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Literature summary for 3.4.22.34 extracted from

  • Ness, K.A.; Eddie, S.L.; Burton, S.; Harrison, T.; Mullan, P.; Williams, R.
    Flat SAR of P3-methylsulphonamide based small molecule legumain inhibitors (2016), Bioorg. Med. Chem. Lett., 26, 413-416 .
    View publication on PubMed
Search for more literature for 3.4.22.34

Inhibitors

Inhibitors Comment Organism Structure
(2S)-N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2-[[(2',3'-difluoro[1,1'-biphenyl]-4-yl)methyl](methanesulfonyl)amino]butanamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-(ethanesulfonyl)-N2-[(3'-fluoro[1,1'-biphenyl]-4-yl)methyl]-L-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-(methanesulfonyl)-N2-[(3'-methoxy[1,1'-biphenyl]-4-yl)methyl]-D-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-(methanesulfonyl)-N2-[(3'-methoxy[1,1'-biphenyl]-4-yl)methyl]-L-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-(methanesulfonyl)-N2-[(3'-propoxy[1,1'-biphenyl]-4-yl)methyl]-D-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-(methanesulfonyl)-N2-[(3'-propoxy[1,1'-biphenyl]-4-yl)methyl]-L-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-(methanesulfonyl)-N2-[[3'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]methyl]-L-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(2',3'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(2-methylpropane-1-sulfonyl)-L-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(2',3'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(ethanesulfonyl)-L-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(2',3'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-D-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(2',3'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-L-norvalinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(2',3'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(propane-1-sulfonyl)-L-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(2'-fluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-L-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3',4'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-D-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3',4'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-L-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3',5'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-D-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3'-chloro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3'-ethoxy[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-L-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3'-fluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(2-methylpropane-1-sulfonyl)-L-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3'-fluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-D-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3'-fluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-L-alaninamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3'-fluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-L-norvalinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(4'-fluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-L-alaninamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q99538
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-Ala-Ala-Asn-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens benzyloxycarbonyl-Ala-Ala-Asn + 7-amino-4-methylcoumarin
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000128
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3'-fluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-L-alaninamide
0.000252
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3',4'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-L-alaninamide
0.000323
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(4'-fluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-L-alaninamide
0.000356
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(2'-fluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-L-alaninamide
0.000378
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-(methanesulfonyl)-N2-[(3'-methoxy[1,1'-biphenyl]-4-yl)methyl]-L-alaninamide
0.000425
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3'-chloro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)alaninamide
0.000586
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3'-ethoxy[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-L-alaninamide
0.000601
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-(methanesulfonyl)-N2-[[3'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]methyl]-L-alaninamide
0.000882
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-(methanesulfonyl)-N2-[(3'-propoxy[1,1'-biphenyl]-4-yl)methyl]-L-alaninamide
0.001035
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(4'-fluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-L-alaninamide
0.001086
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(2',3'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(ethanesulfonyl)-L-alaninamide
0.001359
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3',5'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-D-alaninamide
0.001459
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(2',3'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-D-alaninamide
0.001818
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(2',3'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(2-methylpropane-1-sulfonyl)-L-alaninamide
0.002259
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3'-fluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-D-alaninamide
0.002272
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3'-fluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(2-methylpropane-1-sulfonyl)-L-alaninamide
0.003889
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-(ethanesulfonyl)-N2-[(3'-fluoro[1,1'-biphenyl]-4-yl)methyl]-L-alaninamide
0.004384
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3'-fluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-L-norvalinamide
0.00505
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-(methanesulfonyl)-N2-[(3'-propoxy[1,1'-biphenyl]-4-yl)methyl]-D-alaninamide
0.005854
-
 pH 7.4, 37°C Homo sapiens (2S)-N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2-[[(2',3'-difluoro[1,1'-biphenyl]-4-yl)methyl](methanesulfonyl)amino]butanamide
0.005854
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-(methanesulfonyl)-N2-[(3'-methoxy[1,1'-biphenyl]-4-yl)methyl]-D-alaninamide
0.006296
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3',4'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-D-alaninamide
0.006745
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(2',3'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(propane-1-sulfonyl)-L-alaninamide
0.007749
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(2',3'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-L-norvalinamide
0.009249
-
 pH 7.4, 37°C Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-N2-[(3',5'-difluoro[1,1'-biphenyl]-4-yl)methyl]-N2-(methanesulfonyl)-D-alaninamide