Reaction Details Report a problem with these data
Target
E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM31259
Substrate
biotinylated IP3 peptide
Meas. Tech.
MDM2-p53 Interaction Using a 96-Well Plate Binding Assay (ELISA)
IC50
275000±n/a nM
Citation
Hardcastle, IR; Ahmed, SU; Atkins, H; Farnie, G; Golding, BT; Griffin, RJ; Guyenne, S; Hutton, C; Källblad, P; Kemp, SJ; Kitching, MS; Newell, DR; Norbedo, S; Northen, JS; Reid, RJ; Saravanan, K; Willems, HM; Lunec, J Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold. J Med Chem 49:6209-21 (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:
BDBM31259
Synonyms:
isoindolinone scaffold, 50
Type:
Small organic molecule
Emp. Form.:
C30H28N4O7
Mol. Mass.:
556.5659
SMILES:
COC(=O)C(Cc1ccc(O)cc1)N1C(=O)c2ccccc2C1(OCCn1c(C)ncc1[N+]([O-])=O)c1ccccc1
Substrate
Name:
biotinylated IP3 peptide
Synonyms:
b-IP3
Type:
Peptide
Mol. Mass.:
4116.56
Organism:
n/a
Description:
n/a
Residue:
37
Sequence:
ACMETPRARGPHEMETASPTYRTRPGLGLYLEASNNH