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Target
Lysine-specific demethylase 5B
Ligand
BDBM191604
Substrate
n/a
Meas. Tech.
AlphaLISA Assay
pH
7.2±n/a
Temperature
298.15±n/a K
IC50
5e+3± 2e+3 nM
Comments
extracted
Citation
 Horton, JR; Liu, X; Gale, M; Wu, L; Shanks, JR; Zhang, X; Webber, PJ; Bell, JS; Kales, SC; Mott, BT; Rai, G; Jansen, DJ; Henderson, MJ; Urban, DJ; Hall, MD; Simeonov, A; Maloney, DJ; Johns, MA; Fu, H; Jadhav, A; Vertino, PM; Yan, Q; Cheng, X Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds. Cell Chem Biol 23:769-81 (2016) [PubMed]  Article 
Target
Name:
Lysine-specific demethylase 5B
Synonyms:
CT31 | Cancer/testis antigen 31 | Histone demethylase JARID1B | JARID1B | Jumonji/ARID domain-containing protein 1B | KDM5B | KDM5B_HUMAN | 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:
MEAATTLHPGPRPALPLGGPGPLGEFLPPPECPVFEPSWEEFADPFAFIHKIRPIAEQTGICKVRPPPDWQPPFACDVDKLHFTPRIQRLNELEAQTRVKLNFLDQIAKYWELQGSTLKIPHVERKILDLFQLNKLVAEEGGFAVVCKDRKWTKIATKMGFAPGKAVGSHIRGHYERILNPYNLFLSGDSLRCLQKPNLTTDTKDKEYKPHDIPQRQSVQPSETCPPARRAKRMRAEAMNIKIEPEETTEARTHNLRRRMGCPTPKCENEKEMKSSIKQEPIERKDYIVENEKEKPKSRSKKATNAVDLYVCLLCGSGNDEDRLLLCDGCDDSYHTFCLIPPLHDVPKGDWRCPKCLAQECSKPQEAFGFEQAARDYTLRTFGEMADAFKSDYFNMPVHMVPTELVEKEFWRLVSTIEEDVTVEYGADIASKEFGSGFPVRDGKIKLSPEEEEYLDSGWNLNNMPVMEQSVLAHITADICGMKLPWLYVGMCFSSFCWHIEDHWSYSINYLHWGEPKTWYGVPGYAAEQLENVMKKLAPELFVSQPDLLHQLVTIMNPNTLMTHEVPVYRTNQCAGEFVITFPRAYHSGFNQGFNFAEAVNFCTVDWLPLGRQCVEHYRLLHRYCVFSHDEMICKMASKADVLDVVVASTVQKDMAIMIEDEKALRETVRKLGVIDSERMDFELLPDDERQCVKCKTTCFMSAISCSCKPGLLVCLHHVKELCSCPPYKYKLRYRYTLDDLYPMMNALKLRAESYNEWALNVNEALEAKINKKKSLVSFKALIEESEMKKFPDNDLLRHLRLVTQDAEKCASVAQQLLNGKRQTRYRSGGGKSQNQLTVNELRQFVTQLYALPCVLSQTPLLKDLLNRVEDFQQHSQKLLSEETPSAAELQDLLDVSFEFDVELPQLAEMRIRLEQARWLEEVQQACLDPSSLTLDDMRRLIDLGVGLAPYSAVEKAMARLQELLTVSEHWDDKAKSLLKARPRHSLNSLATAVKEIEEIPAYLPNGAALKDSVQRARDWLQDVEGLQAGGRVPVLDTLIELVTRGRSIPVHLNSLPRLETLVAEVQAWKECAVNTFLTENSPYSLLEVLCPRCDIGLLGLKRKQRKLKEPLPNGKKKSTKLESLSDLERALTESKETASAMATLGEARLREMEALQSLRLANEGKLLSPLQDVDIKICLCQKAPAAPMIQCELCRDAFHTSCVAVPSISQGLRIWLCPHCRRSEKPPLEKILPLLASLQRIRVRLPEGDALRYMIERTVNWQHRAQQLLSSGNLKFVQDRVGSGLLYSRWQASAGQVSDTNKVSQPPGTTSFSLPDDWDNRTSYLHSPFSTGRSCIPLHGVSPEVNELLMEAQLLQVSLPEIQELYQTLLAKPSPAQQTDRSSPVRPSSEKNDCCRGKRDGINSLERKLKRRLEREGLSSERWERVKKMRTPKKKKIKLSHPKDMNNFKLERERSYELVRSAETHSLPSDTSYSEQEDSEDEDAICPAVSCLQPEGDEVDWVQCDGSCNQWFHQVCVGVSPEMAEKEDYICVRCTVKDAPSRK
  
Inhibitor
Name:
BDBM191604
Synonyms:
8-(1-methyl-1Himidazol-4-yl)-2-(4,4,4-trifluorobutoxy)pyrido[3,4-d]pyrimidin-4-ol (N10)
Type:
Small organic molecule
Emp. Form.:
C15H14F3N5O2
Mol. Mass.:
353.2992
SMILES:
Cn1cnc(c1)-c1nccc2c(O)nc(OCCCC(F)(F)F)nc12
Structure:
Search PDB for entries with ligand similarity: