Ki Summary

Reaction Details

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Target

Protein Mdm4

Ligand

BDBM162123

Substrate/Competitor

n/a

Meas. Tech.

Time Resolved Fluorescence Energy Transfer (TR-FRET) Assay

IC50

2100±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

Protein Mdm4

Name:

Protein Mdm4

Synonyms:

Type:

Oncoprotein

Mol. Mass.:

54842.04

Organism:

Homo sapiens (Human)

Description:

The HDMX(1-188) were expressed in Escherichia coli BL21 (DE3) as a GST fusion and purified on glutathione sepharose.

Residue:

490

Sequence:

MTSFSTSAQCSTSDSACRISPGQINQVRPKLPLLKILHAAGAQGEMFTVKEVMHYLGQYI
MVKQLYDQQEQHMVYCGGDLLGELLGRQSFSVKDPSPLYDMLRKNLVTLATATTDAAQTL
ALAQDHSMDIPSQDQLKQSAEESSTSRKRTTEDDIPTLPTSEHKCIHSREDEDLIENLAQ
DETSRLDLGFEEWDVAGLPWWFLGNLRSNYTPRSNGSTDLQTNQDVGTAIVSDTTDDLWF
LNESVSEQLGVGIKVEAADTEQTSEEVGKVSDKKVIEVGKNDDLEDSKSLSDDTDVEVTS
EDEWQCTECKKFNSPSKRYCFRCWALRKDWYSDCSKLTHSLSTSDITAIPEKENEGNDVP
DCRRTISAPVVRPKDAYIKKENSKLFDPCNSVEFLDLAHSSESQETISSMGEQLDNLSEQ
RTDTENMEDCQNLLKPCSLCEKRPRDGNIIHGRTGHLVTCFHCARRLKKAGASCPICKKE
IQLVIKVFIA

BDBM162123

n/a

Name

BDBM162123

Synonyms:

US9051279, 106

Type

Small organic molecule

Emp. Form.

C38H47ClN4O4

Mol. Mass.

659.257

SMILES

COc1cc2CC(=O)N([C@@H](c3ccc(Cl)cc3)c2cc1OC(C)C)c1ccc(cc1)N(C)C[C@H]1CC[C@@H](CC1)N1CCN(C)C(=O)C1 |r,wU:33.36,wD:9.9,36.43,(8.67,.77,;7.34,1.54,;6,.77,;4.67,1.54,;3.33,.77,;2,1.54,;.67,.77,;-.67,1.54,;.67,-.77,;2,-1.54,;2,-3.08,;.67,-3.85,;.67,-5.39,;2,-6.16,;2,-7.7,;3.33,-5.39,;3.33,-3.85,;3.33,-.77,;4.67,-1.54,;6,-.77,;7.34,-1.54,;7.34,-3.08,;8.67,-3.85,;6,-3.85,;-.67,-1.54,;-2,-.77,;-3.33,-1.54,;-3.33,-3.08,;-2,-3.85,;-.67,-3.08,;-4.67,-3.85,;-4.67,-5.39,;-6,-3.08,;-6,-1.54,;-7.34,-.77,;-7.34,.77,;-6,1.54,;-4.67,.77,;-4.67,-.77,;-6,3.08,;-4.67,3.85,;-4.67,5.39,;-6,6.16,;-6,7.7,;-7.34,5.39,;-8.67,6.16,;-7.34,3.85,)|

Structure