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Literature summary for 2.5.1.29 extracted from

  • Lacbay, C.M.; Waller, D.D.; Park, J.; Gomez Palou, M.; Vincent, F.; Huang, X.F.; Ta, V.; Berghuis, A.M.; Sebag, M.; Tsantrizos, Y.S.
    Unraveling the prenylation-cancer paradox in multiple myeloma with novel geranylgeranyl pyrophosphate synthase (GGPPS) inhibitors (2018), J. Med. Chem., 61, 6904-6917 .
    View publication on PubMed
Search for more literature for 2.5.1.29

Application

Application Comment Organism
pharmacology the enzyme is a valuable therapeutic target in oncology and more specifically for the treatment of multiple myeloma Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(((2-(3-((3-fluoro-4-methoxyphenyl)carbamoyl)phenyl)-thieno[2,3-d]pyrimidin-4-yl)amino)methylene)bis-(phosphonic acid)
-
 Homo sapiens
(((2-(3-((4-methoxyphenyl)carbamoyl)phenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)methylene)bis(phosphonic acid)
-
 Homo sapiens
(((2-(3-(4-fluorobenzamido)phenyl)thieno[2,3-d]pyrimidin-4-yl)amino)methylene)bis(phosphonic acid)
-
 Homo sapiens
(((2-(3-(4-methoxybenzamido)phenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)methylene)bis(phosphonic acid)
-
 Homo sapiens
(((2-(3-(4-methylbenzamido)phenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)methylene)bis(phosphonic acid)
-
 Homo sapiens
(((2-(3-(phenylcarbamoyl)phenyl)thieno[2,3-d]pyrimidin-4-yl)amino)methylene)bis(phosphonic acid)
-
 Homo sapiens
(((2-(3-benzamidophenyl)thieno[2,3-d]pyrimidin-4-yl)-amino)methylene)bis(phosphonic acid)
-
 Homo sapiens
[(6E,11E)-2,6,12,16-tetramethylheptadeca-2,6,11,15-tetraene-9,9-diyl]bis(phosphonic acid)
-
 Homo sapiens
[([6-[4-(trifluoromethyl)phenyl]thieno[2,3-d]pyrimidin-4-yl]amino)methylene]bis(phosphonic acid)
-
 Homo sapiens
[[(2-phenylthieno[2,3-d]pyrimidin-4-yl)amino]methylene]bis(phosphonic acid)
-
 Homo sapiens
[[(5,6-dihydrothieno[2,3-d]pyrimidin-4-yl)amino]methylene]bis(phosphonic acid)
-
 Homo sapiens
[[(6-phenylthieno[2,3-d]pyrimidin-4-yl)amino]methylene]bis(phosphonic acid)
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens O95749
-
-

Subunits

Subunits Comment Organism
dimer
-
 Homo sapiens

Synonyms

Synonyms Comment Organism
GGPPS
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.042
-
 pH and temperature not specified in the publication, wild-type enzyme Homo sapiens (((2-(3-(4-fluorobenzamido)phenyl)thieno[2,3-d]pyrimidin-4-yl)amino)methylene)bis(phosphonic acid)
0.049
-
 pH and temperature not specified in the publication, mutant enzyme Y246D Homo sapiens (((2-(3-(phenylcarbamoyl)phenyl)thieno[2,3-d]pyrimidin-4-yl)amino)methylene)bis(phosphonic acid)
0.049
-
 pH and temperature not specified in the publication, wild-type enzyme Homo sapiens (((2-(3-(phenylcarbamoyl)phenyl)thieno[2,3-d]pyrimidin-4-yl)amino)methylene)bis(phosphonic acid)
0.064
-
 pH and temperature not specified in the publication, mutant enzyme Y246D Homo sapiens (((2-(3-benzamidophenyl)thieno[2,3-d]pyrimidin-4-yl)-amino)methylene)bis(phosphonic acid)
0.064
-
 pH and temperature not specified in the publication, wild-type enzyme Homo sapiens (((2-(3-benzamidophenyl)thieno[2,3-d]pyrimidin-4-yl)-amino)methylene)bis(phosphonic acid)
0.082
-
 pH and temperature not specified in the publication, wild-type enzyme Homo sapiens [[(2-phenylthieno[2,3-d]pyrimidin-4-yl)amino]methylene]bis(phosphonic acid)
0.085
-
 pH and temperature not specified in the publication, mutant enzyme Y246D Homo sapiens (((2-(3-(4-methoxybenzamido)phenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)methylene)bis(phosphonic acid)
0.085
-
 pH and temperature not specified in the publication, wild-type enzyme Homo sapiens (((2-(3-(4-methoxybenzamido)phenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)methylene)bis(phosphonic acid)
0.086
-
 pH and temperature not specified in the publication, wild-type enzyme Homo sapiens (((2-(3-((3-fluoro-4-methoxyphenyl)carbamoyl)phenyl)-thieno[2,3-d]pyrimidin-4-yl)amino)methylene)bis-(phosphonic acid)
0.094
-
 pH and temperature not specified in the publication, wild-type enzyme Homo sapiens [[(6-phenylthieno[2,3-d]pyrimidin-4-yl)amino]methylene]bis(phosphonic acid)
0.1
-
 pH and temperature not specified in the publication, mutant enzyme Y246D Homo sapiens (((2-(3-(4-methylbenzamido)phenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)methylene)bis(phosphonic acid)
0.1
-
 pH and temperature not specified in the publication, wild-type enzyme Homo sapiens (((2-(3-(4-methylbenzamido)phenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)methylene)bis(phosphonic acid)
0.43
-
 pH and temperature not specified in the publication, mutant enzyme Y246D Homo sapiens [(6E,11E)-2,6,12,16-tetramethylheptadeca-2,6,11,15-tetraene-9,9-diyl]bis(phosphonic acid)
0.43
-
 pH and temperature not specified in the publication, wild-type enzyme Homo sapiens [(6E,11E)-2,6,12,16-tetramethylheptadeca-2,6,11,15-tetraene-9,9-diyl]bis(phosphonic acid)
1.5
-
 pH and temperature not specified in the publication, wild-type enzyme Homo sapiens [([6-[4-(trifluoromethyl)phenyl]thieno[2,3-d]pyrimidin-4-yl]amino)methylene]bis(phosphonic acid)
75
-
 pH and temperature not specified in the publication, mutant enzyme Y246D Homo sapiens (((2-(3-((4-methoxyphenyl)carbamoyl)phenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)methylene)bis(phosphonic acid)
75
-
 pH and temperature not specified in the publication, wild-type enzyme Homo sapiens (((2-(3-((4-methoxyphenyl)carbamoyl)phenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)methylene)bis(phosphonic acid)