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Literature summary for 3.4.22.34 extracted from

  • Ness, K.A.; Eddie, S.L.; Higgins, C.A.; Templeman, A.; DCosta, Z.; Gaddale, K.K.; Bouzzaoui, S.; Jordan, L.; Janssen, D.; Harrison, T.; Burkamp, F.; Young, A.; Burden, R.; Scott, C.J.; Mullan, P.B.; Williams, R.
    Development of a potent and selective cell penetrant Legumain inhibitor (2015), Bioorg. Med. Chem. Lett., 25, 5642-5645 .
    View publication on PubMed
Search for more literature for 3.4.22.34

Inhibitors

Inhibitors Comment Organism Structure
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(2',4'-dichloro[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(2'-chloro[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(2,4-dichlorobenzene-1-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(3',4'-dichloro[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(3',4'-difluoro[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(3'-fluoro[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4'-chloro[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4'-cyano[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4'-ethyl[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4'-methoxy[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4'-methyl[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4'-tert-butyl[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4-bromobenzene-1-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4-chlorobenzene-1-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4-fluorobenzene-1-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-([1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-[2'-(trifluoromethyl)[1,1'-biphenyl]-4-sulfonyl]-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-[4'-(propan-2-yl)[1,1'-biphenyl]-4-sulfonyl]-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-sulfonyl]-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-[4'-[(propan-2-yl)oxy][1,1'-biphenyl]-4-sulfonyl]-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-[4-(2H-1,3-benzodioxol-5-yl)benzene-1-sulfonyl]-L-prolinamide
-
 Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-[4-(trifluoromethyl)benzene-1-sulfonyl]-L-prolinamide
-
 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
0.000005
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-[4'-(propan-2-yl)[1,1'-biphenyl]-4-sulfonyl]-L-prolinamide
0.000006
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(2',4'-dichloro[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
0.000006
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4'-methoxy[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
0.000012
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-([1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
0.000023
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(3',4'-difluoro[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
0.000032
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4'-methyl[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
0.000033
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(3'-fluoro[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
0.000033
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4'-cyano[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
0.000035
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(2'-chloro[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
0.000045
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4'-chloro[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
0.000047
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(3'-fluoro[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
0.000049
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-[4-(2H-1,3-benzodioxol-5-yl)benzene-1-sulfonyl]-L-prolinamide
0.000067
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4'-chloro[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
0.000071
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4'-ethyl[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
0.000071
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4'-tert-butyl[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
0.000073
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4-chlorobenzene-1-sulfonyl)-L-prolinamide
0.000073
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-[4'-[(propan-2-yl)oxy][1,1'-biphenyl]-4-sulfonyl]-L-prolinamide
0.000093
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-[2'-(trifluoromethyl)[1,1'-biphenyl]-4-sulfonyl]-L-prolinamide
0.000121
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-sulfonyl]-L-prolinamide
0.000169
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(3',4'-dichloro[1,1'-biphenyl]-4-sulfonyl)-L-prolinamide
0.000269
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4-fluorobenzene-1-sulfonyl)-L-prolinamide
0.000282
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(4-bromobenzene-1-sulfonyl)-L-prolinamide
0.000332
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-[4-(trifluoromethyl)benzene-1-sulfonyl]-L-prolinamide
0.000593
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-(2,4-dichlorobenzene-1-sulfonyl)-L-prolinamide
0.000969
-
 pH and temperature not specified in the publication Homo sapiens N-[(1S)-3-amino-1-cyano-3-oxopropyl]-1-[4'-[(propan-2-yl)oxy][1,1'-biphenyl]-4-sulfonyl]-L-prolinamide