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Literature summary for 3.4.21.B39 extracted from

  • Hoelz, L.V.B.; Zorzanelli, B.C.; Azevedo, P.H.R.A.; Passos, S.G.; de Souza, L.R.; Zani, M.; Pinheiro, S.; Puzer, L.; Dias, L.R.S.; Muri, E.M.F.
    Synthesis, biological evaluation and molecular modeling of pseudo-peptides based statine as inhibitors for human tissue kallikrein 5 (2016), Eur. J. Med. Chem., 112, 39-47 .
    View publication on PubMed
Search for more literature for 3.4.21.B39

Application

Application Comment Organism
medicine human kallikrein 5 is a potential target for the treatment of skin inflammation and cancer Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(S)-methyl-1-((3'S,4'S)-4'-(tert-butoxycarbonylamino)-3'-hydroxy-5'-phenylpentanoyl) pyrrolidine-2-carboxylate
-
 Homo sapiens
(S)-methyl-2-((3'S,4'S)-4'-(tert-butoxycarbonylamino)-3'-hydroxy-5'-phenylpentanamido)-3-methylbutanoate
-
 Homo sapiens
(S)-methyl-2-((3'S,4'S)-4'-(tert-butoxycarbonylamino)-3'-hydroxy-5'-phenylpentanamido)-3-phenylpropanoate
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9Y337
-
-

Source Tissue

Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Abz-KLRSSKQ-EDDnp + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
KLK5
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00012
-
 (S)-methyl-2-((3'S,4'S)-4'-(tert-butoxycarbonylamino)-3'-hydroxy-5'-phenylpentanamido)-3-phenylpropanoate pH 7.5, 37°C Homo sapiens
0.00013
-
 (S)-methyl-2-((3'S,4'S)-4'-(tert-butoxycarbonylamino)-3'-hydroxy-5'-phenylpentanamido)-3-methylbutanoate pH 7.5, 37°C Homo sapiens
0.00013
-
 (S)-methyl-1-((3'S,4'S)-4'-(tert-butoxycarbonylamino)-3'-hydroxy-5'-phenylpentanoyl) pyrrolidine-2-carboxylate pH 7.5, 37°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000112
-
 pH 7.5, 37°C Homo sapiens (S)-methyl-2-((3'S,4'S)-4'-(tert-butoxycarbonylamino)-3'-hydroxy-5'-phenylpentanamido)-3-phenylpropanoate
0.000115
-
 pH 7.5, 37°C Homo sapiens (S)-methyl-2-((3'S,4'S)-4'-(tert-butoxycarbonylamino)-3'-hydroxy-5'-phenylpentanamido)-3-methylbutanoate
0.000122
-
 pH 7.5, 37°C Homo sapiens (S)-methyl-1-((3'S,4'S)-4'-(tert-butoxycarbonylamino)-3'-hydroxy-5'-phenylpentanoyl) pyrrolidine-2-carboxylate