compound 1 [PMID: 28621943] [Ligand Id: 11563] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL417799 (Sanguinarine)
  • Bcl2-antagonist of cell death (BAD) in Human [ChEMBL: CHEMBL3817] [UniProtKB: Q92934]
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  • regulator of G-protein signaling 17/Regulator of G-protein signaling 17 in Human [ChEMBL: CHEMBL4295974] [GtoPdb: 2801] [UniProtKB: Q9UGC6]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Bcl2-antagonist of cell death (BAD) in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3817] [UniProtKB: Q92934]
ChEMBL Displacement of fluorescein-labeled Bak-BH3 peptide from human Bcl-XL by fluorescence polarization assay B 4.72 pIC50 19000 nM IC50 J. Med. Chem. (2008) 51: 6699-6710 [PMID:18925736]
Nuclear factor NF-kappa-B complex in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094258] [UniProtKB: P19838Q00653Q04206]
ChEMBL Inhibition of NF-kappaB transactivation in TNF-alpha-stimulated human K562 cells preincubated for 2 hrs followed by TNF-alpha challenge measured after 6 hrs by dual luciferase reporter gene assay B 5.7 pIC50 2000 nM IC50 Bioorg. Med. Chem. (2014) 22: 3008-3015 [PMID:24775915]
regulator of G-protein signaling 17/Regulator of G-protein signaling 17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295974] [GtoPdb: 2801] [UniProtKB: Q9UGC6]
ChEMBL Binding affinity to RGS17 (unknown origin) by ITC method B 6 pKd 1000 nM Kd J Nat Prod (2017) 80: 1992-2000 [PMID:28621943]
ChEMBL Inhibition of RGS17 (unknown origin) C117A mutant interaction with biotinylated Galphao after 30 mins in presence of AMF and GDP by AlphaScreen assay B 4 pIC50 >100000 nM IC50 J Nat Prod (2017) 80: 1992-2000 [PMID:28621943]
ChEMBL Inhibition of wild type GST-tagged RGS17 (unknown origin) interaction with biotinylated Galphao after 30 mins in presence of AMF and GDP by AlphaScreen assay B 4.14 pIC50 72800 nM IC50 J Nat Prod (2017) 80: 1992-2000 [PMID:28621943]
GtoPdb - - 4.14 pIC50 72800 nM IC50 J Nat Prod (2017) 80: 1992-2000 [PMID:28621943]
ChEMBL Inhibition of RGS17 (unknown origin) GAP activity in presence of GTP by malachite green dye based assay B 4.92 pIC50 12000 nM IC50 J Nat Prod (2017) 80: 1992-2000 [PMID:28621943]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]