ChEMBL ligand: CHEMBL2169920
Histone-lysine N-methyltransferase SMYD3 in Human [ChEMBL: CHEMBL2321643] [UniProtKB: Q9H7B4] There should be some charts here, you may need to enable JavaScript!
SET and MYND domain containing 2/N-lysine methyltransferase SMYD2 in Human [ChEMBL: CHEMBL2169716] [GtoPdb: 2714] [UniProtKB: Q9NRG4] 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
Histone-lysine N-methyltransferase SMYD3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321643] [UniProtKB: Q9H7B4]
ChEMBL	Inhibition of SMYD3 (unknown origin) using p53 (361 to 380 residues) and [3H]-SAM as substrate incubated for 90 mins by SPA assay	B	7.08	pIC50	>83.3	nM	IC50	J Med Chem (2022) 65: 10119-10132 [PMID:35914250]
SET and MYND domain containing 2/N-lysine methyltransferase SMYD2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2169716] [GtoPdb: 2714] [UniProtKB: Q9NRG4]
ChEMBL	Competitive inhibition of SMYD2 (unknown origin) assessed as dissociation constant	B	3.3	pKd	500000	nM	Kd	Eur J Med Chem (2021) 213: 113213-113213 [PMID:33540228]
ChEMBL	Binding affinity to recombinant human full-length SMYD2 (1 to 433) by ITC analysis	B	6.3	pKd	500	nM	Kd	J Med Chem (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL	Binding affinity to full length human SMYD2 (1 to 433 residues) expressed in Escherichia coli strain BL21 (DE3) by ITC analysis	B	6.3	pKd	500	nM	Kd	J Med Chem (2022) 65: 10119-10132 [PMID:35914250]
ChEMBL	Competitive binding affinity to full length human SMYD2 amino acid 1 to 433 expressed in Escherichia coli BL21 (DE3) after 90 mins by radioactive filter-binding assay in presence of P53 peptide	B	6.52	pKi	300	nM	Ki	Eur J Med Chem (2012) 56: 179-194 [PMID:22975593]
ChEMBL	Inhibition of FLAG-tagged SMYD2 (unknown origin) expressed in human U2OS cells mediated intracellular p53 methylation incubated for 24 hrs using p53 as substrate by immunofluorescence analysis	B	4	pIC50	<100000	nM	IC50	J Med Chem (2022) 65: 10119-10132 [PMID:35914250]
ChEMBL	Inhibition of human SMYD2 by western blot assay	B	4.7	pIC50	20000	nM	IC50	J Med Chem (2021) 64: 2382-2418 [PMID:33650861]
ChEMBL	Inhibition of SMYD2 (unknown origin) expressed in human U2OS cells assessed as reduction in p53 methylation by Western blot analysis	B	5	pIC50	<10000	nM	IC50	J Med Chem (2016) 59: 4578-4600 [PMID:27075367]
ChEMBL	Inhibition of N-terminal 2xc-myc-tagged human SMYD2 transfected in human MDA-MB-231 cells assessed as reduction in AHNAK methylation after 72 hrs by ICW assay	B	5.54	pIC50	2900	nM	IC50	J Med Chem (2016) 59: 4578-4600 [PMID:27075367]
ChEMBL	Inhibition of full length 6xHis-tagged SMYD2 (unknown origin) expressed in Escherichia coli using Btn-Ahx GSRAHSSHLKSKKGQSTSRH-amide as substrate after 30 mins in presence 3H-SAM of by scintillation proximity assay	B	6.09	pIC50	812	nM	IC50	J Med Chem (2016) 59: 4578-4600 [PMID:27075367]
ChEMBL	Inhibition of SMYD2 (unknown origin) using biotinylated GSRAHSSHLKSKKGQSTSRH as substrate assessed as incorporation of tritium labeled methyl group from [3H]-SAM to biotinylated peptide substrate after 40 mins by scintillation proximity assay	B	6.64	pIC50	230	nM	IC50	ACS Med Chem Lett (2015) 6: 695-700 [PMID:26101576]
GtoPdb	-	-	6.92	pIC50	120	nM	IC50	Structure (2011) 19: 1262-73 [PMID:21782458]
ChEMBL	Inhibition of full length human SMYD2 amino acid 1 to 433 expressed in Escherichia coli BL21 (DE3) using Biotinaminohexanoyl- GSRAHSSHLKSKKGQSTSRH as substrate after 75 mins by AlphaScreen assay	B	6.92	pIC50	120	nM	IC50	Eur J Med Chem (2012) 56: 179-194 [PMID:22975593]
ChEMBL	Inhibition of recombinant full-length human SMYD2 (1 to 433) expressed in Escherichia coli BL21Star(DE3) cells using p53 peptide as substrate after 90 mins by scintillation proximity assay in presence of [3H]-SAM	B	6.92	pIC50	120	nM	IC50	ACS Med Chem Lett (2015) 6: 695-700 [PMID:26101576]
ChEMBL	Inhibition of SMYD2 (unknown origin) expressed in Escherichia coli BL21 (DE3) using Biotinaminohexanoyl-GSRAHSSHLKSKKGQSTSRH as substrate after 75 mins by scintillation proximity assay	B	6.92	pIC50	120	nM	IC50	J Med Chem (2016) 59: 4578-4600 [PMID:27075367]
ChEMBL	Inhibition of SMYD2 (unknown origin) using 3H-SAM as substrate incubated for 1 hr by filter binding method	B	6.92	pIC50	120	nM	IC50	Eur J Med Chem (2022) 227: 113880-113880 [PMID:34656041]
ChEMBL	Inhibition of recombinant human full-length SMYD2 (1 to 433) using biotin-aminohexanoyl GSRAHSSHLKSKKGQSTSRH as substrate after 75 mins by AlphaScreen assay	B	6.92	pIC50	120	nM	IC50	J Med Chem (2015) 58: 1596-1629 [PMID:25406853]
ChEMBL	Inhibition of full length human SMYD2 (1 to 433 residues) expressed in Escherichia coli strain BL21 (DE3) using p53 (361 to 380 residues) and [3H]-SAM as substrate incubated for 90 mins by SPA assay	B	6.92	pIC50	120	nM	IC50	J Med Chem (2022) 65: 10119-10132 [PMID:35914250]

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]