Target
Lysine-specific demethylase 2A
Ligand
BDBM276063
Substrate
n/a
Meas. Tech.
FBXL11 Assay
IC50
300±n/a nM
Citation
 Chen, YKNie, ZStafford, JAVeal, JM Histone demethylase inhibitors US Patent  US9896436 Publication Date 2/20/2018 
Target
Name:
Lysine-specific demethylase 2A
Synonyms:
AA1-1162 | CXXC8 | F-box and leucine-rich repeat protein 11 | FBL11 | FBL7 | FBXL11 | Homo sapiens lysine demethylase 2A (KDM2A) | JHDM1A | KDM2A | KDM2A_HUMAN | KIAA1004 | Lysine-specific demethylase 2A | Lysine-specific demethylase 2A (KDM2A) | NM_012308
Type:
Enzyme Catalytic Domain
Mol. Mass.:
132809.04
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
1162
Sequence:
MEPEEERIRYSQRLRGTMRRRYEDDGISDDEIEGKRTFDLEEKLHTNKYNANFVTFMEGKDFNVEYIQRGGLRDPLIFKNSDGLGIKMPDPDFTVNDVKMCVGSRRMVDVMDVNTQKGIEMTMAQWTRYYETPEEEREKLYNVISLEFSHTRLENMVQRPSTVDFIDWVDNMWPRHLKESQTESTNAILEMQYPKVQKYCLMSVRGCYTDFHVDFGGTSVWYHIHQGGKVFWLIPPTAHNLELYENWLLSGKQGDIFLGDRVSDCQRIELKQGYTFVIPSGWIHAVYTPTDTLVFGGNFLHSFNIPMQLKIYNIEDRTRVPNKFRYPFYYEMCWYVLERYVYCITNRSHLTKEFQKESLSMDLELNGLESGNGDEEAVDREPRRLSSRRSVLTSPVANGVNLDYDGLGKTCRSLPSLKKTLAGDSSSDCSRGSHNGQVWDPQCAPRKDRQVHLTHFELEGLRCLVDKLESLPLHKKCVPTGIEDEDALIADVKILLEELANSDPKLALTGVPIVQWPKRDKLKFPTRPKVRVPTIPITKPHTMKPAPRLTPVRPAAASPIVSGARRRRVRCRKCKACVQGECGVCHYCRDMKKFGGPGRMKQSCVLRQCLAPRLPHSVTCSLCGEVDQNEETQDFEKKLMECCICNEIVHPGCLQMDGEGLLNEELPNCWECPKCYQEDSSEKAQKRKMEESDEEAVQAKVLRPLRSCDEPLTPPPHSPTSMLQLIHDPVSPRGMVTRSSPGAGPSDHHSASRDERFKRRQLLRLQATERTMVREKENNPSGKKELSEVEKAKIRGSYLTVTLQRPTKELHGTSIVPKLQAITASSANLRHSPRVLVQHCPARTPQRGDEEGLGGEEEEEEEEEEEDDSAEEGGAARLNGRGSWAQDGDESWMQREVWMSVFRYLSRRELCECMRVCKTWYKWCCDKRLWTKIDLSRCKAIVPQALSGIIKRQPVSLDLSWTNISKKQLTWLVNRLPGLKDLLLAGCSWSAVSALSTSSCPLLRTLDLRWAVGIKDPQIRDLLTPPADKPGQDNRSKLRNMTDFRLAGLDITDATLRLIIRHMPLLSRLDLSHCSHLTDQSSNLLTAVGSSTRYSLTELNMAGCNKLTDQTLIYLRRIANVTLIDLRGCKQITRKACEHFISDLSINSLYCLSDEKLIQKIS
  
Inhibitor
Name:
BDBM276063
Synonyms:
2-[5-(3-ethoxy-4-fluorophenyl)-1-methylimidazol-4-yl]-4-(1H-triazol-4-yl)pyridine | US10071984, Example 25 | US10174003, Example 25 | US9896436, Example 25
Type:
Small organic molecule
Emp. Form.:
C19H17FN6O
Mol. Mass.:
364.3763
SMILES:
CCOc1cc(ccc1F)-c1c(ncn1C)-c1cc(ccn1)-c1c[nH]nn1
Structure:
Search PDB for entries with ligand similarity: