3.6.5.5 (1R,2R)-2-(aminomethyl)-N,N-diethyl-1-phenyl-cyclopropane-1-carboxamide milnacipran 75638 3.6.5.5 (2-chloro-6-methylpyrimidin-4-yl)butylamine - 245190 3.6.5.5 (2-chloro-6-methylpyrimidin-4-yl)cyclohexylamine - 245191 3.6.5.5 (2-chloro-6-methylpyrimidin-4-yl)cyclopropylmethylpropylamine - 245192 3.6.5.5 (2-chloro-6-methylpyrimidin-4-yl)decylamine - 245193 3.6.5.5 (2-chloro-6-methylpyrimidin-4-yl)dimethylamine - 245194 3.6.5.5 (2-chloro-6-methylpyrimidin-4-yl)ethylamine - 245195 3.6.5.5 (2-chloro-6-methylpyrimidin-4-yl)hexylamine - 245196 3.6.5.5 (2-chloro-6-methylpyrimidin-4-yl)octylamine - 245197 3.6.5.5 (2-chloro-6-methylpyrimidin-4-yl)propylamine - 245198 3.6.5.5 (2-chloro-6-methylpyrimidin-4-yl)tetradecylamine - 245199 3.6.5.5 (2E)-2-cyano-N-(3-[[(2E)-2-cyano-3-(3,4-dimethoxyphenyl)prop-2-enoyl]amino]propyl)-3-(3,4-dihydroxyphenyl)prop-2-enamide - 72577 3.6.5.5 (2E)-2-cyano-N-(3-[[(2E)-2-cyano-3-(4-hydroxyphenyl)prop-2-enoyl]amino]propyl)-3-(3,4-dihydroxyphenyl)prop-2-enamide - 72578 3.6.5.5 (2E)-2-cyano-N-(3-[[(2E)-2-cyano-3-phenylprop-2-enoyl]amino]propyl)-3-(3,4-dihydroxyphenyl)prop-2-enamide - 72457 3.6.5.5 (2E,2'E)-N,N'-(2-hydroxypropane-1,3-diyl)bis[2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide] - 72607 3.6.5.5 (2E,2'E)-N,N'-(2-phenoxypropane-1,3-diyl)bis[2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide] - 72608 3.6.5.5 (2E,2'E)-N,N'-(2-propoxypropane-1,3-diyl)bis[2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide] - 72609 3.6.5.5 (3S-trans)-3-((1,3-benzodioxol-5-yloxy)methyl)-4-(4-fluorophenyl)-piperidine paroxetine 75641 3.6.5.5 (4-chloro-6-methylpyrimidin-2-yl)(1-cyclopropylmethylpropyl)amine - 245377 3.6.5.5 (4-chloro-6-methylpyrimidin-2-yl)-dimethylamine - 245378 3.6.5.5 (4-chloro-6-methylpyrimidin-2-yl)butylamine - 245379 3.6.5.5 (4-chloro-6-methylpyrimidin-2-yl)cyclohexylamine - 245380 3.6.5.5 (4-chloro-6-methylpyrimidin-2-yl)decylamine - 245381 3.6.5.5 (4-chloro-6-methylpyrimidin-2-yl)hexylamine - 245383 3.6.5.5 (4-chloro-6-methylpyrimidin-2-yl)octylamine - 245384 3.6.5.5 (4-chloro-6-methylpyrimidin-2-yl)propylamine - 245385 3.6.5.5 (4-chloro-6-methylpyrimidin-2-yl)tetradecylamine - 245386 3.6.5.5 (5Z)-3-(prop-2-en-1-yl)-5-(quinoxalin-2-ylmethylidene)-2-thioxo-1,3-thiazolidin-4-one - 169351 3.6.5.5 (5Z)-3-benzyl-5-(2H-chromen-3-ylmethylidene)-2-thioxo-1,3-thiazolidin-4-one - 169453 3.6.5.5 (5Z)-3-benzyl-5-(3,5-dichlorobenzylidene)-2-thioxo-1,3-thiazolidin-4-one - 87480 3.6.5.5 (5Z)-3-benzyl-5-(4-bromobenzylidene)-2-thioxo-1,3-thiazolidin-4-one - 87516 3.6.5.5 (5Z)-3-benzyl-5-(biphenyl-4-ylmethylidene)-2-thioxo-1,3-thiazolidin-4-one - 169431 3.6.5.5 (5Z)-3-benzyl-5-(quinoxalin-2-ylmethylidene)-2-thioxo-1,3-thiazolidin-4-one - 169433 3.6.5.5 (5Z)-3-benzyl-5-[(5-chloro-1-benzothiophen-3-yl)methylidene]-2-thioxo-1,3-thiazolidin-4-one - 169432 3.6.5.5 (5Z)-3-benzyl-5-[(6,8-dichloro-4-oxo-4H-chromen-3-yl)methylidene]-2-thioxo-1,3-thiazolidin-4-one - 87481 3.6.5.5 (5Z)-3-benzyl-5-[4-[3-(dimethylamino)propoxy]benzylidene]-2-thioxo-1,3-thiazolidin-4-one - 87482 3.6.5.5 (5Z)-3-ethyl-5-(quinoxalin-2-ylmethylidene)-2-thioxo-1,3-thiazolidin-4-one - 169367 3.6.5.5 (5Z)-5-(2,1,3-benzothiadiazol-5-ylmethylidene)-2-thioxo-1,3-thiazolidin-4-one - 169360 3.6.5.5 (5Z)-5-(2,1,3-benzothiadiazol-5-ylmethylidene)-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one - 169347 3.6.5.5 (5Z)-5-(2,1,3-benzothiadiazol-5-ylmethylidene)-3-benzyl-2-thioxo-1,3-thiazolidin-4-one - 169396 3.6.5.5 (5Z)-5-(2,1,3-benzothiadiazol-5-ylmethylidene)-3-ethyl-2-thioxo-1,3-thiazolidin-4-one - 169352 3.6.5.5 (5Z)-5-(2,1,3-benzoxadiazol-5-ylmethylidene)-2-thioxo-1,3-thiazolidin-4-one - 87490 3.6.5.5 (5Z)-5-(2,1,3-benzoxadiazol-5-ylmethylidene)-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one - 169359 3.6.5.5 (5Z)-5-(2,1,3-benzoxadiazol-5-ylmethylidene)-3-benzyl-2-thioxo-1,3-thiazolidin-4-one - 87502 3.6.5.5 (5Z)-5-(2,1,3-benzoxadiazol-5-ylmethylidene)-3-ethyl-2-thioxo-1,3-thiazolidin-4-one - 169368 3.6.5.5 (5Z)-5-(2H-chromen-3-ylmethylidene)-2-thioxo-1,3-thiazolidin-4-one - 87486 3.6.5.5 (5Z)-5-(2H-chromen-3-ylmethylidene)-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one - 169353 3.6.5.5 (5Z)-5-(2H-chromen-3-ylmethylidene)-3-ethyl-2-thioxo-1,3-thiazolidin-4-one - 169354 3.6.5.5 (5Z)-5-(3,5-dichlorobenzylidene)-2-thioxo-1,3-thiazolidin-4-one - 87488 3.6.5.5 (5Z)-5-(3,5-dichlorobenzylidene)-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one - 87476 3.6.5.5 (5Z)-5-(3,5-dichlorobenzylidene)-3-ethyl-2-thioxo-1,3-thiazolidin-4-one - 87485 3.6.5.5 (5Z)-5-(4-bromobenzylidene)-2-thioxo-1,3-thiazolidin-4-one - 169361 3.6.5.5 (5Z)-5-(4-bromobenzylidene)-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one - 169348 3.6.5.5 (5Z)-5-(4-bromobenzylidene)-3-ethyl-2-thioxo-1,3-thiazolidin-4-one - 169364 3.6.5.5 (5Z)-5-(biphenyl-4-ylmethylidene)-2-thioxo-1,3-thiazolidin-4-one - 169362 3.6.5.5 (5Z)-5-(biphenyl-4-ylmethylidene)-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one - 169349 3.6.5.5 (5Z)-5-(biphenyl-4-ylmethylidene)-3-ethyl-2-thioxo-1,3-thiazolidin-4-one - 169365 3.6.5.5 (5Z)-5-(quinoxalin-2-ylmethylidene)-2-thioxo-1,3-thiazolidin-4-one - 87484 3.6.5.5 (5Z)-5-[(5-chloro-1-benzothiophen-3-yl)methylidene]-2-thioxo-1,3-thiazolidin-4-one - 87483 3.6.5.5 (5Z)-5-[(5-chloro-1-benzothiophen-3-yl)methylidene]-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one - 169350 3.6.5.5 (5Z)-5-[(5-chloro-1-benzothiophen-3-yl)methylidene]-3-ethyl-2-thioxo-1,3-thiazolidin-4-one - 169366 3.6.5.5 (5Z)-5-[(6,8-dichloro-4-oxo-4H-chromen-3-yl)methylidene]-2-thioxo-1,3-thiazolidin-4-one - 87489 3.6.5.5 (5Z)-5-[(6,8-dichloro-4-oxo-4H-chromen-3-yl)methylidene]-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one - 169355 3.6.5.5 (5Z)-5-[(6,8-dichloro-4-oxo-4H-chromen-3-yl)methylidene]-3-ethyl-2-thioxo-1,3-thiazolidin-4-one - 87474 3.6.5.5 (5Z)-5-[4-[3-(dimethylamino)propoxy]benzylidene]-2-thioxo-1,3-thiazolidin-4-one - 169363 3.6.5.5 (5Z)-5-[4-[3-(dimethylamino)propoxy]benzylidene]-3-(prop-2-en-1-yl)-2-thioxo-1,3-thiazolidin-4-one - 87477 3.6.5.5 (5Z)-5-[4-[3-(dimethylamino)propoxy]benzylidene]-3-ethyl-2-thioxo-1,3-thiazolidin-4-one - 87475 3.6.5.5 1,2,3,4,10,14b-hexahydro-2-methyldibenzo[c,f]pyrazino[1,2-a]azepine mianserin 75636 3.6.5.5 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro[2]benzofuran-5-carbonitrile citalopram 75639 3.6.5.5 10,11-dihydro-5-[3-(methylamino)propyl]-5H-dibenz[b,f]azepine desipramine 75633 3.6.5.5 2,5-bis(2-(dimethylamino)ethylamino)-1,4-benzoquinone - 206741 3.6.5.5 2,5-bis(2-(hydroxymethyl)anilino)-1,4-benzoquinone - 206751 3.6.5.5 2,5-bis(2-bromoanilino)-1,4-benzoquinone - 206750 3.6.5.5 2,5-bis(2-carboxyanilino)-1,4-benzoquinone - 206744 3.6.5.5 2,5-bis(3-bromopropylamino)-1,4-benzoquinone - 206740 3.6.5.5 2,5-bis(3-carboxyanilino)-1,4-benzoquinone - 206745 3.6.5.5 2,5-bis(3-hydroxyanilino)-1,4-benzoquinone - 206747 3.6.5.5 2,5-bis(3-methoxyanilino)-1,4-benzoquinone - 206748 3.6.5.5 2,5-bis(3-methoxypropylamino)-1,4-benzoquinone - 206753 3.6.5.5 2,5-bis(4-(hydroxymethyl)phenylamino)-1,4-benzoquinone - 206752 3.6.5.5 2,5-bis(4-carboxyanilino)-1,4-benzoquinone - 206746 3.6.5.5 2,5-bis(4-carboxybenzylamino)-1,4-benzoquinone - 206736 3.6.5.5 2,5-bis(4-hydroxyanilino)-1,4-benzoquinone - 206742 3.6.5.5 2,5-bis(4-hydroxybenzylamino)-1,4-benzoquinone - 206738 3.6.5.5 2,5-bis(4-methoxyanilino)-1,4-benzoquinone - 206749 3.6.5.5 2,5-bis(4-methoxybenzylamino)-1,4-benzoquinone - 206737 3.6.5.5 2,5-bis(hexylamino)-1,4-benzoquinone - 206739 3.6.5.5 2,5-bis(phenylamino)-1,4-benzoquinone - 206743 3.6.5.5 2,5-bis-(benzylamino)-1,4-benzoquinone - 206729 3.6.5.5 2-((8-chlorodibenzo(b,f)thiepin-10-yl)oxy)-N,N-dimethylethylamine zotepine 151939 3.6.5.5 2-(2-carboxyanilino)-1,4-naphthoquinone - 206730 3.6.5.5 2-(2-dimethylaminoethyl)-4-N-(didecylamino)-6-methylpyrimidine - 245557 3.6.5.5 2-(3-(hydroxymethyl)anilino)-1,4-naphthoquinone - 206731 3.6.5.5 2-(3-hydroxyanilino)-1,4-naphthoquinone - 206733 3.6.5.5 2-(4-(hydroxymethyl)anilino)-1,4-naphthoquinone - 206732 3.6.5.5 2-(4-hydroxyanilino)-1,4-naphthoquinone - 206734 3.6.5.5 2-(4-hydroxybenzylamino)-1,4-naphthoquinone - 206735 3.6.5.5 2-chloro-4-(2-dimethylaminopropylamine)-6-methylpyrimidine - 245639 3.6.5.5 2-chloro-5-methyl-4-(4-methylpiperazin-1-yl)pyrimidine - 245641 3.6.5.5 2-chloro-N-(4-methoxybenzyl)-6-methylpyrimidin-4-amine - 245644 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 61016 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 61014 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 61015 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 61006 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 61007 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 61011 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 61012 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 61010 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 61009 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 61008 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 61013 3.6.5.5 2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxyphenyl)acryloylamino]-propyl] 3-[4-(3-trifluoromethyl-3H-diazirin-3-yl)phenyl]acrylamide - 75622 3.6.5.5 3-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-N-methyl-1-propanamine nortriptyline 75635 3.6.5.5 3-(2-chloro-10H-phenothiazin-10-yl)-N,N-dimethyl-propan-1-amine chlorpromazine 75626 3.6.5.5 3-(4-azidophenyl)-2-cyano-N-[3-[2-cyano-3-(3,4-dihydroxyphenyl)acryloylamino]propyl]acrylamide - 75623 3.6.5.5 3-(5,6-dihydrobenzo[b][1]benzazepin-11-yl)-N,N-dimethylpropan-1-amine imipramine 75631 3.6.5.5 3-(9-chloro-5,6-dihydrobenzo[b][1]benzazepin-11-yl)-N,N-dimethylpropan-1-amine clomipramine 75632 3.6.5.5 3-sulfo-N-(2-hydroxyethyl)-1,8-naphthalimide - 206705 3.6.5.5 3-[(5Z)-4-oxo-5-(quinoxalin-2-ylmethylidene)-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid - 169373 3.6.5.5 3-[(5Z)-5-(2,1,3-benzothiadiazol-5-ylmethylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid - 169375 3.6.5.5 3-[(5Z)-5-(2,1,3-benzoxadiazol-5-ylmethylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid - 169374 3.6.5.5 3-[(5Z)-5-(2H-chromen-3-ylmethylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid - 87514 3.6.5.5 3-[(5Z)-5-(3,5-dichlorobenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid - 87501 3.6.5.5 3-[(5Z)-5-(4-bromobenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid - 87504 3.6.5.5 3-[(5Z)-5-(biphenyl-4-ylmethylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid - 87505 3.6.5.5 3-[(5Z)-5-[(5-chloro-1-benzothiophen-3-yl)methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid - 87506 3.6.5.5 3-[(5Z)-5-[(6,8-dichloro-4-oxo-4H-chromen-3-yl)methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid - 87508 3.6.5.5 3-[(5Z)-5-[4-[3-(dimethylamino)propoxy]benzylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid - 169376 3.6.5.5 4-(2-dimethylaminoethyl)-2-N-(didecylamino)-6-methylpyrimidine - 245926 3.6.5.5 4-(N,N-dimethyl-N-butyl-N-ethyl)-4-aza-10-oxatricyclo[5.2.1]decane-3,5-dione methanesulfonate - 69323 3.6.5.5 4-(N,N-dimethyl-N-dodecyl-N-ethyl)-4-aza-10-oxatricyclo[5.2.1]decane-3,5-dione bromide - 69320 3.6.5.5 4-(N,N-dimethyl-N-dodecyl-N-ethyl)-4-aza-10-oxatricyclo[5.2.1]decane-3,5-dione methanesulfonate - 69324 3.6.5.5 4-(N,N-dimethyl-N-dodecyl-N-propyl)-4-aza-10-oxa-6-ethyltricyclo[5.2.1]decane-3,5-dione methanesulfonate - 69328 3.6.5.5 4-(N,N-dimethyl-N-dodecyl-N-propyl)-4-aza-10-oxa-6-methyltricyclo[5.2.1]decane-3,5-dione methanesulfonate - 69327 3.6.5.5 4-(N,N-dimethyl-N-dodecyl-N-propyl)-4-aza-10-oxatricyclo[5.2.1]decane-3,5-dione bromide - 69322 3.6.5.5 4-(N,N-dimethyl-N-dodecyl-N-propyl)-4-aza-10-oxatricyclo[5.2.1]decane-3,5-dione methanesulfonate - 69325 3.6.5.5 4-(N,N-dimethyl-N-octadecyl-N-ethyl)-4-aza-10-oxatricyclo[5.2.1]decane-3,5-dione bromide - 69321 3.6.5.5 4-(N-methyl-N-ethylpiperidine)-4-aza-10-oxatricyclo[5.2.1]decane-3,5-dione methanesulfonate - 69326 3.6.5.5 4-amino-3-sulfo-N-(2-(dimethylamino)ethyl)-1,8-naphthalimide - 206711 3.6.5.5 4-amino-3-sulfo-N-(2-(piperazin-1-yl)ethyl)-1,8-naphthalimide - 206712 3.6.5.5 4-amino-3-sulfo-N-(2-aminobenzyl)-1,8-naphthalimide - 206723 3.6.5.5 4-amino-3-sulfo-N-(2-aminoethyl)-1,8-naphthalimide - 206710 3.6.5.5 4-amino-3-sulfo-N-(2-carboxyethyl)-1,8-naphthalimide - 206709 3.6.5.5 4-amino-3-sulfo-N-(2-hydroxyethyl)-1,8-naphthalimide - 206707 3.6.5.5 4-amino-3-sulfo-N-(2-mercaptoethyl)-1,8-naphthalimide - 206720 3.6.5.5 4-amino-3-sulfo-N-(2-methoxyethyl)-1,8-naphthalimide - 206708 3.6.5.5 4-amino-3-sulfo-N-(3-aminobenzyl)-1,8-naphthalimide - 206724 3.6.5.5 4-amino-3-sulfo-N-(3-hydroxyphenyl)-1,8-naphthalimide - 206714 3.6.5.5 4-amino-3-sulfo-N-(3-hydroxypropyl)-1,8-naphthalimide - 206717 3.6.5.5 4-amino-3-sulfo-N-(4-aminobenzyl)-1,8-naphthalimide - 206725 3.6.5.5 4-amino-3-sulfo-N-(4-carboxybenzyl)-1,8-naphthalimide - 206727 3.6.5.5 4-amino-3-sulfo-N-(4-hydroxybenzyl)-1,8-naphthalimide - 206726 3.6.5.5 4-amino-3-sulfo-N-(4-hydroxyphenyl)-1,8-naphthalimide - 206715 3.6.5.5 4-amino-3-sulfo-N-(4-methoxyphenyl)-1,8-naphthalimide - 206716 3.6.5.5 4-amino-3-sulfo-N-(5-hydroxyhexyl)-1,8-naphthalimide - 206719 3.6.5.5 4-amino-3-sulfo-N-(5-hydroxypentyl)-1,8-naphthalimide - 206718 3.6.5.5 4-amino-3-sulfo-N-(carboxymethyl)-1,8-naphthalimide - 206721 3.6.5.5 4-amino-3-sulfo-N-(phenethyl)-1,8-naphthalimide - 206728 3.6.5.5 4-amino-3-sulfo-N-benzyl-1,8-naphthalimide - 206722 3.6.5.5 4-amino-3-sulfo-N-phenyl-1,8-naphthalimide - 206713 3.6.5.5 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 - 75621 3.6.5.5 4-chloro-6-methyl-2-(4-methylpiperazin-1-yl)pyrimidine - 245996 3.6.5.5 4-chloro-N-(4-methoxybenzyl)-6-methylpyrimidin-2-amine - 245999 3.6.5.5 4-sulfo-N-(2-hydroxyethyl)-1,8-naphthalimide - 206706 3.6.5.5 4-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-1-(4-fluorophenyl)-butan-1-one haloperidol 75627 3.6.5.5 5H-dibenz[b,f]azepine-5-carboxamide carbamazepine 75637 3.6.5.5 Arc/Arg3.1 enhances dynamin polymerization and GTPase activity. The activity-regulated cytoskeleton-associated protein, Arc, is an immediate-early gene product implicated in various forms of synaptic plasticity. Arc promotes endocytosis of AMPA type glutamate receptors and regulates cytoskeletal assembly in neuronal dendrites. Bacterially-expressed His6-Arc facilitates the polymerization of Dyn2 and stimulates its GTPase activity under physiologic conditions (37°C and 100 mM NaCl). At lower ionic strength Arc also stabilizes preformed Dyn2 polymers against GTP-dependent disassembly, thereby prolonging assembly-dependent GTP hydrolysis catalyzed by Dyn2. Analysis of recombinant full-length mouse Arc and of His6-tagged fragments, including Arc-N (residues 1-227), Arc-C (residues 228-396), and Arc-(DELTA195-214). At physiologic ionic strength, Arc facilitates Dyn2 self-assembly but does not prevent GTP-dependent Dyn2 disassembly, which is expected to suppress rather than activate endocytosis 247643 3.6.5.5 beta,gamma-methyleneguanosine-5'-monophosphate - 105555 3.6.5.5 bis-tyrphostin potent inhibitor of the phospholipid-stimulated GTPase activity of dynamin 75620 3.6.5.5 Ca2+ 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 15 3.6.5.5 catechol-acrylamide IC50: 0.0051 mM 61005 3.6.5.5 cyclosporin A treating BL-3 cells with 0.005 mM cyclosporine depletes mitochondrial dynamin-2 1044 3.6.5.5 dynamin inhibitory peptide - 151937 3.6.5.5 dynasore interferes in vitro with Drp1 (the mitochondrial dynamin) activity of dynamin 2, acts as a potent inhibitor of endocytic pathways known to depend on dynamin by rapidly blocking coated vesicle formation; interferes in vitro with the GTPase activity of dynamin1, acts as a potent inhibitor of endocytic pathways known to depend on dynamin by rapidly blocking coated vesicle formation; interferes in vitro with the GTPase activity of dynamin 2, acts as a potent inhibitor of endocytic pathways known to depend on dynamin by rapidly blocking coated vesicle formation 8663 3.6.5.5 dynasore noncompetitive inhibitor of dynamin GTPase activity 8663 3.6.5.5 dynasore - 8663 3.6.5.5 dynasore specific inhibitor of dynamin GTP hydrolysis 8663 3.6.5.5 dynasore a dynamin inhibitor 8663 3.6.5.5 dynasore dynamin specific inhibitor 8663 3.6.5.5 fluvoxamine a noncompetitive inhibitor of dynamin I with respect to GTP and a competitive inhibitor with respect to L-phosphatidylserine 75624 3.6.5.5 GTP-gamma-S - 6532 3.6.5.5 guanylyl-iminodiphosphate - 106243 3.6.5.5 heterotrimeric G protein betagamma subunit complex oligomerization of dynamin prevents inhibition 49108 3.6.5.5 methyl 2-phenyl-2-(2-piperidyl)acetate methylphenidate 75630 3.6.5.5 mitochondrial division inhibitor selectively inhibits the mitochondrial division dynamin, is a selective inhibitor of the mitochondrial division dynamin-related GTPase Drp1, and has no effect on either basal or assembly-stimulated rates of GTP hydrolysis for dynamin-1 151936 3.6.5.5 additional information 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 2 3.6.5.5 additional information human Drp1 is knocked down in HeLa cells by the specific siRNA 2 3.6.5.5 additional information rhodadyns are a class of small molecule inhibitors of dynamin GTPase activity 2 3.6.5.5 additional information 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 2 3.6.5.5 additional information 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 2 3.6.5.5 additional information 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 2 3.6.5.5 myristyl trimethyl ammonium bromide standard inhibitor of dynamin I 75625 3.6.5.5 N'-(2-chloro-6-methylpyrimidin-4-yl)ethane-1,2-diamine - 246367 3.6.5.5 N'-(4-Chloro-6-methylpyrimidin-2-yl)-ethane-1,2-diamine - 246491 3.6.5.5 N-(2-diethylaminoethyl)-2-methoxy-5-methylsulfonyl-benzamide tiapride 75629 3.6.5.5 N-(2-hydroxyethyl)-1,8-naphthalimide - 206704 3.6.5.5 N-benzyl-2-chloro-6-methylpyrimidin-4-amine - 246656 3.6.5.5 N-benzyl-4-chloro-6-methylpyrimidin-2-amine - 246661 3.6.5.5 N-decyl-N'-(2-dimethylaminoethyl)-pyrimidine-4,6-diamine - 246733 3.6.5.5 N-dodecyl-N'-(2-dimethylaminoethyl)pyrimidine-4,6-diamine - 246734 3.6.5.5 N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]-propan-1-amine fluoxetine 75640 3.6.5.5 N-methyl-9,10-ethanoanthracene-9(10H)-propanamine maprotiline 75634 3.6.5.5 N-[(1-ethylpyrrolidin-2-yl)methyl]-2-methoxy-5-sulfamoyl-benzamide sulpiride 75628 3.6.5.5 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 - 73737 3.6.5.5 N1-(4-chloro-6-methylpyrimidin-2-yl)-N3,N3-dimethylpropane-1,3-diamine - 246826 3.6.5.5 N2-(2-dimethylaminoethyl)-6-methyl-N4-octadecylpyrimidine-2,4-diamine - 246832 3.6.5.5 N2-(2-dimethylaminoethyl)-6-methyl-N4-propylpyrimidine-2,4-diamine - 246833 3.6.5.5 N2-(2-dimethylaminoethyl)-6-methyl-N4-tetradecylpyrimidine-2,4-diamine - 246834 3.6.5.5 N2-(2-dimethylaminoethyl)-N4-decyl-6-methylpyrimidine-2,4-diamine - 246835 3.6.5.5 N2-(2-dimethylaminoethyl)-N4-hexyl-6-methylpyrimidine-2,4-diamine - 246836 3.6.5.5 N2-(2-dimethylaminoethyl)-N4-octyl-6-methylpyrimidine-2,4-diamine - 246837 3.6.5.5 N2-benzyl-N4-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine - 246842 3.6.5.5 N2-butyl-N4-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine - 246843 3.6.5.5 N2-cyclohexyl-N4-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine - 246844 3.6.5.5 N2-cyclopropylmethyl-N4-(2-dimethylamin-ethyl)-6-methyl-N2-propylpyrimidine-2,4-diamine - 246845 3.6.5.5 N2-decyl-N4-(2-dimethylaminoethyl)pyrimidine-2,4-diamine - 246846 3.6.5.5 N2-dodecyl-N4-(2-dimethylaminoethyl)-pyrimidine-2,4-diamine - 246847 3.6.5.5 N2-sec-butyl-N4-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine - 246848 3.6.5.5 N4-(2-dimethylaminoethyl)-6-methyl-N2-octadecylpyrimidine-2,4-diamine - 246872 3.6.5.5 N4-(2-dimethylaminoethyl)-6-methyl-N2-propylpyrimidine-2,4-diamine - 246873 3.6.5.5 N4-(2-dimethylaminoethyl)-6-methyl-N2-tetradecylpyrimidine-2,4-diamine - 246874 3.6.5.5 N4-(2-dimethylaminoethyl)-N2-decyl-6-methylpyrimidine-2,4-diamine - 246875 3.6.5.5 N4-(2-dimethylaminoethyl)-N2-hexyl-6-methylpyrimidine-2,4-diamine - 246876 3.6.5.5 N4-(2-dimethylaminoethyl)-N2-octyl-6-methylpyrimidine-2,4-diamine - 246877 3.6.5.5 N4-Benzyl-N2-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine - 246878 3.6.5.5 N4-butyl-N2-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine - 246879 3.6.5.5 N4-cyclohexyl-N2-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine - 246880 3.6.5.5 N4-cyclopropylmethyl-N2-(2-dimethylamin-ethyl)-6-methyl-N2-propylpyrimidine-2,4-diamine - 246881 3.6.5.5 N4-decyl-N2-(2-dimethylaminoethyl)pyrimidine-2,4-diamine - 246882 3.6.5.5 N4-dodecyl-N2-(2-dimethylaminoethyl)pyrimidine-2,4-diamine - 246883 3.6.5.5 N4-sec-butyl-N2-(2-dimethylaminoethyl)-6-methylpyrimidine-2,4-diamine - 246884 3.6.5.5 NEM - 89 3.6.5.5 oligomeric beta-amyloid induces dynamin 1 cleavage and depletion, 0.001 mM of A-705253 potently inhibits oligomeric beta-amyloid-induced dynamin 1 cleavage 151938 3.6.5.5 sec-butyl-(2-chloro-6-methylpyrimidin-4-yl)amine - 246933 3.6.5.5 sec-butyl-(4-chloro-6-methylpyrimidin-2-yl)amine - 246934 3.6.5.5 sertraline a mixed type inhibitor with respect to both GTP and L-phosphatidylserine 10052 3.6.5.5 [(5Z)-4-oxo-5-(quinoxalin-2-ylmethylidene)-2-thioxo-1,3-thiazolidin-3-yl]acetic acid - 169357 3.6.5.5 [(5Z)-5-(2,1,3-benzothiadiazol-5-ylmethylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid - 169377 3.6.5.5 [(5Z)-5-(2,1,3-benzoxadiazol-5-ylmethylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid - 169358 3.6.5.5 [(5Z)-5-(2H-chromen-3-ylmethylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid - 169370 3.6.5.5 [(5Z)-5-(3,5-dichlorobenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid - 87487 3.6.5.5 [(5Z)-5-(4-bromobenzylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid - 169356 3.6.5.5 [(5Z)-5-(biphenyl-4-ylmethylidene)-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid - 87478 3.6.5.5 [(5Z)-5-[(5-chloro-1-benzothiophen-3-yl)methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid - 87479 3.6.5.5 [(5Z)-5-[(6,8-dichloro-4-oxo-4H-chromen-3-yl)methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid - 87503 3.6.5.5 [(5Z)-5-[4-[3-(dimethylamino)propoxy]benzylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid - 169372 3.6.5.5 [2-(2-chloro-6-methylpyrimidin-4-ylamino)ethyl]carbamic acid tert-butyl ester - 246982 3.6.5.5 [2-(4-chloro-6-methylpyrimidin-2-ylamino)ethyl]carbamic acid tert-butyl ester - 246983