Reaction Details
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E3 ubiquitin-protein ligase Mdm2
Ligand
BDBM535427
Substrate
n/a
Meas. Tech.
USP7 Assay B (Ubitquin-Rhodamine110 Assay)
IC50
0.700±n/a nM
Citation
FERRARI, N; SAINI, HK; AHN, JS BIOMARKERS FOR CANCER THERAPY USING MDM2 ANTAGONISTS US Patent US20230338337 Publication Date 10/26/2023 More Info.:
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:
BDBM535427
Synonyms:
(3R)-3-(4-chlorophenyl)-4-fluoro-6-[1- hydroxy-1-(1-methyl-1H-pyrazol-4- yl)ethyl]-3-{[1- (hydroxymethyl)cyclopropyl]methoxy}- 2-[(5-methoxypyridin-2-yl)methyl]- 2,3-dihydro-1H-isoindol-1-one | US11236047, Example 226 | US11236047, Example 224 | US20230338337, Compound 226
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
COc1ccc(CN2C(=O)c3cc(cc(F)c3[C@]2(OCC2(CO)CC2)c2ccc(Cl)cc2)C(C)(O)c2cnn(C)c2)nc1 |r|
