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Literature summary for 2.5.1.46 extracted from

  • Tanaka, Y.; Kurasawa, O.; Yokota, A.; Klein, M.G.; Ono, K.; Saito, B.; Matsumoto, S.; Okaniwa, M.; Ambrus-Aikelin, G.; Morishita, D.; Kitazawa, S.; Uchiyama, N.; Ogawa, K.; Kimura, H.; Imamura, S.
    Discovery of novel allosteric inhibitors of deoxyhypusine synthase (2020), J. Med. Chem., 63, 3215-3226 .
    View publication on PubMed
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Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitors 6-bromo-N-(1H-indol-4-yl)-1-benzothiophene-2-carboxamide and N''-guanyl-1,7-diaminoheptane. Presence of 6-bromo-N-(1H-indol-4-yl)-1-benzothiophene-2-carboxamide induces a dramatic conformational change in DHPS Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
6-bromo-N-(1H-indol-4-yl)-1-benzothiophene-2-carboxamide the 6'-bromo substituent is necessary for binding to DHPS Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P49366
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000062
-
 pH 8.0, 23°C Homo sapiens 6-bromo-N-(1H-indol-4-yl)-1-benzothiophene-2-carboxamide