GSK126 [Ligand Id: 7012] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3287735
  • embryonic ectoderm development/enhancer of zeste 2 polycomb repressive complex 2 subunit/EZH2/SUZ12/EED complex in Human [ChEMBL: CHEMBL3137286] [GtoPdb: 24872654] [UniProtKB: O75530Q15022Q15910]
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  • enhancer of zeste 2 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH2 in Human [ChEMBL: CHEMBL2189110] [GtoPdb: 2654] [UniProtKB: Q15910]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
embryonic ectoderm development/enhancer of zeste 2 polycomb repressive complex 2 subunit/EZH2/SUZ12/EED complex in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3137286] [GtoPdb: 24872654] [UniProtKB: O75530Q15022Q15910]
ChEMBL Inhibition of EZH2 histone methyltransferase activity in EZH2/SUZ12/EED protein complex (unknown origin) using histone H3 peptide/S-adenosylmethionine as substrate after 2 hrs by TR-FRET assay B 7.8 pIC50 16 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 2486-2492 [PMID:24767850]
GtoPdb Measured using expressed and purified five-member PRC2 protein complex (human Flag–EZH2,EED, SUZ12, AEBP2, RbAp48). - 8 pIC50 9.9 nM IC50 Nature (2012) 492: 108-12 [PMID:23051747];
J Biomol Screen (2012) 17: 1279-92 [PMID:22904200]
enhancer of zeste 2 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189110] [GtoPdb: 2654] [UniProtKB: Q15910]
ChEMBL Inhibition of human wild-type EZH2 assessed as H3K27me0 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL Inhibition of human EZH2 A677G mutant assessed as H3K27me0 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL Inhibition of human EZH2 A677G mutant assessed as H3K27me1 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL Inhibition of human EZH2 Y641F mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL Inhibition of human EZH2 Y641H mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL Inhibition of human EZH2 Y641N mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL Inhibition of human EZH2 Y641S mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL Inhibition of human EZH2 Y641C mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAM B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method B 6.55 pIC50 280 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 3644-3649 [PMID:26189078]
GtoPdb Measured using expressed and purified five-member PRC2 protein complex (human Flag–EZH2,EED, SUZ12, AEBP2, RbAp48). - 8 pIC50 9.9 nM IC50 Nature (2012) 492: 108-12 [PMID:23051747];
J Biomol Screen (2012) 17: 1279-92 [PMID:22904200]
ChEMBL Inhibition of EZH2 Y641N mutant (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count based method B 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 3644-3649 [PMID:26189078]
ChEMBL Inhibition of EZH2 (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count based method B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 3644-3649 [PMID:26189078]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]