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Target
Lysine-specific demethylase 5C
Ligand
BDBM223317
Substrate
n/a
Meas. Tech.
AlphaScreen Assay
IC50
1e+3±1.3e+2 nM
Citation
 Tumber, A; Nuzzi, A; Hookway, ES; Hatch, SB; Velupillai, S; Johansson, C; Kawamura, A; Savitsky, P; Yapp, C; Szykowska, A; Wu, N; Bountra, C; Strain-Damerell, C; Burgess-Brown, NA; Ruda, GF; Fedorov, O; Munro, S; England, KS; Nowak, RP; Schofield, CJ; La Thangue, NB; Pawlyn, C; Davies, F; Morgan, G; Athanasou, N; Müller, S; Oppermann, U; Brennan, PE Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Cell Chem Biol 24:371-380 (2017) [PubMed]  Article 
Target
Name:
Lysine-specific demethylase 5C
Synonyms:
DXS1272E | Histone demethylase JARID1C | JARID1C | Jumonji/ARID domain-containing protein 1C | KDM5C | KDM5C_HUMAN | Lysine-specific demethylase 5C (KDM5C) | Lysine-specific demethylase 5C (KDM5Flag-5C-FL) | Protein SmcX | Protein Xe169 | SMCX | XE169
Type:
PROTEIN
Mol. Mass.:
175691.17
Organism:
Homo sapiens (Human)
Description:
P41229
Residue:
1560
Sequence:
MEPGSDDFLPPPECPVFEPSWAEFRDPLGYIAKIRPIAEKSGICKIRPPADWQPPFAVEVDNFRFTPRIQRLNELEAQTRVKLNYLDQIAKFWEIQGSSLKIPNVERRILDLYSLSKIVVEEGGYEAICKDRRWARVAQRLNYPPGKNIGSLLRSHYERIVYPYEMYQSGANLVQCNTRPFDNEEKDKEYKPHSIPLRQSVQPSKFNSYGRRAKRLQPDPEPTEEDIEKNPELKKLQIYGAGPKMMGLGLMAKDKTLRKKDKEGPECPPTVVVKEELGGDVKVESTSPKTFLESKEELSHSPEPCTKMTMRLRRNHSNAQFIESYVCRMCSRGDEDDKLLLCDGCDDNYHIFCLLPPLPEIPKGVWRCPKCVMAECKRPPEAFGFEQATREYTLQSFGEMADSFKADYFNMPVHMVPTELVEKEFWRLVNSIEEDVTVEYGADIHSKEFGSGFPVSDSKRHLTPEEEEYATSGWNLNVMPVLEQSVLCHINADISGMKVPWLYVGMVFSAFCWHIEDHWSYSINYLHWGEPKTWYGVPSLAAEHLEEVMKKLTPELFDSQPDLLHQLVTLMNPNTLMSHGVPVVRTNQCAGEFVITFPRAYHSGFNQGYNFAEAVNFCTADWLPAGRQCIEHYRRLRRYCVFSHEELICKMAACPEKLDLNLAAAVHKEMFIMVQEERRLRKALLEKGITEAEREAFELLPDDERQCIKCKTTCFLSALACYDCPDGLVCLSHINDLCKCSSSRQYLRYRYTLDELPAMLHKLKVRAESFDTWANKVRVALEVEDGRKRSLEELRALESEARERRFPNSELLQQLKNCLSEAEACVSRALGLVSGQEAGPHRVAGLQMTLTELRAFLDQMNNLPCAMHQIGDVKGVLEQVEAYQAEAREALASLPSSPGLLQSLLERGRQLGVEVPEAQQLQRQVEQARWLDEVKRTLAPSARRGTLAVMRGLLVAGASVAPSPAVDKAQAELQELLTIAERWEEKAHLCLEARQKHPPATLEAIIREAENIPVHLPNIQALKEALAKARAWIADVDEIQNGDHYPCLDDLEGLVAVGRDLPVGLEELRQLELQVLTAHSWREKASKTFLKKNSCYTLLEVLCPCADAGSDSTKRSRWMEKELGLYKSDTELLGLSAQDLRDPGSVIVAFKEGEQKEKEGILQLRRTNSAKPSPLASSSTASSTTSICVCGQVLAGAGALQCDLCQDWFHGRCVSVPRLLSSPRPNPTSSPLLAWWEWDTKFLCPLCMRSRRPRLETILALLVALQRLPVRLPEGEALQCLTERAISWQGRARQALASEDVTALLGRLAELRQRLQAEPRPEEPPNYPAAPASDPLREGSGKDMPKVQGLLENGDSVTSPEKVAPEEGSGKRDLELLSSLLPQLTGPVLELPEATRAPLEELMMEGDLLEVTLDENHSIWQLLQAGQPPDLERIRTLLELEKAERHGSRARGRALERRRRRKVDRGGEGDDPAREELEPKRVRSSGPEAEEVQEEEELEEETGGEGPPAPIPTTGSPSTQENQNGLEPAEGTTSGPSAPFSTLTPRLHLPCPQQPPQQQL
  
Inhibitor
Name:
BDBM223317
Synonyms:
KDOAM-1
Type:
Small organic molecule
Emp. Form.:
C11H15N3O2
Mol. Mass.:
221.2557
SMILES:
OC(=O)c1ccnc(CN2CCNCC2)c1
Structure:
Search PDB for entries with ligand similarity: