Target
Histone-lysine N-methyltransferase SMYD3
Ligand
BDBM377919
Substrate
n/a
Meas. Tech.
ChEMBL_1576442 (CHEMBL3803119)
IC50
17000±n/a nM
Citation
 Mitchell, LHBoriack-Sjodin, PASmith, SThomenius, MRioux, NMunchhof, MMills, JEKlaus, CTotman, JRiera, TVRaimondi, AJacques, SLWest, KFoley, MWaters, NJKuntz, KWWigle, TJScott, MPCopeland, RASmith, JJChesworth, R Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor. ACS Med Chem Lett 7:134-8 (2016) [PubMed]  Article 
Target
Name:
Histone-lysine N-methyltransferase SMYD3
Synonyms:
SET and MYND domain-containing protein 3 | SMYD3 | SMYD3_HUMAN | ZMYND1 | ZNFN3A1 | Zinc finger MYND domain-containing protein 1
Type:
Enzyme
Mol. Mass.:
49101.22
Organism:
Homo sapiens (Human)
Description:
Q9H7B4-2
Residue:
428
Sequence:
MEPLKVEKFATAKRGNGLRAVTPLRPGELLFRSDPLAYTVCKGSRGVVCDRCLLGKEKLMRCSQCRVAKYCSAKCQKKAWPDHKRECKCLKSCKPRYPPDSVRLLGRVVFKLMDGAPSESEKLYSFYDLESNINKLTEDKKEGLRQLVMTFQHFMREEIQDASQLPPAFDLFEAFAKVICNSFTICNAEMQEVGVGLYPSISLLNHSCDPNCSIVFNGPHLLLRAVRDIEVGEELTICYLDMLMTSEERRKQLRDQYCFECDCFRCQTQDKDADMLTGDEQVWKEVQESLKKIEELKAHWKWEQVLAMCQAIISSNSERLPDINIYQLKVLDCAMDACINLGLLEEALFYGTRTMEPYRIFFPGSHPVRGVQVMKVGKLQLHQGMFPQAMKNLRLAFDIMRVTHGREHSLIEDLILLLEECDANIRAS
  
Inhibitor
Name:
BDBM377919
Synonyms:
2-oxo-N-(piperidin-4-yl)indoline-5-carboxamide | US10266526, Compound 50
Type:
Small organic molecule
Emp. Form.:
C14H17N3O2
Mol. Mass.:
259.3037
SMILES:
O=C(NC1CCNCC1)c1ccc2NC(=O)Cc2c1
Structure:
Search PDB for entries with ligand similarity: