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TargetLysine-specific demethylase 6B
LigandBDBM191599
Substrate/Competitorn/a
Meas. Tech.AlphaScreen Assay
IC50 1e+4±3.0e+3 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 6B
Name:Lysine-specific demethylase 6B
Synonyms:JMJD3 | JmjC domain-containing protein 3 | Jumonji domain-containing protein 3 | KDM6B | KDM6B_HUMAN | KIAA0346 | Lysine demethylase 6B | Lysine-specific demethylase 6B | Lysine-specific demethylase 6B (KDM6B(JMJD3)) | Lysine-specific demethylase 6B (KDM6B)
Type:Protein
Mol. Mass.:176672.55
Organism:Homo sapiens (Human)
Description:O15054
Residue:1643
Sequence:
MHRAVDPPGARAAREAFALGGLSCAGAWSSCPPHPPPRSAWLPGGRCSASIGQPPLPAPL
PPSHGSSSGHPSKPYYAPGAPTPRPLHGKLESLHGCVQALLREPAQPGLWEQLGQLYESE
HDSEEATRCYHSALRYGGSFAELGPRIGRLQQAQLWNFHTGSCQHRAKVLPPLEQVWNLL
HLEHKRNYGAKRGGPPVKRAAEPPVVQPVPPAALSGPSGEEGLSPGGKRRRGCNSEQTGL
PPGLPLPPPPLPPPPPPPPPPPPPLPGLATSPPFQLTKPGLWSTLHGDAWGPERKGSAPP
ERQEQRHSLPHPYPYPAPAYTAHPPGHRLVPAAPPGPGPRPPGAESHGCLPATRPPGSDL
RESRVQRSRMDSSVSPAATTACVPYAPSRPPGLPGTTTSSSSSSSSNTGLRGVEPNPGIP
GADHYQTPALEVSHHGRLGPSAHSSRKPFLGAPAATPHLSLPPGPSSPPPPPCPRLLRPP
PPPAWLKGPACRAAREDGEILEELFFGTEGPPRPAPPPLPHREGFLGPPASRFSVGTQDS
HTPPTPPTPTTSSSNSNSGSHSSSPAGPVSFPPPPYLARSIDPLPRPPSPAQNPQDPPLV
PLTLALPPAPPSSCHQNTSGSFRRPESPRPRVSFPKTPEVGPGPPPGPLSKAPQPVPPGV
GELPARGPRLFDFPPTPLEDQFEEPAEFKILPDGLANIMKMLDESIRKEEEQQQHEAGVA
PQPPLKEPFASLQSPFPTDTAPTTTAPAVAVTTTTTTTTTTTATQEEEKKPPPALPPPPP
LAKFPPPSQPQPPPPPPPSPASLLKSLASVLEGQKYCYRGTGAAVSTRPGPLPTTQYSPG
PPSGATALPPTSAAPSAQGSPQPSASSSSQFSTSGGPWARERRAGEEPVPGPMTPTQPPP
PLSLPPARSESEVLEEISRACETLVERVGRSATDPADPVDTAEPADSGTERLLPPAQAKE
EAGGVAAVSGSCKRRQKEHQKEHRRHRRACKDSVGRRPREGRAKAKAKVPKEKSRRVLGN
LDLQSEEIQGREKSRPDLGGASKAKPPTAPAPPSAPAPSAQPTPPSASVPGKKAREEAPG
PPGVSRADMLKLRSLSEGPPKELKIRLIKVESGDKETFIASEVEERRLRMADLTISHCAA
DVVRASRNAKVKGKFRESYLSPAQSVKPKINTEEKLPREKLNPPTPSIYLESKRDAFSPV
LLQFCTDPRNPITVIRGLAGSLRLNLGLFSTKTLVEASGEHTVEVRTQVQQPSDENWDLT
GTRQIWPCESSRSHTTIAKYAQYQASSFQESLQEEKESEDEESEEPDSTTGTPPSSAPDP
KNHHIIKFGTNIDLSDAKRWKPQLQELLKLPAFMRVTSTGNMLSHVGHTILGMNTVQLYM
KVPGSRTPGHQENNNFCSVNINIGPGDCEWFAVHEHYWETISAFCDRHGVDYLTGSWWPI
LDDLYASNIPVYRFVQRPGDLVWINAGTVHWVQATGWCNNIAWNVGPLTAYQYQLALERY
EWNEVKNVKSIVPMIHVSWNVARTVKISDPDLFKMIKFCLLQSMKHCQVQRESLVRAGKK
IAYQGRVKDEPAYYCNECDVEVFNILFVTSENGSRNTYLVHCEGCARRRSAGLQGVVVLE
QYRTEELAQAYDAFTLAPASTSR
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM191599
n/a
NameBDBM191599
Synonyms:KDOAM-21 | ethyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate (KDM5-C70)
TypeSmall organic molecule
Emp. Form.C17H28N4O3
Mol. Mass.336.4292
SMILESCCOC(=O)c1ccnc(CNCC(=O)N(CC)CCN(C)C)c1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: