Target
Histone-lysine N-methyltransferase EHMT2
Ligand
BDBM50592395
Substrate
n/a
Meas. Tech.
ChEMBL_2204070 (CHEMBL5116778)
IC50
54±n/a nM
Citation
 Randazzo, PSinisi, RGornati, DBertuolo, SBencheva, LDe Matteo, MNibbio, MMonteagudo, ETurcano, LBianconi, VPeruzzi, GSumma, VBresciani, AMozzetta, CDi Fabio, R Identification and in vitro characterization of a new series of potent and highly selective G9a inhibitors as novel anti-fibroadipogenic agents. Bioorg Med Chem Lett 72:0 (2022) [PubMed] 
Target
Name:
Histone-lysine N-methyltransferase EHMT2
Synonyms:
BAT8 | C6orf30 | EHMT2 | EHMT2_HUMAN | G9A | G9a histone methyltransferase (G9A) | Histone-lysine N-methyltransferase EHMT1/EHMT2 | Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 | KMT1C | NG36 | Protein G9a (G9a)
Type:
Enzyme
Mol. Mass.:
132339.87
Organism:
Homo sapiens (Human)
Description:
Q96KQ7
Residue:
1210
Sequence:
MAAAAGAAAAAAAEGEAPAEMGALLLEKETRGATERVHGSLGDTPRSEETLPKATPDSLEPAGPSSPASVTVTVGDEGADTPVGATPLIGDESENLEGDGDLRGGRILLGHATKSFPSSPSKGGSCPSRAKMSMTGAGKSPPSVQSLAMRLLSMPGAQGAAAAGSEPPPATTSPEGQPKVHRARKTMSKPGNGQPPVPEKRPPEIQHFRMSDDVHSLGKVTSDLAKRRKLNSGGGLSEELGSARRSGEVTLTKGDPGSLEEWETVVGDDFSLYYDSYSVDERVDSDSKSEVEALTEQLSEEEEEEEEEEEEEEEEEEEEEEEEDEESGNQSDRSGSSGRRKAKKKWRKDSPWVKPSRKRRKREPPRAKEPRGVNGVGSSGPSEYMEVPLGSLELPSEGTLSPNHAGVSNDTSSLETERGFEELPLCSCRMEAPKIDRISERAGHKCMATESVDGELSGCNAAILKRETMRPSSRVALMVLCETHRARMVKHHCCPGCGYFCTAGTFLECHPDFRVAHRFHKACVSQLNGMVFCPHCGEDASEAQEVTIPRGDGVTPPAGTAAPAPPPLSQDVPGRADTSQPSARMRGHGEPRRPPCDPLADTIDSSGPSLTLPNGGCLSAVGLPLGPGREALEKALVIQESERRKKLRFHPRQLYLSVKQGELQKVILMLLDNLDPNFQSDQQSKRTPLHAAAQKGSVEICHVLLQAGANINAVDKQQRTPLMEAVVNNHLEVARYMVQRGGCVYSKEEDGSTCLHHAAKIGNLEMVSLLLSTGQVDVNAQDSGGWTPIIWAAEHKHIEVIRMLLTRGADVTLTDNEENICLHWASFTGSAAIAEVLLNARCDLHAVNYHGDTPLHIAARESYHDCVLLFLSRGANPELRNKEGDTAWDLTPERSDVWFALQLNRKLRLGVGNRAIRTEKIICRDVARGYENVPIPCVNGVDGEPCPEDYKYISENCETSTMNIDRNITHLQHCTCVDDCSSSNCLCGQLSIRCWYDKDGRLLQEFNKIEPPLIFECNQACSCWRNCKNRVVQSGIKVRLQLYRTAKMGWGVRALQTIPQGTFICEYVGELISDAEADVREDDSYLFDLDNKDGEVYCIDARYYGNISRFINHLCDPNIIPVRVFMLHQDLRFPRIAFFSSRDIRTGEELGFDYGDRFWDIKSKYFTCQCGSEKCKHSAEAIALEQSRLARLDPHPELLPELGSLPPVNT
  
Inhibitor
Name:
BDBM50592395
Synonyms:
CHEMBL5183771
Type:
Small organic molecule
Emp. Form.:
C22H30N4O2
Mol. Mass.:
382.4992
SMILES:
COc1cc2c(ccnc2cc1OCCCN1CCCC1)N1CC2(CCN2)C1
Structure:
Search PDB for entries with ligand similarity: