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coagulation factor X

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Target not currently curated in GtoImmuPdb

Target id: 2359

Nomenclature: coagulation factor X

Family: S1: Chymotrypsin, Blood coagulation components

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 488 13q34 F10 coagulation factor X
Mouse - 481 8 5.73 cM F10 coagulation factor X
Rat - 482 16q12.5 F10 coagulation factor X
Previous and Unofficial Names Click here for help
Cf10 | coagulation factor 10 | fX | stuart factor
Database Links Click here for help
Specialist databases
MEROPS S01.216 (Hs)
Other databases
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of Human Coagulation Factor XA Complexed with FXV673
PDB Id:  1KSN
Ligand:  otamixaban
Resolution:  2.1Å
Species:  Human
References:  2
Enzyme Reaction Click here for help
EC Number: 3.4.21.6

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
apixaban Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inhibition 10.1 pKi 11
pKi 10.1 (Ki 8x10-11 M) [11]
betrixaban Small molecule or natural product Approved drug Primary target of this compound Hs Inhibition 9.9 pKi 12
pKi 9.9 (Ki 1.17x10-10 M) [12]
Description: Inhibition of human factor Xa.
rivaroxaban Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inhibition 9.4 pKi 7
pKi 9.4 (Ki 4x10-10 M) [7]
otamixaban Small molecule or natural product Ligand has a PDB structure Hs Inhibition 9.4 pKi 2
pKi 9.4 (Ki 4x10-10 M) [2]
Description: Inhibition of Fxa
zifaxaban Small molecule or natural product Primary target of this compound Hs Inhibition 9.3 pKi 9
pKi 9.3 (Ki 5x10-10 M) [9]
Description: Inhibition of factor Xa in a chromogenic enzymatic assay.
edoxaban Small molecule or natural product Approved drug Primary target of this compound Hs Inhibition 9.3 pKi 1,8
pKi 9.3 (Ki 5.6x10-10 M) [1,8]
JTV-803 Small molecule or natural product Hs Inhibition 7.7 pKi 4-5
pKi 7.7 (Ki 1.9x10-8 M) Antithrombotic effect occurs via the inhibition of the activated form, Xa [4-5]
Description: Dissociation constant for Factor Xa
DX-9065a Small molecule or natural product Ligand has a PDB structure Hs Inhibition 7.4 pKi 3,5
pKi 7.4 (Ki 4.1x10-8 M) Antithrombotic effect occurs via the inhibition of the activated form, Xa [3,5]
Description: Dissociation constant for FXa
eribaxaban Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 9.2 pIC50 10
pIC50 9.2 (IC50 5.7x10-10 M) [10]
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
emicizumab Peptide Approved drug Click here for species-specific activity table Hs Binding 5.7 pKd 6
pKd 5.7 (Kd 1.85x10-6 M) [6]
Description: Determined by surface plasmon resonance analysis.
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Factor X deficiency
Disease Ontology: DOID:2222
OMIM: 227600
Orphanet: ORPHA328
General Comments
A plasma-derived blood coagulation factor X concentrate called Coagadex® has been approved by both the European Medicines Agency and the US FDA as the first treatment for hereditary factor X deficiency. Coagadex® can be used to treat bleeding episodes and to manage perioperative care in adults and children >12 years old.

References

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1. Furugohri T, Isobe K, Honda Y, Kamisato-Matsumoto C, Sugiyama N, Nagahara T, Morishima Y, Shibano T. (2008) DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost, 6 (9): 1542-9. [PMID:18624979]

2. Guertin KR, Gardner CJ, Klein SI, Zulli AL, Czekaj M, Gong Y, Spada AP, Cheney DL, Maignan S, Guilloteau JP et al.. (2002) 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. Bioorg Med Chem Lett, 12 (12): 1671-4. [PMID:12039587]

3. Hara T, Yokoyama A, Ishihara H, Yokoyama Y, Nagahara T, Iwamoto M. (1994) DX-9065a, a new synthetic, potent anticoagulant and selective inhibitor for factor Xa. Thromb Haemost, 71 (3): 314-9. [PMID:8029795]

4. Hayashi M, Hamada A, Okaya Y, Wakitani K, Aisaka K. (2001) Inhibitory effect of JTV-803, a new cyclic guanidine derivative, on factor Xa in vitro and in vivo. Eur J Pharmacol, 428 (2): 163-8. [PMID:11675032]

5. Ieko M, Tarumi T, Takeda M, Naito S, Nakabayashi T, Koike T. (2004) Synthetic selective inhibitors of coagulation factor Xa strongly inhibit thrombin generation without affecting initial thrombin forming time necessary for platelet activation in hemostasis. J Thromb Haemost, 2 (4): 612-8. [PMID:15102016]

6. Kitazawa T, Esaki K, Tachibana T, Ishii S, Soeda T, Muto A, Kawabe Y, Igawa T, Tsunoda H, Nogami K et al.. (2017) 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. Thromb Haemost, 117 (7): 1348-1357. [PMID:28451690]

7. Perzborn E, Strassburger J, Wilmen A, Pohlmann J, Roehrig S, Schlemmer KH, Straub A. (2005) In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939--an oral, direct Factor Xa inhibitor. J Thromb Haemost, 3 (3): 514-21. [PMID:15748242]

8. Pinto DJ, Smallheer JM, Cheney DL, Knabb RM, Wexler RR. (2010) Factor Xa inhibitors: next-generation antithrombotic agents. J Med Chem, 53 (17): 6243-74. [PMID:20503967]

9. Qiu X, Zhou J, Wang W, Zhao Z, Tang L, Sun S. (2019) Effect of a new inhibitor of factor Xa zifaxaban, on thrombosis in the inferior vena cava in rabbits. J Thromb Thrombolysis, 47 (1): 80-86. [PMID:30298304]

10. Van Huis CA, Casimiro-Garcia A, Bigge CF, Cody WL, Dudley DA, Filipski KJ, Heemstra RJ, Kohrt JT, Leadley Jr RJ, Narasimhan LS et al.. (2009) Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action. Bioorg Med Chem, 17 (6): 2501-11. [PMID:19231206]

11. Wong PC, Crain EJ, Xin B, Wexler RR, Lam PY, Pinto DJ, Luettgen JM, Knabb RM. (2008) Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies. J Thromb Haemost, 6 (5): 820-9. [PMID:18315548]

12. Zhang P, Huang W, Wang L, Bao L, Jia ZJ, Bauer SM, Goldman EA, Probst GD, Song Y, Su T et al.. (2009) 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. Bioorg Med Chem Lett, 19 (8): 2179-85. [PMID:19297154]

How to cite this page

S1: Chymotrypsin: coagulation factor X. Last modified on 18/01/2021. Accessed on 23/04/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2359.