Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.22.43 extracted from

  • Mons, E.; Jansen, I.D.C.; Loboda, J.; van Doodewaerd, B.R.; Hermans, J.; Verdoes, M.; van Boeckel, C.A.A.; van Veelen, P.A.; Turk, B.; Turk, D.; Ovaa, H.
    The Alkyne moiety as a latent electrophile in irreversible covalent small molecule inhibitors of cathepsin K (2019), J. Am. Chem. Soc., 141, 3507-3514 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
4-fluoro-N-prop-2-yn-1-yl-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
Homo sapiens
N-(3-bromoprop-2-yn-1-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
Homo sapiens
N-(cyanomethyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
Homo sapiens
N-but-3-yn-2-yl-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
Homo sapiens
odanacatib
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P07711
-
-

Synonyms

Synonyms Comment Organism
hcatV
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000016
-
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween 20 (v/v), 37°C Homo sapiens N-(3-bromoprop-2-yn-1-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
0.0006
-
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween 20 (v/v), 37°C Homo sapiens odanacatib
0.00091
-
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween 20 (v/v), 37°C Homo sapiens N-(cyanomethyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
0.024
-
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween 20 (v/v), 37°C Homo sapiens 4-fluoro-N-prop-2-yn-1-yl-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
0.046
-
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween 20 (v/v), 37°C Homo sapiens N-but-3-yn-2-yl-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide