Reaction Details Report a problem with these data
Target
Histone-lysine N-methyltransferase EHMT2
Ligand
BDBM225263
Substrate
n/a
Meas. Tech.
Enzymatic Assay
pH
8.5±n/a
Temperature
298.15±n/a K
IC50
6.10e+3± 3.8e+2 nM
Comments
extracted
Citation
 Zhang, J; Yao, D; Jiang, Y; Huang, J; Yang, S; Wang, J Synthesis and biological evaluation of benzimidazole derivatives as the G9a Histone Methyltransferase inhibitors that induce autophagy and apoptosis of breast cancer cells. Bioorg Chem 72:168-181 (2017) [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:
BDBM225263
Synonyms:
Brd4470
Type:
Small organic molecule
Emp. Form.:
C25H23N3O3
Mol. Mass.:
413.4684
SMILES:
COC(=O)c1ccc2n(CCCc3ccccc3)c(NC(=O)c3ccccc3)nc2c1
Structure:
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