Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Hill, T.; Odell, L.R.; Edwards, J.K.; Graham, M.E.; McGeachie, A.B.; Rusak, J.; Quan, A.; Abagyan, R.; Scott, J.L.; Robinson, P.J.; McCluskey, A.
    Small molecule inhibitors of dynamin I GTPase activity: development of dimeric tyrphostins (2005), J. Med. Chem., 48, 7781-7788.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.6.5.5 2-cyano-3-(3,4-dihydroxyphenyl)acrylic acid 2-[2-cyano-3-(3,4-dihydroxyphenyl)acryloyloxy]butyl ester IC50: 0.061 mM Ovis aries
3.6.5.5 2-cyano-3-(3,4-dihydroxyphenyl)acrylic acid 2-[2-cyano-3-(3,4-dihydroxyphenyl)acryloyloxy]ethyl ester IC50: 0.042 mM Ovis aries
3.6.5.5 2-cyano-3-(3,4-dihydroxyphenyl)acrylic acid 2-[2-cyano-3-(3,4-dihydroxyphenyl)acryloyloxy]propyl ester IC50: 0.038 mM Ovis aries
3.6.5.5 2-cyano-N-[2-[2-cyano-3-(3,4,5-trihydroxyphenyl)acryloylamino]ethyl]-3-(3,4,5-trihydroxyphenyl)acrylamide IC50: 0.0017 mM Ovis aries
3.6.5.5 2-cyano-N-[2-[2-cyano-3-(3,4-dihydroxy-4-methoxyphenyl)acryloylamino]ethyl]-3-(3,4-dihydroxy-5-methoxyphenyl) acrylamide IC50: 0.009 mM Ovis aries
3.6.5.5 2-cyano-N-[3-[2-cyano-3-(3,4,5-trihydroxyphenyl)acryloylamino]hexyl]-3-(3,4,5-trihydroxyphenyl)acrylamide IC50: 0.006 mM Ovis aries
3.6.5.5 2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxy-5-methoxy-phenyl)acryloylamino]hexyl]-3-(3,4-dihydroxy-5-methoxyphenyl)acrylamide IC50: 0.08 mM Ovis aries
3.6.5.5 2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxy-5-methoxy-phenyl)acryloylamino]pentyl]-3-(3,4-dihydroxy-5-methoxyphenyl)acrylamide IC50: 0.008 mM Ovis aries
3.6.5.5 2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxy-5-methoxyphenyl)acryloylamino]butyl]-3-(3,4-dihydroxy-5-methoxyphenyl)acrylamide IC50: 0.008 mM Ovis aries
3.6.5.5 2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxy-5-methoxyphenyl)acryloylamino]propyl]-3-(3,4-dihydroxy-5-meth-oxyphenyl)acrylamide IC50: 0.005 mM Ovis aries
3.6.5.5 2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxyphenyl)acryloylamino]-2-hydroxypropyl]-3-(3,4-dihydroxyphenyl)acrylamide IC50: 0.0051 mM Ovis aries
3.6.5.5 catechol-acrylamide IC50: 0.0051 mM Ovis aries

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.6.5.5 GTP + H2O Ovis aries GTPase is required for endocytosis GDP + phosphate
-
?

Organism

EC Number Organism UniProt Comment Textmining
3.6.5.5 Ovis aries
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.6.5.5 brain
-
Ovis aries
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.6.5.5 GTP + H2O
-
Ovis aries GDP + phosphate
-
?
3.6.5.5 GTP + H2O GTPase is required for endocytosis Ovis aries GDP + phosphate
-
?

Synonyms

EC Number Synonyms Comment Organism
3.6.5.5 dynamin I
-
Ovis aries

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.6.5.5 0.0017
-
IC50: 0.0017 mM Ovis aries 2-cyano-N-[2-[2-cyano-3-(3,4,5-trihydroxyphenyl)acryloylamino]ethyl]-3-(3,4,5-trihydroxyphenyl)acrylamide
3.6.5.5 0.005
-
IC50: 0.005 mM Ovis aries 2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxy-5-methoxyphenyl)acryloylamino]propyl]-3-(3,4-dihydroxy-5-meth-oxyphenyl)acrylamide
3.6.5.5 0.0051
-
IC50: 0.0051 mM Ovis aries catechol-acrylamide
3.6.5.5 0.0051
-
IC50: 0.0051 mM Ovis aries 2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxyphenyl)acryloylamino]-2-hydroxypropyl]-3-(3,4-dihydroxyphenyl)acrylamide
3.6.5.5 0.006
-
IC50: 0.006 mM Ovis aries 2-cyano-N-[3-[2-cyano-3-(3,4,5-trihydroxyphenyl)acryloylamino]hexyl]-3-(3,4,5-trihydroxyphenyl)acrylamide
3.6.5.5 0.008
-
IC50: 0.008 mM Ovis aries 2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxy-5-methoxyphenyl)acryloylamino]butyl]-3-(3,4-dihydroxy-5-methoxyphenyl)acrylamide
3.6.5.5 0.008
-
IC50: 0.008 mM Ovis aries 2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxy-5-methoxy-phenyl)acryloylamino]pentyl]-3-(3,4-dihydroxy-5-methoxyphenyl)acrylamide
3.6.5.5 0.009
-
IC50: 0.009 mM Ovis aries 2-cyano-N-[2-[2-cyano-3-(3,4-dihydroxy-4-methoxyphenyl)acryloylamino]ethyl]-3-(3,4-dihydroxy-5-methoxyphenyl) acrylamide
3.6.5.5 0.038
-
IC50: 0.038 mM Ovis aries 2-cyano-3-(3,4-dihydroxyphenyl)acrylic acid 2-[2-cyano-3-(3,4-dihydroxyphenyl)acryloyloxy]propyl ester
3.6.5.5 0.042
-
IC50: 0.042 mM Ovis aries 2-cyano-3-(3,4-dihydroxyphenyl)acrylic acid 2-[2-cyano-3-(3,4-dihydroxyphenyl)acryloyloxy]ethyl ester
3.6.5.5 0.061
-
IC50: 0.061 mM Ovis aries 2-cyano-3-(3,4-dihydroxyphenyl)acrylic acid 2-[2-cyano-3-(3,4-dihydroxyphenyl)acryloyloxy]butyl ester
3.6.5.5 0.08
-
IC50: 0.08 mM Ovis aries 2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxy-5-methoxy-phenyl)acryloylamino]hexyl]-3-(3,4-dihydroxy-5-methoxyphenyl)acrylamide