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ChEMBL ligand: CHEMBL3109630 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 N-terminal GST tagged human recombinant EHMT2 (785 to 1210 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 mins by AMP Glo detection assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 2516-2524 [PMID:31350126] |
GtoPdb | - | - | 8.48 | pIC50 | 3.3 | nM | IC50 |
A-366: a chemical Probe for G9a/GLP.. thesgc.org; ACS Med Chem Lett (2014) 5: 205-9 [PMID:24900801] |
ChEMBL | Inhibition of G9a (unknown origin) using biotinylated-histone H3(1-21) peptide as substrate after 3 hrs by AlphaLISA assay | B | 8.48 | pIC50 | 3.3 | nM | IC50 | ACS Med Chem Lett (2014) 5: 205-209 [PMID:24900801] |
ChEMBL | Inhibition of G9a (unknown origin) | B | 8.48 | pIC50 | 3.3 | nM | IC50 | J Med Chem (2015) 58: 2569-2583 [PMID:25406944] |
ChEMBL | Inhibition of G9a (unknown origin) | B | 8.48 | pIC50 | 3.3 | nM | IC50 | Bioorg Med Chem (2016) 24: 6102-6108 [PMID:27720557] |
ChEMBL | Inhibition of G9a (unknown origin)-mediated incorporation of methyl group from [3H]-SAM into peptide substrate by scintillation proximity assay | B | 8.52 | pIC50 | 3 | nM | IC50 | ACS Med Chem Lett (2014) 5: 205-209 [PMID:24900801] |
ChEMBL | Inhibition of G9a (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2019) 62: 8996-9007 [PMID:31260300] |
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 GLP (unknown origin)-mediated incorporation of methyl group from [3H]-SAM into peptide substrate by scintillation proximity assay | B | 7.42 | pIC50 | 38 | nM | IC50 | ACS Med Chem Lett (2014) 5: 205-209 [PMID:24900801] |
ChEMBL | Inhibition of N-terminal GST tagged human recombinant EHMT1 (794 to 1294 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 mins by AMP Glo detection assay | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 2516-2524 [PMID:31350126] |
GtoPdb | - | - | 8.52 | pIC50 | 38 | nM | IC50 |
A-366: a chemical Probe for G9a/GLP.. thesgc.org; ACS Med Chem Lett (2014) 5: 205-9 [PMID:24900801] |
Spindlin-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523509] [UniProtKB: Q9Y657] | ||||||||
ChEMBL | Binding affinity to recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetry | B | 6.41 | pKd | 393 | nM | Kd | J Med Chem (2019) 62: 9008-9025 [PMID:31550156] |
ChEMBL | Binding affinity to recombinant human His-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetry | B | 6.74 | pKd | 180 | nM | Kd | J Med Chem (2019) 62: 9008-9025 [PMID:31550156] |
ChEMBL | Inhibition of H3(1-12)K4me3 binding to recombinant human C-terminal His6-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as dissociation constant by FTSA assay | B | 6.96 | pKd | 110 | nM | Kd | J Med Chem (2019) 62: 8996-9007 [PMID:31260300] |
ChEMBL | Displacement of trimethylated biotinylated histone H3 peptide from recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins followed by peptide addition and measured after 1 hr by Alphascreen method | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2019) 62: 9008-9025 [PMID:31550156] |
ChEMBL | Inhibition of FL-H3K4me3 binding to recombinant human C-terminal His6-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 30 mins by fluorescence polarization displacement assay | B | 6.68 | pIC50 | 207 | nM | IC50 | J Med Chem (2019) 62: 8996-9007 [PMID:31260300] |
ChEMBL | Binding affinity to recombinant human His-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by AlphaLISA assay | B | 6.73 | pIC50 | 186 | nM | IC50 | J Med Chem (2019) 62: 9008-9025 [PMID:31550156] |
ChEMBL | Inhibition of biotin-H3(1-23)K4me3 binding to recombinant human C-terminal His6-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 90 mins by AlphaLISA assay | B | 7.14 | pIC50 | 72 | nM | IC50 | J Med Chem (2019) 62: 8996-9007 [PMID:31260300] |
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]