Reaction Details Report a problem with these data
Target
E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM427081
Substrate
n/a
Meas. Tech.
MDM2-p53 Interaction Using a 96-Well Plate Binding Assay (ELISA)
IC50
1.90±n/a nM
Citation
Chessari, G; Howard, S; Buck, IM; Cons, BD; Johnson, CN; Holvey, RS; Rees, DC; St. Denis, JD; Tamanini, E; Golding, BT; Hardcastle, IR; Cano, CF; Miller, DC; Noble, ME; Griffin, RJ; Osborne, JD; Peach, J; Lewis, A; Hirst, KL; Whittaker, BP; Watson, DW; Mitchell, DR Isoindolinone inhibitors of the MDM2-p53 interaction having anticancer activity US Patent US10544132 Publication Date 1/28/2020
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:
Human
Description:
Q00987
Residue:
491
Sequence:
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCNRCWALRENWLPEDKGKDKGEISEKAKLENSTQAEEGFDVPDCKKTIVNDSRESCVEENDDKITQASQSQESEDYSQPSTSSSIIYSSQEDVKEFEREETQDKEESVESSLPLNAIEPCVICQGRPKNGCIVHGKTGHLMACFTCAKKLKKRNKPCPVCRQPIQMIVLTYFP
Inhibitor
Name:
BDBM427081
Synonyms:
(3R)-2-[(4-chloro-2-methanesulfonylphenyl)methyl]-3-(4-chlorophenyl)-3-({1-[hydroxy(2H2)methyl]cyclopropyl}(2H2)methoxy)-6-(2-hydroxypropan-2-yl)-2,3-dihydro-1H-isoindol-1-one | US10544132, Example 36 | US10981898, Example 36 | US11236047, Example 36
Type:
Small organic molecule
Emp. Form.:
C30H31Cl2NO6S
Mol. Mass.:
604.541
SMILES:
CC(C)(O)c1ccc2c(c1)C(=O)N(Cc1ccc(Cl)cc1S(C)(=O)=O)[C@@]2(OCC1(CO)CC1)c1ccc(Cl)cc1 |r|