Ki Summary

Reaction Details

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Target

E3 ubiquitin-protein ligase Mdm2

Ligand

BDBM135300

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 US8846657 Publication Date 9/30/2014

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

BDBM135300

n/a

Name

BDBM135300

Synonyms:

US8846657, 5.3 | US8846657, 5.4

Type

Small organic molecule

Emp. Form.

C31H37ClN8O3

Mol. Mass.

605.13

SMILES

C[C@H]1CC[C@H](Cn2c(nc3cc(nc(-c4cncc(Cl)c4)c23)-c2noc(=O)[nH]2)N2[C@H](C)CN(C[C@H]2C)C(=O)C2CC2)CC1 |r,wU:4.4,29.33,wD:1.0,34.39,(5.68,-3.69,;4.19,-3.29,;3.8,-1.81,;2.31,-1.41,;1.22,-2.5,;-.27,-2.1,;-.67,-.61,;.24,.64,;-.67,1.88,;-2.13,1.41,;-3.47,2.18,;-4.8,1.41,;-4.8,-.13,;-3.47,-.9,;-3.47,-2.44,;-2.13,-3.21,;-2.13,-4.75,;-3.47,-5.52,;-4.8,-4.75,;-6.13,-5.52,;-4.8,-3.21,;-2.13,-.13,;-6.13,2.18,;-7.6,1.7,;-8.5,2.95,;-7.6,4.19,;-8.37,5.52,;-6.13,3.72,;1.78,.64,;2.55,-.7,;1.21,-1.47,;4.09,-.7,;4.86,.64,;4.09,1.97,;2.55,1.97,;1.78,3.3,;6.4,.64,;7.17,1.97,;7.17,-.7,;7.17,-2.24,;8.5,-1.47,;1.62,-3.98,;3.11,-4.38,)|

Structure