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Target
Lysine-specific demethylase 2A
Ligand
BDBM103846
Substrate
n/a
Meas. Tech.
In vitro Hydroxylation Assays for PHD2 (AlphaScreen)
pH
7.5±0
IC50
>1.00e+5±n/a nM
Citation
 Chowdhury, R; Candela-Lena, JI; Chan, MC; Greenald, DJ; Yeoh, KK; Tian, YM; McDonough, MA; Tumber, A; Rose, NR; Conejo-Garcia, A; Demetriades, M; Mathavan, S; Kawamura, A; Lee, MK; van Eeden, F; Pugh, CW; Ratcliffe, PJ; Schofield, CJ Selective Small Molecule Probes for the Hypoxia Inducible Factor (HIF) Prolyl Hydroxylases. ACS Chem Biol 8:1488-96 (2013) [PubMed]  Article 
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:
BDBM103846
Synonyms:
4HQ derivative 9
Type:
Small organic molecule
Emp. Form.:
C19H15BrN2O4
Mol. Mass.:
415.237
SMILES:
OC(=O)CNC(=O)c1nc(Cc2ccccc2)c2ccc(Br)cc2c1O
Structure:
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