Ki Summary

Reaction Details

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Target

Histone-lysine N-methyltransferase EZH2 [A677G]

Ligand

BDBM190194

Substrate/Competitor

n/a

Meas. Tech.

Inhibition Assay

IC50

4.8±n/a nM

Citation

Kuntz, KW; Knutson, SK; Wigle, TJ Inhibitors of human EZH2, and methods of use thereof US Patent US9175331 Publication Date 11/3/2015

More Info.:

Get all data from this article, Assay Method

Histone-lysine N-methyltransferase EZH2 [A677G]

Name:

Histone-lysine N-methyltransferase EZH2 [A677G]

Synonyms:

EZH2 | EZH2_HUMAN | Histone-lysine N-methyltransferase EZH2 (A677G) | KMT6

Type:

Protein

Mol. Mass.:

85381.87

Organism:

Homo sapiens (Human)

Description:

Q15910[A677G]

Residue:

746

Sequence:

MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFH
ATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPN
NSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKM
KPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPA
PAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQ
NFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVS
CKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDK
YMCSFLFNLNNDFVVDGTRKGNKIRFVNHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGE
ELFFDYRYSQADALKYVGIEREMEIP

BDBM190194

n/a

Name

BDBM190194

Synonyms:

EPZ007789 | US9175331, 22

Type

Small organic molecule

Emp. Form.

C28H42N4O4S

Mol. Mass.

530.722

SMILES

CCN([C@H]1CC[C@@H](CC1)N(C)C)c1cc(cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C)S(=O)(=O)CC |r,wU:3.2,wD:6.9,(-5.33,3.08,;-5.33,1.54,;-4,.77,;-4,-.77,;-2.67,-1.54,;-2.67,-3.08,;-4,-3.85,;-5.33,-3.08,;-5.33,-1.54,;-4,-5.39,;-2.67,-6.16,;-5.33,-6.16,;-2.67,1.54,;-2.67,3.08,;-1.33,3.85,;,3.08,;,1.54,;1.33,.77,;2.67,1.54,;1.33,-.77,;2.67,-1.54,;2.67,-3.08,;4,-3.85,;5.33,-3.08,;4,-5.39,;2.67,-6.16,;2.67,-7.7,;1.33,-5.39,;1.33,-3.85,;,-3.08,;-1.33,.77,;-1.33,-.77,;-1.33,5.39,;.21,5.39,;-2.87,5.39,;-1.33,6.93,;,7.7,)|

Structure