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Literature summary for 3.4.17.20 extracted from

  • Polla, M.O.; Tottie, L.; Norden, C.; Linschoten, M.; Muesil, D.; Trumpp-Kallmeyer, S.; Aukrust, I.R.; Ringom, R.; Holm, K.H.; Neset, S.M.; Sandberg, M.; Thurmond, J.; Yu, P.; Hategan, G.; Anderson, H.
    Design and synthesis of potent, orally active, inhibitors of carboxypeptidase U (TAFIa) (2004), Bioorg. Med. Chem., 12, 1151-1175.
    View publication on PubMed
Search for more literature for 3.4.17.20

Inhibitors

Inhibitors Comment Organism Structure
2-(2-amino-pyridin-4-ylmethyl)-3-mercapto-propionic acid reversible inhibition, IC50: 0.0032 mM Homo sapiens
2-(6-amino-pyridin-3-ylmethyl)-2-mercaptomethyl-butyric acid reversible inhibition, IC50: 0.25 mM Homo sapiens
2-mercaptomethyl-3-(6-amino-pyridin-3-yl)-2-fluoro-propionic acid reversible inhibition, IC50: 0.0005 mM Homo sapiens
2-mercaptomethyl-3-(6-amino-pyridin-3-yl)-2-hydroxy-propionic acid reversible inhibition, IC50: 0.0009 mM Homo sapiens
2-mercaptomethyl-3-piperidin-4-yl-propionic acid reversible inhibition, IC50: 0.0032 mM Homo sapiens
2-mercaptomethyl-3-pyrrolidin-3-yl-propionic acid reversible inhibition, IC50: 0.0016 mM Homo sapiens
2-[[(2-carbamimidamidoethyl)sulfanyl]methyl]butanedioic acid reversible inhibition, IC50: 0.27 mM Homo sapiens
3-(2-amino-thiazol-5-yl)-2-mercaptomethyl-propionic acid reversible inhibition, IC50: 0.0013 mM Homo sapiens
3-(6-amino-2-methyl-pyridin-3-yl)-2-mercaptomethyl-propionic acid reversible inhibition, IC50: 0.0063 mM Homo sapiens
3-(6-amino-4-methyl-pyridin-3-yl)-2-mercaptomethyl-propionic acid reversible inhibition, IC50: 0.0079 mM Homo sapiens
3-(6-amino-5-chloro-pyridin-3-yl)-2-mercaptomethyl-propionic acid reversible inhibition, IC50: 0.010 mM Homo sapiens
3-(6-amino-5-hydroxymethyl-pyridin-3-yl)-2-mercaptomethyl-propionic acid reversible inhibition, IC50: 0.013 mM Homo sapiens
3-(6-amino-5-methyl-pyridin-3-yl)-2-(hydroxymethyl)-2-mercaptomethyl-propionic acid reversible inhibition, IC50: 0.083 mM Homo sapiens
3-(6-amino-5-methyl-pyridin-3-yl)-2-mercaptomethyl-2-methyl-propionic acid reversible inhibition, IC50: 0.0016 mM; reversible inhibition, IC50: 0.001 mM Homo sapiens
3-(6-amino-pyridin-3-yl)-2-mercaptomethyl-2-methyl-propionic acid reversible inhibition, IC50: 0.0006 mM Homo sapiens
3-(6-amino-pyridin-3-yl)-2-mercaptomethyl-propionic acid reversible inhibition, IC50: 0.0002 mM Homo sapiens
3-(cis-4-amino-cyclopent-2-yl)-2-mercaptomethyl-propionic acid reversible inhibition, IC50: 0.001 mM Homo sapiens
3-[(2-carbamimidamidoethyl)sulfanyl]-2-(sulfanylmethyl)propanoic acid reversible inhibition, IC50: 0.02 mM Homo sapiens
additional information inhibitor synthesis, overview Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular plasma Homo sapiens
-
-

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+ the enzyme is a metallopeptidase Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
carboxypeptidase U
-
 Homo sapiens
CPU
-
 Homo sapiens
plasma carboxypeptidase U
-
 Homo sapiens
plasma procarboxypeptidase B
-
 Homo sapiens
procarboxypeptidase R
-
 Homo sapiens
TAFIa
-
 Homo sapiens
thrombin activatable fibrinolysis inhibitor
-
 Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0002
-
 reversible inhibition, IC50: 0.0002 mM Homo sapiens 3-(6-amino-pyridin-3-yl)-2-mercaptomethyl-propionic acid
0.0005
-
 reversible inhibition, IC50: 0.0005 mM Homo sapiens 2-mercaptomethyl-3-(6-amino-pyridin-3-yl)-2-fluoro-propionic acid
0.0006
-
 reversible inhibition, IC50: 0.0006 mM Homo sapiens 3-(6-amino-pyridin-3-yl)-2-mercaptomethyl-2-methyl-propionic acid
0.0009
-
 reversible inhibition, IC50: 0.0009 mM Homo sapiens 2-mercaptomethyl-3-(6-amino-pyridin-3-yl)-2-hydroxy-propionic acid
0.001
-
 reversible inhibition, IC50: 0.001 mM Homo sapiens 3-(6-amino-5-methyl-pyridin-3-yl)-2-mercaptomethyl-2-methyl-propionic acid
0.001
-
 reversible inhibition, IC50: 0.001 mM Homo sapiens 3-(cis-4-amino-cyclopent-2-yl)-2-mercaptomethyl-propionic acid
0.0013
-
 reversible inhibition, IC50: 0.0013 mM Homo sapiens 3-(2-amino-thiazol-5-yl)-2-mercaptomethyl-propionic acid
0.0016
-
 reversible inhibition, IC50: 0.0016 mM Homo sapiens 3-(6-amino-5-methyl-pyridin-3-yl)-2-mercaptomethyl-2-methyl-propionic acid
0.0016
-
 reversible inhibition, IC50: 0.0016 mM Homo sapiens 2-mercaptomethyl-3-pyrrolidin-3-yl-propionic acid
0.0032
-
 reversible inhibition, IC50: 0.0032 mM Homo sapiens 2-mercaptomethyl-3-piperidin-4-yl-propionic acid
0.0032
-
 reversible inhibition, IC50: 0.0032 mM Homo sapiens 2-(2-amino-pyridin-4-ylmethyl)-3-mercapto-propionic acid
0.0063
-
 reversible inhibition, IC50: 0.0063 mM Homo sapiens 3-(6-amino-2-methyl-pyridin-3-yl)-2-mercaptomethyl-propionic acid
0.0079
-
 reversible inhibition, IC50: 0.0079 mM Homo sapiens 3-(6-amino-4-methyl-pyridin-3-yl)-2-mercaptomethyl-propionic acid
0.01
-
 reversible inhibition, IC50: 0.010 mM Homo sapiens 3-(6-amino-5-chloro-pyridin-3-yl)-2-mercaptomethyl-propionic acid
0.013
-
 reversible inhibition, IC50: 0.013 mM Homo sapiens 3-(6-amino-5-hydroxymethyl-pyridin-3-yl)-2-mercaptomethyl-propionic acid
0.02
-
 reversible inhibition, IC50: 0.02 mM Homo sapiens 3-[(2-carbamimidamidoethyl)sulfanyl]-2-(sulfanylmethyl)propanoic acid
0.083
-
 reversible inhibition, IC50: 0.083 mM Homo sapiens 3-(6-amino-5-methyl-pyridin-3-yl)-2-(hydroxymethyl)-2-mercaptomethyl-propionic acid
0.25
-
 reversible inhibition, IC50: 0.25 mM Homo sapiens 2-(6-amino-pyridin-3-ylmethyl)-2-mercaptomethyl-butyric acid
0.27
-
 reversible inhibition, IC50: 0.27 mM Homo sapiens 5-bromo-4-chloro-indolyl beta-D-galactopyranosyl-alpha-2,6-N-acetyl-neuraminic acid