Ki Summary

Reaction Details

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Target

E3 ubiquitin-protein ligase Mdm2

Ligand

BDBM135319

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

BDBM135319

n/a

Name

BDBM135319

Synonyms:

US8846657, 5.22

Type

Small organic molecule

Emp. Form.

C30H38ClN9O3

Mol. Mass.

608.134

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)N(C)C)CC1 |r,wU:4.4,29.33,wD:1.0,34.39,(5.58,-4.38,;4.09,-3.98,;3.69,-2.49,;2.21,-2.09,;1.12,-3.18,;-.37,-2.78,;-.77,-.61,;.14,.64,;-.77,1.88,;-2.23,1.41,;-3.57,2.18,;-4.9,1.41,;-4.9,-.13,;-3.57,-.9,;-3.57,-2.44,;-2.23,-3.21,;-2.23,-4.75,;-3.57,-5.52,;-4.9,-4.75,;-6.24,-5.52,;-4.9,-3.21,;-2.23,-.13,;-6.24,2.18,;-7.7,1.7,;-8.61,2.95,;-7.7,4.19,;-8.47,5.52,;-6.24,3.72,;1.68,.64,;2.45,-.7,;1.68,-2.03,;3.99,-.7,;4.76,.64,;3.99,1.97,;2.45,1.97,;1.68,3.3,;6.3,.64,;7.07,1.97,;7.07,-.7,;8.61,-.7,;7.07,-2.24,;1.51,-4.67,;3,-5.07,)|

Structure