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Literature summary for 3.4.21.106 extracted from

  • Kim, K.; Kwon, H.; Choi, D.; Lim, T.; Minn, I.; Son, S.H.; Byun, Y.
    Design and synthesis of dye-conjugated hepsin inhibitors (2019), Bioorg. Chem., 89, 102990 .
    View publication on PubMed
Search for more literature for 3.4.21.106

Inhibitors

Inhibitors Comment Organism Structure
N-[1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]-N2-(20-[3,3-dimethyl-5-sulfo-2-[(1E)-3-[(4E)-4-[(2E)-2-(1,3,3-trimethyl-5-sulfo-1,3-dihydro-2H-indol-2-ylidene)ethylidene]cyclohex-1-en-1-yl]prop-1-en-1-yl]-3H-indolium-1-yl]-16-oxo-4,7,10,13-tetraoxa-15-azaicosan-1-oyl)-L-leucinamide Leu-Arg dipeptide, attached to dye SulfoCy7. Compound shows 1000fold selectivtiy for hepsin over matriptase and selective uptake and retention in hepsin-overexpressing cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P05981
-
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000022
-
 N-[1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]-N2-(20-[3,3-dimethyl-5-sulfo-2-[(1E)-3-[(4E)-4-[(2E)-2-(1,3,3-trimethyl-5-sulfo-1,3-dihydro-2H-indol-2-ylidene)ethylidene]cyclohex-1-en-1-yl]prop-1-en-1-yl]-3H-indolium-1-yl]-16-oxo-4,7,10,13-tetraoxa-15-azaicosan-1-oyl)-L-leucinamide pH not specified in the publication, temperature not specified in the publication Homo sapiens