Ki Summary

Reaction Details

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Target

Protein Mdm4

Ligand

BDBM162151

Substrate/Competitor

n/a

Meas. Tech.

Time Resolved Fluorescence Energy Transfer (TR-FRET) Assay

IC50

5090±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

BDBM162151

n/a

Name

BDBM162151

Synonyms:

US9051279, 134

Type

Small organic molecule

Emp. Form.

C37H46ClN5O4

Mol. Mass.

660.245

SMILES

CCN1CN(CC1=O)[C@H]1CC[C@H](CN(C)c2ccc(cn2)N2[C@@H](c3ccc(Cl)cc3)c3cc(OC(C)C)c(OC)cc3CC2=O)CC1 |r,wU:8.8,wD:22.24,11.12,(-9.51,-6.19,;-10.28,-4.86,;-9.51,-3.52,;-8.05,-3.05,;-8.05,-1.51,;-9.51,-1.03,;-10.42,-2.28,;-11.96,-2.28,;-6.71,-.74,;-6.71,.8,;-5.38,1.57,;-4.05,.8,;-2.71,1.57,;-1.38,.8,;-1.38,-.74,;-.05,1.57,;1.29,.8,;2.62,1.57,;2.62,3.11,;1.29,3.88,;-.05,3.11,;3.96,3.88,;5.29,3.11,;5.29,1.57,;3.96,.8,;3.96,-.74,;5.29,-1.51,;5.29,-3.05,;6.62,-.74,;6.62,.8,;6.62,3.88,;7.96,3.11,;9.29,3.88,;10.62,3.11,;10.62,1.57,;11.96,.8,;9.29,.8,;9.29,5.42,;10.62,6.19,;11.96,5.42,;7.96,6.19,;6.62,5.42,;5.29,6.19,;3.96,5.42,;2.62,6.19,;-4.05,-.74,;-5.38,-1.51,)|

Structure