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Target
Histone-lysine N-methyltransferase EHMT2
Ligand
BDBM50430056
Substrate
n/a
Meas. Tech.
ChEMBL_1722466 (CHEMBL4137466)
IC50
>10000±n/a nM
Citation
 Rabal, O; San José-Enériz, E; Agirre, X; Sánchez-Arias, JA; Vilas-Zornoza, A; Ugarte, A; de Miguel, I; Miranda, E; Garate, L; Fraga, M; Santamarina, P; Fernandez Perez, R; Ordoñez, R; Sáez, E; Roa, S; García-Barchino, MJ; Martínez-Climent, JA; Liu, Y; Wu, W; Xu, M; Prosper, F; Oyarzabal, J Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy. J Med Chem 61:6518-6545 (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:
BDBM50430056
Synonyms:
CHEMBL2336409 | SGI-1027
Type:
Small organic molecule
Emp. Form.:
C27H23N7O
Mol. Mass.:
461.5178
SMILES:
Cc1cc(Nc2ccc(NC(=O)c3ccc(Nc4ccnc5ccccc45)cc3)cc2)nc(N)n1
Structure:
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