Reaction Details Report a problem with these data
Target
A disintegrin and metalloproteinase with thrombospondin motifs 5 [262-930,L692P]
Ligand
BDBM24016
Substrate
BDBM23993
Meas. Tech.
ADAMTS-5 Inhibition Assay
IC50
2600±n/a nM
Citation
 Bursavich, MG; Gilbert, AM; Lombardi, S; Georgiadis, KE; Reifenberg, E; Flannery, CR; Morris, EA 5'-Phenyl-3'H-spiro[indoline-3,2'-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (aggrecanase-2). Bioorg Med Chem Lett 17:5630-3 (2007) [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:
BDBM24016
Synonyms:
1,5'-diphenyl-1,2-dihydro-3'H-spiro[indole-3,2'-[1,3,4]thiadiazole]-2-one | thiadiazole derivative, 28
Type:
Small organic molecule
Emp. Form.:
C21H15N3OS
Mol. Mass.:
357.428
SMILES:
O=C1N(c2ccccc2C11NN=C(S1)c1ccccc1)c1ccccc1 |c:13|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM23993
Synonyms:
Peptide contains an aggrecanase cleavage site | QF-peptide
Type:
Fluorescent peptide substrate
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
n/a
Structure: