Literature summary for 3.4.21.6 extracted from

Abboud, M.A.; Needle, S.J.; Burns-Kurtis, C.L.; Valocik, R.E.; Koster, P.F.; Amour, A.J.; Chan, C.; Brown, D.; Chaudry, L.; Zhou, P.; Patikis, A.; Patel, C.; Pateman, A.J.; Young, R.J.; Watson, N.S.; Toomey, J.R.
Antithrombotic potential of GW813893: a novel, orally active, active-site directed factor Xa inhibitor (2008), J. Cardiovasc. Pharmacol., 52, 66-71.

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Inhibitors

Inhibitors	Comment	Organism	Structure
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide	i.e. GW813893. More than 90fold selective over all enzymes tested, including thrombin, factor IXa, factor XIa, kallikrein, plasmin and several more	Homo sapiens
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide	i.e. GW813893. Suppresses thrombotic activity correlating with the suppression of plasma-based clotting activity and the inhibition of plasma factor Xa activity. Inhibitor is orally active	Oryctolagus cuniculus
(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide	i.e. GW813893. Suppresses thrombotic activity correlating with the suppression of plasma-based clotting activity and the inhibition of plasma factor Xa activity. Inhibitor is orally active	Rattus norvegicus

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-
Oryctolagus cuniculus	-	-	-
Rattus norvegicus	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
commercial preparation	-	Homo sapiens	-
commercial preparation	-	Rattus norvegicus	-
commercial preparation	-	Oryctolagus cuniculus	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
prothrombin + H2O	-	Homo sapiens	thrombin + ?	-	?

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.000004	-	(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide	factor Xa, pH 7.5, 22°C	Homo sapiens
0.0000097	-	(E)-2-(5-chlorothien-2-yl)-N-[(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide	factor Xa assembled in prothrombinase complex, pH 7.5, 22°C	Homo sapiens

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Release 2023.1 (January 2023)