CM-272 [Ligand Id: 13289] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4170114 |
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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 recombinant full-length DNMT1 expressed in Sf9 cells assessed as inhibition of methylated dI-dC formation using 100 ug/ml poly dI-dC and [Me-3H]SAM as substrate incubated for 2 hrs by liquid scintillation counting analysis | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (2022) 65: 5462-5494 [PMID:35324190] |
| ChEMBL | Inhibition of human recombinant full-length DNMT1 expressed in Sf9 cells assessed as inhibition of methylated dI-dC formation using poly dI-dC and [Me-3H]SAM as substrate incubated for 2 hrs by liquid scintillation counting analysis | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2022) 65: 5462-5494 [PMID:35324190] |
| ChEMBL | Inhibition of DNMT1 (unknown origin) by TR-FRET assay | B | 6.42 | pIC50 | 382 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| ChEMBL | Inhibition of human DNMT1 using polydeoxyinosine polydeoxycytosine DNA as substrate after 15 mins in presence of SAM by TR-FRET assay | B | 6.42 | pIC50 | 382 | nM | IC50 | J Med Chem (2018) 61: 6518-6545 [PMID:29953809] |
| ChEMBL | Inhibition of DNMT1 (unknown origin) using biotinylated histone monomethyl-H3K9 peptide by TR-FRET assay | B | 6.42 | pIC50 | 382 | nM | IC50 | J Med Chem (2021) 64: 18114-18142 [PMID:34878770] |
| ChEMBL | Inhibition of human DNMT1 enzyme using polydeoxy-inosine polydeoxy-cytosine DNA as substrate incubated for 15 mins in presence of SAM by TR-FRET assay | B | 6.42 | pIC50 | 382 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| ChEMBL | Inhibition of human DNMT1 using polydeoxyinosine polydeoxycytosine DNA as substrate after 15 mins in presence of SAM by TR-FRET assay | B | 6.42 | pIC50 | 382 | nM | IC50 | J Med Chem (2018) 61: 6546-6573 [PMID:29890830] |
| GtoPdb | - | - | 6.44 | pIC50 | 362 | nM | IC50 | Nat Commun (2017) 8: 15424 [PMID:28548080] |
| DNA (cytosine-5)-methyltransferase 3B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6095] [UniProtKB: Q9UBC3] | ||||||||
| ChEMBL | Inhibition of human C-terminal domain DNMT3b catalytic domain (568 to 853 residues) expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as inhibition of methylated dI-dC formation using poly dI-dC and [Me-3H]SAM as substrate incubated for 45 mins in presence of DNMT3L by liquid scintillation counting analysis | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2022) 65: 5462-5494 [PMID:35324190] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of Tracer Red binding to human ERG in membranes after 2 hrs by fluorescence polarization assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2018) 61: 6546-6573 [PMID:29890830] |
| ChEMBL | Inhibition of Tracer Red binding to human ERG in membranes after 2 hrs by fluorescence polarization assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2018) 61: 6546-6573 [PMID:29890830] |
| histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547] | ||||||||
| ChEMBL | Inhibition of full length human C-terminal His-tagged/C-terminal Flag-tagged HDAC1 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] | ||||||||
| ChEMBL | Inhibition of full length human C-terminal His-tagged HDAC2 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| histone deacetylase 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379, Q9Y618] | ||||||||
| ChEMBL | Inhibition of full length human C-terminal His-tagged HDAC3/human N-terminal GST-agged NCOR2 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
| ChEMBL | Inhibition of full length human N-terminal GST-tagged HDAC6 using fluorogenic acetylated peptide as substrate incubated for 30 mins by fluorescence plate reader assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| 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) by TR-FRET assay | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| ChEMBL | Inhibition of human G9a using biotinylated-H3K9 peptide as substrate after 1 hr in presence of SAM by TR-FRET assay | B | 8.1 | pIC50 | 8 | 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 | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2018) 61: 6546-6573 [PMID:29890830] |
| ChEMBL | Inhibition of human G9a enzyme using histone monomethyl-H3K9 peptide as substrate incubated for 1 hr in presence of SAM by TR-FRET assay | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2021) 64: 3392-3426 [PMID:33661013] |
| ChEMBL | Inhibition of G9a (unknown origin) using biotinylated histone monomethyl-H3K9 peptide by TR-FRET assay | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2021) 64: 18114-18142 [PMID:34878770] |
| ChEMBL | Inhibition of G9a (unknown origin) | B | 8.1 | pIC50 | 8 | nM | IC50 | ACS Med Chem Lett (2023) 14: 1531-1536 [PMID:37974951] |
| GtoPdb | - | - | 8.1 | pIC50 | 8 | nM | IC50 | Nat Commun (2017) 8: 15424 [PMID:28548080] |
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]
