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Literature summary for 3.4.23.5 extracted from

  • Low, J.D.; Bartberger, M.D.; Chen, K.; Cheng, Y.; Fielden, M.R.; Gore, V.; Hickman, D.; Liu, Q.; Allen Sickmier, E.; Vargas, H.M.; Werner, J.; White, R.D.; Whittington, D.A.; Wood, S.; Minatti, A.E.
    Development of 2-aminooxazoline 3-azaxanthene beta-amyloid cleaving enzyme (BACE) inhibitors with improved selectivity against cathepsin D (2017), MedChemComm, 8, 1196-1206 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(4'S)-3-(2-fluoropyridin-4-yl)-7-[5-(prop-1-yn-1-yl)pyridin-3-yl]-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
-
Homo sapiens
(4'S)-3-(3,6-dihydro-2H-pyran-4-yl)-7-[5-(prop-1-yn-1-yl)pyridin-3-yl]-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
-
Homo sapiens
(4'S)-3-(3,6-dihydro-2H-pyran-4-yl)-7-[5-[(3-methyloxetan-3-yl)ethynyl]pyridin-3-yl]-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
-
Homo sapiens
(4'S)-3-(5,6-dihydro-2H-pyran-3-yl)-1-fluoro-7-(2-fluoropyridin-3-yl)-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
-
Homo sapiens
(4'S)-3-(5,6-dihydro-2H-pyran-3-yl)-7-[5-(prop-1-yn-1-yl)pyridin-3-yl]-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
-
Homo sapiens
(4'S)-3-chloro-7-(5-fluoropyridin-3-yl)-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
-
Homo sapiens
(4'S)-3-chloro-7-[5-(prop-1-yn-1-yl)pyridin-3-yl]-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
-
Homo sapiens
(4'S)-3-methoxy-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazole]-2',7-diamine
-
Homo sapiens
(4'S)-7-(2-fluoropyridin-3-yl)-3-(2-fluoropyridin-4-yl)-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
-
Homo sapiens
(4'S)-7-[5-(cyclopropylethynyl)pyridin-3-yl]-3-(3,6-dihydro-2H-pyran-4-yl)-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
-
Homo sapiens
3-[5-[(4'S)-2'-amino-3-(3,6-dihydro-2H-pyran-4-yl)-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-7-yl]pyridin-3-yl]prop-2-yn-1-ol
-
Homo sapiens
N-[(4'S)-2'-amino-3-(3,6-dihydro-2H-pyran-4-yl)-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-7-yl]-5-chloropyridine-2-carboxamide
-
Homo sapiens
N-[(4'S)-2'-amino-3-(5,6-dihydro-2H-pyran-3-yl)-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-7-yl]-5-chloropyridine-2-carboxamide
-
Homo sapiens
N-[(4'S)-2'-amino-3-chloro-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-7-yl]-5-chloropyridine-2-carboxamide
-
Homo sapiens
N-[(4'S)-2'-amino-3-cyclopropyl-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-7-yl]-5-chloropyridine-2-carboxamide
-
Homo sapiens
N-[(4'S)-2'-amino-3-methoxy-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-7-yl]-5-chloropyridine-2-carboxamide
-
Homo sapiens
N-[(4'S)-2'-amino-3-methyl-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-7-yl]-5-chloropyridine-2-carboxamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
CatD
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00009
-
pH and temperature not specified in the publication Homo sapiens (4'S)-3-(5,6-dihydro-2H-pyran-3-yl)-1-fluoro-7-(2-fluoropyridin-3-yl)-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
0.00066
-
pH and temperature not specified in the publication Homo sapiens (4'S)-7-(2-fluoropyridin-3-yl)-3-(2-fluoropyridin-4-yl)-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
0.0027
-
pH and temperature not specified in the publication Homo sapiens (4'S)-3-(5,6-dihydro-2H-pyran-3-yl)-7-[5-(prop-1-yn-1-yl)pyridin-3-yl]-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
0.0036
-
pH and temperature not specified in the publication Homo sapiens (4'S)-7-[5-(cyclopropylethynyl)pyridin-3-yl]-3-(3,6-dihydro-2H-pyran-4-yl)-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
0.0044
-
pH and temperature not specified in the publication Homo sapiens 3-[5-[(4'S)-2'-amino-3-(3,6-dihydro-2H-pyran-4-yl)-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-7-yl]pyridin-3-yl]prop-2-yn-1-ol
0.0045
-
pH and temperature not specified in the publication Homo sapiens (4'S)-3-(2-fluoropyridin-4-yl)-7-[5-(prop-1-yn-1-yl)pyridin-3-yl]-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
0.0059
-
pH and temperature not specified in the publication Homo sapiens (4'S)-3-(3,6-dihydro-2H-pyran-4-yl)-7-[5-(prop-1-yn-1-yl)pyridin-3-yl]-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
0.012
-
pH and temperature not specified in the publication Homo sapiens (4'S)-3-(3,6-dihydro-2H-pyran-4-yl)-7-[5-[(3-methyloxetan-3-yl)ethynyl]pyridin-3-yl]-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
0.015
-
pH and temperature not specified in the publication Homo sapiens (4'S)-7-(2-fluoropyridin-3-yl)-3-(2-fluoropyridin-4-yl)-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
0.072
-
pH and temperature not specified in the publication Homo sapiens (4'S)-3-chloro-7-[5-(prop-1-yn-1-yl)pyridin-3-yl]-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
0.13
-
pH and temperature not specified in the publication Homo sapiens (4'S)-3-chloro-7-(5-fluoropyridin-3-yl)-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-2'-amine
0.31
-
pH and temperature not specified in the publication Homo sapiens N-[(4'S)-2'-amino-3-cyclopropyl-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-7-yl]-5-chloropyridine-2-carboxamide
0.48
-
pH and temperature not specified in the publication Homo sapiens N-[(4'S)-2'-amino-3-(5,6-dihydro-2H-pyran-3-yl)-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-7-yl]-5-chloropyridine-2-carboxamide
0.64
-
pH and temperature not specified in the publication Homo sapiens N-[(4'S)-2'-amino-3-methyl-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-7-yl]-5-chloropyridine-2-carboxamide
1
-
pH and temperature not specified in the publication Homo sapiens N-[(4'S)-2'-amino-3-(3,6-dihydro-2H-pyran-4-yl)-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-7-yl]-5-chloropyridine-2-carboxamide
1.1
-
pH and temperature not specified in the publication Homo sapiens N-[(4'S)-2'-amino-3-chloro-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-7-yl]-5-chloropyridine-2-carboxamide
1.2
-
pH and temperature not specified in the publication Homo sapiens N-[(4'S)-2'-amino-3-methoxy-5'H-spiro[[1]benzopyrano[2,3-c]pyridine-5,4'-[1,3]oxazol]-7-yl]-5-chloropyridine-2-carboxamide