Ki Summary

Reaction Details

Report a problem with these data

Target

E3 ubiquitin-protein ligase Mdm2

Ligand

BDBM162023

Substrate/Competitor

n/a

Meas. Tech.

Time Resolved Fluorescence Energy Transfer (TR-FRET) Assay

IC50

1.9±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

BDBM162023

n/a

Name

BDBM162023

Synonyms:

US9051279, 73a | US9051279, 73b

Type

Small organic molecule

Emp. Form.

C36H46ClN3O3

Mol. Mass.

604.222

SMILES

CC[C@@H](C)Oc1cc2[C@@H](N(C(=O)Cc2cc1OC)c1ccc(cc1)N(C)C[C@H]1CC[C@@H](CC1)N(C)C)c1ccc(Cl)cc1 |r,wU:30.36,wD:8.39,2.2,27.29,(9.34,7.63,;8,6.86,;6.67,7.63,;6.67,9.17,;5.33,6.86,;4,7.63,;2.67,6.86,;1.33,7.63,;,6.86,;-1.33,7.63,;-1.33,9.17,;-2.67,9.94,;,9.94,;1.33,9.17,;2.67,9.94,;4,9.17,;5.33,9.94,;5.33,11.48,;-2.67,6.86,;-2.67,5.32,;-4,4.55,;-5.33,5.32,;-5.33,6.86,;-4,7.63,;-6.67,4.55,;-6.67,3.01,;-8,5.32,;-8,6.86,;-6.67,7.63,;-6.67,9.17,;-8,9.94,;-9.34,9.17,;-9.34,7.63,;-8,11.48,;-9.34,12.25,;-6.67,12.25,;,5.32,;-1.33,4.55,;-1.33,3.01,;,2.24,;,.7,;1.33,3.01,;1.33,4.55,)|

Structure