Reaction Details |
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Target | Histone-lysine N-methyltransferase EHMT2 |
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Ligand | BDBM50323808 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_647515 (CHEMBL1217455) |
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IC50 | 8000±n/a nM |
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Citation | Liu, F; Chen, X; Allali-Hassani, A; Quinn, AM; Wigle, TJ; Wasney, GA; Dong, A; Senisterra, G; Chau, I; Siarheyeva, A; Norris, JL; Kireev, DB; Jadhav, A; Herold, JM; Janzen, WP; Arrowsmith, CH; Frye, SV; Brown, PJ; Simeonov, A; Vedadi, M; Jin, J Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem53:5844-57 (2010) [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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BDBM50323808 |
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n/a |
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Name | BDBM50323808 |
Synonyms: | 6-Methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine | CHEMBL1213903 |
Type | Small organic molecule |
Emp. Form. | C28H45N7O2 |
Mol. Mass. | 511.7026 |
SMILES | COc1cc2c(NC3CCN(C)CC3)nc(nc2cc1OCCCN1CCCC1)N1CCCN(C)CC1 |
Structure |
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