calpain 1 | C2: Calpain | IUPHAR/BPS Guide to PHARMACOLOGY

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calpain 1

Target not currently curated in GtoImmuPdb

Target id: 2336

Nomenclature: calpain 1

Family: C2: Calpain

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Contents:

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 714 11q13 CAPN1 calpain 1
Mouse - 713 19 A Capn1 calpain 1
Rat - 713 1q43 Capn1 calpain 1
Previous and Unofficial Names
calcium-activated neutral proteinase 1 | calpain mu-type | calpain-1 catalytic subunit | CANP | CANP 1 | Capa1 | micromolar-calpain | mu-calpain | muCANP | calpain 1, (mu/I) large subunit
Database Links
Specialist databases
MEROPS C02.001 (Hs)
Other databases
BRENDA 3.4.22.52
ChEMBL Target CHEMBL3891 (Hs), CHEMBL3747 (Rn)
Ensembl Gene ENSG00000014216 (Hs), ENSMUSG00000024942 (Mm), ENSRNOG00000020935 (Rn)
Entrez Gene 823 (Hs), 12333 (Mm), 29153 (Rn)
Human Protein Atlas ENSG00000014216 (Hs)
KEGG Enzyme 3.4.22.52
KEGG Gene hsa:823 (Hs), mmu:12333 (Mm), rno:29153 (Rn)
OMIM 114220 (Hs)
Pharos P07384 (Hs)
RefSeq Nucleotide NM_001198868 (Hs), NM_001198869 (Hs), NM_005186 (Hs), NM_001110504 (Mm), NM_007600 (Mm), NM_019152 (Rn)
RefSeq Protein NP_001185798 (Hs), NP_005177 (Hs), NP_001185797 (Hs), NP_031626 (Mm), NP_001103974 (Mm), NP_062025 (Rn)
UniProtKB P07384 (Hs), O35350 (Mm), P97571 (Rn)
Wikipedia CAPN1 (Hs)
Enzyme Reaction
EC Number: 3.4.22.52

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 Value Parameter Reference
compound 4b [PMID: 20690647] Pig Inhibition 7.6 pKi 2
⤷ pKi 7.6 (Ki 2.3x10-8 M) [2]
mercaptoacrylate inhibitor of calpain 1 Pig Inhibition 8.2 pIC50 1
⤷ pIC50 8.2 (IC50 6x10-9 M) [1]
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 2 GO processes
GO:0043312 neutrophil degranulation TAS
GO:1903238 positive regulation of leukocyte tethering or rolling ISO
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0043312 neutrophil degranulation TAS
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:1903238 positive regulation of leukocyte tethering or rolling ISO
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:1903238 positive regulation of leukocyte tethering or rolling ISO

References

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1. Adams SE, Parr C, Miller DJ, Allemann RK, Hallett MB. (2012) Potent inhibition of Ca2+-dependent activation of calpain-1 by novel mercaptoacrylates. Medchemcomm, 3: 566 (Concise Article). DOI: 10.1039/C2MD00280A

2. Ovat A, Li ZZ, Hampton CY, Asress SA, Fernández FM, Glass JD, Powers JC. (2010) Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. J. Med. Chem., 53 (17): 6326-36. [PMID:20690647]

How to cite this page

C2: Calpain: calpain 1. Last modified on 29/01/2016. Accessed on 10/08/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2336.