ChEMBL ligand: CHEMBL1784369
ADAMTS4/A disintegrin and metalloproteinase with thrombospondin motifs 4 in Human [ChEMBL: CHEMBL2318] [GtoPdb: 1677] [UniProtKB: O75173] There should be some charts here, you may need to enable JavaScript!
ADAMTS5/A disintegrin and metalloproteinase with thrombospondin motifs 5 in Human [ChEMBL: CHEMBL2285] [GtoPdb: 1678] [UniProtKB: Q9UNA0] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
ADAMTS4/A disintegrin and metalloproteinase with thrombospondin motifs 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2318] [GtoPdb: 1677] [UniProtKB: O75173]
GtoPdb	-	-	8.92	pIC50	1.2	nM	IC50	Bioorg Med Chem Lett (2011) 21: 3301-6 [PMID:21536437]
ChEMBL	Inhibition of ADAMTS-4 assessed as substrate cleavage after 16 hrs by fluorescence assay	B	8.92	pIC50	1.2	nM	IC50	Bioorg Med Chem Lett (2011) 21: 3301-3306 [PMID:21536437]
ChEMBL	Immunoblotting: Protein concentrations were measured using the Micro BCA Protein Assay Kit (Pierce/Thermo Scientific, IL). Sample buffer was mixed with 5-25 μg (G-samples) or 30 μg (NaCl and SDS samples) of the protein lysate, denatured at 96° C. for 10 min, and run on 1.5 mm 4-12% Bis-Tris gradient gels (Nupage, Invitrogen, CA), with MOPS SDS running buffer until the 37 kDa protein marker reached the bottom of the gel. All protein extracts were loaded blinded to group.SDS-PAGE and immunoblotting was performed as described in the Criterion BioRad protocol, using polyvinylidene fluoride (PVDF) membranes (GE Healthcare Life Sciences, Uppsala, Sweden). Blots were developed using the ECL Plus Western Blotting Detection System (GE Healthcare) and visualized in the Las-4000 mini from Fujifilm (Japan). Before reprobing, stripping was performed using the Restore Western Blot Stripping Buffer (21059, Thermo Scientific, IL).	B	8.92	pIC50	1.2	nM	IC50	US-10322143-B2. Inhibitors of ADAMTS4 or ADAMTS5 for use in preventing or treating cardiac remodeling and chronic heart failure (2019)
ADAMTS5/A disintegrin and metalloproteinase with thrombospondin motifs 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2285] [GtoPdb: 1678] [UniProtKB: Q9UNA0]
ChEMBL	Inhibition of ADAMTS-5 assessed as substrate cleavage after 16 hrs by fluorescence assay	B	7.7	pIC50	20	nM	IC50	Bioorg Med Chem Lett (2011) 21: 3301-3306 [PMID:21536437]
GtoPdb	-	-	7.7	pIC50	20	nM	IC50	Bioorg Med Chem Lett (2011) 21: 3301-6 [PMID:21536437]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]