Reaction Details Report a problem with these data
Target
E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM31198
Substrate
PMDM6-F Peptide
Meas. Tech.
Fluorescence Polarization-Based (FP-Based) Binding Assay
pH
7.5±n/a
Temperature
296.15±n/a K
Ki
13±4 nM
Citation
Ding, K; Lu, Y; Nikolovska-Coleska, Z; Wang, G; Qiu, S; Shangary, S; Gao, W; Qin, D; Stuckey, J; Krajewski, K; Roller, PP; Wang, S Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction. J Med Chem 49:3432-5 (2006) [PubMed] Article
More Info.:
Target
Name:
E3 ubiquitin-protein ligase Mdm2
Synonyms:
Double minute 2 protein | Double minute 2 protein (HDM2) | E3 ubiquitin-protein ligase Mdm2 (p53-binding protein Mdm2) | Hdm2 | Human Double Minute 2 (HDM2) | MDM2 | MDM2-MDMX | MDM2_HUMAN | p53-Binding Protein MDM2 | p53-binding protein
Type:
Oncoprotein
Mol. Mass.:
55196.54
Organism:
Homo sapiens (Human)
Description:
Q00987
Residue:
491
Sequence:
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCNRCWALRENWLPEDKGKDKGEISEKAKLENSTQAEEGFDVPDCKKTIVNDSRESCVEENDDKITQASQSQESEDYSQPSTSSSIIYSSQEDVKEFEREETQDKEESVESSLPLNAIEPCVICQGRPKNGCIVHGKTGHLMACFTCAKKLKKRNKPCPVCRQPIQMIVLTYFP
Inhibitor
Name:
BDBM31198
Synonyms:
spiro-oxindole, 4
Type:
Small organic molecule
Emp. Form.:
C29H36Cl2N4O3
Mol. Mass.:
559.527
SMILES:
CC(C)(C)C[C@H]1N[C@H]([C@H](c2cccc(Cl)c2)[C@@]11C(=O)Nc2cc(Cl)ccc12)C(=O)NCCN1CCOCC1 |r|
Substrate
Name:
PMDM6-F Peptide
Synonyms:
n/a
Type:
Fluorescence probe
Mol. Mass.:
4802.47
Organism:
n/a
Description:
n/a
Residue:
45
Sequence:
FAMETAALAETAALAPHEMETAIPTYRCLLTRPGLACCLEASNNH