Ki Summary

Reaction Details

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Target

E3 ubiquitin-protein ligase Mdm2

Ligand

BDBM161883

Substrate/Competitor

n/a

Meas. Tech.

Time Resolved Fluorescence Energy Transfer (TR-FRET) Assay

IC50

2.3±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

BDBM161883

n/a

Name

BDBM161883

Synonyms:

US9051279, 53

Type

Small organic molecule

Emp. Form.

C37H48ClN3O3

Mol. Mass.

618.248

SMILES

CC[C@@H](C)Oc1cc2C(N(C(=O)Cc2cc1OC)c1ccc(cc1)N(C)C[C@H]1CC[C@@H](CC1)N(C)CC)c1ccc(Cl)cc1 |r,wU:27.29,wD:30.36,2.2,(9.34,.38,;8,-.38,;6.67,.38,;6.67,1.93,;5.33,-.38,;4,.38,;2.67,-.38,;1.33,.38,;,-.38,;-1.33,.38,;-1.33,1.93,;-2.67,2.69,;,2.69,;1.33,1.93,;2.67,2.69,;4,1.93,;5.33,2.69,;5.33,4.23,;-2.67,-.38,;-4,.38,;-5.33,-.38,;-5.33,-1.93,;-4,-2.69,;-2.67,-1.93,;-6.67,-2.69,;-6.67,-4.23,;-8,-1.93,;-8,-.38,;-9.34,.38,;-9.34,1.93,;-8,2.69,;-6.67,1.93,;-6.67,.38,;-8,4.23,;-9.34,5,;-6.67,5,;-6.67,6.54,;,-1.93,;-1.33,-2.69,;-1.33,-4.23,;,-5,;,-6.54,;1.33,-4.23,;1.33,-2.69,)|

Structure