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

BRENDA support

Literature summary for 3.4.14.1 extracted from

  • Bondebjerg, J.; Fuglsang, H.; Valeur, K.R.; Kaznelson, D.W.; Hansen, J.A.; Pedersen, R.O.; Krogh, B.O.; Jensen, B.S.; Lauritzen, C.; Petersen, G.; Pedersen, J.; Naerum, L.
    Novel semicarbazide-derived inhibitors of human dipeptidyl peptidase I (hDPPI) (2005), Bioorg. Med. Chem., 13, 4408-4424.
    View publication on PubMed
Search for more literature for 3.4.14.1

Inhibitors

Inhibitors Comment Organism Structure
1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(2-naphthyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide IC50: 19 nM Homo sapiens
1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(benzo[b]-thiophen-3-yl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide IC50: 22 nM Homo sapiens
1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(indol-3-yl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide IC50: 21 nM Homo sapiens
1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(m-fluorophenyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide IC50: 31 nM, competitive inhibition, selective for DPP I over other cysteine and serine proteases, noncytotoxic Homo sapiens
1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(m-methoxyphenyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide IC50: 39 nM Homo sapiens
1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(p-chlorophenyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide IC50: 45 nM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 recombinant
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Gly-Tyr(3'NO2)-Gly-Pro-Pro-Lys(epsilon-(2-aminobenzoyl))-Gly + H2O
-
 Homo sapiens Gly-Tyr(3'NO2) + Gly-Pro-Pro-Lys(epsilon-(2-aminobenzoyl))-Gly
-
 ?

Synonyms

Synonyms Comment Organism
dipeptidyl peptidase I
-
 Homo sapiens
hDPPI
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000045
-
 1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(m-fluorophenyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000019
-
 IC50: 19 nM Homo sapiens 1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(2-naphthyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide
0.000021
-
 IC50: 21 nM Homo sapiens 1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(indol-3-yl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide
0.000022
-
 IC50: 22 nM Homo sapiens 1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(benzo[b]-thiophen-3-yl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide
0.000031
-
 IC50: 31 nM, competitive inhibition, selective for DPP I over other cysteine and serine proteases, noncytotoxic Homo sapiens 1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(m-fluorophenyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide
0.000039
-
 IC50: 39 nM Homo sapiens 1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(m-methoxyphenyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide
0.000045
-
 IC50: 45 nM Homo sapiens 1-(2S-2-aminobutanoyl)-4-(2S-N-(2S-3-(p-chlorophenyl)propan-2-yl-amide)4-phenylbutan-2-yl-amide)semicarbazide