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TargetA disintegrin and metalloproteinase with thrombospondin motifs 5 (ADAMTS-5)
LigandBDBM50341809
Substrate/Competitorn/a
Meas. Tech.ChEMBL_743598
IC50 8.6±n/a nM
Citation Shiozaki, MMaeda, KMiura, TKotoku, MYamasaki, TMatsuda, IAoki, KYasue, KImai, HUbukata, MSuma, AYokota, MHotta, TTanaka, MHase, YHaas, JFryer, AMLaird, ERLittmann, NMAndrews, SWJosey, JAMimura, TShinozaki, YYoshiuchi, HInaba, T Discovery of (1S,2R,3R)-2,3-dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: novel and highly selective aggrecanase inhibitors. J Med Chem54:2839-63 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
A disintegrin and metalloproteinase with thrombospondin motifs 5 (ADAMTS-5)
Name:A disintegrin and metalloproteinase with thrombospondin motifs 5 (ADAMTS-5)
Synonyms:ADAMTS5 | Aggrecanase-2 | Metalloproteinase with thrombospondin motifs 5 (ADAMTS-5)
Type:Enzyme
Mol. Mass.:101769.09
Organism:Homo sapiens (Human)
Description:Q9UNA0
Residue:930
Sequence:
MLLGWASLLLCAFRLPLAAVGPAATPAQDKAGQPPTAAAAAQPRRRQGEEVQERAEPPGH
PHPLAQRRRSKGLVQNIDQLYSGGGKVGYLVYAGGRRFLLDLERDGSVGIAGFVPAGGGT
SAPWRHRSHCFYRGTVDGSPRSLAVFDLCGGLDGFFAVKHARYTLKPLLRGPWAEEEKGR
VYGDGSARILHVYTREGFSFEALPPRASCETPASTPEAHEHAPAHSNPSGRAALASQLLD
QSALSPAGGSGPQTWWRRRRRSISRARQVELLLVADASMARLYGRGLQHYLLTLASIANR
LYSHASIENHIRLAVVKVVVLGDKDKSLEVSKNAATTLKNFCKWQHQHNQLGDDHEEHYD
AAILFTREDLCGHHSCDTLGMADVGTICSPERSCAVIEDDGLHAAFTVAHEIGHLLGLSH
DDSKFCEETFGSTEDKRLMSSILTSIDASKPWSKCTSATITEFLDDGHGNCLLDLPRKQI
LGPEELPGQTYDATQQCNLTFGPEYSVCPGMDVCARLWCAVVRQGQMVCLTKKLPAVEGT
PCGKGRICLQGKCVDKTKKKYYSTSSHGNWGSWGSWGQCSRSCGGGVQFAYRHCNNPAPR
NNGRYCTGKRAIYRSCSLMPCPPNGKSFRHEQCEAKNGYQSDAKGVKTFVEWVPKYAGVL
PADVCKLTCRAKGTGYYVVFSPKVTDGTECRLYSNSVCVRGKCVRTGCDGIIGSKLQYDK
CGVCGGDNSSCTKIVGTFNKKSKGYTDVVRIPEGATHIKVRQFKAKDQTRFTAYLALKKK
NGEYLINGKYMISTSETIIDINGTVMNYSGWSHRDDFLHGMGYSATKEILIVQILATDPT
KPLDVRYSFFVPKKSTPKVNSVTSHGSNKVGSHTSQPQWVTGPWLACSRTCDTGWHTRTV
QCQDGNRKLAKGCPLSQRPSAFKQCLLKKC
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50341809
NameBDBM50341809
Synonyms:(1S,2R,3R)-1-(7-Fluoro-1,2,3,4-tetrahydropyrido[3'4':3,4]pyrazolo[1,5-a]pyridine-2-sulfonylamino)-2-methyl-3-phenylcyclopropanecarboxylicAcid | CHEMBL1767011
TypeSmall organic molecule
Emp. Form.C21H21FN4O4S
Mol. Mass.444.479
SMILESC[C@@H]1[C@H](c2ccccc2)[C@]1(NS(=O)(=O)N1CCc2c(C1)nn1cc(F)ccc21)C(O)=O |r|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
n/a