DZNep [Ligand Id: 8392] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL154745
  • S-Adenosylhomocysteine hydrolase/Adenosylhomocysteinase in Human [ChEMBL: CHEMBL2664] [GtoPdb: 1233] [UniProtKB: P23526]
  • S-Adenosylhomocysteine hydrolase in Hamster [GtoPdb: 1233]
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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
S-Adenosylhomocysteine hydrolase/Adenosylhomocysteinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2664] [GtoPdb: 1233] [UniProtKB: P23526]
ChEMBL Inhibition of SAH hydrolase (unknown origin) assessed as inhibition constant B 11 pKi 0.01 nM Ki J Med Chem (2022) 65: 7016-7043 [PMID:35531606]
ChEMBL Inhibition of recombinant human placental AdoHcy hydrolase expressed in Escherichia coli BL21 using AdoHcy as substrate preincubated for 10 mins followed by substrate addition measured after 20 mins by DTNB coupled assay B 6.36 pIC50 440 nM IC50 J Med Chem (2015) 58: 5108-5120 [PMID:26010585]
S-Adenosylhomocysteine hydrolase in Hamster [GtoPdb: 1233]
GtoPdb Inhibition of a SAHH preparation isolated from hamster liver. - 12.3 pKi 0 nM Ki Biochem Biophys Res Commun (1986) 135: 688-94 [PMID:3457563]
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 EZH2 (unknown origin) B 7.1 pIC50 80 nM IC50 J Med Chem (2022) 65: 7016-7043 [PMID:35531606]

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]