SGI-1027 [Ligand Id: 8891] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2336409 |
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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 human N-terminal 600 residues-deleted DNMT1 using hemimethylated (GAC)12 as substrate preincubated for 5 mins followed by substrate addition measured after 15 mins by liquid scintillation counting analysis in presence of [methyl-3H]-AdoMet | B | 4.46 | pIC50 | 35000 | nM | IC50 | J Med Chem (2014) 57: 701-713 [PMID:24387159] |
| ChEMBL | Inhibition of human DNMT1 using polydeoxyinosine polydeoxycytosine DNA as substrate by radioactive methyl transfer assay | B | 4.9 | pIC50 | 12500 | nM | IC50 | J Med Chem (2018) 61: 6518-6545 [PMID:29953809] |
| ChEMBL | Inhibition of human DNMT1 using AdoMet and poly dI-dC after 2 hrs by radioactive assay | B | 4.95 | pIC50 | 11220 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1631-1635 [PMID:23402879] |
| ChEMBL | Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintillation counting method | B | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (2015) 58: 2569-2583 [PMID:25406944] |
| ChEMBL | Inhibition of human DNMT1 using hemimethylated DNA as substrate by radioactive methyl transfer assay | B | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (2018) 61: 6518-6545 [PMID:29953809] |
| ChEMBL | Inhibition of human DNMT1 using polydeoxyinosine polydeoxycytosine DNA as substrate after 15 mins in presence of SAM by TR-FRET assay | B | 5.45 | pIC50 | 3550 | nM | IC50 | J Med Chem (2018) 61: 6518-6545 [PMID:29953809] |
| GtoPdb | Value derived from a nanoscale HTS assay. | - | 6.07 | pIC50 | 850 | nM | IC50 | J Med Chem (2014) 57: 701-13 [PMID:24387159] |
| ChEMBL | Inhibition of human N-terminal 600 residues-deleted DNMT1 using poly(dI-dC) as substrate in presence of AdoMet | B | 6.07 | pIC50 | 850 | nM | IC50 | J Med Chem (2014) 57: 701-713 [PMID:24387159] |
| ChEMBL | Inhibition of human His-DNMT1 using [methyl-3H]SAM as substrate after 2 hrs | B | 4.99 | pEC50 | 10200 | nM | EC50 | Bioorg Med Chem (2015) 23: 5946-5953 [PMID:26220519] |
| 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 His6-tagged human recombinant DNMT3a expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintillation counting method | B | 5.1 | pIC50 | 8000 | nM | IC50 | J Med Chem (2015) 58: 2569-2583 [PMID:25406944] |
| ChEMBL | Inhibition of human C-terminal DNMT3A (623 to 908 residues) using 5'-biotin labeled oligonucleotide as substrate measured after 1 hr | B | 6.05 | pIC50 | 900 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127296-127296 [PMID:32631516] |
| ChEMBL | Inhibition of human C-terminal DNMT3A after 1 hr by fluorescence assay | B | 6.05 | pEC50 | 900 | nM | EC50 | Bioorg Med Chem (2015) 23: 5946-5953 [PMID:26220519] |
| DNA (cytosine-5)-methyltransferase 3B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6095] [UniProtKB: Q9UBC3] | ||||||||
| ChEMBL | Inhibition of His6-tagged human recombinant DNMT3b expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintillation counting method | B | 5.12 | pIC50 | 7500 | nM | IC50 | J Med Chem (2015) 58: 2569-2583 [PMID:25406944] |
| DNA (cytosine-5-)-methyltransferase 3α/DNMT3A2/3L complex in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3137291] [GtoPdb: 2750] [UniProtKB: Q9UJW3, Q9Y6K1] | ||||||||
| ChEMBL | Inhibition of human DNMT3A2/3L using unmethylated DNA as substrate in presence of [methyl-3H]-AdoMet | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2014) 57: 701-713 [PMID:24387159] |
| 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 (unknown origin) | B | 4.23 | pIC50 | 59000 | nM | IC50 | J Med Chem (2018) 61: 6518-6545 [PMID:29953809] |
| ChEMBL | Inhibition of human G9a using biotinylated-H3K9 peptide as substrate after 1 hr in presence of SAM by TR-FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 6518-6545 [PMID:29953809] |
| 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 | Inhibition of human GLP (734 to 1235) using histone as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by liquid scintillation counting analysis in presence of [methyl-3H]-AdoMet | B | 4.19 | pIC50 | 65000 | nM | IC50 | J Med Chem (2014) 57: 701-713 [PMID:24387159] |
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]
