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Literature summary extracted from

  • Marzinzik, A.L.; Amstutz, R.; Bold, G.; Bourgier, E.; Cotesta, S.; Glickman, J.F.; Goette, M.; Henry, C.; Lehmann, S.; Hartwieg, J.C.; Ofner, S.; Pelle, X.; Roddy, T.P.; Rondeau, J.M.; Stauffer, F.; Stout, S.J.; Widmer, A.; Zimmermann, J.; Zoller, T.; Jahnke, W.
    Discovery of novel allosteric non-bisphosphonate inhibitors of farnesyl pyrophosphate synthase by integrated lead finding (2015), ChemMedChem, 10, 1884-1891.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.10 1-[(3-carboxy-1,2-oxazol-5-yl)methyl]-1H-benzo[g]indole-2-carboxylic acid
-
 Homo sapiens
2.5.1.10 1-[(benzyloxy)carbonyl]-2,3-dihydro-1H-indole-2-carboxylic acid
-
 Homo sapiens
2.5.1.10 1H,1'H-4,4'-biindole-2-carboxylic acid
-
 Homo sapiens
2.5.1.10 2-(naphthalen-1-ylmethoxy)-4-(phenylamino)benzoic acid
-
 Homo sapiens
2.5.1.10 2-(naphthalen-1-ylmethoxy)benzoic acid
-
 Homo sapiens
2.5.1.10 3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
-
 Homo sapiens
2.5.1.10 4'-(hydroxymethyl)-3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
-
 Homo sapiens
2.5.1.10 4'-(methylcarbamoyl)-3-[(naphthalen-1-yl)methoxy][1,1'-biphenyl]-4-carboxylic acid
-
 Homo sapiens
2.5.1.10 4'-acetamido-3-[(naphthalen-1-yl)methoxy][1,1'-biphenyl]-4-carboxylic acid
-
 Homo sapiens
2.5.1.10 4'-carbamoyl-3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
-
 Homo sapiens
2.5.1.10 4'-fluoro-3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
-
 Homo sapiens
2.5.1.10 4'-[(methanesulfonyl)amino]-3-[(naphthalen-1-yl)methoxy][1,1'-biphenyl]-4-carboxylic acid
-
 Homo sapiens
2.5.1.10 4-(1,3-benzodioxol-5-yl)-2-(naphthalen-1-ylmethoxy)benzoic acid
-
 Homo sapiens
2.5.1.10 4-(1-methyl-1H-indol-5-yl)-2-[(naphthalen-1-yl)methoxy]benzoic acid
-
 Homo sapiens
2.5.1.10 4-(1H-indol-5-yl)-2-(naphthalen-1-ylmethoxy)benzoic acid
-
 Homo sapiens
2.5.1.10 4-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-[(naphthalen-1-yl)methoxy]benzoic acid
-
 Homo sapiens
2.5.1.10 4-(6-methoxynaphthalen-2-yl)-2-[(naphthalen-1-yl)methoxy]benzoic acid
-
 Homo sapiens
2.5.1.10 4-(naphthalen-1-yl)-1H-indole-2-carboxylic acid
-
 Homo sapiens
2.5.1.10 6-amino-5-ethoxy-8-(naphthalen-1-yl)quinoline-2-carboxylic acid
-
 Homo sapiens
2.5.1.10 6-amino-8-(naphthalen-1-yl)quinoline-2-carboxylic acid
-
 Homo sapiens
2.5.1.10 6-[(ethoxycarbonyl)amino]-8-(naphthalen-1-yl)quinoline-2-carboxylic acid
-
 Homo sapiens
2.5.1.10 8-(1H-indol-4-yl)quinoline-2-carboxylic acid
-
 Homo sapiens
2.5.1.10 8-(naphthalen-1-yl)-6-(1H-pyrrol-2-yl)quinoline-2-carboxylic acid
-
 Homo sapiens
2.5.1.10 8-(naphthalen-1-yl)-6-(thiophen-3-yl)quinoline-2-carboxylic acid
-
 Homo sapiens
2.5.1.10 8-(naphthalen-1-yl)quinoline-2-carboxylic acid
-
 Homo sapiens
2.5.1.10 zoledronic acid
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.5.1.10 geranyl diphosphate + isopentenyl diphosphate Homo sapiens
-
 diphosphate + (2E,6E)-farnesyl diphosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.10 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.10 geranyl diphosphate + isopentenyl diphosphate
-
 Homo sapiens diphosphate + (2E,6E)-farnesyl diphosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.5.1.10 farnesyl pyrophosphate synthase
-
 Homo sapiens
2.5.1.10 FPPS
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.5.1.10 0.000017
-
 pH and temperature not specified in the publication Homo sapiens 4'-acetamido-3-[(naphthalen-1-yl)methoxy][1,1'-biphenyl]-4-carboxylic acid
2.5.1.10 0.000024
-
 pH and temperature not specified in the publication Homo sapiens 6-amino-5-ethoxy-8-(naphthalen-1-yl)quinoline-2-carboxylic acid
2.5.1.10 0.000037
-
 pH and temperature not specified in the publication Homo sapiens 6-[(ethoxycarbonyl)amino]-8-(naphthalen-1-yl)quinoline-2-carboxylic acid
2.5.1.10 0.000038
-
 pH and temperature not specified in the publication Homo sapiens 4-(6-methoxynaphthalen-2-yl)-2-[(naphthalen-1-yl)methoxy]benzoic acid
2.5.1.10 0.000049
-
 pH and temperature not specified in the publication Homo sapiens 4-(1,3-benzodioxol-5-yl)-2-(naphthalen-1-ylmethoxy)benzoic acid
2.5.1.10 0.000058
-
 pH and temperature not specified in the publication Homo sapiens 4'-(hydroxymethyl)-3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
2.5.1.10 0.000069
-
 pH and temperature not specified in the publication Homo sapiens 6-amino-8-(naphthalen-1-yl)quinoline-2-carboxylic acid
2.5.1.10 0.000077
-
 pH and temperature not specified in the publication Homo sapiens 8-(naphthalen-1-yl)-6-(1H-pyrrol-2-yl)quinoline-2-carboxylic acid
2.5.1.10 0.00008
-
 pH and temperature not specified in the publication Homo sapiens 4'-fluoro-3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
2.5.1.10 0.0001
-
 pH and temperature not specified in the publication Homo sapiens 8-(naphthalen-1-yl)-6-(thiophen-3-yl)quinoline-2-carboxylic acid
2.5.1.10 0.00011
-
 pH and temperature not specified in the publication Homo sapiens 4'-carbamoyl-3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
2.5.1.10 0.00014
-
 pH and temperature not specified in the publication Homo sapiens 4'-(methylcarbamoyl)-3-[(naphthalen-1-yl)methoxy][1,1'-biphenyl]-4-carboxylic acid
2.5.1.10 0.00019
-
 pH and temperature not specified in the publication Homo sapiens 4-(1H-indol-5-yl)-2-(naphthalen-1-ylmethoxy)benzoic acid
2.5.1.10 0.00025
-
 pH and temperature not specified in the publication Homo sapiens 4-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-[(naphthalen-1-yl)methoxy]benzoic acid
2.5.1.10 0.00027
-
 pH and temperature not specified in the publication Homo sapiens 4-(1-methyl-1H-indol-5-yl)-2-[(naphthalen-1-yl)methoxy]benzoic acid
2.5.1.10 0.00085
-
 pH and temperature not specified in the publication Homo sapiens 3-(naphthalen-1-ylmethoxy)biphenyl-4-carboxylic acid
2.5.1.10 0.0012
-
 pH and temperature not specified in the publication Homo sapiens 8-(naphthalen-1-yl)quinoline-2-carboxylic acid
2.5.1.10 0.00123
-
 pH and temperature not specified in the publication Homo sapiens 4'-[(methanesulfonyl)amino]-3-[(naphthalen-1-yl)methoxy][1,1'-biphenyl]-4-carboxylic acid
2.5.1.10 0.0068
-
 pH and temperature not specified in the publication Homo sapiens 2-(naphthalen-1-ylmethoxy)benzoic acid
2.5.1.10 0.0071
-
 pH and temperature not specified in the publication Homo sapiens 4-(naphthalen-1-yl)-1H-indole-2-carboxylic acid
2.5.1.10 0.0139
-
 pH and temperature not specified in the publication Homo sapiens 1H,1'H-4,4'-biindole-2-carboxylic acid
2.5.1.10 0.02
-
 pH and temperature not specified in the publication Homo sapiens 2-(naphthalen-1-ylmethoxy)-4-(phenylamino)benzoic acid
2.5.1.10 0.02
-
 pH and temperature not specified in the publication Homo sapiens 8-(1H-indol-4-yl)quinoline-2-carboxylic acid