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Literature summary for 3.4.23.16 extracted from

  • Ghosh, A.K.; Chapsal, B.D.; Baldridge, A.; Steffey, M.P.; Walters, D.E.; Koh, Y.; Amano, M.; Mitsuya, H.
    Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P2 ligands: structure-activity studies and biological evaluation (2011), J. Med. Chem., 54, 622-634.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(3aR,4R,7aS)-hexahydro-4H-furo[2,3-b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
-
Human immunodeficiency virus 1
(3aR,7aR)-octahydro-1-benzofuran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
-
Human immunodeficiency virus 1
(3aR,7aR)-octahydro-1H-inden-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
-
Human immunodeficiency virus 1
(3aS,4S,7aR)-hexahydro-4H-furo[2,3-b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
-
Human immunodeficiency virus 1
(3aS,4S,7aR)-hexahydro-4H-furo[2,3-b]pyran-4-yl [(2S,3R)-4-{[(4-aminophenyl)sulfonyl](2-methylpropyl)amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate
-
Human immunodeficiency virus 1
(3aS,4S,7aR)-hexahydro-4H-furo[2,3-b]pyran-4-yl {(2S,3R)-3-hydroxy-4-[{[4-(hydroxymethyl)phenyl]sulfonyl}(2-methylpropyl)amino]-1-phenylbutan-2-yl}carbamate
-
Human immunodeficiency virus 1
(3aS,5R,7aR)-hexahydro-4H-furo[2,3-b]pyran-5-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
-
Human immunodeficiency virus 1
(4aR,7aS)-octahydrocyclopenta[b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
-
Human immunodeficiency virus 1
(4aS,7aR)-hexahydro-2H-furo[3,4-b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
-
Human immunodeficiency virus 1
amprenavir
-
Human immunodeficiency virus 1
atazanavir
-
Human immunodeficiency virus 1
darunavir
-
Human immunodeficiency virus 1
indinavir
-
Human immunodeficiency virus 1
lopinavir
-
Human immunodeficiency virus 1
ritonavir
-
Human immunodeficiency virus 1
saquinavir
-
Human immunodeficiency virus 1

Organism

Organism UniProt Comment Textmining
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
0.0000000027
-
(3aS,4S,7aR)-hexahydro-4H-furo[2,3-b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate pH and temperature not specified in the publication Human immunodeficiency virus 1
0.000000005
-
(3aR,7aR)-octahydro-1-benzofuran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate pH and temperature not specified in the publication Human immunodeficiency virus 1
0.00000001
-
(3aS,4S,7aR)-hexahydro-4H-furo[2,3-b]pyran-4-yl [(2S,3R)-4-{[(4-aminophenyl)sulfonyl](2-methylpropyl)amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate pH and temperature not specified in the publication Human immunodeficiency virus 1
0.000000068
-
(3aR,4R,7aS)-hexahydro-4H-furo[2,3-b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate pH and temperature not specified in the publication Human immunodeficiency virus 1
0.000000085
-
(3aS,4S,7aR)-hexahydro-4H-furo[2,3-b]pyran-4-yl {(2S,3R)-3-hydroxy-4-[{[4-(hydroxymethyl)phenyl]sulfonyl}(2-methylpropyl)amino]-1-phenylbutan-2-yl}carbamate pH and temperature not specified in the publication Human immunodeficiency virus 1
0.00000011
-
(3aS,5R,7aR)-hexahydro-4H-furo[2,3-b]pyran-5-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate pH and temperature not specified in the publication Human immunodeficiency virus 1
0.00000143
-
(4aR,7aS)-octahydrocyclopenta[b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate pH and temperature not specified in the publication Human immunodeficiency virus 1
0.0000053
-
(4aS,7aR)-hexahydro-2H-furo[3,4-b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate pH and temperature not specified in the publication Human immunodeficiency virus 1
0.000009
-
(3aR,7aR)-octahydro-1H-inden-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate pH and temperature not specified in the publication Human immunodeficiency virus 1

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000005
-
pH and temperature not specified in the publication Human immunodeficiency virus 1 (3aS,4S,7aR)-hexahydro-4H-furo[2,3-b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
0.0000045
-
pH and temperature not specified in the publication Human immunodeficiency virus 1 (3aS,4S,7aR)-hexahydro-4H-furo[2,3-b]pyran-4-yl {(2S,3R)-3-hydroxy-4-[{[4-(hydroxymethyl)phenyl]sulfonyl}(2-methylpropyl)amino]-1-phenylbutan-2-yl}carbamate
0.0000065
-
pH and temperature not specified in the publication Human immunodeficiency virus 1 (3aS,4S,7aR)-hexahydro-4H-furo[2,3-b]pyran-4-yl [(2S,3R)-4-{[(4-aminophenyl)sulfonyl](2-methylpropyl)amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate
0.000008
-
pH and temperature not specified in the publication Human immunodeficiency virus 1 (3aR,7aR)-octahydro-1-benzofuran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
0.000019
-
pH and temperature not specified in the publication Human immunodeficiency virus 1 (3aR,4R,7aS)-hexahydro-4H-furo[2,3-b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
0.001
-
IC50 above 0.001 mM, pH and temperature not specified in the publication Human immunodeficiency virus 1 (3aR,7aR)-octahydro-1H-inden-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate
0.001
-
IC50 above 0.001 mM, pH and temperature not specified in the publication Human immunodeficiency virus 1 (4aS,7aR)-hexahydro-2H-furo[3,4-b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate