Target
Histone-lysine N-methyltransferase EHMT2
Ligand
BDBM50457756
Substrate
n/a
Meas. Tech.
ChEMBL_1760554 (CHEMBL4195562)
IC50
13±n/a nM
Citation
 Rabal, OSánchez-Arias, JASan José-Enériz, EAgirre, Xde Miguel, IGarate, LMiranda, ESáez, ERoa, SMartínez-Climent, JALiu, YWu, WXu, MProsper, FOyarzabal, J Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces. J Med Chem 61:6546-6573 (2018) [PubMed]  Article 
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:
BDBM50457756
Synonyms:
CHEMBL4203647
Type:
Small organic molecule
Emp. Form.:
C31H44N4O3
Mol. Mass.:
520.7061
SMILES:
COc1cc2c(NCC3CCN(CC3)C(C)C)cc(nc2cc1OCCCN1CCCC1)-c1ccc(C)o1
Structure:
Search PDB for entries with ligand similarity: