Ki Summary

Reaction Details

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Target

E3 ubiquitin-protein ligase Mdm2

Ligand

BDBM135253

Substrate/Competitor

n/a

Meas. Tech.

FRET Assay

IC50

1±n/a nM

Citation

Christopher, MP; Fradera Llinas, FX; Machacek, M; Martinez, M; Reutershan, MH; Shizuka, M; Sun, B; Thompson, CF; Trotter, BW; Voss, ME; Altman, MD; Bogen, SL; Doll, RJ Substituted imidazopyridines as HDM2 inhibitors US Patent US8962611 Publication Date 2/24/2015

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

BDBM135253

n/a

Name

BDBM135253

Synonyms:

US8846657, 3.146

Type

Small organic molecule

Emp. Form.

C29H34ClN7O3

Mol. Mass.

564.078

SMILES

C[C@H]1CC[C@H](Cn2c(nc3cc(nc(-c4cncc(Cl)c4)c23)-c2noc(=O)[nH]2)N2[C@@H]3CCC[C@H]3OCC2C)CC1 |r,wU:1.0,33.36,wD:4.4,29.33,(7.18,-4.41,;5.69,-4.02,;4.61,-5.1,;3.12,-4.71,;2.72,-3.22,;1.23,-2.82,;.65,-.61,;1.56,.64,;.65,1.88,;-.81,1.41,;-2.15,2.18,;-3.48,1.41,;-3.48,-.13,;-2.15,-.9,;-2.15,-2.44,;-.81,-3.21,;-.81,-4.75,;-2.15,-5.52,;-3.48,-4.75,;-4.81,-5.52,;-3.48,-3.21,;-.81,-.13,;-4.81,2.18,;-6.28,1.7,;-7.18,2.95,;-6.28,4.19,;-7.05,5.52,;-4.81,3.72,;3.1,.64,;3.87,1.97,;3.39,3.43,;4.64,4.34,;5.88,3.43,;5.41,1.97,;6.18,.64,;5.41,-.7,;3.87,-.7,;3.1,-2.03,;3.81,-2.13,;5.3,-2.53,)|

Structure