Reaction Details Report a problem with these data
Target
A disintegrin and metalloproteinase with thrombospondin motifs 5 [262-930,L692P]
Ligand
BDBM28309
Substrate
WAAG-3R
Meas. Tech.
ADAMTS-5 Enzyme Inhibition Assay
pH
7.5±n/a
Temperature
310.15±n/a K
Comments
46% inhibition @ 10 uM.
Citation
 Shiozaki, M; Maeda, K; Miura, T; Ogoshi, Y; Haas, J; Fryer, AM; Laird, ER; Littmann, NM; Andrews, SW; Josey, JA; Mimura, T; Shinozaki, Y; Yoshiuchi, H; Inaba, T Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (Aggrecanase-2) inhibitors. Bioorg Med Chem Lett 19:1575-80 (2009) [PubMed]  Article 
Target
Name:
A disintegrin and metalloproteinase with thrombospondin motifs 5 [262-930,L692P]
Synonyms:
A disintegrin and metalloproteinase with thrombospondin motifs 5 | ADAM-TS 11 | ADAMTS-5 (Aggrecanase-2) | ADAMTS11 | ADAMTS5 | ADMP-2 | ADMP2 | ATS5_HUMAN
Type:
Metalloprotease
Mol. Mass.:
73728.14
Organism:
Homo sapiens (Human)
Description:
Q9UNA0[262-930,L692P]
Residue:
669
Sequence:
SISRARQVELLLVADASMARLYGRGLQHYLLTLASIANRLYSHASIENHIRLAVVKVVVLGDKDKSLEVSKNAATTLKNFCKWQHQHNQLGDDHEEHYDAAILFTREDLCGHHSCDTLGMADVGTICSPERSCAVIEDDGLHAAFTVAHEIGHLLGLSHDDSKFCEETFGSTEDKRLMSSILTSIDASKPWSKCTSATITEFLDDGHGNCLLDLPRKQILGPEELPGQTYDATQQCNLTFGPEYSVCPGMDVCARLWCAVVRQGQMVCLTKKLPAVEGTPCGKGRICLQGKCVDKTKKKYYSTSSHGNWGSWGSWGQCSRSCGGGVQFAYRHCNNPAPRNNGRYCTGKRAIYRSCSLMPCPPNGKSFRHEQCEAKNGYQSDAKGVKTFVEWVPKYAGVLPADVCKLTCRAKGTGYYVVFSPKVTDGTECRPYSNSVCVRGKCVRTGCDGIIGSKLQYDKCGVCGGDNSSCTKIVGTFNKKSKGYTDVVRIPEGATHIKVRQFKAKDQTRFTAYLALKKKNGEYLINGKYMISTSETIIDINGTVMNYSGWSHRDDFLHGMGYSATKEILIVQILATDPTKPLDVRYSFFVPKKSTPKVNSVTSHGSNKVGSHTSQPQWVTGPWLACSRTCDTGWHTRTVQCQDGNRKLAKGCPLSQRPSAFKQCLLKKC
  
Inhibitor
Name:
BDBM28309
Synonyms:
(2R)-2-{[4-(4-chlorophenyl)benzene](cyclopropylmethyl)sulfonamido}-3-phenylpropanoic acid | sulfonylamino-alkanecarboxylate, 4
Type:
Small organic molecule
Emp. Form.:
C25H24ClNO4S
Mol. Mass.:
469.98
SMILES:
OC(=O)[C@@H](Cc1ccccc1)N(CC1CC1)S(=O)(=O)c1ccc(cc1)-c1ccc(Cl)cc1 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
WAAG-3R
Synonyms:
n/a
Type:
Fluorescent peptide
Mol. Mass.:
1954.08
Organism:
n/a
Description:
n/a
Residue:
19
Sequence:
ATEGEARGSVIDAPDNPKK