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Literature summary for 3.4.21.106 extracted from

  • Goswami, R.; Wohlfahrt, G.; Toermaekangas, O.; Moilanen, A.; Lakshminarasimhan, A.; Nagaraj, J.; Arumugam, K.N.; Mukherjee, S.; Chacko, A.R.; Krishnamurthy, N.R.; Jaleel, M.; Palakurthy, R.K.; Samiulla, D.S.; Ramachandra, M.
    Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors (2015), Bioorg. Med. Chem. Lett., 25, 5309-5314 .
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
1-[6-(6-methyl-3H-indol-2-yl)pyridin-2-yl]cyclohexan-1-ol compounds exhibits inhibition of invasion and migration of hepsin-overexpressing cell line. The selective inhibition of hepsin is likely due to interactions of the midine group at the S1 site with the cyclohexyl ring from the 2-aryl group projecting towards the S1' site and the tert-hydroxyl group interacting with His57 side-chain Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P05981
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-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0001
-
 1-[6-(6-methyl-3H-indol-2-yl)pyridin-2-yl]cyclohexan-1-ol pH not specified in the publication, temperature not specified in the publication Homo sapiens