ChEMBL ligand: CHEMBL3798741
SET and MYND domain containing 3/Histone-lysine N-methyltransferase SMYD3 in Human [ChEMBL: CHEMBL2321643] [GtoPdb: 3313] [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
SET and MYND domain containing 3/Histone-lysine N-methyltransferase SMYD3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321643] [GtoPdb: 3313] [UniProtKB: Q9H7B4]
ChEMBL	Non-competitive inhibition of full length N-terminal His-tagged SMYD3 (1 to 428 residues) (unknown origin) expressed in Escherichia coli using fixed N-terminal GST-tagged MEKK2 substrate and varying SAM levels preincubated for 30 mins followed by substrate addition by filter plate assay	B	8.92	pKi	1.2	nM	Ki	ACS Med Chem Lett (2016) 7: 134-138 [PMID:26985287]
ChEMBL	Non-competitive inhibition of full length N-terminal His-tagged SMYD3 (1 to 428 residues) (unknown origin) expressed in Escherichia coli using varying N-terminal GST-tagged MEKK2 substrate and fixed SAM levels preincubated for 30 mins followed by substrate addition by filter plate assay	B	8.96	pKi	1.1	nM	Ki	ACS Med Chem Lett (2016) 7: 134-138 [PMID:26985287]
ChEMBL	Inhibition of human SMYD3 expressed in HEK293T/17 cells using FLAG-tagged MEKK2 as substrate incubated for 30 mins in low air flow area followed by incubation for 24 hrs at 37 degC by Western blot analysis	B	7.44	pIC50	36	nM	IC50	ACS Med Chem Lett (2016) 7: 134-138 [PMID:26985287]
GtoPdb	Enzyme inhibition in a biochemical assay	-	8.52	pIC50	3	nM	IC50	ACS Med Chem Lett (2016) 7: 134-8 [PMID:26985287]
ChEMBL	Inhibition of full length N-terminal His-tagged SMYD3 (1 to 428 residues) (unknown origin) expressed in Escherichia coli using N-terminal GST-tagged MEKK2 as substrate preincubated for 30 mins followed by substrate addition by scintillation proximity assay in presence of [3H]SAM	B	8.52	pIC50	3	nM	IC50	ACS Med Chem Lett (2016) 7: 134-138 [PMID:26985287]
SET and MYND domain containing 2/N-lysine methyltransferase SMYD2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2169716] [GtoPdb: 2714] [UniProtKB: Q9NRG4]
ChEMBL	Inhibition of SMYD2 (unknown origin)	B	4.3	pIC50	>50000	nM	IC50	ACS Med Chem Lett (2016) 7: 134-138 [PMID:26985287]

ChEMBL data shown on this page come from version 35:

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]