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Literature summary for 3.4.21.6 extracted from

  • Noguchi, T.; Tanaka, N.; Nishimata, T.; Goto, R.; Hayakawa, M.; Sugidachi, A.; Ogawa, T.; Niitsu, Y.; Asai, F.; Ishizuka, T.; Fujimoto, K.
    Discovery of R-142086 as a factor Xa (FXa) inhibitor: syntheses and structure-activity relationships of cinnamyl derivatives (2009), Chem. Pharm. Bull., 57, 22-33.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(N-[4-[1-(acetimidoyl)-piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid i.e. R-142086. Exhibits potent anti-factor Xa activity and anticoagulant activity when administered orally Canis lupus familiaris
(N-[4-[1-(acetimidoyl)-piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid potent anticoagulant activity, no mutagenic potential and high selectivity for factor Xa over trypsin Homo sapiens

Organism

Organism UniProt Comment Textmining
Canis lupus familiaris
-
-
-
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
Homo sapiens
-
commercial preparation
-
Canis lupus familiaris
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000012
-
37°C, pH 8.4 Homo sapiens (N-[4-[1-(acetimidoyl)-piperidin-4-yloxy]-3-carbamoylphenyl]-N-[(Z)-3-(3-amidinophenyl)-2-fluoro-2-propenyl]sulfamoyl)acetic acid