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Literature summary for 3.4.22.38 extracted from

  • Morley, A.D.; Kenny, P.W.; Burton, B.; Heald, R.A.; Macfaul, P.A.; Mullett, J.; Page, K.; Porres, S.S.; Ribeiro, L.R.; Smith, P.; Ward, S.; Wilkinson, T.J.
    5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 1658-1661.
    View publication on PubMed

Application

Application Comment Organism
drug development cathepsin K is seen as an attractive target for intervention in the treatment of both osteoporosis and osteoarthritis Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-(4-acetylpiperazin-1-yl)-5-amino-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-(3-hydroxyazetidin-1-yl)-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-(bicyclo[2.2.1]hept-2-ylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-(cyclohexylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-(cyclopentylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-morpholin-4-yl-6-(phenylamino)pyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-morpholin-4-yl-6-(tetrahydrofuran-3-ylamino)pyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-morpholin-4-yl-6-piperidin-1-ylpyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-morpholin-4-yl-6-pyrrolidin-1-ylpyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-[(1,1-dioxidotetrahydrothiophen-3-yl)amino]-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-[(1-methylethyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-[(1-methylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-[(2,2-dimethylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-[(2-methoxyethyl)amino]-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-[(2-methylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-[(2-methylpropyl)amino]-6-piperazin-1-ylpyrimidine-2-carbonitrile
-
Homo sapiens
5-amino-4-[(2-methylpropyl)amino]-6-[(tetrazolidin-5-ylmethyl)amino]pyrimidine-2-carbonitrile
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
Homo sapiens 5764
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000002
-
-
Homo sapiens 5-amino-4-(bicyclo[2.2.1]hept-2-ylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
0.000006
-
-
Homo sapiens 5-amino-4-[(2-methylpropyl)amino]-6-piperazin-1-ylpyrimidine-2-carbonitrile
0.000009
-
-
Homo sapiens 4-(4-acetylpiperazin-1-yl)-5-amino-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
0.000013
-
-
Homo sapiens 5-amino-4-(cyclopentylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
0.000014
-
-
Homo sapiens 5-amino-4-[(1,1-dioxidotetrahydrothiophen-3-yl)amino]-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
0.000017
-
-
Homo sapiens 5-amino-4-[(2,2-dimethylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
0.000018
-
-
Homo sapiens 5-amino-4-[(2-methylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
0.000022
-
-
Homo sapiens 5-amino-4-morpholin-4-yl-6-pyrrolidin-1-ylpyrimidine-2-carbonitrile
0.000023
-
-
Homo sapiens 5-amino-4-(cyclohexylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
0.000024
-
-
Homo sapiens 5-amino-4-[(2-methoxyethyl)amino]-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
0.000032
-
-
Homo sapiens 5-amino-4-(3-hydroxyazetidin-1-yl)-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
0.00006
-
-
Homo sapiens 5-amino-4-morpholin-4-yl-6-piperidin-1-ylpyrimidine-2-carbonitrile
0.000062
-
-
Homo sapiens 5-amino-4-[(2-methylpropyl)amino]-6-[(tetrazolidin-5-ylmethyl)amino]pyrimidine-2-carbonitrile
0.00011
-
-
Homo sapiens 5-amino-4-morpholin-4-yl-6-(phenylamino)pyrimidine-2-carbonitrile
0.0003
-
-
Homo sapiens 5-amino-4-[(1-methylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
0.00034
-
-
Homo sapiens 5-amino-4-morpholin-4-yl-6-(tetrahydrofuran-3-ylamino)pyrimidine-2-carbonitrile
0.00056
-
-
Homo sapiens 5-amino-4-[(1-methylethyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile