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Results 1 - 10 of 248 > >>
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EC Number Inhibitors Commentary Structure
Display the word mapDisplay the reaction diagram Show all sequences 3.6.5.5more depolarization of primary neurons includes direct association of receptor-type protein tyrosine phosphatase PTP-NP with dynamin-1 within 30 s. This association results in significant inhibition of dynamin-1 GTPase activity (about 75% inhibition). Mutation within the phosphatase domain of PTP-NP (PTP-NP(D947A)) abolishes the direct interaction of PTP-NP with dynamin-1 and fails to inhibit dynamin-1 GTPase activity Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 3.6.5.5more human Drp1 is knocked down in HeLa cells by the specific siRNA Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 3.6.5.5more rhodadyns are a class of small molecule inhibitors of dynamin GTPase activity Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 3.6.5.5more development of quinone analogues as dynamin GTPase inhibitors, docking study and molecular modelling, overview. No or poor inhibition by 2,5-bis(2-methylanilino)-1,4-benzoquinone, 2,5-bis(2-methoxyanilino)-1,4-benzoquinone, 2,5-bis(3-(hydroxymethyl)phenylamino)-1,4-benzoquinone, 2,5-b+F49is(2-hydroxyethylamino)-1,4-benzoquinone, 2,5-bis(3-hydroxypropylamino)-1,4-benzoquinone, 2,5-bis(4-hydroxybutylamino)-1,4-benzoquinone, 2,5-bis(2-methoxyethylamino)-1,4-benzoquinone, 2,5-bis(2-(methylthio)ethylamino)-1,4-benzoquinone, 2,5-bis(2-chloroethylamino)-1,4-benzoquinone, 2,5-bis(2-bromoethylamino)-1,4-benzoquinone, 2,5-bis(3-chloropropylamino)-1,4-benzoquinone, 2,5-bis(3-pyridylmethylamino)-1,4-benzoquinone, 2,5-bis(4-methylbenzylamino)-1,4-benzoquinone, 2,5-bis(4-fluorobenzylamino)-1,4-benzoquinone, 2,5-bis(4-bromobenzylamino)-1,4-benzoquinone, 2,5-bis(4-chlorobenzylamino)-1,4-benzoquinone, 2,5-bis(phenethylamino)-1,4-benzoquinone, 2,5-bis(ethylamino)-1,4-benzoquinone, 2,5-bis(propylamino)-1,4-benzoquinone, 2,5-bis(butylamino)-1,4-benzoquinone, 2,5-bis(pentylamino)-1,4-benzoquinone, 2,5-bis(isopentylamino)-1,4-benzoquinone, 2,5-bis(allylamino)-1,4-benzoquinone, 2-(2-hydroxyethylamino)-1,4-naphthoquinone, 2-(3-hydroxypropylamino)-1,4-naphthoquinone, 2-(anilino)-1,4-naphthoquinone, 2-(3-carboxyanilino)-1,4-naphthoquinone, 2-(4-carboxyanilino)-1,4-naphthoquinone, 2-(benzylamino)-1,4-naphthoquinone, and 2-(4-methoxybenzylamino)-1,4-naphthoquinone Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 3.6.5.5more fragment-based in silico screening against dynamin I GTPase activity identified the 1,8-naphthalimide framework as a potential scaffold for the design of new inhibitors targeting the GTP binding pocket of dynI. Structure-based design, synthesis and subsequent optimization resulted in the development of a library of 1,8-naphthalimide derivatives. Development of optimised GTP-competitive lead Naphthaladyn compound for the further development of naphthalimide-based dynI GTPase inhibitor. Molecular docking and molecular modelling representation of the predicted binding pose of naphthalimide 4-amino-3-sulfo-N-(2-aminoethyl)-1,8-naphthalimide within the GTP binding pocket of dynI, crystal structure, PDB ID 3ZYCS Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 3.6.5.5more computational approach of binding site identification, docking, and interaction energy calculations to design a library of aminopyrimidine analogues targeting site-2 of the pleckstrin homology (PH) domain. Synthesis and evaluation of pyrimidine-based inhibitors of dynamin I GTPase activity, competitive inhibition at the pleckstrin homology domain, overview. The optimized analogues show low micromolar inhibition against both dynamin I and CME and off-target effects at the cholecystokinin, dopamine D2, histamine H1 and H2, melanocortin, melatonin, muscarinic M1 and M3, neurokinin, opioid KOP and serotonin receptors. No inhibition by (4-chloro-6-methylpyrimidin-2-yl)ethylamine at 0.3 mM Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 3.6.5.5Ca2+ inhibits dynamin I GTPase activity after stimulation by phosphorylation or by phospholipids but not after stimulation a glutathione S-transferase-SH3 fusion protein containing the SH3-domain of phosphoinositide 3-kinase Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 3.6.5.5NEM - Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 3.6.5.5cyclosporin A treating BL-3 cells with 0.005 mM cyclosporine depletes mitochondrial dynamin-2 Go to the Ligand Summary Page
Display the word mapDisplay the reaction diagram Show all sequences 3.6.5.5GTP-gamma-S - Go to the Ligand Summary Page
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