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Literature summary for 3.4.23.46 extracted from

  • Ghosh, A.K.; Ghosh, K.; Brindisi, M.; Lendy, E.K.; Yen, Y.C.; Kumaragurubaran, N.; Huang, X.; Tang, J.; Mesecar, A.D.
    Design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors with bicyclic isoxazoline carboxamides as the P3 ligand (2018), Bioorg. Med. Chem. Lett., 28, 2605-2610 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.23.46

Inhibitors

Inhibitors Comment Organism Structure
(3aR,6aS)-N-[(2R)-1-([(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]amino)-3-(methylsulfonyl)-1-oxopropan-2-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
 Homo sapiens
(3aR,6aS)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
 Homo sapiens
(3aR,6aS)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-5,11,14-trioxo-13-(propan-2-yl)-2-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
 Homo sapiens
(3aR,7aS)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,5,6,7a-tetrahydro-4H-pyrano[3,2-d][1,2]oxazole-3-carboxamide
-
 Homo sapiens
(3aS,6aR)-N-[(2R)-1-([(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]amino)-3-(methylsulfonyl)-1-oxopropan-2-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
 Homo sapiens
(3aS,6aR)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
 Homo sapiens
(3aS,6aR)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-5,11,14-trioxo-13-(propan-2-yl)-2-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
 Homo sapiens
(3aS,7aR)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,5,6,7a-tetrahydro-4H-pyrano[3,2-d][1,2]oxazole-3-carboxamide
-
 Homo sapiens
OM99-2
-
 Homo sapiens
tert-butyl [(2S)-3-[[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-([(2S)-3-methyl-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-8-oxooctan-4-yl]amino]-3-oxo-2-[[(3aR,6aS)-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazol-3-ylcarbonyl]amino]propyl]carbamate
-
 Homo sapiens
tert-butyl [(2S)-3-[[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-([(2S)-3-methyl-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-8-oxooctan-4-yl]amino]-3-oxo-2-[[(3aS,6aR)-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazol-3-ylcarbonyl]amino]propyl]carbamate
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
amyloid-beta precursor protein + H2O Homo sapiens
-
 ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P56817
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
amyloid-beta precursor protein + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
BACE1
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000109
-
 (3aR,6aS)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-5,11,14-trioxo-13-(propan-2-yl)-2-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0000281
-
 (3aR,7aS)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,5,6,7a-tetrahydro-4H-pyrano[3,2-d][1,2]oxazole-3-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0001105
-
 (3aR,6aS)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0002799
-
 (3aS,6aR)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0005537
-
 (3aS,6aR)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-5,11,14-trioxo-13-(propan-2-yl)-2-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide pH and temperature not specified in the publication Homo sapiens
0.00063
-
 (3aS,7aR)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,5,6,7a-tetrahydro-4H-pyrano[3,2-d][1,2]oxazole-3-carboxamide pH and temperature not specified in the publication Homo sapiens
0.0008086
-
 tert-butyl [(2S)-3-[[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-([(2S)-3-methyl-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-8-oxooctan-4-yl]amino]-3-oxo-2-[[(3aR,6aS)-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazol-3-ylcarbonyl]amino]propyl]carbamate pH and temperature not specified in the publication Homo sapiens
0.004124
-
 tert-butyl [(2S)-3-[[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-([(2S)-3-methyl-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-8-oxooctan-4-yl]amino]-3-oxo-2-[[(3aS,6aR)-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazol-3-ylcarbonyl]amino]propyl]carbamate pH and temperature not specified in the publication Homo sapiens
0.028758
-
 (3aS,6aR)-N-[(2R)-1-([(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]amino)-3-(methylsulfonyl)-1-oxopropan-2-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide pH and temperature not specified in the publication Homo sapiens
0.041126
-
 (3aR,6aS)-N-[(2R)-1-([(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]amino)-3-(methylsulfonyl)-1-oxopropan-2-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide pH and temperature not specified in the publication Homo sapiens