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ChEMBL ligand: CHEMBL3287735 (Gsk2816126) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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 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 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]