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Literature summary for 5.6.1.3 extracted from

  • Barsanti, P.A.; Wang, W.; Ni, Z.J.; Duhl, D.; Brammeier, N.; Martin, E.; Bussiere, D.; Walter, A.O.
    The discovery of tetrahydro-beta-carbolines as inhibitors of the kinesin Eg5 (2010), Bioorg. Med. Chem. Lett., 20, 157-160.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(1-(3-hydroxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)(1-methylpiperidin-3-yl)methanone
-
Homo sapiens
(2R)-2-amino-1-(6-chloro-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)-3-methylbutan-1-one
-
Homo sapiens
(2S)-2-amino-1-(6-chloro-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)-3-methylbutan-1-one
-
Homo sapiens
1-(1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)ethanone i.e. tetrahydro-beta-carboline Homo sapiens
1-(1-(3-hydroxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)-3-(piperidin-1-yl)propan-1-one
-
Homo sapiens
1-(1-(3-hydroxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)ethanone
-
Homo sapiens
1-(1-(3-hydroxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
1-(6-chloro-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)-2-(piperidin-4-yl)ethanone
-
Homo sapiens
2-amino-1-(1-(3-hydroxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)ethanone
-
Homo sapiens
3-(2-((2-aminoethyl)sulfonyl)-6-chloro-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenol
-
Homo sapiens
3-amino-1-(1-(2-aminopyridin-4-yl)-6-chloro-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
3-amino-1-(1-(3-fluorophenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
3-amino-1-(1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
3-amino-1-(1-(3-hydroxyphenyl)-6-(trifluoromethoxy)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
3-amino-1-(1-(3-hydroxyphenyl)-6-isopropyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
3-amino-1-(1-(3-hydroxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
3-amino-1-(1-(3-hydroxyphenyl)-6-phenyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
3-amino-1-(1-(3-methoxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
3-amino-1-(6-bromo-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
3-amino-1-(6-chloro-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
3-amino-1-(6-chloro-1-cyclohexyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
3-amino-1-(6-ethyl-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
3-amino-1-(6-fluoro-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
3-amino-1-(6-hydroxy-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
3-amino-1-(6-methyl-1-phenyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
-
Homo sapiens
4-amino-1-(1-(3-hydroxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)butan-1-one
-
Homo sapiens
5-(2-(3-aminopropanoyl)-6-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)benzo[d]oxazol-2(3H)-one
-
Homo sapiens
N-(3-(2-(3-aminopropanoyl)-6-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)methanesulfonamide
-
Homo sapiens
N-(3-(6-chloro-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)-3-oxopropyl)methanesulfonamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P52732
-
-

Synonyms

Synonyms Comment Organism
kinesin Eg5
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000011
-
pH and temperature not specified in the publication Homo sapiens 3-amino-1-(6-ethyl-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.00002
-
pH and temperature not specified in the publication Homo sapiens 3-amino-1-(1-(3-hydroxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.000027
-
pH and temperature not specified in the publication Homo sapiens 3-amino-1-(6-bromo-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.000039
-
pH and temperature not specified in the publication Homo sapiens 3-amino-1-(6-chloro-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.000049
-
pH and temperature not specified in the publication Homo sapiens 2-amino-1-(1-(3-hydroxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)ethanone
0.000058
-
pH and temperature not specified in the publication Homo sapiens 3-amino-1-(1-(3-hydroxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.000086
-
pH and temperature not specified in the publication Homo sapiens 4-amino-1-(1-(3-hydroxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)butan-1-one
0.0001
-
pH and temperature not specified in the publication Homo sapiens 3-amino-1-(1-(3-fluorophenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.0001
-
pH and temperature not specified in the publication Homo sapiens 1-(1-(3-hydroxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)-3-(piperidin-1-yl)propan-1-one
0.000155
-
pH and temperature not specified in the publication Homo sapiens N-(3-(6-chloro-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)-3-oxopropyl)methanesulfonamide
0.000175
-
pH and temperature not specified in the publication Homo sapiens 3-amino-1-(6-methyl-1-phenyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.000186
-
pH and temperature not specified in the publication Homo sapiens 3-(2-((2-aminoethyl)sulfonyl)-6-chloro-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenol
0.0002
-
pH and temperature not specified in the publication Homo sapiens 1-(1-(3-hydroxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)ethanone
0.0002
-
pH and temperature not specified in the publication Homo sapiens 3-amino-1-(1-(3-hydroxyphenyl)-6-(trifluoromethoxy)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.00023
-
pH and temperature not specified in the publication Homo sapiens 3-amino-1-(6-chloro-1-cyclohexyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.00046
-
pH and temperature not specified in the publication Homo sapiens 1-(1-(3-hydroxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.00063
-
pH and temperature not specified in the publication Homo sapiens 3-amino-1-(1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.00076
-
pH and temperature not specified in the publication Homo sapiens 3-amino-1-(6-fluoro-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.00076
-
pH and temperature not specified in the publication Homo sapiens (2S)-2-amino-1-(6-chloro-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)-3-methylbutan-1-one
0.00086
-
pH and temperature not specified in the publication Homo sapiens 1-(6-chloro-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)-2-(piperidin-4-yl)ethanone
0.0009
-
pH and temperature not specified in the publication Homo sapiens (1-(3-hydroxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)(1-methylpiperidin-3-yl)methanone
0.0017
-
pH and temperature not specified in the publication Homo sapiens 3-amino-1-(1-(3-hydroxyphenyl)-6-phenyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.0025
-
i.e. tetrahydro-beta-carboline, pH and temperature not specified in the publication Homo sapiens 1-(1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)ethanone
0.0045
-
pH and temperature not specified in the publication Homo sapiens 3-amino-1-(6-hydroxy-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.0066
-
pH and temperature not specified in the publication Homo sapiens 3-amino-1-(1-(2-aminopyridin-4-yl)-6-chloro-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.0081
-
pH and temperature not specified in the publication Homo sapiens (2R)-2-amino-1-(6-chloro-1-(3-hydroxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)-3-methylbutan-1-one
0.011
-
pH and temperature not specified in the publication Homo sapiens 3-amino-1-(1-(3-methoxyphenyl)-6-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.025
-
above 0.025 mM, pH and temperature not specified in the publication Homo sapiens 3-amino-1-(1-(3-hydroxyphenyl)-6-isopropyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)propan-1-one
0.025
-
above 0.025 mM, pH and temperature not specified in the publication Homo sapiens 5-(2-(3-aminopropanoyl)-6-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)benzo[d]oxazol-2(3H)-one
0.025
-
above 0.025 mM, pH and temperature not specified in the publication Homo sapiens N-(3-(2-(3-aminopropanoyl)-6-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)methanesulfonamide

General Information

General Information Comment Organism
physiological function kinesin Eg5 is a member of the kinesin family of proteins, which hydrolyze ATP as they migrate along microtubules Homo sapiens