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Literature summary extracted from

  • Feng, Y.; Park, J.; Li, S.G.; Boutin, R.; Viereck, P.; Schilling, M.A.; Berghuis, A.M.; Tsantrizos, Y.S.
    Chirality-driven mode of binding of alpha-aminophosphonic acid-based allosteric inhibitors of the human farnesyl pyrophosphate synthase (hFPPS) (2019), J. Med. Chem., 62, 9691-9702 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.10 (R)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-(3-fluorophenyl)ethyl)phosphonic acid
-
 Homo sapiens
2.5.1.10 (R)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-cyclohexylethyl)phosphonic acid
-
 Homo sapiens
2.5.1.10 (R)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-phenylethyl)phosphonic acid
-
 Homo sapiens
2.5.1.10 (R)-(2-(3-fluorophenyl)-1-((6-(p-tolyl)thieno[2,3-d]-pyrimidin-4-yl)amino)ethyl)phosphonic acid
-
 Homo sapiens
2.5.1.10 (R)-(2-phenyl-1-((6-(p-tolyl)thieno[2,3-d]pyrimidin-4-yl)-amino)ethyl)phosphonic acid
-
 Homo sapiens
2.5.1.10 (R)-2-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-3-(3-fluorophenyl)propanoic acid
-
 Homo sapiens
2.5.1.10 (S)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-(3-fluorophenyl)ethyl)phosphonic acid
-
 Homo sapiens
2.5.1.10 (S)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-cyclohexylethyl)phosphonic acid
-
 Homo sapiens
2.5.1.10 (S)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-phenylethyl)phosphonic acid
-
 Homo sapiens
2.5.1.10 (S)-(2-(3-fluorophenyl)-1-((6-(p-tolyl)thieno[2,3-d]-pyrimidin-4-yl)amino)ethyl)phosphonic acid
-
 Homo sapiens
2.5.1.10 (S)-(2-phenyl-1-((6-(p-tolyl)thieno[2,3-d]pyrimidin-4-yl)-amino)ethyl)phosphonic acid
-
 Homo sapiens
2.5.1.10 ([[6-(4-methylphenyl)-5,6-dihydrothieno[2,3-d]pyrimidin-4-yl]amino]methyl)phosphonic acid
-
 Homo sapiens
2.5.1.10 1-(carboxymethyl)-5,9b-dihydro-1H-benzo[g]indole-2-carboxylic 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 P14324
-
-

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 hFPPS
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.5.1.10 0.00054
-
 (R)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-(3-fluorophenyl)ethyl)phosphonic acid pH 7.7, 37°C Homo sapiens
2.5.1.10 0.001
-
 (R)-2-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-3-(3-fluorophenyl)propanoic acid pH 7.7, 37°C Homo sapiens
2.5.1.10 0.0011
-
 (S)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-(3-fluorophenyl)ethyl)phosphonic acid pH 7.7, 37°C Homo sapiens
2.5.1.10 0.0012
-
 (S)-(2-(3-fluorophenyl)-1-((6-(p-tolyl)thieno[2,3-d]-pyrimidin-4-yl)amino)ethyl)phosphonic acid pH 7.7, 37°C Homo sapiens
2.5.1.10 0.0015
-
 (R)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-phenylethyl)phosphonic acid pH 7.7, 37°C Homo sapiens
2.5.1.10 0.0028
-
 (S)-(2-phenyl-1-((6-(p-tolyl)thieno[2,3-d]pyrimidin-4-yl)-amino)ethyl)phosphonic acid pH 7.7, 37°C Homo sapiens
2.5.1.10 0.0028
-
 (R)-(2-(3-fluorophenyl)-1-((6-(p-tolyl)thieno[2,3-d]-pyrimidin-4-yl)amino)ethyl)phosphonic acid pH 7.7, 37°C Homo sapiens
2.5.1.10 0.003
-
 (R)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-cyclohexylethyl)phosphonic acid pH 7.7, 37°C Homo sapiens
2.5.1.10 0.0037
-
 (S)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-phenylethyl)phosphonic acid pH 7.7, 37°C Homo sapiens
2.5.1.10 0.0077
-
 (R)-(2-phenyl-1-((6-(p-tolyl)thieno[2,3-d]pyrimidin-4-yl)-amino)ethyl)phosphonic acid pH 7.7, 37°C Homo sapiens
2.5.1.10 0.0081
-
 (S)-(1-((6-(3-chloro-4-methylphenyl)thieno[2,3-d]-pyrimidin-4-yl)amino)-2-cyclohexylethyl)phosphonic acid pH 7.7, 37°C Homo sapiens