Ki Summary

Reaction Details

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Target

Cellular tumor antigen p53 [18-26]/E3 ubiquitin-protein ligase Mdm2 [2-188]

Ligand

BDBM236464

Substrate/Competitor

n/a

Meas. Tech.

Time Resolved Fluorescence Energy Transfer (TR-FRET) Assay

Temperature

298.15±n/a K

IC50

0.134±n/a nM

Comments

extracted

Citation

Cotesta, S; Furet, P; Guagnano, V; Holzer, P; Kallen, J; Mah, R; Masuya, K; Schlapbach, A; Stutz, S; Vaupel, A Pyrrolopyrrolidinone compounds US Patent US9365576 Publication Date 6/14/2016

More Info.:

Get all data from this article, Assay Method

Cellular tumor antigen p53 [18-26]/E3 ubiquitin-protein ligase Mdm2 [2-188]

Name:

Cellular tumor antigen p53 [18-26]/E3 ubiquitin-protein ligase Mdm2 [2-188]

Synonyms:

p53-MDM2

Type:

Protein

Mol. Mass.:

n/a

Description:

n/a

Components:

This complex has 2 components.

Component 1

Name:

Cellular tumor antigen p53 [18-26]

Synonyms:

P53 | P53_HUMAN | TP53 | Tumor suppressor p53

Type:

Protein

Mol. Mass.:

1122.31

Organism:

Homo sapiens (Human)

Description:

aa 18-26

Residue:

Sequence:

TFSDLWKLL

Component 2

Name:

E3 ubiquitin-protein ligase Mdm2 [2-188]

Synonyms:

E3 ubiquitin-protein ligase Mdm2 | MDM2 | MDM2_HUMAN

Type:

Protein

Mol. Mass.:

21187.98

Organism:

Homo sapiens (Human)

Description:

aa 2-188

Residue:

187

Sequence:

CNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYI
MTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTS
VSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQR
KRHKSDS

BDBM236464

n/a

Name

BDBM236464

Synonyms:

US9365576, 220

Type

Small organic molecule

Emp. Form.

C30H29Cl2N5O6

Mol. Mass.

626.487

SMILES

CCOC(=O)c1c2C(=O)N(C(c2n(C(C)C)c1-c1cnc(OC)nc1OC)c1ccc(Cl)cc1)c1cc(Cl)c(=O)n(C)c1 |(3.26,6.8,;2.17,5.71,;2.57,4.22,;1.48,3.13,;.39,4.22,;1.08,1.64,;-.38,1.17,;-1.85,1.64,;-2.62,2.98,;-2.75,.4,;-1.85,-.85,;-.38,-.37,;1.08,-.85,;1.48,-2.33,;.39,-3.42,;2.97,-2.73,;1.98,.4,;3.52,.4,;4.29,-.94,;5.83,-.94,;6.6,.4,;8.14,.4,;8.91,-.94,;5.83,1.73,;4.29,1.73,;3.52,3.07,;4.29,4.4,;-2.25,-2.33,;-3.74,-2.73,;-4.13,-4.22,;-3.05,-5.31,;-3.44,-6.8,;-1.56,-4.91,;-1.16,-3.42,;-4.29,.4,;-5.06,1.73,;-6.6,1.73,;-7.37,3.07,;-7.37,.4,;-8.91,.4,;-6.6,-.94,;-7.37,-2.27,;-5.06,-.94,)|

Structure