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Literature summary extracted from

  • Lethu, S.; Bosc, D.; Mouray, E.; Grellier, P.; Dubois, J.
    New protein farnesyltransferase inhibitors in the 3-arylthiophene 2-carboxylic acid series: diversification of the aryl moiety by solid-phase synthesis (2013), J. Enzyme Inhib. Med. Chem., 28, 163-171.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.5.1.58
-
Trypanosoma brucei

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.5.1.58 3-(4-chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid
-
Homo sapiens
2.5.1.58 3-(4-chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid
-
Saccharomyces cerevisiae
2.5.1.58 3-(4-chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid
-
Trypanosoma brucei
2.5.1.58 3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Homo sapiens
2.5.1.58 3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Saccharomyces cerevisiae
2.5.1.58 3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Trypanosoma brucei
2.5.1.58 4-cyano-3-(3-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Homo sapiens
2.5.1.58 4-cyano-3-(3-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Saccharomyces cerevisiae
2.5.1.58 4-cyano-3-(3-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Trypanosoma brucei
2.5.1.58 4-cyano-3-(4-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Homo sapiens
2.5.1.58 4-cyano-3-(4-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Saccharomyces cerevisiae
2.5.1.58 4-cyano-3-(4-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Trypanosoma brucei
2.5.1.58 4-cyano-3-(4-methoxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Homo sapiens
2.5.1.58 4-cyano-3-(4-methoxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Saccharomyces cerevisiae
2.5.1.58 4-cyano-3-(4-methoxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Trypanosoma brucei
2.5.1.58 4-cyano-3-(dibenzo[b,d]furan-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Homo sapiens
2.5.1.58 4-cyano-3-(dibenzo[b,d]furan-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Saccharomyces cerevisiae
2.5.1.58 4-cyano-3-(dibenzo[b,d]furan-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Trypanosoma brucei
2.5.1.58 4-cyano-3-(naphthalen-2-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Homo sapiens
2.5.1.58 4-cyano-3-(naphthalen-2-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Saccharomyces cerevisiae
2.5.1.58 4-cyano-3-(naphthalen-2-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Trypanosoma brucei
2.5.1.58 4-cyano-3-[3-(methoxycarbonyl)phenyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Homo sapiens
2.5.1.58 4-cyano-3-[3-(methoxycarbonyl)phenyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Saccharomyces cerevisiae
2.5.1.58 4-cyano-3-[3-(methoxycarbonyl)phenyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
-
Trypanosoma brucei
2.5.1.58 FTI-276
-
Homo sapiens
2.5.1.58 FTI-276
-
Saccharomyces cerevisiae
2.5.1.58 FTI-276
-
Trypanosoma brucei

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.58 Homo sapiens
-
-
-
2.5.1.58 Saccharomyces cerevisiae
-
-
-
2.5.1.58 Trypanosoma brucei
-
-
-

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.5.1.58 0.00000078
-
pH 7.5, 30°C Saccharomyces cerevisiae FTI-276
2.5.1.58 0.00001
-
pH 7.5, 30°C Trypanosoma brucei FTI-276
2.5.1.58 0.000015
-
pH 7.5, 30°C Homo sapiens FTI-276
2.5.1.58 0.00011
-
pH 7.5, 30°C Saccharomyces cerevisiae 3-(4-chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid
2.5.1.58 0.00025
-
pH 7.5, 30°C Saccharomyces cerevisiae 4-cyano-3-(4-methoxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.00027
-
pH 7.5, 30°C Saccharomyces cerevisiae 4-cyano-3-(4-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.00032
-
pH 7.5, 30°C Saccharomyces cerevisiae 4-cyano-3-(naphthalen-2-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.00046
-
pH 7.5, 30°C Saccharomyces cerevisiae 4-cyano-3-(3-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.00062
-
pH 7.5, 30°C Saccharomyces cerevisiae 4-cyano-3-[3-(methoxycarbonyl)phenyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.00064
-
pH 7.5, 30°C Saccharomyces cerevisiae 3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.001
-
pH 7.5, 30°C Saccharomyces cerevisiae 4-cyano-3-(dibenzo[b,d]furan-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.0033
-
pH 7.5, 30°C Homo sapiens 3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.0033
-
pH 7.5, 30°C Trypanosoma brucei 4-cyano-3-(dibenzo[b,d]furan-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.0048
-
pH 7.5, 30°C Homo sapiens 4-cyano-3-[3-(methoxycarbonyl)phenyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.0054
-
pH 7.5, 30°C Trypanosoma brucei 3-(biphenyl-3-yl)-4-cyano-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.0055
-
pH 7.5, 30°C Homo sapiens 4-cyano-3-(naphthalen-2-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.0069
-
pH 7.5, 30°C Trypanosoma brucei 4-cyano-3-(4-methoxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.007
-
pH 7.5, 30°C Homo sapiens 4-cyano-3-(4-methoxyphenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.0086
-
pH 7.5, 30°C Trypanosoma brucei 4-cyano-3-(3-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.0097
-
pH 7.5, 30°C Trypanosoma brucei 4-cyano-3-[3-(methoxycarbonyl)phenyl]-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.0106
-
pH 7.5, 30°C Trypanosoma brucei 3-(4-chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid
2.5.1.58 0.015
-
pH 7.5, 30°C Homo sapiens 4-cyano-3-(dibenzo[b,d]furan-1-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.016
-
pH 7.5, 30°C Homo sapiens 3-(4-chlorophenyl)-4-cyano-5-(isopropylthio)thiophene-2-carboxylic acid
2.5.1.58 0.02
-
pH 7.5, 30°C Homo sapiens 4-cyano-3-(4-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.029
-
pH 7.5, 30°C Trypanosoma brucei 4-cyano-3-(4-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.032
-
pH 7.5, 30°C Trypanosoma brucei 4-cyano-3-(naphthalen-2-yl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid
2.5.1.58 0.039
-
pH 7.5, 30°C Homo sapiens 4-cyano-3-(3-fluorophenyl)-5-(propan-2-ylsulfanyl)thiophene-2-carboxylic acid