Literature summary for 3.6.5.5 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.

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Inhibitors

Inhibitors	Comment	Organism	Structure
2-cyano-3-(3,4-dihydroxyphenyl)acrylic acid 2-[2-cyano-3-(3,4-dihydroxyphenyl)acryloyloxy]butyl ester	IC50: 0.061 mM	Ovis aries
2-cyano-3-(3,4-dihydroxyphenyl)acrylic acid 2-[2-cyano-3-(3,4-dihydroxyphenyl)acryloyloxy]ethyl ester	IC50: 0.042 mM	Ovis aries
2-cyano-3-(3,4-dihydroxyphenyl)acrylic acid 2-[2-cyano-3-(3,4-dihydroxyphenyl)acryloyloxy]propyl ester	IC50: 0.038 mM	Ovis aries
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
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
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
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
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
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
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
2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxyphenyl)acryloylamino]-2-hydroxypropyl]-3-(3,4-dihydroxyphenyl)acrylamide	IC50: 0.0051 mM	Ovis aries
catechol-acrylamide	IC50: 0.0051 mM	Ovis aries

Natural Substrates/ Products (Substrates)

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

Organism

Organism	UniProt	Comment	Textmining
Ovis aries	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
brain	-	Ovis aries	-

Substrates and Products (Substrate)

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

Synonyms

Synonyms	Comment	Organism
dynamin I	-	Ovis aries

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
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
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
0.0051	-	IC50: 0.0051 mM	Ovis aries	catechol-acrylamide
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
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
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
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
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
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
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
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
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

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Release 2023.1 (January 2023)