coagulation factor X | S1: Chymotrypsin | IUPHAR/BPS Guide to PHARMACOLOGY

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
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 5
pKi 10.1 (Ki 8x10-11 M) [5]
betrixaban Hs Inhibition 9.9 pKi 6
pKi 9.9 (Ki 1.17x10-10 M) [6]
Description: Inhibition of human factor Xa.
rivaroxaban Hs Inhibition 9.4 pKi 2
pKi 9.4 (Ki 4x10-10 M) [2]
edoxaban Hs Inhibition 9.3 pKi 3
pKi 9.3 (Ki 5.6x10-10 M) [3]
eribaxaban Hs Inhibition 9.2 pIC50 4
pIC50 9.2 (IC50 5.7x10-10 M) [4]
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Affinity Units Reference
emicizumab Hs Binding 5.7 pKd 1
pKd 5.7 (Kd 1.85x10-6 M) [1]
Description: Determined by surface plasmon resonance analysis.
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

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1. 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]

2. 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]

3. 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]

4. 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]

5. 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]

6. 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 03/01/2018. Accessed on 19/10/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2359.