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Literature summary for 5.2.1.8 extracted from

  • Yamashita, D.S.; Oh, H.J.; Yen, H.K.; Bossard, M.J.; Brandt, M.; Levy, M.A.; Newman-Tarr,T.; Badger,A.; Luengo J.I.; Halt, D.A.
    Design, synthesis and evaluation of dual domain FKBP ligands (1994), Bioorg. Med. Chem. Lett., 4, 325-328.
No PubMed abstract available

Inhibitors

Inhibitors Comment Organism Structure
(1R)-1-[3-(diethenylcarbamoyl)phenyl]-3-phenylpropyl 1-(3,3-dimethyl-2-oxopentanoyl)piperidine-2-carboxylate inhibition of FKBP12 cis-trans peptidylprolyl isomerase activity, but no activity in splenocyte mitogenesis assay for immunosuppression Homo sapiens
(1R)-3-phenyl-1-[3-(phenylcarbonyl)phenyl]propyl 1-(3,3-dimethyl-2-oxopentanoyl)piperidine-2-carboxylate inhibition of FKBP12 cis-trans peptidylprolyl isomerase activity, but no activity in splenocyte mitogenesis assay for immunosuppression 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
0.000005
-
(1R)-3-phenyl-1-[3-(phenylcarbonyl)phenyl]propyl 1-(3,3-dimethyl-2-oxopentanoyl)piperidine-2-carboxylate
-
Homo sapiens
0.000005
-
(1R)-1-[3-(diethenylcarbamoyl)phenyl]-3-phenylpropyl 1-(3,3-dimethyl-2-oxopentanoyl)piperidine-2-carboxylate
-
Homo sapiens