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Literature summary for 3.4.22.15 extracted from

  • Irie, O.; Kosaka, T.; Kishida, M.; Sakaki, J.; Masuya, K.; Konishi, K.; Yokokawa, F.; Ehara, T.; Iwasaki, A.; Iwaki, Y.; Hitomi, Y.; Toyao, A.; Gunji, H.; Teno, N.; Iwasaki, G.; Hirao, H.; Kanazawa, T.; Tanabe, K.; Hiestand, P.C.; Malcangio, M.; Fox, A.J.; Bevan, S.J.; Yaqoob, M.; Culshaw, A.J.; Hart, T.W.; Hallet, A.
    Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2 (2008), Bioorg. Med. Chem. Lett., 18, 5280-5284.
    View publication on PubMed
Search for more literature for 3.4.22.15

Inhibitors

Inhibitors Comment Organism Structure
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
 Homo sapiens
2-cyano-4-[(1,4-dioxaspiro[4.5]dec-8-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
-
 Homo sapiens
2-cyano-4-[(2-cyclopentylethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
-
 Homo sapiens
2-cyano-4-[(6,8-dioxaspiro[3.5]non-7-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
-
 Homo sapiens
2-cyano-4-[[1-(2-hydroxyethyl)piperidin-4-yl]methoxy]-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
 Homo sapiens
2-cyano-N-methyl-4-(piperidin-4-ylmethoxy)-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
 Homo sapiens
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
 Homo sapiens
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[4.5]dec-8-ylmethyl)amino]pyrimidine-5-carboxamide
-
 Homo sapiens
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
-
 Homo sapiens
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
 Homo sapiens
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
 Homo sapiens
2-cyano-N-methyl-4-[[1-(1-methylethyl)piperidin-4-yl]methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
 Homo sapiens
4-[(1-acetylpiperidin-4-yl)methoxy]-2-cyano-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens catL is essential for epidermal homeostasis and regular hair follicle morphogenesis and cycling ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P07711
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information catL is essential for epidermal homeostasis and regular hair follicle morphogenesis and cycling Homo sapiens ?
-
 ?
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Z-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
cathepsin L
-
 Homo sapiens
CatL
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
 IC50 is above 0.001 mM, determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate Homo sapiens 2-cyano-4-[(6,8-dioxaspiro[3.5]non-7-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
0.00012
-
 determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate Homo sapiens 2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
0.000276
-
 determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate Homo sapiens 2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[4.5]dec-8-ylmethyl)amino]pyrimidine-5-carboxamide
0.0003
-
 determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate Homo sapiens 2-cyano-4-[[1-(2-hydroxyethyl)piperidin-4-yl]methoxy]-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
0.00033
-
 determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate Homo sapiens 2-cyano-N-methyl-4-[[1-(1-methylethyl)piperidin-4-yl]methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
0.00036
-
 determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate Homo sapiens 2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
0.0004
-
 determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate Homo sapiens 2-cyano-4-[(2-cyclopentylethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
0.000426
-
 determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate Homo sapiens 2-cyano-4-[(1,4-dioxaspiro[4.5]dec-8-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
0.00044
-
 determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate Homo sapiens 2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
0.00046
-
 determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate Homo sapiens 2-cyano-N-methyl-4-(piperidin-4-ylmethoxy)-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
0.0012
-
 determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate Homo sapiens 2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
0.00139
-
 determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate Homo sapiens 2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
0.0025
-
 determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate Homo sapiens 4-[(1-acetylpiperidin-4-yl)methoxy]-2-cyano-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide