyl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide

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Release 2023.1 (January 2023)