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TargetLysine-specific demethylase 5B
LigandBDBM50153069
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1561971
IC50 18±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
 
Lysine-specific demethylase 5B
Name:Lysine-specific demethylase 5B
Synonyms:CT31 | Cancer/testis antigen 31 | Histone demethylase JARID1B | JARID1B | Jumonji/ARID domain-containing protein 1B | KDM5B | Lysine-specific demethylase 5B (KDM5B) | Lysine-specific demethylase 5B (KDM5Flag-5B-FL) | PLU-1 | PLU1 | RBBP2H1 | RBP2-H1 | Retinoblastoma-binding protein 2 homolog 1
Type:Protein
Mol. Mass.:175659.67
Organism:Homo sapiens (Human)
Description:Q9UGL1
Residue:1544
Sequence:
MEAATTLHPGPRPALPLGGPGPLGEFLPPPECPVFEPSWEEFADPFAFIHKIRPIAEQTG
ICKVRPPPDWQPPFACDVDKLHFTPRIQRLNELEAQTRVKLNFLDQIAKYWELQGSTLKI
PHVERKILDLFQLNKLVAEEGGFAVVCKDRKWTKIATKMGFAPGKAVGSHIRGHYERILN
PYNLFLSGDSLRCLQKPNLTTDTKDKEYKPHDIPQRQSVQPSETCPPARRAKRMRAEAMN
IKIEPEETTEARTHNLRRRMGCPTPKCENEKEMKSSIKQEPIERKDYIVENEKEKPKSRS
KKATNAVDLYVCLLCGSGNDEDRLLLCDGCDDSYHTFCLIPPLHDVPKGDWRCPKCLAQE
CSKPQEAFGFEQAARDYTLRTFGEMADAFKSDYFNMPVHMVPTELVEKEFWRLVSTIEED
VTVEYGADIASKEFGSGFPVRDGKIKLSPEEEEYLDSGWNLNNMPVMEQSVLAHITADIC
GMKLPWLYVGMCFSSFCWHIEDHWSYSINYLHWGEPKTWYGVPGYAAEQLENVMKKLAPE
LFVSQPDLLHQLVTIMNPNTLMTHEVPVYRTNQCAGEFVITFPRAYHSGFNQGFNFAEAV
NFCTVDWLPLGRQCVEHYRLLHRYCVFSHDEMICKMASKADVLDVVVASTVQKDMAIMIE
DEKALRETVRKLGVIDSERMDFELLPDDERQCVKCKTTCFMSAISCSCKPGLLVCLHHVK
ELCSCPPYKYKLRYRYTLDDLYPMMNALKLRAESYNEWALNVNEALEAKINKKKSLVSFK
ALIEESEMKKFPDNDLLRHLRLVTQDAEKCASVAQQLLNGKRQTRYRSGGGKSQNQLTVN
ELRQFVTQLYALPCVLSQTPLLKDLLNRVEDFQQHSQKLLSEETPSAAELQDLLDVSFEF
DVELPQLAEMRIRLEQARWLEEVQQACLDPSSLTLDDMRRLIDLGVGLAPYSAVEKAMAR
LQELLTVSEHWDDKAKSLLKARPRHSLNSLATAVKEIEEIPAYLPNGAALKDSVQRARDW
LQDVEGLQAGGRVPVLDTLIELVTRGRSIPVHLNSLPRLETLVAEVQAWKECAVNTFLTE
NSPYSLLEVLCPRCDIGLLGLKRKQRKLKEPLPNGKKKSTKLESLSDLERALTESKETAS
AMATLGEARLREMEALQSLRLANEGKLLSPLQDVDIKICLCQKAPAAPMIQCELCRDAFH
TSCVAVPSISQGLRIWLCPHCRRSEKPPLEKILPLLASLQRIRVRLPEGDALRYMIERTV
NWQHRAQQLLSSGNLKFVQDRVGSGLLYSRWQASAGQVSDTNKVSQPPGTTSFSLPDDWD
NRTSYLHSPFSTGRSCIPLHGVSPEVNELLMEAQLLQVSLPEIQELYQTLLAKPSPAQQT
DRSSPVRPSSEKNDCCRGKRDGINSLERKLKRRLEREGLSSERWERVKKMRTPKKKKIKL
SHPKDMNNFKLERERSYELVRSAETHSLPSDTSYSEQEDSEDEDAICPAVSCLQPEGDEV
DWVQCDGSCNQWFHQVCVGVSPEMAEKEDYICVRCTVKDAPSRK
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  Blast E-value cutoff:
BDBM50153069
n/a
NameBDBM50153069
Synonyms:CHEMBL3775953
TypeSmall organic molecule
Emp. Form.C23H23FN6O
Mol. Mass.418.4667
SMILESFc1ccc(cc1)C1CCN(CCc2cnn(c2)-c2nccc3c2nc[nH]c3=O)CC1
Structure
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