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TargetLysine-specific demethylase 2A
LigandBDBM191598
Substrate/Competitorn/a
Meas. Tech.AlphaScreen Assay
IC50 2e+3±2.3e+2 nM
Citation Tumber, ANuzzi, AHookway, ESHatch, SBVelupillai, SJohansson, CKawamura, ASavitsky, PYapp, CSzykowska, AWu, NBountra, CStrain-Damerell, CBurgess-Brown, NARuda, GFFedorov, OMunro, SEngland, KSNowak, RPSchofield, CJLa Thangue, NBPawlyn, CDavies, FMorgan, GAthanasou, NMüller, SOppermann, UBrennan, PE Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Cell Chem Biol24:371-380 (2017) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Lysine-specific demethylase 2A
Name:Lysine-specific demethylase 2A
Synonyms:F-box and leucine-rich repeat protein 11 | Lysine-specific demethylase 2A (KDM2A)
Type:PROTEIN
Mol. Mass.:132809.04
Organism:Homo sapiens
Description:Q9Y2K7
Residue:1162
Sequence:
MEPEEERIRYSQRLRGTMRRRYEDDGISDDEIEGKRTFDLEEKLHTNKYNANFVTFMEGK
DFNVEYIQRGGLRDPLIFKNSDGLGIKMPDPDFTVNDVKMCVGSRRMVDVMDVNTQKGIE
MTMAQWTRYYETPEEEREKLYNVISLEFSHTRLENMVQRPSTVDFIDWVDNMWPRHLKES
QTESTNAILEMQYPKVQKYCLMSVRGCYTDFHVDFGGTSVWYHIHQGGKVFWLIPPTAHN
LELYENWLLSGKQGDIFLGDRVSDCQRIELKQGYTFVIPSGWIHAVYTPTDTLVFGGNFL
HSFNIPMQLKIYNIEDRTRVPNKFRYPFYYEMCWYVLERYVYCITNRSHLTKEFQKESLS
MDLELNGLESGNGDEEAVDREPRRLSSRRSVLTSPVANGVNLDYDGLGKTCRSLPSLKKT
LAGDSSSDCSRGSHNGQVWDPQCAPRKDRQVHLTHFELEGLRCLVDKLESLPLHKKCVPT
GIEDEDALIADVKILLEELANSDPKLALTGVPIVQWPKRDKLKFPTRPKVRVPTIPITKP
HTMKPAPRLTPVRPAAASPIVSGARRRRVRCRKCKACVQGECGVCHYCRDMKKFGGPGRM
KQSCVLRQCLAPRLPHSVTCSLCGEVDQNEETQDFEKKLMECCICNEIVHPGCLQMDGEG
LLNEELPNCWECPKCYQEDSSEKAQKRKMEESDEEAVQAKVLRPLRSCDEPLTPPPHSPT
SMLQLIHDPVSPRGMVTRSSPGAGPSDHHSASRDERFKRRQLLRLQATERTMVREKENNP
SGKKELSEVEKAKIRGSYLTVTLQRPTKELHGTSIVPKLQAITASSANLRHSPRVLVQHC
PARTPQRGDEEGLGGEEEEEEEEEEEDDSAEEGGAARLNGRGSWAQDGDESWMQREVWMS
VFRYLSRRELCECMRVCKTWYKWCCDKRLWTKIDLSRCKAIVPQALSGIIKRQPVSLDLS
WTNISKKQLTWLVNRLPGLKDLLLAGCSWSAVSALSTSSCPLLRTLDLRWAVGIKDPQIR
DLLTPPADKPGQDNRSKLRNMTDFRLAGLDITDATLRLIIRHMPLLSRLDLSHCSHLTDQ
SSNLLTAVGSSTRYSLTELNMAGCNKLTDQTLIYLRRIANVTLIDLRGCKQITRKACEHF
ISDLSINSLYCLSDEKLIQKIS
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM191598
NameBDBM191598
Synonyms:2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinic acid (KDM5-C49) | KDM5-C49 | KDOAM-20
TypeSmall organic molecule
Emp. Form.C15H24N4O3
Mol. Mass.308.3761
SMILESCCN(CCN(C)C)C(=O)CNCc1cc(ccn1)C(O)=O
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
n/a