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Literature summary for 5.2.1.8 extracted from

  • Babine, R.E.; Bleckman, T.M.; Kissinger, C.R.; Showalter, R.; Pelletier, L.A.; Lewis, C.; Tucker, K.; Moomaw, E.; Parge H.E.; Villafranca, J.E.
    Design, synthesis and X-ray crystallographic studies of novel FKBP-12 ligands (1995), Bioorg. Med. Chem. Lett., 5, 1719-1724.
No PubMed abstract available

Crystallization (Commentary)

Crystallization (Comment) Organism
mutant P9Q/R13F/K17V/R18F in complex with 1-(pyridin-4-ylthio)bicyclo[3.3.1]nonan-3-one Homo sapiens

Protein Variants

Protein Variants Comment Organism
P9Q/R13F/K17V/R18F mutant designed for crytallizability, crystal structure in complex with 1-(pyridin-4-ylthio)bicyclo[3.3.1]nonan-3-one Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(3-hydroxyphenoxy)bicyclo[3.3.1]nonan-3-one
-
Homo sapiens
1-(phenylthio)bicyclo[3.3.1]nonan-3-one
-
Homo sapiens
1-(pyridin-4-ylthio)bicyclo[3.3.1]nonan-3-one
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isoform FKBP12
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0079
-
1-(pyridin-4-ylthio)bicyclo[3.3.1]nonan-3-one
-
Homo sapiens
0.0092
-
1-(phenylthio)bicyclo[3.3.1]nonan-3-one
-
Homo sapiens
0.0167
-
1-(3-hydroxyphenoxy)bicyclo[3.3.1]nonan-3-one
-
Homo sapiens