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Literature summary for 3.6.5.5 extracted from

  • Odell, L.R.; Chau, N.; Mariana, A.; Graham, M.E.; Robinson, P.J.; McCluskey, A.
    Azido and diazarinyl analogues of bis-tyrphostin as asymmetrical inhibitors of dynamin GTPase (2009), ChemMedChem, 4, 1182-1188.
    View publication on PubMed
Search for more literature for 3.6.5.5

Activating Compound

Activating Compound Comment Organism Structure
Phospholipid stimulates GTPase activity of dynamin Ovis aries

Inhibitors

Inhibitors Comment Organism Structure
(2E)-2-cyano-N-(3-[[(2E)-2-cyano-3-(3,4-dimethoxyphenyl)prop-2-enoyl]amino]propyl)-3-(3,4-dihydroxyphenyl)prop-2-enamide
-
 Ovis aries
(2E)-2-cyano-N-(3-[[(2E)-2-cyano-3-(4-hydroxyphenyl)prop-2-enoyl]amino]propyl)-3-(3,4-dihydroxyphenyl)prop-2-enamide
-
 Ovis aries
(2E)-2-cyano-N-(3-[[(2E)-2-cyano-3-phenylprop-2-enoyl]amino]propyl)-3-(3,4-dihydroxyphenyl)prop-2-enamide
-
 Ovis aries
(2E,2'E)-N,N'-(2-hydroxypropane-1,3-diyl)bis[2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide]
-
 Ovis aries
(2E,2'E)-N,N'-(2-phenoxypropane-1,3-diyl)bis[2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide]
-
 Ovis aries
(2E,2'E)-N,N'-(2-propoxypropane-1,3-diyl)bis[2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide]
-
 Ovis aries
2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxyphenyl)acryloylamino]-propyl] 3-[4-(3-trifluoromethyl-3H-diazirin-3-yl)phenyl]acrylamide
-
 Ovis aries
3-(4-azidophenyl)-2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxyphenyl)acryloylamino]propyl]acrylamide
-
 Ovis aries
4-azido-N-(2-[2-cyano-3-(3,4-dihydroxyphenyl)acryloylamino]-1-[[2-cyano-3-(3,4-dihydroxyphenyl)acryloylamino]methyl]ethyl)-2,3,5,6-tetrafluorobenzamide
-
 Ovis aries
bis-tyrphostin potent inhibitor of the phospholipid-stimulated GTPase activity of dynamin Ovis aries
N-[2-[[(2E)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enoyl]amino]-1-([[(2E)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enoyl]amino]methyl)ethyl]benzamide
-
 Ovis aries

Organism

Organism UniProt Comment Textmining
Ovis aries
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 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
-
 ?

Synonyms

Synonyms Comment Organism
dynamin I
-
 Ovis aries

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0017
-
 in 10 mM Tris, 10 mM NaCl, 2 mM Mg2+, at 30°C Ovis aries bis-tyrphostin
0.0051
-
 in 10 mM Tris, 10 mM NaCl, 2 mM Mg2, at 30°C Ovis aries (2E,2'E)-N,N'-(2-hydroxypropane-1,3-diyl)bis[2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide]
0.0064
-
 in 10 mM Tris, 10 mM NaCl, 2 mM Mg2+, at 30°C Ovis aries 3-(4-azidophenyl)-2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxyphenyl)acryloylamino]propyl]acrylamide
0.0369
-
 in 10 mM Tris, 10 mM NaCl, 2 mM Mg2+, at 30°C Ovis aries 2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxyphenyl)acryloylamino]-propyl] 3-[4-(3-trifluoromethyl-3H-diazirin-3-yl)phenyl]acrylamide
0.044
-
 in 10 mM Tris, 10 mM NaCl, 2 mM Mg2, at 30°C Ovis aries (2E)-2-cyano-N-(3-[[(2E)-2-cyano-3-(3,4-dimethoxyphenyl)prop-2-enoyl]amino]propyl)-3-(3,4-dihydroxyphenyl)prop-2-enamide
0.051
-
 in 10 mM Tris, 10 mM NaCl, 2 mM Mg2, at 30°C Ovis aries (2E)-2-cyano-N-(3-[[(2E)-2-cyano-3-(4-hydroxyphenyl)prop-2-enoyl]amino]propyl)-3-(3,4-dihydroxyphenyl)prop-2-enamide
0.146
-
 in 10 mM Tris, 10 mM NaCl, 2 mM Mg2, at 30°C Ovis aries (2E)-2-cyano-N-(3-[[(2E)-2-cyano-3-phenylprop-2-enoyl]amino]propyl)-3-(3,4-dihydroxyphenyl)prop-2-enamide
0.5
-
 IC50 above 0.5 mM, in 10 mM Tris, 10 mM NaCl, 2 mM Mg2+, at 30°C Ovis aries 4-azido-N-(2-[2-cyano-3-(3,4-dihydroxyphenyl)acryloylamino]-1-[[2-cyano-3-(3,4-dihydroxyphenyl)acryloylamino]methyl]ethyl)-2,3,5,6-tetrafluorobenzamide
0.5
-
 IC50 above 0.5 mM, in 10 mM Tris, 10 mM NaCl, 2 mM Mg2, at 30°C Ovis aries (2E,2'E)-N,N'-(2-phenoxypropane-1,3-diyl)bis[2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide]
0.5
-
 IC50 above 0.5 mM, in 10 mM Tris, 10 mM NaCl, 2 mM Mg2, at 30°C Ovis aries (2E,2'E)-N,N'-(2-propoxypropane-1,3-diyl)bis[2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide]
0.5
-
 IC50 above 0.5 mM, in 10 mM Tris, 10 mM NaCl, 2 mM Mg2, at 30°C Ovis aries N-[2-[[(2E)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enoyl]amino]-1-([[(2E)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enoyl]amino]methyl)ethyl]benzamide