Reaction Details Report a problem with these data
Target
Lysine-specific demethylase 4E
Ligand
BDBM223317
Substrate
n/a
Meas. Tech.
AlphaScreen Assay
IC50
1e+4±3.7e+3 nM
Citation
 Tumber, A; Nuzzi, A; Hookway, ES; Hatch, SB; Velupillai, S; Johansson, C; Kawamura, A; Savitsky, P; Yapp, C; Szykowska, A; Wu, N; Bountra, C; Strain-Damerell, C; Burgess-Brown, NA; Ruda, GF; Fedorov, O; Munro, S; England, KS; Nowak, RP; Schofield, CJ; La Thangue, NB; Pawlyn, C; Davies, F; Morgan, G; Athanasou, N; Müller, S; Oppermann, U; Brennan, PE Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Cell Chem Biol 24:371-380 (2017) [PubMed]  Article 
Target
Name:
Lysine-specific demethylase 4E
Synonyms:
2-OG-Dependent Histone Demethylase JMJD2E | Histone Lysine Demethylase | Jumonji domain-containing protein 2E (JMJD2E) | KDM4D-like protein | KDM4DL | KDM4E | KDM4E_HUMAN | Lysine-specific demethylase 4D-like | Lysine-specific demethylase 4E | Lysine-specific demethylase 4E (KDM4E)
Type:
Enzyme
Mol. Mass.:
56815.71
Organism:
Homo sapiens (Human)
Description:
B2RXH2
Residue:
506
Sequence:
MKSVHSSPQNTSHTIMTFYPTMEEFADFNTYVAYMESQGAHQAGLAKVIPPKEWKARQMYDDIEDILIATPLQQVTSGQGGVFTQYHKKKKAMRVGQYRRLANSKKYQTPPHQNFADLEQRYWKSHPGNPPIYGADISGSLFEESTKQWNLGHLGTILDLLEQECGVVIEGVNTPYLYFGMWKTTFAWHTEDMDLYSINYLHFGEPKTWYVVPPEHGQHLERLARELFPDISRGCEAFLRHKVALISPTVLKENGIPFNCMTQEAGEFMVTFPYGYHAGFNHGFNCAEAINFATPRWIDYGKMASQCSCGESTVTFSMDPFVRIVQPESYELWKHRQDLAIVEHTEPRVAESQELSNWRDDIVLRRAALGLRLLPNLTAQCPTQPVSSGHCYNPKGCGTDAVPGSAFQSSAYHTQTQSLTLGMSARVLLPSTGSWGSGRGRGRGQGQGRGCSRGRGHGCCTRELGTEEPTVQPASKRRLLMGTRSRAQGHRPQLPLANDLMTNLSL
  
Inhibitor
Name:
BDBM223317
Synonyms:
KDOAM-1
Type:
Small organic molecule
Emp. Form.:
C11H15N3O2
Mol. Mass.:
221.2557
SMILES:
OC(=O)c1ccnc(CN2CCNCC2)c1
Structure:
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