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Literature summary for 2.5.1.58 extracted from

  • Qiao, Y.; Gao, J.; Qiu, Y.; Wu, L.; Guo, F.; Lo, K.K.; Li, D.
    Design, synthesis, and characterization of piperazinedione-based dual protein inhibitors for both farnesyltransferase and geranylgeranyltransferase-I (2011), Eur. J. Med. Chem., 46, 2264-2273.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
(S)-N-(4-(3,4-dichlorophenoxy)benzyl)-6-(1H-indol-3-yl)piperazine-2,5-dione dual inhibitor for both farnesyl transferase and geranygeranyltransferase-I. Compound occupies both isoprenoid and peptide substrate binding sites Rattus norvegicus
(S)-N-(4-(3-chlorophenoxy)benzyl)-6-(1H-indol-3-yl)piperazine-2,5-dione dual inhibitor for both farnesyl transferase and geranygeranyltransferase-I Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0131
-
 pH 7.4, 30°C Rattus norvegicus (S)-N-(4-(3,4-dichlorophenoxy)benzyl)-6-(1H-indol-3-yl)piperazine-2,5-dione
0.0178
-
 pH 7.4, 30°C Rattus norvegicus (S)-N-(4-(3-chlorophenoxy)benzyl)-6-(1H-indol-3-yl)piperazine-2,5-dione