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show all sequences of 3.6.4.4

The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5

Schiemann, K.; Finsinger, D.; Zenke, F.; Amendt, C.; Knoechel, T.; Bruge, D.; Buchstaller, H.P.; Emde, U.; Staehle, W.; Anzali, S.; Bioorg. Med. Chem. Lett. 20, 1491-1495 (2010)

Data extracted from this reference:

Crystallization (Commentary)
Crystallization
Organism
study of the discovery and optimization of hexahydr-2H-pyranol[3,2-c]quinolines, HHPQs as inhibitors. Crystallographic data demonstrate that these potent and selectve inhibitors bind in an allosteric pocket of kinesin-5 distant from the nucleotide and microtubule binding sites
Homo sapiens
Inhibitors
Inhibitors
Commentary
Organism
Structure
((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methanamine
-
Homo sapiens
(2R,4aS,5R,10bS)-2-((1H-1,2,4-triazol-1-yl)methyl)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,10bS)-9-(tert-butyl)-5-(3-chlorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,10bS)-9-(tert-butyl)-5-(3-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline-9-carbonitrile
-
Homo sapiens
(4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline-9-carboxylic acid
-
Homo sapiens
(4aS,5R,10bS)-5-phenyl-9-(trifluoromethoxy)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-5-phenyl-9-propyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-7,9-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-7-fluoro-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-8,10-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-8,9-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-8-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-8-chloro-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(pentafluoro-lambda6-sulfanyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(1H-imidazol-2-yl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(2-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(3-chlorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(3-fluoro-4-methoxyphenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(3-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(4-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(pyridin-3-yl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(thiazol-2-yl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-chloro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-ethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-isopropyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-methyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-N,N-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-9-amine
-
Homo sapiens
(4aS,5S,10bS)-9-(tert-butyl)-5-cyclohexyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
1-((2R,4aS,5R,10bS)-5-(4-fluorophenyl)-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
-
Homo sapiens
1-((2R,4aS,5R,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
-
Homo sapiens
1-((2R,4aS,5R,10bS)-9-bromo-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
-
Homo sapiens
1-((2R,4aS,5R,10bS)-9-cyclopropyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
-
Homo sapiens
1-(2-(dimethylamino)ethyl)-3-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)urea
-
Homo sapiens
1-(3-hydroxypropyl)-3-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)urea
-
Homo sapiens
1-(4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenyl)ethanone
-
Homo sapiens
2-((((2R,4aS,5R,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)(ethyl)amino)ethanol
-
Homo sapiens
2-((((2R,4aS,5R,10bS)-9-chloro-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)amino)ethanol
-
Homo sapiens
2-((2R,4aS,5R,10bS)-9-(tert-butyl)-2-((methylamino)methyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzenethiol
-
Homo sapiens
2-((4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-9-yl)acetonitrile
-
Homo sapiens
2-((4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-9-yl)ethanol
-
Homo sapiens
2-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)-4-chlorobenzenethiol
-
Homo sapiens
2-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzenethiol
-
Homo sapiens
2-(dimethylamino)ethyl (((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)carbamate
-
Homo sapiens
2-(methylamino)-N-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)ethanesulfonothioamide
-
Homo sapiens
3-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)aniline
-
Homo sapiens
3-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzenethiol
-
Homo sapiens
3-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenol
-
Homo sapiens
3-(dimethylamino)-N-(((2R,4aS,5R,10bS)-9-isopropyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)propane-1-sulfonamide
-
Homo sapiens
3-amino-N-methyl-N-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)propane-1-sulfonothioamide
-
Homo sapiens
4-((2R,4aS,5R,10bS)-2-((methylamino)methyl)-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenol
-
Homo sapiens
4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)-2-fluorophenol
-
Homo sapiens
4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzene-1,2-diol
-
Homo sapiens
4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenol
-
Homo sapiens
4-((4aS,5S,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)butan-1-ol
-
Homo sapiens
additional information
study of the discovery and optimization of hexahydro-2H-pyranol[3,2-c]quinolines, HHPQs, as inhibitors. Crystallographic data demonstrate that these potent and selectve inhibitors bind in an allosteric pocket of kinesin-5 distant from the nucleotide and microtubule binding sites; the activity assay for inhibition analysis are performed with a coupled ATP regeneration system with a total concentration of the kinesin-5 protein of approximately 50 nM in the reaction
Homo sapiens
N-(((2R,4aS,5R,10bS)-9-bromo-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)-4-(dimethylamino)butanamide
-
Homo sapiens
N-(((2R,4aS,5R,10bS)-9-chloro-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)-2-(dimethylamino)ethanesulfonamide
-
Homo sapiens
N-(2-((((2R,4aS,5R,10bS)-9-bromo-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)amino)ethyl)acetamide
-
Homo sapiens
N-(2-aminoethyl)-4-methyl-N-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)benzamide
-
Homo sapiens
N-(4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenyl)acetamide
-
Homo sapiens
N1-phenyl-N1-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)ethane-1,2-diamine
-
Homo sapiens
Localization
Localization
Commentary
Organism
GeneOntology No.
Textmining
microtubule
paclitaxel-stabilized microtubules are used for activity assays
Homo sapiens
5874
-
Organism
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
Homo sapiens
P52732
-
-
Temperature Optimum [C]
Temperature Optimum [C]
Temperature Optimum Maximum [C]
Commentary
Organism
22
-
assay at room temperature
Homo sapiens
IC50 Value
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.000002
-
pH and temperature not specified in the publication
Homo sapiens
3-(dimethylamino)-N-(((2R,4aS,5R,10bS)-9-isopropyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)propane-1-sulfonamide
0.000002
-
pH and temperature not specified in the publication
Homo sapiens
N-(((2R,4aS,5R,10bS)-9-chloro-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)-2-(dimethylamino)ethanesulfonamide
0.000003
-
pH and temperature not specified in the publication
Homo sapiens
1-((2R,4aS,5R,10bS)-9-bromo-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
0.000004
-
pH and temperature not specified in the publication
Homo sapiens
1-((2R,4aS,5R,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
0.000004
-
pH and temperature not specified in the publication
Homo sapiens
2-(methylamino)-N-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)ethanesulfonothioamide
0.000004
-
pH and temperature not specified in the publication
Homo sapiens
4-((2R,4aS,5R,10bS)-2-((methylamino)methyl)-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenol
0.000005
-
pH and temperature not specified in the publication
Homo sapiens
2-((2R,4aS,5R,10bS)-9-(tert-butyl)-2-((methylamino)methyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzenethiol
0.000005
-
pH and temperature not specified in the publication
Homo sapiens
N-(((2R,4aS,5R,10bS)-9-bromo-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)-4-(dimethylamino)butanamide
0.000006
-
pH and temperature not specified in the publication
Homo sapiens
(2R,4aS,5R,10bS)-2-((1H-1,2,4-triazol-1-yl)methyl)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.000006
-
pH and temperature not specified in the publication
Homo sapiens
N-(2-((((2R,4aS,5R,10bS)-9-bromo-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)amino)ethyl)acetamide
0.000007
-
pH and temperature not specified in the publication
Homo sapiens
2-((((2R,4aS,5R,10bS)-9-chloro-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)amino)ethanol
0.000007
-
pH and temperature not specified in the publication
Homo sapiens
3-amino-N-methyl-N-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)propane-1-sulfonothioamide
0.000008
-
i.e. EMD 534085, pH and temperature not specified in the publication
Homo sapiens
1-(2-(dimethylamino)ethyl)-3-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)urea
0.00001
-
pH and temperature not specified in the publication
Homo sapiens
1-(3-hydroxypropyl)-3-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)urea
0.000011
-
pH and temperature not specified in the publication
Homo sapiens
1-((2R,4aS,5R,10bS)-9-cyclopropyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
0.000014
-
pH and temperature not specified in the publication
Homo sapiens
2-(dimethylamino)ethyl (((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)carbamate
0.000017
-
pH and temperature not specified in the publication
Homo sapiens
4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)-2-fluorophenol
0.000019
-
pH and temperature not specified in the publication
Homo sapiens
2-((((2R,4aS,5R,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)(ethyl)amino)ethanol
0.000019
-
pH and temperature not specified in the publication
Homo sapiens
N1-phenyl-N1-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)ethane-1,2-diamine
0.00002
-
pH and temperature not specified in the publication
Homo sapiens
((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methanamine
0.000025
-
pH and temperature not specified in the publication
Homo sapiens
2-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzenethiol
0.000034
-
pH and temperature not specified in the publication
Homo sapiens
4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenol
0.00004
-
pH and temperature not specified in the publication
Homo sapiens
3-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenol
0.000058
-
pH and temperature not specified in the publication
Homo sapiens
1-((2R,4aS,5R,10bS)-5-(4-fluorophenyl)-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
0.000065
-
pH and temperature not specified in the publication
Homo sapiens
N-(2-aminoethyl)-4-methyl-N-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)benzamide
0.00009
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-7-fluoro-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.000095
-
pH and temperature not specified in the publication
Homo sapiens
4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzene-1,2-diol
0.00011
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00012
-
pH and temperature not specified in the publication
Homo sapiens
3-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzenethiol
0.00012
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00013
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-ethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00013
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-isopropyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00017
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(2-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00027
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(4-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.0003
-
pH and temperature not specified in the publication
Homo sapiens
2-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)-4-chlorobenzenethiol
0.0003
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00035
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(3-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00036
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-5-phenyl-9-propyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00042
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-methyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.0005
-
pH and temperature not specified in the publication
Homo sapiens
2-((4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-9-yl)acetonitrile
0.00053
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(thiazol-2-yl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00054
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-8-chloro-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00072
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-chloro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00087
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,10bS)-9-(tert-butyl)-5-(3-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00091
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(pentafluoro-lambda6-sulfanyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.0011
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(pyridin-3-yl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00125
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-8,9-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.0023
-
pH and temperature not specified in the publication
Homo sapiens
3-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)aniline
0.0037
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-5-phenyl-9-(trifluoromethoxy)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.0053
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-N,N-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-9-amine
0.0068
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(3-chlorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
1-(4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenyl)ethanone
0.01
-
pH and temperature not specified in the publication
Homo sapiens
2-((4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-9-yl)ethanol
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
4-((4aS,5S,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)butan-1-ol
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,10bS)-9-(tert-butyl)-5-(3-chlorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline-9-carbonitrile
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline-9-carboxylic acid
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-7,9-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-8,10-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-8-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(1H-imidazol-2-yl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(3-fluoro-4-methoxyphenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5S,10bS)-9-(tert-butyl)-5-cyclohexyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
N-(4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenyl)acetamide
Crystallization (Commentary) (protein specific)
Crystallization
Organism
study of the discovery and optimization of hexahydr-2H-pyranol[3,2-c]quinolines, HHPQs as inhibitors. Crystallographic data demonstrate that these potent and selectve inhibitors bind in an allosteric pocket of kinesin-5 distant from the nucleotide and microtubule binding sites
Homo sapiens
IC50 Value (protein specific)
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.000002
-
pH and temperature not specified in the publication
Homo sapiens
3-(dimethylamino)-N-(((2R,4aS,5R,10bS)-9-isopropyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)propane-1-sulfonamide
0.000002
-
pH and temperature not specified in the publication
Homo sapiens
N-(((2R,4aS,5R,10bS)-9-chloro-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)-2-(dimethylamino)ethanesulfonamide
0.000003
-
pH and temperature not specified in the publication
Homo sapiens
1-((2R,4aS,5R,10bS)-9-bromo-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
0.000004
-
pH and temperature not specified in the publication
Homo sapiens
1-((2R,4aS,5R,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
0.000004
-
pH and temperature not specified in the publication
Homo sapiens
2-(methylamino)-N-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)ethanesulfonothioamide
0.000004
-
pH and temperature not specified in the publication
Homo sapiens
4-((2R,4aS,5R,10bS)-2-((methylamino)methyl)-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenol
0.000005
-
pH and temperature not specified in the publication
Homo sapiens
2-((2R,4aS,5R,10bS)-9-(tert-butyl)-2-((methylamino)methyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzenethiol
0.000005
-
pH and temperature not specified in the publication
Homo sapiens
N-(((2R,4aS,5R,10bS)-9-bromo-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)-4-(dimethylamino)butanamide
0.000006
-
pH and temperature not specified in the publication
Homo sapiens
(2R,4aS,5R,10bS)-2-((1H-1,2,4-triazol-1-yl)methyl)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.000006
-
pH and temperature not specified in the publication
Homo sapiens
N-(2-((((2R,4aS,5R,10bS)-9-bromo-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)amino)ethyl)acetamide
0.000007
-
pH and temperature not specified in the publication
Homo sapiens
2-((((2R,4aS,5R,10bS)-9-chloro-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)amino)ethanol
0.000007
-
pH and temperature not specified in the publication
Homo sapiens
3-amino-N-methyl-N-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)propane-1-sulfonothioamide
0.000008
-
i.e. EMD 534085, pH and temperature not specified in the publication
Homo sapiens
1-(2-(dimethylamino)ethyl)-3-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)urea
0.00001
-
pH and temperature not specified in the publication
Homo sapiens
1-(3-hydroxypropyl)-3-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)urea
0.000011
-
pH and temperature not specified in the publication
Homo sapiens
1-((2R,4aS,5R,10bS)-9-cyclopropyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
0.000014
-
pH and temperature not specified in the publication
Homo sapiens
2-(dimethylamino)ethyl (((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)carbamate
0.000017
-
pH and temperature not specified in the publication
Homo sapiens
4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)-2-fluorophenol
0.000019
-
pH and temperature not specified in the publication
Homo sapiens
2-((((2R,4aS,5R,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)(ethyl)amino)ethanol
0.000019
-
pH and temperature not specified in the publication
Homo sapiens
N1-phenyl-N1-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)ethane-1,2-diamine
0.00002
-
pH and temperature not specified in the publication
Homo sapiens
((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methanamine
0.000025
-
pH and temperature not specified in the publication
Homo sapiens
2-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzenethiol
0.000034
-
pH and temperature not specified in the publication
Homo sapiens
4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenol
0.00004
-
pH and temperature not specified in the publication
Homo sapiens
3-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenol
0.000058
-
pH and temperature not specified in the publication
Homo sapiens
1-((2R,4aS,5R,10bS)-5-(4-fluorophenyl)-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
0.000065
-
pH and temperature not specified in the publication
Homo sapiens
N-(2-aminoethyl)-4-methyl-N-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)benzamide
0.00009
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-7-fluoro-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.000095
-
pH and temperature not specified in the publication
Homo sapiens
4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzene-1,2-diol
0.00011
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00012
-
pH and temperature not specified in the publication
Homo sapiens
3-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzenethiol
0.00012
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00013
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-ethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00013
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-isopropyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00017
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(2-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00027
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(4-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.0003
-
pH and temperature not specified in the publication
Homo sapiens
2-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)-4-chlorobenzenethiol
0.0003
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00035
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(3-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00036
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-5-phenyl-9-propyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00042
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-methyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.0005
-
pH and temperature not specified in the publication
Homo sapiens
2-((4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-9-yl)acetonitrile
0.00053
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(thiazol-2-yl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00054
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-8-chloro-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00072
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-chloro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00087
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,10bS)-9-(tert-butyl)-5-(3-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00091
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(pentafluoro-lambda6-sulfanyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.0011
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(pyridin-3-yl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.00125
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-8,9-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.0023
-
pH and temperature not specified in the publication
Homo sapiens
3-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)aniline
0.0037
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-5-phenyl-9-(trifluoromethoxy)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.0053
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-N,N-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-9-amine
0.0068
-
pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(3-chlorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
1-(4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenyl)ethanone
0.01
-
pH and temperature not specified in the publication
Homo sapiens
2-((4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-9-yl)ethanol
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
4-((4aS,5S,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)butan-1-ol
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,10bS)-9-(tert-butyl)-5-(3-chlorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline-9-carbonitrile
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline-9-carboxylic acid
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-7,9-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-8,10-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-8-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(1H-imidazol-2-yl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(3-fluoro-4-methoxyphenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
(4aS,5S,10bS)-9-(tert-butyl)-5-cyclohexyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
0.01
-
above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
N-(4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenyl)acetamide
Inhibitors (protein specific)
Inhibitors
Commentary
Organism
Structure
((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methanamine
-
Homo sapiens
(2R,4aS,5R,10bS)-2-((1H-1,2,4-triazol-1-yl)methyl)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,10bS)-9-(tert-butyl)-5-(3-chlorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,10bS)-9-(tert-butyl)-5-(3-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline-9-carbonitrile
-
Homo sapiens
(4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline-9-carboxylic acid
-
Homo sapiens
(4aS,5R,10bS)-5-phenyl-9-(trifluoromethoxy)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-5-phenyl-9-propyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-7,9-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-7-fluoro-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-8,10-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-8,9-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-8-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-8-chloro-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(pentafluoro-lambda6-sulfanyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(1H-imidazol-2-yl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(2-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(3-chlorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(3-fluoro-4-methoxyphenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(3-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(4-fluorophenyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(pyridin-3-yl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-(thiazol-2-yl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-chloro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-ethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-isopropyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-9-methyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
(4aS,5R,10bS)-N,N-dimethyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-9-amine
-
Homo sapiens
(4aS,5S,10bS)-9-(tert-butyl)-5-cyclohexyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinoline
-
Homo sapiens
1-((2R,4aS,5R,10bS)-5-(4-fluorophenyl)-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
-
Homo sapiens
1-((2R,4aS,5R,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
-
Homo sapiens
1-((2R,4aS,5R,10bS)-9-bromo-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
-
Homo sapiens
1-((2R,4aS,5R,10bS)-9-cyclopropyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)-N-methylmethanamine
-
Homo sapiens
1-(2-(dimethylamino)ethyl)-3-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)urea
-
Homo sapiens
1-(3-hydroxypropyl)-3-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)urea
-
Homo sapiens
1-(4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenyl)ethanone
-
Homo sapiens
2-((((2R,4aS,5R,10bS)-9-(tert-butyl)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)(ethyl)amino)ethanol
-
Homo sapiens
2-((((2R,4aS,5R,10bS)-9-chloro-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)amino)ethanol
-
Homo sapiens
2-((2R,4aS,5R,10bS)-9-(tert-butyl)-2-((methylamino)methyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzenethiol
-
Homo sapiens
2-((4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-9-yl)acetonitrile
-
Homo sapiens
2-((4aS,5R,10bS)-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-9-yl)ethanol
-
Homo sapiens
2-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)-4-chlorobenzenethiol
-
Homo sapiens
2-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzenethiol
-
Homo sapiens
2-(dimethylamino)ethyl (((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)carbamate
-
Homo sapiens
2-(methylamino)-N-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)ethanesulfonothioamide
-
Homo sapiens
3-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)aniline
-
Homo sapiens
3-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzenethiol
-
Homo sapiens
3-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenol
-
Homo sapiens
3-(dimethylamino)-N-(((2R,4aS,5R,10bS)-9-isopropyl-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)propane-1-sulfonamide
-
Homo sapiens
3-amino-N-methyl-N-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)propane-1-sulfonothioamide
-
Homo sapiens
4-((2R,4aS,5R,10bS)-2-((methylamino)methyl)-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenol
-
Homo sapiens
4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)-2-fluorophenol
-
Homo sapiens
4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)benzene-1,2-diol
-
Homo sapiens
4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenol
-
Homo sapiens
4-((4aS,5S,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)butan-1-ol
-
Homo sapiens
additional information
study of the discovery and optimization of hexahydro-2H-pyranol[3,2-c]quinolines, HHPQs, as inhibitors. Crystallographic data demonstrate that these potent and selectve inhibitors bind in an allosteric pocket of kinesin-5 distant from the nucleotide and microtubule binding sites; the activity assay for inhibition analysis are performed with a coupled ATP regeneration system with a total concentration of the kinesin-5 protein of approximately 50 nM in the reaction
Homo sapiens
N-(((2R,4aS,5R,10bS)-9-bromo-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)-4-(dimethylamino)butanamide
-
Homo sapiens
N-(((2R,4aS,5R,10bS)-9-chloro-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)-2-(dimethylamino)ethanesulfonamide
-
Homo sapiens
N-(2-((((2R,4aS,5R,10bS)-9-bromo-7-fluoro-5-phenyl-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)amino)ethyl)acetamide
-
Homo sapiens
N-(2-aminoethyl)-4-methyl-N-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)benzamide
-
Homo sapiens
N-(4-((4aS,5R,10bS)-9-(tert-butyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-5-yl)phenyl)acetamide
-
Homo sapiens
N1-phenyl-N1-(((2R,4aS,5R,10bS)-5-phenyl-9-(trifluoromethyl)-3,4,4a,5,6,10b-hexahydro-2H-pyrano[3,2-c]quinolin-2-yl)methyl)ethane-1,2-diamine
-
Homo sapiens
Localization (protein specific)
Localization
Commentary
Organism
GeneOntology No.
Textmining
microtubule
paclitaxel-stabilized microtubules are used for activity assays
Homo sapiens
5874
-
Temperature Optimum [C] (protein specific)
Temperature Optimum [C]
Temperature Optimum Maximum [C]
Commentary
Organism
22
-
assay at room temperature
Homo sapiens
Other publictions for EC 3.6.4.4
No.
1st author
Pub Med
title
organims
journal
volume
pages
year
Activating Compound
Application
Cloned(Commentary)
Crystallization (Commentary)
Engineering
General Stability
Inhibitors
KM Value [mM]
Localization
Metals/Ions
Molecular Weight [Da]
Natural Substrates/ Products (Substrates)
Organic Solvent Stability
Organism
Oxidation Stability
Posttranslational Modification
Purification (Commentary)
Reaction
Renatured (Commentary)
Source Tissue
Specific Activity [micromol/min/mg]
Storage Stability
Substrates and Products (Substrate)
Subunits
Temperature Optimum [C]
Temperature Range [C]
Temperature Stability [C]
Turnover Number [1/s]
pH Optimum
pH Range
pH Stability
Cofactor
Ki Value [mM]
pI Value
IC50 Value
Activating Compound (protein specific)
Application (protein specific)
Cloned(Commentary) (protein specific)
Cofactor (protein specific)
Crystallization (Commentary) (protein specific)
Engineering (protein specific)
General Stability (protein specific)
IC50 Value (protein specific)
Inhibitors (protein specific)
Ki Value [mM] (protein specific)
KM Value [mM] (protein specific)
Localization (protein specific)
Metals/Ions (protein specific)
Molecular Weight [Da] (protein specific)
Natural Substrates/ Products (Substrates) (protein specific)
Organic Solvent Stability (protein specific)
Oxidation Stability (protein specific)
Posttranslational Modification (protein specific)
Purification (Commentary) (protein specific)
Renatured (Commentary) (protein specific)
Source Tissue (protein specific)
Specific Activity [micromol/min/mg] (protein specific)
Storage Stability (protein specific)
Substrates and Products (Substrate) (protein specific)
Subunits (protein specific)
Temperature Optimum [C] (protein specific)
Temperature Range [C] (protein specific)
Temperature Stability [C] (protein specific)
Turnover Number [1/s] (protein specific)
pH Optimum (protein specific)
pH Range (protein specific)
pH Stability (protein specific)
pI Value (protein specific)
Expression
General Information
General Information (protein specific)
Expression (protein specific)
KCat/KM [mM/s]
KCat/KM [mM/s] (protein specific)
732986
Yokoyama
Structural basis of new allost ...
Homo sapiens
ACS Chem. Biol.
10
1128-1136
2015
-
1
1
1
-
-
2
-
-
1
-
1
-
1
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
1
-
1
-
-
-
2
-
-
-
1
-
1
-
-
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
4
4
-
-
-
732988
Braun
Synthesis and biological evalu ...
Homo sapiens
ACS Chem. Biol.
10
554-560
2015
-
-
-
-
-
-
22
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2
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-
686499
Roehlk
Properties of the Kinesin-1 mo ...
Dictyostelium discoideum
Eur. J. Cell Biol.
87
237-249
2008
2
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1
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1
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6
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7
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6
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1
2
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3
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687306
Luo
Conformation-dependent ligand ...
Homo sapiens
J. Am. Chem. Soc.
130
7584-7591
2008
1
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1
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2
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2
4
2
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2
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4
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1
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2
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4
2
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1
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1
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1
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2
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4
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696293
Thoresen
Processive movement by a kines ...
Drosophila melanogaster
Biochemistry
47
9514-9521
2008
-
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1
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1
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1
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2
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1
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1
1
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1
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1
1
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-
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697183
Taba
Direction and speed of microtu ...
Rattus norvegicus
Cell Motil. Cytoskeleton
65
816-826
2008
-
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1
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2
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1
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1
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-
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-
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697234
Yildiz
Intramolecular strain coordina ...
Homo sapiens
Cell
134
1030-1041
2008
-
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1
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-
-
-
-
-
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1
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1
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1
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1
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1
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-
-
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697482
van den Wildenberg
The homotetrameric kinesin-5 K ...
Drosophila melanogaster
Curr. Biol.
18
1860-1864
2008
-
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1
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-
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1
2
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2
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1
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1
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1
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1
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2
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1
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1
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3
1
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-
-
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-
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-
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-
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-
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697787
Mans
Mobility of the von Hippel-Lin ...
Mus musculus
Exp. Cell Res.
314
1229-1236
2008
-
-
-
-
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1
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1
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2
-
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2
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-
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-
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699094
Kapitein
Microtubule cross-linking trig ...
Xenopus laevis
J. Cell Biol.
182
421-428
2008
-
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1
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-
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1
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1
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1
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1
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1
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1
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-
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2
1
-
-
-
-
-
-
-
-
-
-
-
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-
699906
Martinez
Kinesin KIF4 regulates intrace ...
Homo sapiens
J. Virol.
82
9937-9950
2008
1
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1
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1
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1
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1
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2
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2
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1
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1
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1
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1
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1
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2
-
-
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-
-
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-
-
-
-
-
-
-
-
700986
Dietrich
The kinesin-1 motor protein is ...
Homo sapiens
Proc. Natl. Acad. Sci. USA
105
8938-8943
2008
1
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-
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1
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1
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-
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-
-
-
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685523
Klein
New chemical tools for investi ...
Homo sapiens
Bioorg. Med. Chem.
15
6474-6488
2007
1
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-
-
-
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6
-
-
-
-
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2
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-
-
-
-
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1
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-
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12
1
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-
-
-
-
-
12
6
-
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-
-
-
-
-
1
-
-
-
-
-
-
-
-
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-
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-
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-
687450
Yamada
Photocontrol of kinesin ATPase ...
Mus musculus
J. Biochem.
142
691-698
2007
1
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1
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2
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-
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1
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1
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5
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1
-
1
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2
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-
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-
-
-
-
1
-
-
-
-
5
-
-
-
-
-
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-
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688256
Parrish
Novel ATP-competitive kinesin ...
Homo sapiens
J. Med. Chem.
50
4939-4952
2007
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1
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18
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1
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8
-
16
-
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1
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16
18
8
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-
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-
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-
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-
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689127
Luo
ATP-competitive inhibitors of ...
Homo sapiens
Nat. Chem. Biol.
3
722-726
2007
-
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1
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5
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3
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-
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1
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3
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6
-
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1
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5
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6
3
3
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-
-
-
-
-
-
-
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-
-
-
-
-
-
-
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690055
Alonso
An ATP gate controls tubulin b ...
Neurospora crassa, Rattus norvegicus
Science
316
120-123
2007
4
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-
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-
-
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2
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2
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4
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-
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2
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
667706
Cochran
Pathway of ATP hydrolysis by m ...
Homo sapiens
Biochemistry
45
12334-12344
2006
-
-
1
-
-
-
-
1
1
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1
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2
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1
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2
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1
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1
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1
1
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1
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-
-
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2
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
668189
Moores
The role of the kinesin-13 nec ...
Cricetulus griseus
Cell Cycle
5
1812-1815
2006
-
-
-
-
-
-
-
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1
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1
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-
-
1
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-
-
-
-
-
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-
-
-
-
-
-
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668211
Dastidar
Eh Klp5 is a divergent member ...
Entamoeba histolytica
Cell. Microbiol.
9
316-328
2006
-
-
-
-
-
-
1
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1
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1
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4
-
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2
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1
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1
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1
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-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
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-
668409
Krzysiak
A structural model for monastr ...
Homo sapiens
EMBO J.
25
2263-2273
2006
-
-
-
-
-
-
1
1
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-
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1
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2
-
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-
-
-
-
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2
1
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-
1
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1
-
1
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-
1
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-
-
-
2
1
-
-
-
1
-
-
-
-
-
-
-
-
-
-
668512
Jimeno
Kinesin-2 and photoreceptor ce ...
Mus musculus
Exp. Eye Res.
82
351-353
2006
-
-
-
-
-
-
-
-
-
-
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1
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3
-
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-
-
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1
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-
1
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1
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1
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-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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669012
Jimeno
Analysis of kinesin-2 function ...
Gallus gallus
Invest. Ophthalmol. Vis. Sci.
47
5039-5046
2006
-
-
-
-
-
-
-
-
-
-
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1
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3
-
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1
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3
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2
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1
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1
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3
-
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2
-
-
-
-
-
-
-
-
-
-
-
-
-
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669173
Adio
Kinetic and mechanistic basis ...
Neurospora crassa
J. Biol. Chem.
248
37782-37793
2006
-
-
-
-
-
-
-
-
1
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-
1
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2
-
-
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-
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1
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2
1
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1
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1
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1
-
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2
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
669467
Skoufias
S-trityl-L-cysteine is a rever ...
Homo sapiens
J. Biol. Chem.
281
17559-17569
2006
-
-
-
-
-
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1
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1
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2
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-
-
-
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1
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1
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-
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-
1
1
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1
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-
-
-
1
-
-
-
-
-
-
-
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669917
Kinoshita
Global and local control of mi ...
Xenopus sp.
J. Muscle Res. Cell Motil.
27
107-114
2006
-
-
-
-
-
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-
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1
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2
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-
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1
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1
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1
-
-
-
-
-
-
-
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669918
Marx
Interaction of kinesin motors, ...
Rattus norvegicus
J. Muscle Res. Cell Motil.
27
125-137
2006
-
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-
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1
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1
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-
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1
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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670212
Kopp
The kinesin KIF1C and microtub ...
Homo sapiens
Mol. Biol. Cell
17
2811-2823
2006
-
-
-
-
-
-
-
-
1
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-
1
-
2
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-
-
-
-
1
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2
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1
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1
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1
-
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2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
670213
Straube
Conventional kinesin mediates ...
Ustilago maydis
Mol. Biol. Cell
17
907-916
2006
-
-
-
-
-
-
-
-
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1
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2
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2
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-
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1
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2
-
-
-
-
-
-
-
-
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-
670351
Valentine
Individual dimers of the mitot ...
Homo sapiens
Nat. Cell Biol.
8
470-476
2006
-
-
1
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2
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1
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1
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1
-
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670352
Gupta
Plus end-specific depolymerase ...
Saccharomyces cerevisiae
Nat. Cell Biol.
8
913-923
2006
2
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4
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1
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1
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2
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4
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1
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1
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-
-
-
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670353
Varga
Yeast kinesin-8 depolymerizes ...
Saccharomyces cerevisiae
Nat. Cell Biol.
8
957-962
2006
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2
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1
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1
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2
-
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-
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-
-
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-
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-
-
670354
Kwok
Allosteric inhibition of kines ...
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The depolymerizing kinesin MCA ...
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Nature
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Phenothiazine and carbazole-re ...
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Mechanism of tail-mediated inh ...
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Hoepfner
Modulation of receptor recycli ...
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The DASH complex and Klp5/Klp6 ...
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Alternating site ATPase pathwa ...
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Mueller
The FLA3 KAP subunit is requir ...
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Myosin-V, kinesin-1, and kines ...
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Kapitein
The bipolar mitotic kinesin Eg ...
Xenopus sp.
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Kinesin-2 is a motor for late ...
Homo sapiens
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2005
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Mechanistic analysis of the mi ...
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Transport of African swine fev ...
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Kikkawa
Switch-based mechanism of kine ...
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Awan
Cloning and characterization o ...
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Zhang
Comparative analysis of two C- ...
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Zhang
Rat kinesin light chain 3 asso ...
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Kinesin I and cytoplasmic dyne ...
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2003
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Zhang
Accumulation of cytoplasmic dy ...
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Okada
Processivity of the single-hea ...
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The role of ATP hydrolysis for ...
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The calmodulin-binding domain ...
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Kinesin I-dependent cortical e ...
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Role of the kinesin neck linke ...
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210556
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Controlling kinesin by reversi ...
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Lane
Microtubule-based endoplasmic ...
Doryteuthis pealeii, Tetrahymena sp., Xenopus laevis
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Kirchner
Universal and unique features ...
Bos taurus, Caenorhabditis elegans, Doryteuthis pealeii, Drosophila melanogaster, Drosophila sp. (in: Insecta), Homo sapiens, Mus musculus, Nectria haematococca, Neurospora crassa, Rattus norvegicus, Strongylocentrotus purpuratus, Ustilago maydis
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Reconstitution of membrane tra ...
Caenorhabditis elegans, Dictyostelium discoideum, Mus musculus, Thermomyces lanuginosus
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Rice
A structural change in the kin ...
Homo sapiens, Rattus norvegicus
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Santama
KIF2beta, a new kinesin superf ...
Cricetulus griseus, Homo sapiens, Mus musculus, Trypanosoma cruzi, Xenopus laevis
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1998
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210549
Nakagawa
Identification and classificat ...
Caenorhabditis elegans, Mus musculus, Saccharomyces cerevisiae, Xenopus laevis
Proc. Natl. Acad. Sci. USA
94
9654-9659
1997
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1
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8
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5
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4
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9
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8
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8
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9
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8
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210568
Blocker
Molecular requirements for bi- ...
Mus musculus
J. Cell Biol.
137
113-129
1997
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2
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1
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2
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210548
Song
Binding sites on microtubules ...
Drosophila sp. (in: Insecta), Xenopus laevis
Biochemistry
35
11203-11209
1996
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1
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1
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2
4
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2
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2
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1
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4
1
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210567
Crevel
Weak and strong states of kine ...
Drosophila sp. (in: Insecta)
J. Mol. Biol.
257
66-76
1996
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210544
Lippincott-Schwartz
Kinesin is the motor for micro ...
Homo sapiens
J. Cell Biol.
128
293-306
1995
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2
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2
2
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3
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1
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1
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1
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2
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1
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2
1
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210545
Endow
Determinants of motor polarity ...
Arabidopsis sp., Aspergillus sp., Drosophila sp. (in: Insecta), Homo sapiens, Schizosaccharomyces pombe
Biophys. J.
68
271S-274S
1995
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10
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5
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5
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10
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210546
Kuriyama
Characterization of a minus en ...
Arabidopsis sp., Aspergillus sp., Drosophila sp. (in: Insecta), Homo sapiens, Strongylocentrotus purpuratus
J. Cell Biol.
129
1049-1059
1995
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1
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2
10
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6
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10
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10
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1
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1
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10
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210547
Yamazaki
KIF3A/B: a heterodimeric kines ...
Bos taurus, Chlamydomonas sp., Mus musculus
J. Cell Biol.
130
1387-1399
1995
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1
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6
6
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3
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1
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1
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6
6
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5
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6
1
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210562
Walker
Ncd and kinesin motor domains ...
Drosophila sp. (in: Insecta)
Proc. Natl. Acad. Sci. USA
92
5960-5964
1995
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2
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210543
Schnapp
Kinesin is bound with high aff ...
Doryteuthis pealeii, Drosophila sp. (in: Insecta)
J. Cell Biol.
119
389-399
1992
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5
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210542
Schnapp
Delayed start-up of kinesin-dr ...
Doryteuthis pealeii
Proc. Natl. Acad. Sci. USA
87
10053-10057
1990
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1
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210541
Mitchison
The role of microtubule polari ...
Doryteuthis pealeii, Homo sapiens, Strongylocentrotus purpuratus
J. Cell Sci. Suppl.
5
121-128
1986
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2
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2
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6
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3
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3
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6
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1
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6
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210540
Vale
Identification of a novel forc ...
Bos taurus, Doryteuthis pealeii
Cell
42
39-50
1985
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4
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1
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4
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4
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2
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2
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1
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4
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4
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1
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