Reaction Details |
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Target | Histone-lysine N-methyltransferase EHMT2 |
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Ligand | BDBM50300032 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_593231 (CHEMBL1046738) |
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IC50 | 1600±n/a nM |
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Citation | Liu, F; Chen, X; Allali-Hassani, A; Quinn, AM; Wasney, GA; Dong, A; Barsyte, D; Kozieradzki, I; Senisterra, G; Chau, I; Siarheyeva, A; Kireev, DB; Jadhav, A; Herold, JM; Frye, SV; Arrowsmith, CH; Brown, PJ; Simeonov, A; Vedadi, M; Jin, J Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a. J Med Chem52:7950-3 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Histone-lysine N-methyltransferase EHMT2 |
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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: | MAAAAGAAAAAAAEGEAPAEMGALLLEKETRGATERVHGSLGDTPRSEETLPKATPDSLE
PAGPSSPASVTVTVGDEGADTPVGATPLIGDESENLEGDGDLRGGRILLGHATKSFPSSP
SKGGSCPSRAKMSMTGAGKSPPSVQSLAMRLLSMPGAQGAAAAGSEPPPATTSPEGQPKV
HRARKTMSKPGNGQPPVPEKRPPEIQHFRMSDDVHSLGKVTSDLAKRRKLNSGGGLSEEL
GSARRSGEVTLTKGDPGSLEEWETVVGDDFSLYYDSYSVDERVDSDSKSEVEALTEQLSE
EEEEEEEEEEEEEEEEEEEEEEEDEESGNQSDRSGSSGRRKAKKKWRKDSPWVKPSRKRR
KREPPRAKEPRGVNGVGSSGPSEYMEVPLGSLELPSEGTLSPNHAGVSNDTSSLETERGF
EELPLCSCRMEAPKIDRISERAGHKCMATESVDGELSGCNAAILKRETMRPSSRVALMVL
CETHRARMVKHHCCPGCGYFCTAGTFLECHPDFRVAHRFHKACVSQLNGMVFCPHCGEDA
SEAQEVTIPRGDGVTPPAGTAAPAPPPLSQDVPGRADTSQPSARMRGHGEPRRPPCDPLA
DTIDSSGPSLTLPNGGCLSAVGLPLGPGREALEKALVIQESERRKKLRFHPRQLYLSVKQ
GELQKVILMLLDNLDPNFQSDQQSKRTPLHAAAQKGSVEICHVLLQAGANINAVDKQQRT
PLMEAVVNNHLEVARYMVQRGGCVYSKEEDGSTCLHHAAKIGNLEMVSLLLSTGQVDVNA
QDSGGWTPIIWAAEHKHIEVIRMLLTRGADVTLTDNEENICLHWASFTGSAAIAEVLLNA
RCDLHAVNYHGDTPLHIAARESYHDCVLLFLSRGANPELRNKEGDTAWDLTPERSDVWFA
LQLNRKLRLGVGNRAIRTEKIICRDVARGYENVPIPCVNGVDGEPCPEDYKYISENCETS
TMNIDRNITHLQHCTCVDDCSSSNCLCGQLSIRCWYDKDGRLLQEFNKIEPPLIFECNQA
CSCWRNCKNRVVQSGIKVRLQLYRTAKMGWGVRALQTIPQGTFICEYVGELISDAEADVR
EDDSYLFDLDNKDGEVYCIDARYYGNISRFINHLCDPNIIPVRVFMLHQDLRFPRIAFFS
SRDIRTGEELGFDYGDRFWDIKSKYFTCQCGSEKCKHSAEAIALEQSRLARLDPHPELLP
ELGSLPPVNT
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BDBM50300032 |
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n/a |
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Name | BDBM50300032 |
Synonyms: | 6,7-Dimethoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine | CHEMBL571717 |
Type | Small organic molecule |
Emp. Form. | C20H29N5O3 |
Mol. Mass. | 387.476 |
SMILES | COc1cc2nc(nc(NC3CCN(C)CC3)c2cc1OC)N1CCOCC1 |
Structure |
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