UNC0321 [Ligand Id: 8389] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1214066
  • euchromatic histone lysine methyltransferase 2/Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 in Human [ChEMBL: CHEMBL6032] [GtoPdb: 2652] [UniProtKB: Q96KQ7]
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  • euchromatic histone lysine methyltransferase 1/Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 in Human [ChEMBL: CHEMBL6031] [GtoPdb: 2651] [UniProtKB: Q9H9B1]
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  • SET domain containing 7, histone lysine methyltransferase/Histone-lysine N-methyltransferase SETD7 in Human [ChEMBL: CHEMBL5523] [GtoPdb: 2703] [UniProtKB: Q8WTS6]
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  • lysine methyltransferase 5A/N-lysine methyltransferase SETD8 in Human [ChEMBL: CHEMBL1795176] [GtoPdb: 2704] [UniProtKB: Q9NQR1]
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  • protein arginine methyltransferase 3/Protein arginine N-methyltransferase 3 in Human [ChEMBL: CHEMBL5891] [GtoPdb: 1254] [UniProtKB: O60678]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
euchromatic histone lysine methyltransferase 2/Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6032] [GtoPdb: 2652] [UniProtKB: Q96KQ7]
GtoPdb - - 10.2 pKi 0.06 nM Ki J Med Chem (2010) 53: 5844-57 [PMID:20614940]
ChEMBL Inhibition of G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay B 4.96 pIC50 11000 nM IC50 J Med Chem (2011) 54: 6139-6150 [PMID:21780790]
ChEMBL Activity at methyl transferase activity G9a by enzyme coupled S-adenocylehomocystein detection assay B 5.05 pIC50 9000 nM IC50 J Med Chem (2010) 53: 5844-5857 [PMID:20614940]
ChEMBL Inhibition of methyl transferase activity of G9a assessed as inhibition of H3K9 methylation by chemiluminescence based oxygen tunneling assay B 5.22 pIC50 6000 nM IC50 J Med Chem (2010) 53: 5844-5857 [PMID:20614940]
ChEMBL Inhibition of G9a assessed as hydrolysis of S-adenosyl-L-homocysteine after 2 mins by SAHH-coupled fluorescence assay B 8.05 pIC50 9 nM IC50 J Med Chem (2011) 54: 6139-6150 [PMID:21780790]
euchromatic histone lysine methyltransferase 1/Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6031] [GtoPdb: 2651] [UniProtKB: Q9H9B1]
ChEMBL Activity at methyl transferase activity GLP by chemiluminescence based oxygen tunneling assay B 7.64 pIC50 23 nM IC50 J Med Chem (2010) 53: 5844-5857 [PMID:20614940]
ChEMBL Activity at methyl transferase activity GLP by enzyme coupled S-adenocylehomocystein detection assay B 7.82 pIC50 15 nM IC50 J Med Chem (2010) 53: 5844-5857 [PMID:20614940]
SET domain containing 7, histone lysine methyltransferase/Histone-lysine N-methyltransferase SETD7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5523] [GtoPdb: 2703] [UniProtKB: Q8WTS6]
ChEMBL Activity at methyl transferase activity SET7/9 by enzyme coupled S-adenocylehomocystein detection assay B 4.4 pIC50 >40000 nM IC50 J Med Chem (2010) 53: 5844-5857 [PMID:20614940]
lysine methyltransferase 5A/N-lysine methyltransferase SETD8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795176] [GtoPdb: 2704] [UniProtKB: Q9NQR1]
ChEMBL Activity at methyl transferase activity SET8/preSet7 by enzyme coupled S-adenocylehomocystein detection assay B 4.4 pIC50 >40000 nM IC50 J Med Chem (2010) 53: 5844-5857 [PMID:20614940]
protein arginine methyltransferase 3/Protein arginine N-methyltransferase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5891] [GtoPdb: 1254] [UniProtKB: O60678]
ChEMBL Activity at methyl transferase activity PRMT3 by enzyme coupled S-adenocylehomocystein detection assay B 4.4 pIC50 >40000 nM IC50 J Med Chem (2010) 53: 5844-5857 [PMID:20614940]

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]