ChEMBL ligand: CHEMBL569864 (BIX-01294)
DNA methyltransferase 1/DNA (cytosine-5)-methyltransferase 1 in Human [ChEMBL: CHEMBL1993] [GtoPdb: 2605] [UniProtKB: P26358] There should be some charts here, you may need to enable JavaScript!
euchromatic histone lysine methyltransferase 2/Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 in Human [ChEMBL: CHEMBL6032] [GtoPdb: 2652] [UniProtKB: Q96KQ7] There should be some charts here, you may need to enable JavaScript!
euchromatic histone lysine methyltransferase 1/Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 in Human [ChEMBL: CHEMBL6031] [GtoPdb: 2651] [UniProtKB: Q9H9B1] There should be some charts here, you may need to enable JavaScript!
nuclear receptor binding SET domain protein 2/Histone-lysine N-methyltransferase NSD2 in Human [ChEMBL: CHEMBL3108645] [GtoPdb: 3220] [UniProtKB: O96028] There should be some charts here, you may need to enable JavaScript!
lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum [ChEMBL: CHEMBL364] There should be some charts here, you may need to enable JavaScript!

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 DNMT1 using polydeoxyinosine polydeoxycytosine DNA as substrate after 15 mins in presence of SAM by TR-FRET assay	B	5	pIC50	>10000	nM	IC50	J Med Chem (2018) 61: 6518-6545 [PMID:29953809]
ChEMBL	Inhibition of DNMT1 (unknown origin)	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	Binding affinity to G9a by isothermal titration colorimetry	B	6.89	pKd	130	nM	Kd	J Med Chem (2010) 53: 5844-5857 [PMID:20614940]
ChEMBL	Inhibition of G9a in human MDA-MB-231 cells assessed as reduction in H3K9me2 level after 2 days by immunofluorescence in-cell western analysis	B	5.34	pIC50	4563	nM	IC50	ACS Med Chem Lett (2018) 9: 167-168 [PMID:29541353]
ChEMBL	Inhibition of human G9a expressed in HEK293 cells	B	5.42	pIC50	3830	nM	IC50	Eur J Med Chem (2021) 226: 113865-113865 [PMID:34655985]
ChEMBL	Inhibition of G9a (685 to 1000) (unknown origin) expressed in Escherichia coli BL21 assessed as reduction of H3K9me2 level by DELFIA assay	B	5.52	pIC50	3000	nM	IC50	Medchemcomm (2010) 1: 114-124
ChEMBL	Inhibition of recombinant GST-tagged G9a (685 to 1000 amino acids) (unknown origin) expressed in Escherichia coli BL21 using biotinylated histone H3 peptide as substrate by DELFIA	B	5.57	pIC50	2700	nM	IC50	Medchemcomm (2012) 3: 135-161
ChEMBL	Inhibition of lysine methyltransferase G9a	B	5.57	pIC50	2700	nM	IC50	Bioorg Med Chem (2011) 19: 3605-3615 [PMID:21316248]
ChEMBL	Inhibition of human G9a using core histone H3 as substrate incubated for 1 hr in presence of [3H]-SAM by filter binding method	B	5.7	pIC50	2000	nM	IC50	Eur J Med Chem (2019) 184: 111755-111755 [PMID:31627059]
ChEMBL	Inhibition of G9a (unknown origin)	B	5.72	pIC50	1900	nM	IC50	Medchemcomm (2010) 1: 16-29
ChEMBL	Inhibition of human N-terminal hexahistidine-tagged G9a SET domain amino acid 913 to 1193 expressed in Escherichia coli BL21 (DE3) using Histone H3 peptide as substrate preincubated for 15 mins before substrate addition by mass spectrophotometric analysis	B	5.72	pIC50	1900	nM	IC50	Eur J Med Chem (2012) 56: 179-194 [PMID:22975593]
ChEMBL	Inhibition of GST-fused G9a (amino acids 685 to 1000) (unknown origin) expressed in Escherichia coli BL21 by DELFIA assay	B	5.72	pIC50	1900	nM	IC50	J Med Chem (2023) 66: 8086-8102 [PMID:37268593]
ChEMBL	Inhibition of G9a (unknown origin) by mas spectrometric method	B	5.72	pIC50	1900	nM	IC50	J Med Chem (2018) 61: 6518-6545 [PMID:29953809]
ChEMBL	Inhibition of N-terminal hexahistidine-tagged SET domain of human G9a (913 to 1193) expressed in Escherichia coli BL21 (DE3) using Histone H3 peptide (1 to 15) as substrate preincubated on ice for 15 mins followed by 5 mins incubation at 30 degC measured post substrate addition by mass spectrophotometric analysis	B	5.72	pIC50	1900	nM	IC50	J Med Chem (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL	Inhibition of recombinant human G9a (685 to 1000 residues) using H3 peptide (1 to 20 residues) by mass spectrometry	B	5.72	pIC50	1900	nM	IC50	J Med Chem (2019) 62: 2666-2689 [PMID:30753076]
ChEMBL	Inhibition of N-terminal hexahistidine-tagged human G9a (913 to 1193 residues) expressed in Escherichia coli BL21 (DE3)-Gold cells using histone H3 (1 to 15 residues) as substrate preincubated for 20 mins followed by substrate addition by mass spectrometry	B	5.72	pIC50	1900	nM	IC50	Bioorg Med Chem (2016) 24: 6102-6108 [PMID:27720557]
ChEMBL	Inhibition of GST-tagged G9a (685 to 1000 residues) (unknown origin) expressed in Escherichia coli BL21 using biotinylated H3 (1to20 residues) as substrate after 60 mins in presence of SAM by fluorescence immunoassay	B	5.72	pIC50	1900	nM	IC50	Bioorg Med Chem (2017) 25: 4579-4594 [PMID:28739157]
ChEMBL	Inhibition of N-terminal GST-tagged human recombinant G9a (785 to 1210 residues) expressed in baculovirus-infected Sf9 cells using biotinylated histone H3 peptide substrate incubated for 2 hrs by AlphaLISA assay	B	5.77	pIC50	1700	nM	IC50	ACS Med Chem Lett (2023) 14: 1531-1536 [PMID:37974951]
ChEMBL	Inhibition of recombinant G9a	B	5.77	pIC50	1700	nM	IC50	Nat Chem Biol (2008) 4: 590-597 [PMID:18800048]
ChEMBL	Inhibition of G9a (685 to 1000) (unknown origin) assessed as H3K9me2 level by mass spectrophotometric analysis	B	5.77	pIC50	1700	nM	IC50	J Med Chem (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL	Inhibition of GST-tagged full length human G9a (685 to 1000 residues) methylation activity expressed in Escherichia coli BL21 assessed as reduction in H3K9 level using H3(1 to 20 residues)-cys-biotin and SAM as substrate incubated for 60 mins by Dissociation enhanced lanthanide fluoro-immuno assay	B	5.77	pIC50	1700	nM	IC50	J Med Chem (2021) 64: 11798-11815 [PMID:34378389]
ChEMBL	Inhibition of G9a (unknown origin)	B	5.77	pIC50	1700	nM	IC50	Eur J Med Chem (2021) 222: 113588-113588 [PMID:34107385]
ChEMBL	Inhibition of G9a (unknown origin) using H3(1-20)-cys as substrate by HPLC analysis	B	5.77	pIC50	1700	nM	IC50	Eur J Med Chem (2023) 246: 115028-115028 [PMID:36528996]
ChEMBL	Inhibition of G9a	B	5.77	pIC50	1700	nM	IC50	J Med Chem (2009) 52: 7950-7953 [PMID:19891491]
GtoPdb	Antibody-based detection of in vitro methylation.	-	5.77	pIC50	1700	nM	IC50	Mol Cell (2007) 25: 473-81 [PMID:17289593]
ChEMBL	Inhibition of human G9a using biotinylated-H3K9 peptide as substrate after 1 hr in presence of SAM by TR-FRET assay	B	5.92	pIC50	1200	nM	IC50	J Med Chem (2018) 61: 6518-6545 [PMID:29953809]
ChEMBL	Inhibition of G9a (685 to 1000 residues) (unknown origin) expressed in Escherichia coli BL21	B	5.92	pIC50	1200	nM	IC50	J Med Chem (2021) 64: 3392-3426 [PMID:33661013]
ChEMBL	Inhibition of G9a by Alpha screen assay	B	6.54	pIC50	290	nM	IC50	J Med Chem (2009) 52: 7950-7953 [PMID:19891491]
ChEMBL	Inhibition of G9a (913 to 1193 residues) (unknown origin) using biotin-ARTKQTARKST peptide as substrate pretreated for 15 mins followed by substrate addition measured after 2 hrs in presence of SAM by chemiluminescence-based oxygen tunnelling assay	B	6.54	pIC50	290	nM	IC50	Medchemcomm (2017) 8: 1069-1092 [PMID:29308121]
ChEMBL	Inhibition of G9a (unknown origin)	B	6.74	pIC50	180	nM	IC50	Eur J Med Chem (2019) 184: 111755-111755 [PMID:31627059]
ChEMBL	Inhibition of G9a by Thioglo assay	B	6.96	pIC50	110	nM	IC50	J Med Chem (2009) 52: 7950-7953 [PMID:19891491]
ChEMBL	Inhibition of G9a (913 to 1193 residues) (unknown origin) using peptide H3 (1 to 25 residues) as substrate pretreated for 5 mins followed by substrate addition by Thioglo reagent based enzyme coupled SAH detection assay	B	6.96	pIC50	110	nM	IC50	Medchemcomm (2017) 8: 1069-1092 [PMID:29308121]
ChEMBL	Inhibition of human G9a using biotinylated peptide H3( 1 to 25 residues) as substrate measured after 15 mins in presence of [3H]-SAM by scintillation proximity assay	B	7.17	pIC50	67	nM	IC50	Medchemcomm (2017) 8: 1069-1092 [PMID:29308121]
ChEMBL	Inhibition of G9a (unknown origin) using [histone H3 1 to 25 residues] and SAM substrate by scintillation proximity assay	B	7.17	pIC50	67	nM	IC50	Medchemcomm (2014) 5: 1821-1828 [PMID:25750706]
ChEMBL	Inhibition of G9a (unknown origin)	B	8.57	pIC50	2.7	nM	IC50	J Med Chem (2023) 66: 4059-4085 [PMID:36882960]
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]
GtoPdb	-	-	4.42	pIC50	38000	nM	IC50	Mol Cell (2007) 25: 473-81 [PMID:17289593]
ChEMBL	Inhibition of Histone H3 lysine 9 of GLP methyltransferase	B	4.42	pIC50	38000	nM	IC50	Nat Chem Biol (2008) 4: 590-597 [PMID:18800048]
ChEMBL	Inhibition of GLP (unknown origin) using H3(1-20)-cys as substrate by HPLC analysis	B	4.42	pIC50	38000	nM	IC50	Eur J Med Chem (2023) 246: 115028-115028 [PMID:36528996]
ChEMBL	Inhibition of GLP (610 to 917) (unknown origin) assessed as H3K9me2 level by mass spectrophotometric analysis	B	4.42	pIC50	38000	nM	IC50	J Med Chem (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL	Inhibition of GST-fused GLP (amino acids 610 to 917) (unknown origin) expressed in Escherichia coli BL21 by DELFIA assay	B	6.15	pIC50	700	nM	IC50	J Med Chem (2023) 66: 8086-8102 [PMID:37268593]
ChEMBL	Inhibition of human N-terminal hexahistidine-tagged GLP SET domain amino acid 951 to 1235 expressed in Escherichia coli BL21 (DE3) using Histone H3 peptide as substrate preincubated for 15 mins before substrate addition by mass spectrophotometric analysis	B	6.15	pIC50	700	nM	IC50	Eur J Med Chem (2012) 56: 179-194 [PMID:22975593]
ChEMBL	Inhibition of GLP (unknown origin)	B	6.15	pIC50	700	nM	IC50	Medchemcomm (2010) 1: 16-29
ChEMBL	Inhibition of recombinant human GLP (610 to 917 residues) using H3 peptide (1 to 20 residues) by mass spectrometry	B	6.15	pIC50	700	nM	IC50	J Med Chem (2019) 62: 2666-2689 [PMID:30753076]
ChEMBL	Inhibition of GLP	B	6.15	pIC50	700	nM	IC50	J Med Chem (2009) 52: 7950-7953 [PMID:19891491]
ChEMBL	Inhibition of N-terminal hexahistidine-tagged SET domain of human GLP (951 to 1235) expressed in Escherichia coli BL21 (DE3) using Histone H3 peptide (1 to 15) as substrate preincubated on ice for 15 mins followed by 5 mins incubation at 30 degC measured post substrate addition by mass spectrophotometric analysis	B	6.15	pIC50	700	nM	IC50	J Med Chem (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL	Inhibition of EHMT1 (unknown origin)	B	6.15	pIC50	700	nM	IC50	Bioorg Med Chem (2017) 25: 4579-4594 [PMID:28739157]
ChEMBL	Activity at methyl transferase activity GLP by enzyme coupled S-adenocylehomocystein detection assay	B	7.47	pIC50	34	nM	IC50	J Med Chem (2010) 53: 5844-5857 [PMID:20614940]
ChEMBL	Activity at methyl transferase activity GLP by chemiluminescence based oxygen tunneling assay	B	7.57	pIC50	27	nM	IC50	J Med Chem (2010) 53: 5844-5857 [PMID:20614940]
nuclear receptor binding SET domain protein 2/Histone-lysine N-methyltransferase NSD2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108645] [GtoPdb: 3220] [UniProtKB: O96028]
ChEMBL	Inhibition of human NSD2 SET domain (948 to 1239 residues)-mediated mono-methylation activity assessed as reduction in H3K36me1 level incubated for 1 hr	B	4.39	pIC50	41000	nM	IC50	J Med Chem (2023) 66: 1634-1651 [PMID:36642961]
lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
ChEMBL	Inhibition of human LSD1 (unknown orgin)	B	6.74	pIC50	180	nM	IC50	Eur J Med Chem (2021) 222: 113588-113588 [PMID:34107385]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL	Antimalarial activity against ring stage Plasmodium falciparum K1 incubated for 48 hrs by Hoechst 33342 staining based fluorescence based assay	F	6.74	pIC50	180	nM	IC50	Eur J Med Chem (2019) 184: 111755-111755 [PMID:31627059]
ChEMBL	Antimalarial activity against ring stage Plasmodium falciparum 3D7 incubated for 48 hrs by Hoechst 33342 staining based fluorescence based assay	F	6.82	pIC50	152	nM	IC50	Eur J Med Chem (2019) 184: 111755-111755 [PMID:31627059]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum 3D7 after 3 days by SYBR green1 dye based assay	F	7.37	pIC50	43	nM	IC50	Medchemcomm (2017) 8: 1069-1092 [PMID:29308121]
ChEMBL	Antiplasmodial activity against asynchronous form of Plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasite growth inhibition after 48 hrs by SYBR green1 staining based flow cytometry	F	7.68	pIC50	20.8	nM	IC50	Eur J Med Chem (2019) 161: 277-291 [PMID:30366254]
ChEMBL	Antiplasmodial activity against asynchronous form of Plasmodium falciparum W2 infected in human erythrocytes assessed as parasite growth inhibition after 48 hrs by SYBR green1 staining based flow cytometry	F	7.78	pIC50	16.7	nM	IC50	Eur J Med Chem (2019) 161: 277-291 [PMID:30366254]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum Dd2 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation measured after 48 hrs by microbeta liquid scintillation counting method	F	8.01	pIC50	9.7	nM	IC50	Eur J Med Chem (2019) 161: 277-291 [PMID:30366254]
ChEMBL	Antiplasmodial activity against drug-sensitive Plasmodium falciparum 3D7	F	7.12	pEC50	75	nM	EC50	Bioorg Med Chem Lett (2013) 23: 2829-2843 [PMID:23587422]

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]