Details of the Target

General Information of Target

Target ID LDTP13649
Target Name A disintegrin and metalloproteinase with thrombospondin motifs 5 (ADAMTS5)
Gene Name ADAMTS5
Gene ID 11096
Synonyms
ADAMTS11; ADMP2; A disintegrin and metalloproteinase with thrombospondin motifs 5; ADAM-TS 5; ADAM-TS5; ADAMTS-5; EC 3.4.24.-; A disintegrin and metalloproteinase with thrombospondin motifs 11; ADAM-TS 11; ADAMTS-11; ADMP-2; Aggrecanase-2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGIRGMLRAAVILLLIRTWLAEGNYPSPIPKFHFEFSSAVPEVVLNLFNCKNCANEAVVQ
KILDRVLSRYDVRLRPNFGGAPVPVRISIYVTSIEQISEMNMDYTITMFFHQTWKDSRLA
YYETTLNLTLDYRMHEKLWVPDCYFLNSKDAFVHDVTVENRVFQLHPDGTVRYGIRLTTT
AACSLDLHKFPMDKQACNLVVESYGYTVEDIILFWDDNGNAIHMTEELHIPQFTFLGRTI
TSKEVYFYTGSYIRLILKFQVQREVNSYLVQVYWPTVLTTITSWISFWMNYDSSAARVTI
GLTSMLILTTIDSHLRDKLPNISCIKAIDIYILVCLFFVFLSLLEYVYINYLFYSRGPRR
QPRRHRRPRRVIARYRYQQVVVGNVQDGLINVEDGVSSLPITPAQAPLASPESLGSLTST
SEQAQLATSESLSPLTSLSGQAPLATGESLSDLPSTSEQARHSYGVRFNGFQADDSIIPT
EIRNRVEAHGHGVTHDHEDSNESLSSDERHGHGPSGKPMLHHGEKGVQEAGWDLDDNNDK
SDCLAIKEQFKCDTNSTWGLNDDELMAHGQEKDSSSESEDSCPPSPGCSFTEGFSFDLFN
PDYVPKVDKWSRFLFPLAFGLFNIVYWVYHMY
Target Type
Clinical trial
Target Bioclass
Enzyme
Subcellular location
Secreted, extracellular space, extracellular matrix
Function
Metalloproteinase that plays an important role in connective tissue organization, development, inflammation and cell migration. Extracellular matrix (ECM) degrading enzyme that show proteolytic activity toward the hyalectan group of chondroitin sulfate proteoglycans (CSPGs) including ACAN, VCAN, BCAN and NCAN. Cleavage within the hyalectans occurs at Glu-Xaa recognition motifs. Plays a role in embryonic development, including limb and cardiac morphogenesis, and skeletal muscle development through its VCAN remodeling properties. Cleaves VCAN in the pericellular matrix surrounding myoblasts, facilitating myoblast contact and fusion which is required for skeletal muscle development and regeneration. Participates in development of brown adipose tissue and browning of white adipose tissue. Plays an important role for T-lymphocyte migration from draining lymph nodes following viral infection.
TTD ID
T98896
Uniprot ID
Q9UNA0
DrugMap ID
TTXSU2Y
Ensemble ID
ENST00000284987.6
HGNC ID
HGNC:221
ChEMBL ID
CHEMBL2285

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C209(1.54); C594(1.77)  LDD3401  [1]
N1
 Probe Info  		C902(0.00); N906(0.00); Q903(0.00)  LDD0245  [2]
IA-alkyne
 Probe Info  		N.A.  LDD0165  [3]
IPM
 Probe Info  		N.A.  LDD0147  [4]
TFBX
 Probe Info  		N.A.  LDD0148  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 CAL-78 C594(2.82)  LDD2291  [1]
 LDCM0023  KB03 CAL-78 C594(3.88)  LDD2708  [1]
 LDCM0024  KB05 RD C209(1.54); C594(1.77)  LDD3401  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Agg-523 . D0C5NP
Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Batimastat Small molecular drug DB03880
Pmid21536437c15c Small molecular drug D0FD9M
(2r)-n~4~-hydroxy-2-(3-hydroxybenzyl)-n~1~-[(1s2r)-2-hydroxy-23-dihydro-1h-inden-1-yl]Butanediamide . DB06837
Cr-5259 . D0MI1N
N-hydroxy-4-({4-[4-(Trifluoromethyl)Phenoxy]Phenyl}Sulfonyl)Tetrahydro-2h-pyran-4-carboxamide . DB06945
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Sc-44463 Small molecular drug D0Y1XT

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
3 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
4 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255