GSK343 [Ligand Id: 8240] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2204995 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| DNA methyltransferase 1/DNA (cytosine-5)-methyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1993] [GtoPdb: 2605] [UniProtKB: P26358] | ||||||||
| ChEMBL | Inhibition of DNMT1 using polydi-dc as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| DNA (cytosine-5-)-methyltransferase 3α/DNA (cytosine-5)-methyltransferase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1992] [GtoPdb: 2750] [UniProtKB: Q9Y6K1] | ||||||||
| ChEMBL | Inhibition of DNMT3a using lambda DNA as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| DNA (cytosine-5)-methyltransferase 3B in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189115] [UniProtKB: O88509] | ||||||||
| ChEMBL | Inhibition of mouse DNMT3b1 using lambda DNA as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| embryonic ectoderm development/enhancer of zeste 1 polycomb repressive complex 2 subunit/EZH1/SUZ12/EED/AEBP2/RBBP4 complex in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3137287] [GtoPdb: 2487, 2835] [UniProtKB: O75530, Q09028, Q15022, Q6ZN18, Q92800] | ||||||||
| ChEMBL | Inhibition of PRC2 complex of EZH1, EED, SUZ12, AEBP2 and RbAp48 using histone H3 peptide (21 to 44) as substrate and [3H]SAM after 1 hr by SPA | B | 6.62 | pIC50 | 240 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| GtoPdb | - | - | 6.62 | pIC50 | 240 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-6 [PMID:24900432] |
| embryonic ectoderm development/enhancer of zeste 2 polycomb repressive complex 2 subunit/EZH2/SUZ12/EED/RBBP7/RBBP4 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301388] [GtoPdb: 2487, 2654] [UniProtKB: O75530, Q09028, Q15022, Q15910, Q16576] | ||||||||
| ChEMBL | Inhibition of PRC2 complex of FLAG-EZH2, EED, SUZ12, AEBP2 and RbAp48 using histone H3 peptide (21 to 44) as substrate and [3H]SAM after 30 mins | B | 8.92 | pKi | 1.2 | nM | Ki | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| ChEMBL | Inhibition of PRC2 complex of FLAG-EZH2, EED, SUZ12, AEBP2 and RbAp48 using histone H3 peptide (21 to 44) as substrate and [3H]SAM after 1 hr | B | 8.4 | pIC50 | 4 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| GtoPdb | - | - | 8.4 | pIC50 | 4 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-6 [PMID:24900432] |
| 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-mediated proliferation of human LNCaP cells after 6 days by chemiluminescence analysis | B | 5.54 | pIC50 | 2900 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| ChEMBL | Inhibition of EZH2-mediated nuclear H3K27 methylation in human HCC1806 cells after 72 hrs by immunofluorescence analysis | B | 6.76 | pIC50 | 174 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| GtoPdb | - | - | 8.4 | pIC50 | 4 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-6 [PMID:24900432] |
| DOT1 like histone lysine methyltransferase/Histone-lysine N-methyltransferase, H3 lysine-79 specific in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795117] [GtoPdb: 2650] [UniProtKB: Q8TEK3] | ||||||||
| ChEMBL | Inhibition of DOT1L using core histone as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| 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] | ||||||||
| ChEMBL | Inhibition of G9a using histone H3 as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| lysine methyltransferase 2A/Histone-lysine N-methyltransferase MLL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293299] [GtoPdb: 2688] [UniProtKB: Q03164] | ||||||||
| ChEMBL | Inhibition of MLL1 using core histone as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| lysine methyltransferase 2D/Histone-lysine N-methyltransferase MLL2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189114] [GtoPdb: 2691] [UniProtKB: O14686] | ||||||||
| ChEMBL | Inhibition of MLL2 using core histone as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| lysine methyltransferase 2C/Histone-lysine N-methyltransferase MLL3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189113] [GtoPdb: 2690] [UniProtKB: Q8NEZ4] | ||||||||
| ChEMBL | Inhibition of MLL3 using core histone as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| lysine methyltransferase 2B/Histone-lysine N-methyltransferase MLL4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189112] [GtoPdb: 2689] [UniProtKB: Q9UMN6] | ||||||||
| ChEMBL | Inhibition of MLL4 using core histone as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| 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 | Inhibition of SET7 using histone H3 as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins | B | 4.2 | pIC50 | 63000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| Histone-lysine N-methyltransferase SETMAR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189111] [UniProtKB: Q53H47] | ||||||||
| ChEMBL | Inhibition of SETMAR using histone H3 as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| SUV39H1 histone lysine methyltransferase/Histone-lysine N-methyltransferase SUV39H1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795118] [GtoPdb: 2715] [UniProtKB: O43463] | ||||||||
| ChEMBL | Inhibition of SUV39H1 using histone H3 as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| protein arginine methyltransferase 1 /Protein-arginine N-methyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5524] [GtoPdb: 1252] [UniProtKB: Q99873] | ||||||||
| ChEMBL | Inhibition of PRMT1 using histone H4 as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| protein arginine methyltransferase 3/Protein arginine N-methyltransferase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5891] [GtoPdb: 1254] [UniProtKB: O60678] | ||||||||
| ChEMBL | Inhibition of PRMT3 using histone H3 as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins | B | 4.13 | pIC50 | 74000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
| protein arginine methyltransferase 5 /Protein arginine N-methyltransferase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795116] [GtoPdb: 1256] [UniProtKB: O14744] | ||||||||
| ChEMBL | Inhibition of PRMT5 using histone H3 as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-1096 [PMID:24900432] |
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]
