Target
Lysine-specific demethylase 5C
Ligand
BDBM281089
Substrate
n/a
Meas. Tech.
ChEBML_1685381
IC50
55±n/a nM
Citation
 Liang, JLabadie, SZhang, BOrtwine, DFPatel, SVinogradova, MKiefer, JRMauer, TGehling, VSHarmange, JCCummings, RLai, TLiao, JZheng, XLiu, YGustafson, AVan der Porten, EMao, WLiederer, BMDeshmukh, GAn, LRan, YClasson, MTrojer, PDragovich, PSMurray, L From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors. Bioorg Med Chem Lett 27:2974-2981 (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:
BDBM281089
Synonyms:
US10022354, Example 29
Type:
Small organic molecule
Emp. Form.:
C15H22N4O2
Mol. Mass.:
290.3608
SMILES:
CC(C)c1cc([nH]n1)C(=O)N1CC[C@H](C1)NC(=O)C1CC1 |r|
Structure:
Search PDB for entries with ligand similarity: