Literature summary for 3.4.21.106 extracted from

Kwon, H.; Kim, Y.; Park, K.; Choi, S.A.; Son, S.H.; Byun, Y.
Structure-based design, synthesis, and biological evaluation of Leu-Arg dipeptide analogs as novel hepsin inhibitors (2016), Bioorg. Med. Chem. Lett., 26, 310-314 .

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Inhibitors

Inhibitors	Comment	Organism	Structure
N2-acetyl-N-[1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]-L-leucinamide	inhibitor based on tetrapeptide hepsin inhibitor acetyl-KQLR-ketothiazole. Hepsin affinity of the (R)-epimer is similar to that of the corresponding (S)-epimer	Homo sapiens
N2-acetyl-N-[5-carbamimidamido-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]-L-leucinamide	inhibitor based on tetrapeptide hepsin inhibitor acetyl-KQLR-ketothiazole. Hepsin affinity of the (R)-epimer is similar to that of the corresponding (S)-epimer	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P05981	-	-

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.000003	-	N2-acetyl-N-[1-(1,3-benzothiazol-2-yl)-5-carbamimidamido-1-oxopentan-2-yl]-L-leucinamide	pH not specified in the publication, temperature not specified in the publication	Homo sapiens
0.000022	-	N2-acetyl-N-[5-carbamimidamido-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]-L-leucinamide	pH not specified in the publication, temperature not specified in the publication	Homo sapiens

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Release 2023.1 (January 2023)