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TargetHomo sapiens lysine demethylase 2A (KDM2A)
LigandBDBM50153093
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1562165
IC50 2400±n/a nM
Citation Bavetsias VLanigan RMRuda GFAtrash BMcLaughlin MGTumber AMok NYLe Bihan YVDempster SBoxall KJJeganathan FHatch SBSavitsky PVelupillai SKrojer TEngland KSSejberg JThai CDonovan APal AScozzafava GBennett JMKawamura AJohansson CSzykowska AGileadi CBurgess-Brown NAvon Delft FOppermann UWalters ZShipley JRaynaud FIWestaway SMPrinjha RKFedorov OBurke RSchofield CJWestwood IMBountra CMüller Svan Montfort RLBrennan PEBlagg J 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors. J Med Chem 59:1388-409 (2016) [PubMed]
More Info.:Get all data from this article,  Assay Method
 
Homo sapiens lysine demethylase 2A (KDM2A)
Name:Homo sapiens lysine demethylase 2A (KDM2A)
Synonyms:AA1-1162 | F-box and leucine-rich repeat protein 11 | FBXL11 | Lysine-specific demethylase 2A | Lysine-specific demethylase 2A (KDM2A) | NM_012308
Type:Enzyme Catalytic Domain
Mol. Mass.:132809.04
Organism:Homo sapiens (Human)
Description:n/a
Residue:1162
Sequence:
MEPEEERIRYSQRLRGTMRRRYEDDGISDDEIEGKRTFDLEEKLHTNKYNANFVTFMEGK
DFNVEYIQRGGLRDPLIFKNSDGLGIKMPDPDFTVNDVKMCVGSRRMVDVMDVNTQKGIE
MTMAQWTRYYETPEEEREKLYNVISLEFSHTRLENMVQRPSTVDFIDWVDNMWPRHLKES
QTESTNAILEMQYPKVQKYCLMSVRGCYTDFHVDFGGTSVWYHIHQGGKVFWLIPPTAHN
LELYENWLLSGKQGDIFLGDRVSDCQRIELKQGYTFVIPSGWIHAVYTPTDTLVFGGNFL
HSFNIPMQLKIYNIEDRTRVPNKFRYPFYYEMCWYVLERYVYCITNRSHLTKEFQKESLS
MDLELNGLESGNGDEEAVDREPRRLSSRRSVLTSPVANGVNLDYDGLGKTCRSLPSLKKT
LAGDSSSDCSRGSHNGQVWDPQCAPRKDRQVHLTHFELEGLRCLVDKLESLPLHKKCVPT
GIEDEDALIADVKILLEELANSDPKLALTGVPIVQWPKRDKLKFPTRPKVRVPTIPITKP
HTMKPAPRLTPVRPAAASPIVSGARRRRVRCRKCKACVQGECGVCHYCRDMKKFGGPGRM
KQSCVLRQCLAPRLPHSVTCSLCGEVDQNEETQDFEKKLMECCICNEIVHPGCLQMDGEG
LLNEELPNCWECPKCYQEDSSEKAQKRKMEESDEEAVQAKVLRPLRSCDEPLTPPPHSPT
SMLQLIHDPVSPRGMVTRSSPGAGPSDHHSASRDERFKRRQLLRLQATERTMVREKENNP
SGKKELSEVEKAKIRGSYLTVTLQRPTKELHGTSIVPKLQAITASSANLRHSPRVLVQHC
PARTPQRGDEEGLGGEEEEEEEEEEEDDSAEEGGAARLNGRGSWAQDGDESWMQREVWMS
VFRYLSRRELCECMRVCKTWYKWCCDKRLWTKIDLSRCKAIVPQALSGIIKRQPVSLDLS
WTNISKKQLTWLVNRLPGLKDLLLAGCSWSAVSALSTSSCPLLRTLDLRWAVGIKDPQIR
DLLTPPADKPGQDNRSKLRNMTDFRLAGLDITDATLRLIIRHMPLLSRLDLSHCSHLTDQ
SSNLLTAVGSSTRYSLTELNMAGCNKLTDQTLIYLRRIANVTLIDLRGCKQITRKACEHF
ISDLSINSLYCLSDEKLIQKIS
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BDBM50153093
n/a
NameBDBM50153093
Synonyms:CHEMBL3775668
TypeSmall organic molecule
Emp. Form.C21H22N6OS
Mol. Mass.406.504
SMILESO=c1[nH]cnc2c(nccc12)-n1cc(CCN2CCC(CC2)c2cccs2)cn1
Structure
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