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 |
|---|---|---|---|---|---|---|---|---|
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Selectivity interaction (Receptors and enzyme panel (internal screening at GSK)) EUB0000215b ADRA1B | B | 5 | pIC50 | 10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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 1 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189116] [GtoPdb: 2835] [UniProtKB: Q92800] | ||||||||
| ChEMBL | Selectivity interaction (Methyltransferase panel (HotSpot screen, Reaction Biology, radioisotope-based filter binding assays)) EUB0000215b EZH1 | B | 6.62 | pIC50 | 240 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| GtoPdb | - | - | 6.62 | pIC50 | 240 | 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 | Affinity Phenotypic Cellular interaction (CellTiter-Glo assay (Promega, cell proliferation assay in LNCaP cell line)) EUB0000215b EZH2 | F | 5.54 | pIC50 | 2900 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Affinity On-target Cellular interaction (Immunofluorescence (inhibition of H3K27 methylation in HCC1806 cells)) EUB0000215b EZH2 | B | 6.76 | pIC50 | 174 | nM | IC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| GtoPdb | - | - | 8.4 | pIC50 | 4 | nM | IC50 | ACS Med Chem Lett (2012) 3: 1091-6 [PMID:24900432] |
| ChEMBL | Inhibition of EZH2 (unknown origin) | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2022) 65: 1662-1684 [PMID:35014841] |
| 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 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]
