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Literature summary for 3.4.21.6 extracted from

  • Gould, W.R.; Cladera, E.; Harris, M.S.; Zhang, E.; Narasimhan, L.; Thorn, J.M.; Leadley, R.J.
    Co-crystal structure and inhibition of factor Xa by PD0313052 identifies structurally stabilized active site residues of factor Xa and prothrombinase (2005), Biochemistry, 44, 9280-9289.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
structure of factor Xa in complex with PD0313052 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
DX-9065a competitive, factor Xa Homo sapiens
PD0313052 slow, tight-binding mechanism, factor Xa; slow, tight-binding mechanism, prothrombinase Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
FS-2765 + H2O FS-2765 is a fluorescent peptidyl substrate, factor Xa Homo sapiens ?
-
?
FS-2765 + H2O FS-2765 is a fluorescent peptidyl substrate, prothrombinase Homo sapiens ?
-
?
prothrombin + H2O prothrombinase Homo sapiens thrombin + ?
-
?

Synonyms

Synonyms Comment Organism
factor Xa
-
Homo sapiens
prothrombinase complex consisting of factor Xa and Va Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000017
-
PD0313052 prothrombinase, substrate: FS-2765 Homo sapiens
0.00000025
-
PD0313052 prothrombinase, substrate: prothrombin Homo sapiens
0.00000029
-
PD0313052 substrate: FS-2765, factor Xa Homo sapiens
0.0000357
-
DX-9065a substrate: FS-2765, factor Xa Homo sapiens