Target
Lysine-specific demethylase 5A [1-588]
Ligand
BDBM191600
Substrate
n/a
Meas. Tech.
Isothermal Titration Calorimetry (ITC)
Kd
6e+1± 1e+1 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:
JARID1A | KDM5A | KDM5A_HUMAN | Lysine-specific demethylase 5A (KDM5A(aa 1-588)-AP) | RBBP2 | RBP2
Type:
Protein
Mol. Mass.:
66955.44
Organism:
Homo sapiens (Human)
Description:
Truncation 1-588 aa. Contains deletion of ARID and PhD1 domains.
Residue:
588
Sequence:
MAGVGPGGYAAEFVPPPECPVFEPSWEEFTDPLSFIGRIRPLAEKTGICKIRPPKDWQPPFACEVKSFRFTPRVQRLNELEAMTRVRLDFLDQLAKFWELQGSTLKIPVVERKILDLYALSKIVASKGGFEMVTKEKKWSKVGSRLGYLPGKGTGSLLKSHYERILYPYELFQSGVSLMGVQMPNLDLKEKVEPEVLSTDTQTSPEPGTRMNILPKRTRRVKTQSESGDVSRNTELKKLQIFGAGPKVVGLAMGTKDKEDEVTRRRKVTNRSDAFNMQMRQRKGTLSVNFVDLYVCMFCGRGNNEDKLLLCDGCDDSYHTFCLIPPLPDVPKGDWRCPKCVAEECSKPREAFGFEQAVREYTLQSFGEMADNFKSDYFNMPVHMVPTELVEKEFWRLVSSIEEDVIVEYGADISSKDFGSGFPVKDGRRKILPEEEEYALSGWNLNNMPVLEQSVLAHINVDISGMKVPWLYVGMCFSSFCWHIEDHWSYSINYLHWGEPKTWYGVPSHAAEQLEEVMRELAPELFESQPDLLHQLVTIMNPNVLMEHGVPVYRTNQCAGEFVVTFPRAYHSGFNQGYNFAEAVNFCT
  
Inhibitor
Name:
BDBM191600
Synonyms:
2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl)isonicotinic acid (N19) | US10173996, Example 89 | US9604961, Example 89 | US9714230, 89 | US9908865, Example 89
Type:
Small organic molecule
Emp. Form.:
C17H14ClN3O3
Mol. Mass.:
343.764
SMILES:
Cc1cc(Cl)ccc1COc1ccnn1-c1cc(ccn1)C(O)=O
Structure:
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