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Target
E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM50339392
Substrate
n/a
Meas. Tech.
ChEMBL_736488 (CHEMBL1694433)
IC50
11000±n/a nM
Citation
Hardcastle, IR; Liu, J; Valeur, E; Watson, A; Ahmed, SU; Blackburn, TJ; Bennaceur, K; Clegg, W; Drummond, C; Endicott, JA; Golding, BT; Griffin, RJ; Gruber, J; Haggerty, K; Harrington, RW; Hutton, C; Kemp, S; Lu, X; McDonnell, JM; Newell, DR; Noble, ME; Payne, SL; Revill, CH; Riedinger, C; Xu, Q; Lunec, J Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency. J Med Chem 54:1233-43 (2011) [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:
BDBM50339392
Synonyms:
(+/-)-3-(4-chlorophenyl)-3-((1-(hydroxymethyl)cyclopropyl)methoxy)-2-(pyridin-2-ylmethyl)isoindolin-1-one | CHEMBL1688297 | US8618158, NU8429
Type:
Small organic molecule
Emp. Form.:
C25H23ClN2O3
Mol. Mass.:
434.915
SMILES:
OCC1(COC2(N(Cc3ccccn3)C(=O)c3ccccc23)c2ccc(Cl)cc2)CC1