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Target
A disintegrin and metalloproteinase with thrombospondin motifs 5
Ligand
BDBM379697
Substrate
n/a
Meas. Tech.
ChEMBL_2125867 (CHEMBL4835212)
IC50
<1500±n/a nM
Citation
 Brebion, F; Gosmini, R; Deprez, P; Varin, M; Peixoto, C; Alvey, L; Jary, H; Bienvenu, N; Triballeau, N; Blanque, R; Cottereaux, C; Christophe, T; Vandervoort, N; Mollat, P; Touitou, R; Leonard, P; De Ceuninck, F; Botez, I; Monjardet, A; van der Aar, E; Amantini, D Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis. J Med Chem 64:2937-2952 (2021) [PubMed]  Article 
Target
Name:
A disintegrin and metalloproteinase with thrombospondin motifs 5
Synonyms:
3.4.24.- | A disintegrin and metalloproteinase with thrombospondin motifs 5 | ADAM-TS 5 | ADAM-TS5 | ADAMTS-5 | ADMP-2 | ATS5_MOUSE | Adamts5 | Aggrecanase-2 | Implantin
Type:
PROTEIN
Mol. Mass.:
101888.97
Organism:
Mus musculus
Description:
ChEMBL_120487
Residue:
930
Sequence:
MRLEWAPLLLLLLLLSASCLSLAADSPAAAPAQDKTRQPQAAAAAAEPDQPQGEETRERGHLQPLAGQRRSGGLVQNIDQLYSGGGKVGYLVYAGGRRFLLDLERDDTVGAAGSIVTAGGGLSASSGHRGHCFYRGTVDGSPRSLAVFDLCGGLDGFFAVKHARYTLKPLLRGSWAEYERIYGDGSSRILHVYNREGFSFEALPPRASCETPASPSGPQESPSVHSRSRRRSALAPQLLDHSAFSPSGNAGPQTWWRRRRRSISRARQVELLLVADSSMARMYGRGLQHYLLTLASIANRLYSHASIENHIRLAVVKVVVLTDKDTSLEVSKNAATTLKNFCKWQHQHNQLGDDHEEHYDAAILFTREDLCGHHSCDTLGMADVGTICSPERSCAVIEDDGLHAAFTVAHEIGHLLGLSHDDSKFCEENFGTTEDKRLMSSILTSIDASKPWSKCTSATITEFLDDGHGNCLLDLPRKQILGPEELPGQTYDATQQCNLTFGPEYSVCPGMDVCARLWCAVVRQGQMVCLTKKLPAVEGTPCGKGRVCLQGKCVDKTKKKYYSTSSHGNWGSWGPWGQCSRSCGGGVQFAYRHCNNPAPRNSGRYCTGKRAIYRSCSVTPCPPNGKSFRHEQCEAKNGYQSDAKGVKTFVEWVPKYAGVLPADVCKLTCRAKGTGYYVVFSPKVTDGTECRPYSNSVCVRGRCVRTGCDGIIGSKLQYDKCGVCGGDNSSCTKIIGTFNKKSKGYTDVVRIPEGATHIKVRQFKAKDQTRFTAYLALKKKTGEYLINGKYMISTSETIIDINGTVMNYSGWSHRDDFLHGMGYSATKEILIVQILATDPTKALDVRYSFFVPKKTTQKVNSVISHGSNKVGPHSTQLQWVTGPWLACSRTCDTGWHTRTVQCQDGNRKLAKGCLLSQRPSAFKQCLLKKC
  
Inhibitor
Name:
BDBM379697
Synonyms:
US9926281, Compound 255
Type:
Small organic molecule
Emp. Form.:
C20H24F2N4O3
Mol. Mass.:
406.4264
SMILES:
C[C@H]1CN(CCN1c1cc(F)cc(F)c1)C(=O)CC[C@]1(NC(=O)NC1=O)C1CC1 |r|
Structure:
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