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 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 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 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 DNMT1 (unknown origin) | B | 6.42 | pIC50 | 382 | nM | IC50 | Eur J Med Chem (2021) 220: 113555-113555 [PMID:34052677] |
| 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 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]
