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Literature summary for 3.4.24.19 extracted from

  • Bailey, S.; Fish, P.V.; Billotte, S.; Bordner, J.; Greiling, D.; James, K.; McElroy, A.; Mills, J.E.; Reed, C.; Webster, R.
    Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents (2008), Bioorg. Med. Chem. Lett., 18, 6562-6567.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-5-methyl-1,3-oxazole-4-carboxamide
-
Homo sapiens
2-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-N,N-dimethyl-5-methyl-1,3-oxazole-4-carboxamide
-
Homo sapiens
5-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-1,2,4-oxadiazole-3-carboxamide i.e. UK-383,367. Good selectivity over matrix metalloproteinases involved in wound healing, effective in a cell-based model of collagen deposition and in penetrating human skin in vitro Homo sapiens
5-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-N,N-dimethyl-1,2,4-oxadiazole-3-carboxamide good selectivity over matrix metalloproteinases involved in wound healing Homo sapiens
5-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-N-isopropyl-1,2,4-oxadiazole-3-carboxamide
-
Homo sapiens
N-[(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)carbonyl]glycine
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-(4'-(dimethylaminophenylazo)-benzoyl)-Arg-Tyr-Tyr-Arg-Ala-Asp-Asp-Ala-Asn-Val-Glu-(EDANS)-NH2 + H2O
-
Homo sapiens ?
-
?
procollagen 1 + H2O
-
Homo sapiens ?
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00001
-
-
Homo sapiens 5-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-N,N-dimethyl-1,2,4-oxadiazole-3-carboxamide
0.000017
-
-
Homo sapiens 2-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-N,N-dimethyl-5-methyl-1,3-oxazole-4-carboxamide
0.000017
-
-
Homo sapiens 2-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-5-methyl-1,3-oxazole-4-carboxamide
0.000021
-
-
Homo sapiens 5-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-N-isopropyl-1,2,4-oxadiazole-3-carboxamide
0.000021
-
-
Homo sapiens N-[(5-[(1R)-4-cyclohexyl-1-[2-(hydroxyamino)-2-oxoethyl]butyl]-1,2,4-oxadiazol-3-yl)carbonyl]glycine
0.000044
-
-
Homo sapiens 5-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-1,2,4-oxadiazole-3-carboxamide