Target
Lysine-specific demethylase 5B [1-755]
Ligand
BDBM191596
Substrate
n/a
Meas. Tech.
Formaldehyde Dehydrogenase-Coupled Demethylase (FDH) Assay
Temperature
298.15±n/a K
IC50
7e+2± 1e+2 nM
Comments
extracted
Citation
 Horton, JRLiu, XGale, MWu, LShanks, JRZhang, XWebber, PJBell, JSKales, SCMott, BTRai, GJansen, DJHenderson, MJUrban, DJHall, MDSimeonov, AMaloney, DJJohns, MAFu, HJadhav, AVertino, PMYan, QCheng, 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 [1-755]
Synonyms:
JARID1B | KDM5B | KDM5B_HUMAN | Lysine-specific demethylase 5B (KDM5B(aa 1-755)-AP) | PLU1 | RBBP2H1
Type:
Protein
Mol. Mass.:
86559.22
Organism:
Homo sapiens (Human)
Description:
Truncation 1-755 aa. Contains deletion of ARID and PhD1 domains.
Residue:
755
Sequence:
MEAATTLHPGPRPALPLGGPGPLGEFLPPPECPVFEPSWEEFADPFAFIHKIRPIAEQTGICKVRPPPDWQPPFACDVDKLHFTPRIQRLNELEAQTRVKLNFLDQIAKYWELQGSTLKIPHVERKILDLFQLNKLVAEEGGFAVVCKDRKWTKIATKMGFAPGKAVGSHIRGHYERILNPYNLFLSGDSLRCLQKPNLTTDTKDKEYKPHDIPQRQSVQPSETCPPARRAKRMRAEAMNIKIEPEETTEARTHNLRRRMGCPTPKCENEKEMKSSIKQEPIERKDYIVENEKEKPKSRSKKATNAVDLYVCLLCGSGNDEDRLLLCDGCDDSYHTFCLIPPLHDVPKGDWRCPKCLAQECSKPQEAFGFEQAARDYTLRTFGEMADAFKSDYFNMPVHMVPTELVEKEFWRLVSTIEEDVTVEYGADIASKEFGSGFPVRDGKIKLSPEEEEYLDSGWNLNNMPVMEQSVLAHITADICGMKLPWLYVGMCFSSFCWHIEDHWSYSINYLHWGEPKTWYGVPGYAAEQLENVMKKLAPELFVSQPDLLHQLVTIMNPNTLMTHEVPVYRTNQCAGEFVITFPRAYHSGFNQGFNFAEAVNFCTVDWLPLGRQCVEHYRLLHRYCVFSHDEMICKMASKADVLDVVVASTVQKDMAIMIEDEKALRETVRKLGVIDSERMDFELLPDDERQCVKCKTTCFMSAISCSCKPGLLVCLHHVKELCSCPPYKYKLRYRYTLDDLYPMMNALKLRAESY
  
Inhibitor
Name:
BDBM191596
Synonyms:
6-isopropyl-5-methyl-7-oxo-4,7-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile (N8)
Type:
Small organic molecule
Emp. Form.:
C11H12N4O
Mol. Mass.:
216.2392
SMILES:
CC(C)c1c(C)[nH]c2c(cnn2c1=O)C#N
Structure:
Search PDB for entries with ligand similarity: