Target
Lysine-specific demethylase 5A [1-588]
Ligand
BDBM191596
Substrate
n/a
Meas. Tech.
Isothermal Titration Calorimetry (ITC)
Kd
27± 6 nM
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 5A [1-588]
Synonyms:
KDM5A_HUMAN | KDM5A | JARID1A | RBBP2 | RBP2 | Lysine-specific demethylase 5A (KDM5A(aa 1-588)-AP)
Type:
Protein
Mol. Mass.:
66955.44
Organism:
Human
Description:
Truncation 1-588 aa. Contains deletion of ARID and PhD1 domains.
Residue:
588
Sequence:
MAGVGPGGYAAEFVPPPECPVFEPSWEEFTDPLSFIGRIRPLAEKTGICKIRPPKDWQPPFACEVKSFRFTPRVQRLNELEAMTRVRLDFLDQLAKFWELQGSTLKIPVVERKILDLYALSKIVASKGGFEMVTKEKKWSKVGSRLGYLPGKGTGSLLKSHYERILYPYELFQSGVSLMGVQMPNLDLKEKVEPEVLSTDTQTSPEPGTRMNILPKRTRRVKTQSESGDVSRNTELKKLQIFGAGPKVVGLAMGTKDKEDEVTRRRKVTNRSDAFNMQMRQRKGTLSVNFVDLYVCMFCGRGNNEDKLLLCDGCDDSYHTFCLIPPLPDVPKGDWRCPKCVAEECSKPREAFGFEQAVREYTLQSFGEMADNFKSDYFNMPVHMVPTELVEKEFWRLVSSIEEDVIVEYGADISSKDFGSGFPVKDGRRKILPEEEEYALSGWNLNNMPVLEQSVLAHINVDISGMKVPWLYVGMCFSSFCWHIEDHWSYSINYLHWGEPKTWYGVPSHAAEQLEEVMRELAPELFESQPDLLHQLVTIMNPNVLMEHGVPVYRTNQCAGEFVVTFPRAYHSGFNQGYNFAEAVNFCT
  
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.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
Structure:
Search PDB for entries with ligand similarity: