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

BRENDA support

Literature summary for 3.4.19.6 extracted from

  • Kelly, J.A.; Scalabrino, G.A.; Slator, G.R.; Cullen, A.A.; Gilmer, J.F.; Lloyd, D.G.; Bennett, G.W.; Bauer, K.; Tipton, K.F.; Williams, C.H.
    Structure-activity studies with high-affinity inhibitors of pyroglutamyl-peptidase II (2005), Biochem. J., 389, 569-576.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
1,3-benzodioxol-5-amine
-
Rattus norvegicus
2-Aminobenzyl alcohol
-
Rattus norvegicus
2-hydroxyaniline
-
Rattus norvegicus
2-Phenylethylamine
-
Rattus norvegicus
3,4-dimethoxyaniline
-
Rattus norvegicus
3,5-dimethoxyaniline
-
Rattus norvegicus
3-(trifluoromethoxy)aniline
-
Rattus norvegicus
3-phenyl-1-propylamine
-
Rattus norvegicus
4-(trifluoromethyl)aniline
-
Rattus norvegicus
4-amino-N-methylphthalamide
-
Rattus norvegicus
4-phenylbutylamine
-
Rattus norvegicus
5,6,7,8-tetrahydro-1-naphthylamine
-
Rattus norvegicus
5-amino-2-chloropyridine
-
Rattus norvegicus
5-amino-2-methoxyphenol
-
Rattus norvegicus
5-aminoindan
-
Rattus norvegicus
5-chloro-2-methoxyaniline
-
Rattus norvegicus
6-amino-1,3-dihydroisobenzofuran-1-one
-
Rattus norvegicus
6-amino-2-mercaptobenzothiazole
-
Rattus norvegicus
6-amino-3,4-benzocoumarin
-
Rattus norvegicus
7-amino-4-methylcoumarin
-
Rattus norvegicus
aniline
-
Rattus norvegicus
benzyl alcohol
-
Rattus norvegicus
benzylamine
-
Rattus norvegicus
m-anisidine
-
Rattus norvegicus
m-phenethidine
-
Rattus norvegicus
methyl alcohol
-
Rattus norvegicus
methylamine
-
Rattus norvegicus
o-anisidine
-
Rattus norvegicus
p-anisidine
-
Rattus norvegicus
pyroglutamyl-Asn(N-benzyl)-ProNH2
-
Rattus norvegicus
pyroglutamyl-Asn(N-hydroxyl)-ProNH2
-
Rattus norvegicus
pyroglutamyl-Asn(N-methyl)-ProNH2
-
Rattus norvegicus
pyroglutamyl-Asn(N-phenyl)-ProNH2
-
Rattus norvegicus
pyroglutamyl-Asn-Pro-7-amido-4-methylcoumarin
-
Rattus norvegicus
pyroglutamyl-Asn-Pro-Ser-TyrNH2
-
Rattus norvegicus
pyroglutamyl-Asn-Pro-Trp-7-amido-4-methylcoumarin
-
Rattus norvegicus
pyroglutamyl-Asn-Pro-Trp-Trp-7-amido-4-methylcoumarin
-
Rattus norvegicus
pyroglutamyl-Asn-Pro-Trp-TyrNH2
-
Rattus norvegicus
pyroglutamyl-Asn-Pro-TrpNH2
-
Rattus norvegicus
pyroglutamyl-Asn-Pro-Tyr-Trp-7-amido-4-methylcoumarin
-
Rattus norvegicus
pyroglutamyl-Asn-Pro-Tyr-Trp-Trp-7-amido-4-methylcoumarin
-
Rattus norvegicus
pyroglutamyl-Asn-Pro-Tyr-Trp-TrpNH2
-
Rattus norvegicus
pyroglutamyl-Asn-Pro-Tyr-TrpNH2
-
Rattus norvegicus
pyroglutamyl-Asn-Pro-TyrNH2
-
Rattus norvegicus
pyroglutamyl-Asn-ProNH2
-
Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Rattus norvegicus
-
hypothalamus
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
pyroglutamyl-Asn(N-benzyl)-ProNH2 + H2O
-
Rattus norvegicus L-pyroglutamate + Asn(N-benzyl)-ProNH2
-
?
pyroglutamyl-Asn(N-methyl)-ProNH2 + H2O
-
Rattus norvegicus L-pyroglutamate + Asn(N-methyl)-ProNH2
-
?
pyroglutamyl-histidyl-prolyl-7-amido-4-methylcoumarin + H2O
-
Rattus norvegicus pyroglutamic acid + histidyl-prolyl-7-amido-4-methylcoumarin
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000001
-
pyroglutamyl-Asn-Pro-Tyr-Trp-Trp-7-amido-4-methylcoumarin
-
Rattus norvegicus
0.000038
-
pyroglutamyl-Asn-Pro-Tyr-Trp-7-amido-4-methylcoumarin
-
Rattus norvegicus
0.000047
-
7-amino-4-methylcoumarin
-
Rattus norvegicus
0.000072
-
pyroglutamyl-Asn-Pro-Trp-Trp-7-amido-4-methylcoumarin
-
Rattus norvegicus
0.000083
-
pyroglutamyl-Asn-Pro-Trp-7-amido-4-methylcoumarin
-
Rattus norvegicus
0.000458
-
pyroglutamyl-Asn-Pro-7-amido-4-methylcoumarin
-
Rattus norvegicus
0.000639
-
pyroglutamyl-Asn-Pro-Tyr-TrpNH2
-
Rattus norvegicus
0.000734
-
pyroglutamyl-Asn-Pro-Tyr-Trp-TrpNH2
-
Rattus norvegicus
0.00084
-
5-aminoindan
-
Rattus norvegicus
0.00085
-
3,5-dimethoxyaniline
-
Rattus norvegicus
0.00097
-
4-(trifluoromethyl)aniline
-
Rattus norvegicus
0.00124
-
1,3-benzodioxol-5-amine
-
Rattus norvegicus
0.00125
-
3-(trifluoromethoxy)aniline
-
Rattus norvegicus
0.00127
-
m-anisidine
-
Rattus norvegicus
0.00163
-
5-amino-2-chloropyridine
-
Rattus norvegicus
0.00167
-
m-phenethidine
-
Rattus norvegicus
0.0019
-
6-amino-3,4-benzocoumarin
-
Rattus norvegicus
0.00254
-
5-amino-2-methoxyphenol
-
Rattus norvegicus
0.00278
-
6-amino-1,3-dihydroisobenzofuran-1-one
-
Rattus norvegicus
0.0028
-
aniline
-
Rattus norvegicus
0.00318
-
3,4-dimethoxyaniline
-
Rattus norvegicus
0.00345
-
4-phenylbutylamine
-
Rattus norvegicus
0.00362
-
6-amino-2-mercaptobenzothiazole
-
Rattus norvegicus
0.00398
-
2-Phenylethylamine
-
Rattus norvegicus
0.00407
-
p-anisidine
-
Rattus norvegicus
0.00498
-
3-phenyl-1-propylamine
-
Rattus norvegicus
0.00517
-
pyroglutamyl-Asn-Pro-TrpNH2
-
Rattus norvegicus
0.00591
-
pyroglutamyl-Asn-Pro-Trp-TyrNH2
-
Rattus norvegicus
0.00742
-
2-hydroxyaniline
-
Rattus norvegicus
0.00811
-
pyroglutamyl-Asn-Pro-Ser-TyrNH2
-
Rattus norvegicus
0.0089
-
4-amino-N-methylphthalamide
-
Rattus norvegicus
0.01014
-
5,6,7,8-tetrahydro-1-naphthylamine
-
Rattus norvegicus
0.0103
-
pyroglutamyl-Asn-Pro-TyrNH2
-
Rattus norvegicus
0.01084
-
methylamine
-
Rattus norvegicus
0.01085
-
5-chloro-2-methoxyaniline
-
Rattus norvegicus
0.01263
-
o-anisidine
-
Rattus norvegicus
0.01281
-
benzylamine
-
Rattus norvegicus
0.01529
-
benzyl alcohol
-
Rattus norvegicus
0.0161
-
pyroglutamyl-Asn-ProNH2
-
Rattus norvegicus
0.0161
-
pyroglutamyl-Asn-ProNH2 37°C, pH 7.5 Rattus norvegicus
0.02187
-
2-Aminobenzyl alcohol
-
Rattus norvegicus
0.08416
-
methyl alcohol
-
Rattus norvegicus
0.0996
-
pyroglutamyl-Asn(N-benzyl)-ProNH2 37°C, pH 7.5 Rattus norvegicus
0.103
-
pyroglutamyl-Asn(N-methyl)-ProNH2 37°C, pH 7.5 Rattus norvegicus
0.115
-
pyroglutamyl-Asn(N-hydroxyl)-ProNH2 37°C, pH 7.5 Rattus norvegicus
0.133
-
pyroglutamyl-Asn(N-phenyl)-ProNH2 37°C, pH 7.5 Rattus norvegicus