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Target
Protein Mdm4
Ligand
BDBM129733
Substrate
n/a
Meas. Tech.
Time Resolved Fluorescence Energy Transfer (TR-FRET) Assay
IC50
217±n/a nM
Citation
 Furet, P; Guagnano, V; Holzer, P; Kallen, J; Liao, L; Mah, R; Mao, L; Masuya, K; Schlapbach, A; Stutz, S; Vaupel, A Substituted pyrrolo[3,4-D]imidazoles for the treatment of MDM2/4 mediated diseases US Patent  US8815926 Publication Date 8/26/2014 
Target
Name:
Protein Mdm4
Synonyms:
Double minute 4 protein | Double minute 4 protein (HDM4) | MDM2-MDMX | MDM4 | MDM4_HUMAN | MDMX | Mdm2-like p53-binding protein | Protein Mdm4 | Protein Mdmx | p53-Binding Protein HDMX | p53-binding protein | p53-binding protein Mdm4
Type:
Oncoprotein
Mol. Mass.:
54842.04
Organism:
Homo sapiens (Human)
Description:
The HDMX(1-188) were expressed in Escherichia coli BL21 (DE3) as a GST fusion and purified on glutathione sepharose.
Residue:
490
Sequence:
MTSFSTSAQCSTSDSACRISPGQINQVRPKLPLLKILHAAGAQGEMFTVKEVMHYLGQYIMVKQLYDQQEQHMVYCGGDLLGELLGRQSFSVKDPSPLYDMLRKNLVTLATATTDAAQTLALAQDHSMDIPSQDQLKQSAEESSTSRKRTTEDDIPTLPTSEHKCIHSREDEDLIENLAQDETSRLDLGFEEWDVAGLPWWFLGNLRSNYTPRSNGSTDLQTNQDVGTAIVSDTTDDLWFLNESVSEQLGVGIKVEAADTEQTSEEVGKVSDKKVIEVGKNDDLEDSKSLSDDTDVEVTSEDEWQCTECKKFNSPSKRYCFRCWALRKDWYSDCSKLTHSLSTSDITAIPEKENEGNDVPDCRRTISAPVVRPKDAYIKKENSKLFDPCNSVEFLDLAHSSESQETISSMGEQLDNLSEQRTDTENMEDCQNLLKPCSLCEKRPRDGNIIHGRTGHLVTCFHCARRLKKAGASCPICKKEIQLVIKVFIA
  
Inhibitor
Name:
BDBM129733
Synonyms:
US8815926, 12
Type:
Small organic molecule
Emp. Form.:
C33H34Cl2N4O3
Mol. Mass.:
605.554
SMILES:
COc1ccc(cc1-c1nc2C(=O)N(C(c2n1C(C)C)c1ccc(Cl)cc1C)c1cc(Cl)ccc1C)C(=O)NC(C)C
Structure:
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