ChEMBL ligand: CHEMBL2169919
DOT1 like histone lysine methyltransferase/Histone-lysine N-methyltransferase, H3 lysine-79 specific in Human [ChEMBL: CHEMBL1795117] [GtoPdb: 2650] [UniProtKB: Q8TEK3] There should be some charts here, you may need to enable JavaScript!
protein arginine methyltransferase 5 /PRMT5/MEP50 complex in Human [ChEMBL: CHEMBL3137261] [GtoPdb: 1256] [UniProtKB: O14744, Q9BQA1] There should be some charts here, you may need to enable JavaScript!
protein arginine methyltransferase 7 /Protein arginine N-methyltransferase 7 in Human [ChEMBL: CHEMBL3562175] [GtoPdb: 1258] [UniProtKB: Q9NVM4] 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
DOT1 like histone lysine methyltransferase/Histone-lysine N-methyltransferase, H3 lysine-79 specific in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795117] [GtoPdb: 2650] [UniProtKB: Q8TEK3]
ChEMBL	Binding affinity to DOT1L (unknown origin) by surface plasmon resonance analysis	B	9.6	pKd	0.25	nM	Kd	J Med Chem (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL	Inhibition of human recombinant DOT1L using [3H]-SAM as substrate after 30 mins	B	6.52	pKi	300	nM	Ki	Eur J Med Chem (2012) 56: 179-194 [PMID:22975593]
ChEMBL	Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactor	B	9.52	pKi	0.3	nM	Ki	J Med Chem (2013) 56: 8972-8983 [PMID:23879463]
ChEMBL	Inhibition of human recombinant DOT1L (catalytic domain 1 to 472) using [3H]-SAM by scintillation containing	B	9.52	pKi	0.3	nM	Ki	Medchemcomm (2013) 4: 822-826 [PMID:23795283]
ChEMBL	Inhibition of human DOT1L using oligo-nucleosome/[3H]-SAM as substrate preincubated for 30 mins followed by substrate addition measured after 120 mins by Morrison plot analysis	B	9.52	pKi	0.3	nM	Ki	J Med Chem (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL	Binding affinity to human DOT1L after 120 mins	B	9.52	pKi	0.3	nM	Ki	J Med Chem (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL	Inhibition of human recombinant DOT1L (1 to 416 residues) using chicken erythrocyte oligonucleosomes as substrate and [3H]-SAM incubated for 120 mins by flashplate based assay	B	9.52	pKi	0.3	nM	Ki	Bioorg Med Chem Lett (2016) 26: 4518-4522 [PMID:27485386]
ChEMBL	Displacement of [3H]-SAM in recombinant human His-tagged DOT1L (1 to 416 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 120 mins by radioligand binding assay	B	9.52	pKi	0.3	nM	Ki	Eur J Med Chem (2020) 189: 112023-112023 [PMID:31978781]
ChEMBL	Inhibition of DOT1L in human MV4-11 cells assessed as downregulation of HOXA9/MEIS1 mRNA expression after 6 days by real-time PCR analysis	B	6.15	pIC50	700	nM	IC50	Medchemcomm (2012) 3: 135-161
ChEMBL	Inhibition of DOT1L in human MOLM13 cells assessed as downregulation of HOXA9/MEIS1 mRNA expression after 6 days by real-time PCR analysis	B	6.15	pIC50	700	nM	IC50	Medchemcomm (2012) 3: 135-161
ChEMBL	Inhibition of DOT1L in human MCF10A cells assessed as reduction of H3K79 level	B	7.08	pIC50	84	nM	IC50	J Med Chem (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL	Inhibition of recombinant human N-terminal GST-tagged DOT1L (1 to 420 residues) expressed in Escherichia coli BL21 (DE3) using histone as substrate incubated for 1 hr by MTase-glo based luminescence assay	B	9.07	pIC50	0.86	nM	IC50	Eur J Med Chem (2020) 189: 112023-112023 [PMID:31978781]
ChEMBL	Inhibition of recombinant human DOT1L using chicken erythrocyte oligonucleosomes/[3H]-SAM as substrate assessed as incorporation of radioactivity into oligonucleosome preincubated for 30 mins followed by substrate addition measured after 120 mins	B	9.4	pIC50	0.4	nM	IC50	Medchemcomm (2012) 3: 135-161
ChEMBL	Competitive inhibition of human recombinant DOT1L (1 to 416 amino acid residues) using [3H]-SAM assessed as inhibition of nucleosome methylation incubated for 30 mins prior to substrate addition measured after 120 mins	B	9.4	pIC50	0.4	nM	IC50	Bioorg Med Chem (2013) 21: 1787-1794 [PMID:23433670]
ChEMBL	Inhibition of human recombinant DOT1L using [3H]-SAM as substrate after 30 mins	B	9.4	pIC50	0.4	nM	IC50	Eur J Med Chem (2012) 56: 179-194 [PMID:22975593]
ChEMBL	Inhibition of recombinant human DOT1L (1 to 416) using [3H]-SAM, SAM and nucleosome as substrate assessed as incorporation of radioactivity into nucleosome preincubated for 30 mins followed by substrate addition measured after 120 mins by flash plate assay	B	9.4	pIC50	0.4	nM	IC50	J Med Chem (2015) 58: 1596-1629 [PMID:25406853]
GtoPdb	-	-	9.4	pIC50	0.4	nM	IC50	Cancer Cell (2011) 20: 53-65 [PMID:21741596]
ChEMBL	Inhibition of DOT1L (unknown origin)-mediated H3K79 methylation by cell based assay	B	8.05	pEC50	9	nM	EC50	J Med Chem (2013) 56: 8972-8983 [PMID:23879463]
protein arginine methyltransferase 5 /PRMT5/MEP50 complex in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3137261] [GtoPdb: 1256] [UniProtKB: O14744, Q9BQA1]
ChEMBL	Inhibition of human full length PRMT5-MEP50 complex expressed in Sf9 cells	B	4.7	pIC50	>20000	nM	IC50	ACS Med Chem Lett (2015) 6: 408-412 [PMID:25893041]
protein arginine methyltransferase 7 /Protein arginine N-methyltransferase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3562175] [GtoPdb: 1258] [UniProtKB: Q9NVM4]
ChEMBL	Inhibition of human full length PRMT7 expressed in Sf9 cells	B	5.12	pIC50	7500	nM	IC50	ACS Med Chem Lett (2015) 6: 408-412 [PMID:25893041]

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]