ChEMBL ligand: CHEMBL3287735 (Gsk2816126)
embryonic ectoderm development/enhancer of zeste 2 polycomb repressive complex 2 subunit/EZH2/SUZ12/EED complex in Human [ChEMBL: CHEMBL3137286] [GtoPdb: 2487, 2654] [UniProtKB: O75530, Q15022, Q15910] There should be some charts here, you may need to enable JavaScript!
enhancer of zeste 2 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH2 in Human [ChEMBL: CHEMBL2189110] [GtoPdb: 2654] [UniProtKB: Q15910] 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
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: 2487, 2654] [UniProtKB: O75530, Q15022, Q15910]
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]
ChEMBL	Inhibition of EZH2 (unknown origin) using SAM as substrate incubated for 60 mins by luminescence microplate reader assay	B	7.89	pIC50	12.9	nM	IC50	J Med Chem (2021) 64: 15170-15188 [PMID:34664960]
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 (unknown origin)	B	8	pIC50	10	nM	IC50	J Med Chem (2022) 65: 1662-1684 [PMID:35014841]
ChEMBL	Inhibition of wild-type EZH2 (unknown origin)	B	8	pIC50	9.9	nM	IC50	J Med Chem (2022) 65: 7016-7043 [PMID:35531606]
ChEMBL	Inhibition of EZH2 (unknown origin)	B	8	pIC50	9.9	nM	IC50	Eur J Med Chem (2022) 238: 114419-114419 [PMID:35569264]
ChEMBL	Inhibition of EZH2 Y641F mutant (unknown origin) using SAM as substrate incubated for 60 mins by luminescence microplate reader assay	B	8.26	pIC50	5.5	nM	IC50	J Med Chem (2021) 64: 15170-15188 [PMID:34664960]
ChEMBL	Inhibition of human EZH2 using SAM as substrate incubated for 1 hr by microplate luminescence based HMT assay	B	8.49	pIC50	3.25	nM	IC50	J Med Chem (2023) 66: 5685-5702 [PMID:37021456]
ChEMBL	Inhibition of N-terminal His-tagged EZH2 in human PRC2 complex (2 to end residues) expressed in Sf9 cells using [3H]-SAM as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA immunodetection assay	B	8.57	pIC50	2.7	nM	IC50	J Med Chem (2021) 64: 2829-2848 [PMID:33606537]
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 wild type EZH2 (unknown origin) by AlphaLlSA assay	B	8.79	pIC50	1.62	nM	IC50	J Med Chem (2023) 66: 1725-1741 [PMID:36692394]
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 34:

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]