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Target
Lysine-specific demethylase 2A
Ligand
BDBM191600
Substrate
n/a
Meas. Tech.
ChEMBL_1771184 (CHEMBL4223296)
IC50
820±n/a nM
Citation
 Nie, Z; Shi, L; Lai, C; O'Connell, SM; Xu, J; Stansfield, RK; Hosfield, DJ; Veal, JM; Stafford, JA Structure-based design and discovery of potent and selective KDM5 inhibitors. Bioorg Med Chem Lett 28:1490-1494 (2018) [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:
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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