Reaction Details |
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Target | A disintegrin and metalloproteinase with thrombospondin motifs 5 |
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Ligand | BDBM379975 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2125827 (CHEMBL4835172) |
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IC50 | 22±n/a nM |
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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 Chem64:2937-2952 (2021) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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A disintegrin and metalloproteinase with thrombospondin motifs 5 |
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Name: | A disintegrin and metalloproteinase with thrombospondin motifs 5 |
Synonyms: | A disintegrin and metalloproteinase with thrombospondin motifs 5 (ADAMTS-5) | ADAMTS11 | ADAMTS5 | ADMP2 | ATS5_HUMAN | 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
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BDBM379975 |
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n/a |
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Name | BDBM379975 |
Synonyms: | US9926281, Compound 436 |
Type | Small organic molecule |
Emp. Form. | C19H24Cl2N4O4 |
Mol. Mass. | 443.324 |
SMILES | COCC(CC1(C)NC(=O)NC1=O)C(=O)N1CCN(CC1)c1cc(Cl)cc(Cl)c1 |
Structure |
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