Ki Summary

Reaction Details

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Target

Protein Mdm4

Ligand

BDBM162166

Substrate/Competitor

n/a

Meas. Tech.

Time Resolved Fluorescence Energy Transfer (TR-FRET) Assay

IC50

4130±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

BDBM162166

n/a

Name

BDBM162166

Synonyms:

US9051279, 149

Type

Small organic molecule

Emp. Form.

C35H43ClN6O4

Mol. Mass.

647.207

SMILES

COc1cc2CC(=O)N([C@@H](c3ccc(Cl)cc3)c2cc1OC(C)C)c1cnc(cn1)N(C)C[C@H]1CC[C@@H](CC1)N1CN(C)C(=O)C1 |r,wU:36.43,wD:9.9,33.36,(11.96,4.75,;10.62,5.52,;9.29,4.75,;7.96,5.52,;6.62,4.75,;5.29,5.52,;3.96,4.75,;2.62,5.52,;3.96,3.21,;5.29,2.44,;5.29,.9,;3.96,.13,;3.96,-1.41,;5.29,-2.18,;5.29,-3.72,;6.62,-1.41,;6.62,.13,;6.62,3.21,;7.96,2.44,;9.29,3.21,;10.62,2.44,;10.62,.9,;11.96,.13,;9.29,.13,;2.62,2.44,;2.62,.9,;1.29,.13,;-.05,.9,;-.05,2.44,;1.29,3.21,;-1.38,.13,;-1.38,-1.41,;-2.71,.9,;-4.05,.13,;-5.38,.9,;-6.71,.13,;-6.71,-1.41,;-5.38,-2.18,;-4.05,-1.41,;-8.05,-2.18,;-8.05,-3.72,;-9.51,-4.19,;-10.28,-5.52,;-10.42,-2.95,;-11.96,-2.95,;-9.51,-1.7,)|

Structure