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

BRENDA support

Literature summary for 3.4.22.34 extracted from

  • Eddie, S.L.; Gregson, A.; Graham, E.; Burton, S.; Harrison, T.; Burden, R.; Scott, C.J.; Mullan, P.B.; Williams, R.
    Identification and SAR exploration of a novel series of legumain inhibitors (2019), Bioorg. Med. Chem. Lett., 29, 1546-1548 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[2'-(trifluoromethyl)[1,1'-biphenyl]-4-sulfonyl]propanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-sulfonyl]propanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-(1-methyl-1H-indazol-5-yl)benzene-1-sulfonyl]propanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-(1-methyl-1H-indazol-7-yl)benzene-1-sulfonyl]propanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-(2-methyl-2H-indazol-5-yl)benzene-1-sulfonyl]propanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-(2-methyl-2H-indazol-7-yl)benzene-1-sulfonyl]propanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-(4-methylpyridin-3-yl)benzene-1-sulfonyl]propanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-(5-methylpyridin-3-yl)benzene-1-sulfonyl]propanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-[4-(trifluoromethyl)pyridin-3-yl]benzene-1-sulfonyl]propanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-[5-(trifluoromethyl)pyridin-3-yl]benzene-1-sulfonyl]propanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(2',3'-difluoro[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(2',4'-dichloro[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(2',4'-difluoro[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(3',5'-difluoro[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(3'-fluoro[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(4'-butyl[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(4'-chloro[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(4'-fluoro[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(4'-tert-butyl[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-([1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-[4-(1,3-benzothiazol-5-yl)benzene-1-sulfonyl]-2,2-dimethylpropanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-[4-(4-chloropyridin-3-yl)benzene-1-sulfonyl]-2,2-dimethylpropanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-[4-(4-fluoropyridin-3-yl)benzene-1-sulfonyl]-2,2-dimethylpropanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-[4-(4-tert-butylpyridin-3-yl)benzene-1-sulfonyl]-2,2-dimethylpropanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-[4-(5-chloropyridin-3-yl)benzene-1-sulfonyl]-2,2-dimethylpropanamide
-
Homo sapiens
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-[4-(5-fluoropyridin-3-yl)benzene-1-sulfonyl]-2,2-dimethylpropanamide
-
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
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000012
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-(1-methyl-1H-indazol-7-yl)benzene-1-sulfonyl]propanamide pH 7.4, 37°C Homo sapiens
0.00000026
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-(2-methyl-2H-indazol-5-yl)benzene-1-sulfonyl]propanamide pH 7.4, 37°C Homo sapiens
0.00000047
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-[4-(1,3-benzothiazol-5-yl)benzene-1-sulfonyl]-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens
0.0000013
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(3'-fluoro[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens
0.0000014
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-[4-(4-tert-butylpyridin-3-yl)benzene-1-sulfonyl]-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens
0.0000015
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-[4-(5-chloropyridin-3-yl)benzene-1-sulfonyl]-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens
0.0000036
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-(1-methyl-1H-indazol-5-yl)benzene-1-sulfonyl]propanamide pH 7.4, 37°C Homo sapiens
0.0000055
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(4'-fluoro[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens
0.0000071
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(4'-chloro[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens
0.0000098
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-(2-methyl-2H-indazol-7-yl)benzene-1-sulfonyl]propanamide pH 7.4, 37°C Homo sapiens
0.000012
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-[5-(trifluoromethyl)pyridin-3-yl]benzene-1-sulfonyl]propanamide pH 7.4, 37°C Homo sapiens
0.000012
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-[4-(4-chloropyridin-3-yl)benzene-1-sulfonyl]-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens
0.000015
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-(5-methylpyridin-3-yl)benzene-1-sulfonyl]propanamide pH 7.4, 37°C Homo sapiens
0.000018
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-[4-(trifluoromethyl)pyridin-3-yl]benzene-1-sulfonyl]propanamide pH 7.4, 37°C Homo sapiens
0.000026
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4-(4-methylpyridin-3-yl)benzene-1-sulfonyl]propanamide pH 7.4, 37°C Homo sapiens
0.000033
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(2',3'-difluoro[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens
0.000034
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-([1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens
0.000059
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[2'-(trifluoromethyl)[1,1'-biphenyl]-4-sulfonyl]propanamide pH 7.4, 37°C Homo sapiens
0.000078
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-[4-(5-fluoropyridin-3-yl)benzene-1-sulfonyl]-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens
0.000082
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(2',4'-difluoro[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens
0.000096
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-[4-(4-fluoropyridin-3-yl)benzene-1-sulfonyl]-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens
0.00011
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(3',5'-difluoro[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens
0.00016
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(4'-butyl[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens
0.00028
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(2',4'-dichloro[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens
0.00029
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-2,2-dimethyl-3-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-sulfonyl]propanamide pH 7.4, 37°C Homo sapiens
0.00087
-
N-[(1S)-3-amino-1-cyano-3-oxopropyl]-3-(4'-tert-butyl[1,1'-biphenyl]-4-sulfonyl)-2,2-dimethylpropanamide pH 7.4, 37°C Homo sapiens