coagulation factor X

Target id: 2359

Nomenclature: coagulation factor X

Family: S1: Chymotrypsin

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for coagulation factor X in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 488 13q34 F10 coagulation factor X
Mouse - 493 8 A1.1 F10 coagulation factor X
Rat - 482 16q12.5 F10 coagulation factor X
Previous and Unofficial Names
Cf10 | coagulation factor 10 | fX | stuart factor
Database Links
Specialist databases
MEROPS S01.216 (Hs)
Other databases
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.21.6

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
apixaban Hs Inhibition 10.1 pKi 4
pKi 10.1 (Ki 8x10-11 M) [4]
betrixaban Hs Inhibition 9.9 pKi 5
pKi 9.9 (Ki 1.17x10-10 M) [5]
Description: Inhibition of human factor Xa.
rivaroxaban Hs Inhibition 9.4 pKi 1
pKi 9.4 (Ki 4x10-10 M) [1]
edoxaban Hs Inhibition 9.3 pKi 2
pKi 9.3 (Ki 5.6x10-10 M) [2]
eribaxaban Hs Inhibition 9.2 pIC50 3
pIC50 9.2 (IC50 5.7x10-10 M) [3]
Clinically-Relevant Mutations and Pathophysiology
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

Show »

1. Perzborn E, Roehrig S, Straub A, Kubitza D, Mueck W, Laux V. (2010) Rivaroxaban: a new oral factor Xa inhibitor. Arterioscler. Thromb. Vasc. Biol.30 (3): 376-81. [PMID:20139357]

2. 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]

3. 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]

4. 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]

5. 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 26/06/2017. Accessed on 24/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2359.