Ki Summary

Reaction Details

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Target

E3 ubiquitin-protein ligase Mdm2

Ligand

BDBM161880

Substrate/Competitor

n/a

Meas. Tech.

Time Resolved Fluorescence Energy Transfer (TR-FRET) Assay

IC50

3.7±n/a nM

Citation

Berghausen, J; Buschmann, N; Furet, P; Gessier, F; Hergovich Lisztwan, J; Holzer, P; Jacoby, E; Kallen, J; Masuya, K; Pissot Soldermann, C; Ren, H; Stutz, S Substituted isoquinolinones and quinazolinones US Patent US9051279 Publication Date 6/9/2015

More Info.:

Get all data from this article, Assay Method

E3 ubiquitin-protein ligase Mdm2

Name:

E3 ubiquitin-protein ligase Mdm2

Synonyms:

Type:

Oncoprotein

Mol. Mass.:

55196.54

Organism:

Homo sapiens (Human)

Description:

Q00987

Residue:

491

Sequence:

MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQY
IMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGT
SVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQ
RKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDS
VSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLA
DYWKCTSCNEMNPPLPSHCNRCWALRENWLPEDKGKDKGEISEKAKLENSTQAEEGFDVP
DCKKTIVNDSRESCVEENDDKITQASQSQESEDYSQPSTSSSIIYSSQEDVKEFEREETQ
DKEESVESSLPLNAIEPCVICQGRPKNGCIVHGKTGHLMACFTCAKKLKKRNKPCPVCRQ
PIQMIVLTYFP

BDBM161880

n/a

Name

BDBM161880

Synonyms:

US9051279, 51

Type

Small organic molecule

Emp. Form.

C34H42ClN3O3

Mol. Mass.

576.169

SMILES

CC[C@@H](C)Oc1cc2C(N(C(=O)Cc2cc1OC)c1ccc(cc1)N(C)C[C@H]1CC[C@H](N)CC1)c1ccc(Cl)cc1 |r,wU:27.29,wD:2.2,30.33,(9.34,1.54,;8,.77,;6.67,1.54,;6.67,3.08,;5.33,.77,;4,1.54,;2.67,.77,;1.33,1.54,;,.77,;-1.33,1.54,;-1.33,3.08,;-2.67,3.85,;,3.85,;1.33,3.08,;2.67,3.85,;4,3.08,;5.33,3.85,;5.33,5.39,;-2.67,.77,;-4,1.54,;-5.33,.77,;-5.33,-.77,;-4,-1.54,;-2.67,-.77,;-6.67,-1.54,;-6.67,-3.08,;-8,-.77,;-8,.77,;-9.34,1.54,;-9.34,3.08,;-8,3.85,;-8,5.39,;-6.67,3.08,;-6.67,1.54,;,-.77,;-1.33,-1.54,;-1.33,-3.08,;,-3.85,;,-5.39,;1.33,-3.08,;1.33,-1.54,)|

Structure