Reaction Details |
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Target | A disintegrin and metalloproteinase with thrombospondin motifs 4 |
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Ligand | BDBM194644 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2125911 (CHEMBL4835256) |
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IC50 | 2.0±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 4 |
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Name: | A disintegrin and metalloproteinase with thrombospondin motifs 4 |
Synonyms: | A disintegrin and metalloproteinase with thrombospondin motifs 4 (ADAMTS-4) | ADAMTS4 | ATS4_HUMAN | Aggrecanase-1 | KIAA0688 | Metalloproteinase with thrombospondin motifs 4 (ADAMTS-4) |
Type: | Enzyme |
Mol. Mass.: | 90214.54 |
Organism: | Homo sapiens (Human) |
Description: | O75173 |
Residue: | 837 |
Sequence: | MSQTGSHPGRGLAGRWLWGAQPCLLLPIVPLSWLVWLLLLLLASLLPSARLASPLPREEE
IVFPEKLNGSVLPGSGAPARLLCRLQAFGETLLLELEQDSGVQVEGLTVQYLGQAPELLG
GAEPGTYLTGTINGDPESVASLHWDGGALLGVLQYRGAELHLQPLEGGTPNSAGGPGAHI
LRRKSPASGQGPMCNVKAPLGSPSPRPRRAKRFASLSRFVETLVVADDKMAAFHGAGLKR
YLLTVMAAAAKAFKHPSIRNPVSLVVTRLVILGSGEEGPQVGPSAAQTLRSFCAWQRGLN
TPEDSDPDHFDTAILFTRQDLCGVSTCDTLGMADVGTVCDPARSCAIVEDDGLQSAFTAA
HELGHVFNMLHDNSKPCISLNGPLSTSRHVMAPVMAHVDPEEPWSPCSARFITDFLDNGY
GHCLLDKPEAPLHLPVTFPGKDYDADRQCQLTFGPDSRHCPQLPPPCAALWCSGHLNGHA
MCQTKHSPWADGTPCGPAQACMGGRCLHMDQLQDFNIPQAGGWGPWGPWGDCSRTCGGGV
QFSSRDCTRPVPRNGGKYCEGRRTRFRSCNTEDCPTGSALTFREEQCAAYNHRTDLFKSF
PGPMDWVPRYTGVAPQDQCKLTCQAQALGYYYVLEPRVVDGTPCSPDSSSVCVQGRCIHA
GCDRIIGSKKKFDKCMVCGGDGSGCSKQSGSFRKFRYGYNNVVTIPAGATHILVRQQGNP
GHRSIYLALKLPDGSYALNGEYTLMPSPTDVVLPGAVSLRYSGATAASETLSGHGPLAQP
LTLQVLVAGNPQDTRLRYSFFVPRPTPSTPRPTPQDWLHRRAQILEILRRRPWAGRK
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BDBM194644 |
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n/a |
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Name | BDBM194644 |
Synonyms: | US9206139, 3 |
Type | Small organic molecule |
Emp. Form. | C20H22F3N3O3 |
Mol. Mass. | 409.4022 |
SMILES | FC(F)(F)c1ccc(C[C@@H](C2CC2)C(=O)NC[C@]2(NC(=O)NC2=O)C2CC2)cc1 |r| |
Structure |
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