Reaction Details
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E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM31286
Substrate
Fl 9mer
Meas. Tech.
Fluorescent Peptide Displacement Assay
pH
7.5000±n/a
Temperature
296.1500±n/a K
Kd
4800±n/a nM
Citation
Grasberger, BL; Lu, T; Schubert, C; Parks, DJ; Carver, TE; Koblish, HK; Cummings, MD; LaFrance, LV; Milkiewicz, KL; Calvo, RR; Maguire, D; Lattanze, J; Franks, CF; Zhao, S; Ramachandren, K; Bylebyl, GR; Zhang, M; Manthey, CL; Petrella, EC; Pantoliano, MW; Deckman, IC; Spurlino, JC; Maroney, AC; Tomczuk, BE; Molloy, CJ; Bone, RF Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells. J Med Chem 48:909-12 (2005) [PubMed] Article Target
Name:
E3 ubiquitin-protein ligase Mdm2
Synonyms:
MDM2_HUMAN | MDM2 | Double minute 2 protein | Double minute 2 protein (HDM2) | E3 ubiquitin-protein ligase Mdm2 (p53-binding protein Mdm2) | Hdm2 | Human Double Minute 2 (HDM2) | p53-Binding Protein MDM2 | p53-binding protein | MDM2-MDMX
Type:
Oncoprotein
Mol. Mass.:
55196.54
Organism:
Human
Description:
Q00987
Residue:
491
Sequence:
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCNRCWALRENWLPEDKGKDKGEISEKAKLENSTQAEEGFDVPDCKKTIVNDSRESCVEENDDKITQASQSQESEDYSQPSTSSSIIYSSQEDVKEFEREETQDKEESVESSLPLNAIEPCVICQGRPKNGCIVHGKTGHLMACFTCAKKLKKRNKPCPVCRQPIQMIVLTYFP
Inhibitor
Name:
BDBM31286
Synonyms:
benzodiazepinedione, 2
Type:
Small organic molecule
Emp. Form.:
C23H15Cl2IN2O4
Mol. Mass.:
579.95
SMILES:
OC(=O)[C@H](N1[C@H](c2ccc(Cl)cc2)C(=O)Nc2ccc(I)cc2C1=O)c1ccc(Cl)cc1 |r|
Substrate
Name:
Fl 9mer
Synonyms:
n/a
Type:
fluorescent peptide
Mol. Mass.:
2263.48
Organism:
n/a
Description:
n/a
Residue:
18
Sequence:
FLRESCEINFMDYWEGLN
