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Literature summary for 3.4.21.5 extracted from

  • Turpie, A.G.
    Direct Factor Xa and direct thrombin inhibitors: a clinical trial update (2009), Curr. Opin. Drug Discov. Devel., 12, 497-508.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
factor Xa active factor Xa hydrolyzes and activates prothrombin to thrombin Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
ARH-067637 the prodrug AZD-0837 is bioactively converted into the direct thrombin inhibitor ARH-067637 Homo sapiens
AZD-0837 direct thrombin inhibitor, the prodrug AZD-0837 is bioactively converted into the direct thrombin inhibitor ARH-067637 Homo sapiens
dabigatran specific, competitive and reversible inhibitor of thrombin, dabigatran binds to the active site of thrombin via hydrophobic interactions and can inhibit both free and fibrin-bound thrombin Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
fibrinogen + H2O Homo sapiens
-
fibrin + fibrinopeptide A + fibrinopeptide B
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
fibrinogen + H2O
-
Homo sapiens fibrin + fibrinopeptide A + fibrinopeptide B
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000045
-
dabigatran
-
Homo sapiens