Target family: S1: Chymotrypsin (type: enzyme)
Target: coagulation factor X

Ligand: zifaxaban (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.300000190734863 pKi
Reference (Journal): Effect of a new inhibitor of factor Xa zifaxaban, on thrombosis in the inferior vena cava in rabbits.
Published in: J Thromb Thrombolysis

Ligand: rivaroxaban (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2008), FDA (2011)
Primary target: yes
Median affinity: 9.399999618530273 pKi
Reference (Journal): In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939--an oral, direct Factor Xa inhibitor.
Published in: J Thromb Haemost

Ligand: otamixaban (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pKi
Reference (Journal): Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.
Published in: Bioorg Med Chem Lett

Ligand: JTV-803 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.71999979019165 pKi
Reference (Journal): Synthetic selective inhibitors of coagulation factor Xa strongly inhibit thrombin generation without affecting initial thrombin forming time necessary for platelet activation in hemostasis.
Published in: J Thromb Haemost

Ligand: JTV-803 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.71999979019165 pKi
Reference (Journal): Inhibitory effect of JTV-803, a new cyclic guanidine derivative, on factor Xa in vitro and in vivo.
Published in: Eur J Pharmacol

Ligand: eribaxaban (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.239999771118164 pIC50
Reference (Journal): Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action.
Published in: Bioorg Med Chem

Ligand: emicizumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA (2017), EMA (2018)
Primary target: no
Median affinity: 5.730000019073486 pKd
Reference (Journal): Factor VIIIa-mimetic cofactor activity of a bispecific antibody to factors IX/IXa and X/Xa, emicizumab, depends on its ability to bridge the antigens.
Published in: Thromb Haemost

Ligand: edoxaban (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2015)
Primary target: yes
Median affinity: 9.25 pKi
Reference (Journal): DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles.
Published in: J Thromb Haemost

Ligand: edoxaban (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2015)
Primary target: yes
Median affinity: 9.25 pKi
Reference (Journal): Factor Xa inhibitors: next-generation antithrombotic agents.
Published in: J Med Chem

Ligand: DX-9065a (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.389999866485596 pKi
Reference (Journal): Synthetic selective inhibitors of coagulation factor Xa strongly inhibit thrombin generation without affecting initial thrombin forming time necessary for platelet activation in hemostasis.
Published in: J Thromb Haemost

Ligand: DX-9065a (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.389999866485596 pKi
Reference (Journal): DX-9065a, a new synthetic, potent anticoagulant and selective inhibitor for factor Xa.
Published in: Thromb Haemost

Ligand: betrixaban (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2017)
Primary target: yes
Median affinity: 9.930000305175781 pKi
Reference (Journal): Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.
Published in: Bioorg Med Chem Lett

Ligand: apixaban (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2011), FDA (2012)
Primary target: yes
Median affinity: 10.100000381469727 pKi
Reference (Journal): Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies.
Published in: J Thromb Haemost