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kallikrein B1

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Target not currently curated in GtoImmuPdb

Target id: 2379

Nomenclature: kallikrein B1

Family: S1: Chymotrypsin

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 638 4q35.2 KLKB1 kallikrein B1
Mouse - 638 8 25.17 cM Klkb1 kallikrein B, plasma 1
Rat - 638 16q11 Klkb1 kallikrein B1
Previous and Unofficial Names Click here for help
antigen, prostate specific | APS | Kal3 | kallikrein 3, plasma | Kalp1 | KALP15 | kininogenin | Klk3 | plasma kallikrein | kallikrein B, plasma (Fletcher factor) 1 | kallikrein B, plasma 1 | kallikrein B
Database Links Click here for help
Specialist databases
MEROPS S01.212 (Hs)
Other databases
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 3.4.21.34

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
compound 11 [PMID: 16413183] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.3 pKi 3
pKi 9.3 (Ki 5x10-10 M) [3]
berotralstat Small molecule or natural product Approved drug Hs Inhibition 7.3 – 10.0 pKi 1
pKi 7.3 – 10.0 (Ki 5x10-8 – 1x10-10 M) [1]
Description: Ki determined in a biochemical assay, using example 52h which has no specified stereochemistry.
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
lanadelumab Peptide Approved drug Primary target of this compound Hs Binding 10.1 pIC50 2
pIC50 10.1 (IC50 9x10-11 M) [2]
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 2 GO processes
GO:0002542 Factor XII activation TAS
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GO:0006954 inflammatory response IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:0002542 Factor XII activation TAS
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Prekallikrein deficiency
Synonyms: Fletcher factor deficiency
OMIM: 612423
Orphanet: ORPHA749

References

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1. Kotian PL, Babu YS, Wu M, Chintareddy VR, Kumar VS, Zhang W. (2015) Human plasma kallikrein inhibitors. Patent number: WO2015134998A1. Assignee: Biocryst Pharmaceuticals. Priority date: 07/03/2014. Publication date: 11/09/2015.

2. Sexton DJ, Viswanathan M. (2014) Plasma kallikrein binding proteins. Patent number: US8816055 B2. Assignee: Dyax Corp.. Priority date: 06/01/2011. Publication date: 26/08/2014.

3. Young WB, Rai R, Shrader WD, Burgess-Henry J, Hu H, Elrod KC, Sprengeler PA, Katz BA, Sukbuntherng J, Mordenti J. (2006) Small molecule inhibitors of plasma kallikrein. Bioorg Med Chem Lett, 16 (7): 2034-6. [PMID:16413183]

How to cite this page

S1: Chymotrypsin: kallikrein B1. Last modified on 08/12/2020. Accessed on 20/04/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2379.