ADAM10

Target id: 1658

Nomenclature: ADAM10

Family: M12: Astacin/Adamalysin

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

   GtoImmuPdb view: OFF :     Currently no data for ADAM10 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 748 15q2 ADAM10 ADAM metallopeptidase domain 10
Mouse - 749 9 D Adam10 a disintegrin and metallopeptidase domain 10
Rat - 544 8q24 Adam10 ADAM metallopeptidase domain 10
Previous and Unofficial Names
Kuzbanian protein homolog | Mammalian disintegrin-metalloprotease | CD156c | kuz | MADM | a disintegrin and metallopeptidase domain 10 | ADAM metallopeptidase domain 10 | HER-2 sheddase
Database Links
Specialist databases
MEROPS M12.210 (Hs)
Other databases
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.24.81

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
ilomastat Hs Inhibition 8.1 pIC50 2
pIC50 8.1 (IC50 8.1x10-9 M) [2]
Description: Measured in an in vitro assay.
compound 25 [PMID: 18068976] Hs Inhibition 7.8 pIC50 1
pIC50 7.8 (IC50 1.6x10-8 M) [1]
Clinically-Relevant Mutations and Pathophysiology
Disease:  Reticulate acropigmentation of Kitamura; RAK
OMIM: 615537
Orphanet: ORPHA178307

References

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1. Burns DM, He C, Li Y, Scherle P, Liu X, Marando CA, Covington MB, Yang G, Pan M, Turner S et al.. (2008) Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations. Bioorg. Med. Chem. Lett.18 (2): 560-4. [PMID:18068976]

2. Oh M, Im I, Lee YJ, Kim YH, Yoon JH, Park HG, Higashiyama S, Kim YC, Park WJ. (2004) Structure-based virtual screening and biological evaluation of potent and selective ADAM12 inhibitors. Bioorg. Med. Chem. Lett.14 (24): 6071-4. [PMID:15546732]

How to cite this page

M12: Astacin/Adamalysin: ADAM10. Last modified on 29/07/2015. Accessed on 23/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1658.