Ki Summary

Reaction Details

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Target

Protein Mdm4

Ligand

BDBM162076

Substrate/Competitor

n/a

Meas. Tech.

Time Resolved Fluorescence Energy Transfer (TR-FRET) Assay

IC50

3010±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

BDBM162076

n/a

Name

BDBM162076

Synonyms:

US9051279, 83

Type

Small organic molecule

Emp. Form.

C37H46ClN5O5

Mol. Mass.

676.245

SMILES

COc1cc2CC(=O)N([C@@H](c3ccc(Cl)cc3)c2cc1OC(C)C)c1ccc(cc1)N(C)C[C@H]1CC[C@@H](CC1)N(CC(N)=O)CC(N)=O |r,wU:36.43,wD:9.9,33.36,(7.33,3.85,;7.33,2.31,;5.99,1.54,;4.66,2.31,;3.33,1.54,;1.99,2.31,;.66,1.54,;-.68,2.31,;.66,,;1.99,-.77,;1.99,-2.31,;.66,-3.08,;.66,-4.62,;1.99,-5.39,;1.99,-6.93,;3.33,-4.62,;3.33,-3.08,;3.33,,;4.66,-.77,;5.99,,;7.33,-.77,;8.66,,;9.99,-.77,;8.66,1.54,;-.68,-.77,;-2.01,,;-3.34,-.77,;-3.34,-2.31,;-2.01,-3.08,;-.68,-2.31,;-4.68,-3.08,;-4.68,-4.62,;-6.01,-2.31,;-6.01,-.77,;-4.68,,;-4.68,1.54,;-6.01,2.31,;-7.34,1.54,;-7.34,,;-6.01,3.85,;-4.68,4.62,;-4.68,6.16,;-3.34,6.93,;-6.01,6.93,;-7.33,4.62,;-8.66,3.85,;-9.99,4.62,;-8.66,2.31,)|

Structure