Reaction Details Report a problem with these data
Target
Lysine-specific demethylase 2A
Ligand
BDBM50193145
Substrate
n/a
Meas. Tech.
In vitro Hydroxylation Assays for PHD2 (AlphaScreen)
pH
7.5±0
IC50
>2.0e+4±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
More Info.:
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:
BDBM50193145
Synonyms:
2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)acetic acid | CHEMBL426560 | Isoquinoline 3 | N-[(1-CHLORO-4-HYDROXYISOQUINOLIN-3-YL)CARBONYL]GLYCINE
Type:
Small organic molecule
Emp. Form.:
C12H9ClN2O4
Mol. Mass.:
280.664
SMILES:
OC(=O)CNC(=O)c1nc(Cl)c2ccccc2c1O