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Literature summary for 3.4.14.10 extracted from

  • Ganellin, C.R.; Bishop, P.B.; Bambal, R.B.; Chan, S.M.; Leblond, B.; Moore, A.N.; Zhao, L.; Bourgeat, P.; Rose, C.; Vargas, F.; Schwartz, J.C.
    Inhibitors of tripeptidyl peptidase II. 3. Derivation of butabindide by successive structure optimizations leading to a potential general approach to designing exopeptidase inhibitors (2005), J. Med. Chem., 48, 7333-7342.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2S)-aminobutyryl-(4S)-fluoro-L-proline n-butylamide
-
Rattus norvegicus
(2S)-aminobutyryl-4-cis-benzyl-L-proline n-butylamide
-
Rattus norvegicus
aminobutyryl-L-Pro-n-butylamide
-
Rattus norvegicus
aminobutyryl-Phe-n-butylamide
-
Rattus norvegicus
aminobutyryl-Pro-n-butylamide
-
Rattus norvegicus
azetepane
-
Rattus norvegicus
azetidine
-
Rattus norvegicus
butabindide reversible Rattus norvegicus
pipecolinic acid
-
Rattus norvegicus
piperidine
-
Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane cerebral Rattus norvegicus 16020
-

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
cerebral cortex
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ala-Ala-Phe-7-amido-4-methylcoumarin + H2O
-
Rattus norvegicus Ala-Ala-Phe + 7-amino-4-methylcoumarin
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000007
-
butabindide
-
Rattus norvegicus
0.00008
-
aminobutyryl-Pro-n-butylamide
-
Rattus norvegicus
0.00014
-
(2S)-aminobutyryl-4-cis-benzyl-L-proline n-butylamide
-
Rattus norvegicus
0.00032
-
(2S)-aminobutyryl-(4S)-fluoro-L-proline n-butylamide
-
Rattus norvegicus
0.006
-
azetepane
-
Rattus norvegicus
0.0094
-
aminobutyryl-Phe-n-butylamide
-
Rattus norvegicus
0.012
-
piperidine
-
Rattus norvegicus
0.02
-
azetidine
-
Rattus norvegicus
0.035
-
pipecolinic acid
-
Rattus norvegicus