Ki Summary

Reaction Details

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Target

Histone-lysine N-methyltransferase EZH2 [Y641F]

Ligand

BDBM190208

Substrate/Competitor

n/a

Meas. Tech.

Inhibition Assay

IC50

2.9±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 [Y641F]

Name:

Histone-lysine N-methyltransferase EZH2 [Y641F]

Synonyms:

EZH2 | EZH2(Y641F) | EZH2_HUMAN | Histone-lysine N-methyltransferase EZH2 (Y641F) | KMT6

Type:

n/a

Mol. Mass.:

85351.84

Organism:

Homo sapiens (Human)

Description:

Q15910[Y641F]

Residue:

746

Sequence:

MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFH
ATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPN
NSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKM
KPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPA
PAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQ
NFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVS
CKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEFCGEIISQDEADRRGKVYDK
YMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGE
ELFFDYRYSQADALKYVGIEREMEIP

BDBM190208

n/a

Name

BDBM190208

Synonyms:

EPZ008630 | US9175331, 43

Type

Small organic molecule

Emp. Form.

C25H34BrClN4O2

Mol. Mass.

537.92

SMILES

CCN([C@H]1CC[C@@H](CC1)N(C)C)c1cc(Br)cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1Cl |r,wU:3.2,wD:6.9,(-5.33,.77,;-5.33,-.77,;-4,-1.54,;-4,-3.08,;-2.67,-3.85,;-2.67,-5.39,;-4,-6.16,;-5.33,-5.39,;-5.33,-3.85,;-4,-7.7,;-2.67,-8.47,;-5.33,-8.47,;-2.67,-.77,;-1.33,-1.54,;,-.77,;1.33,-1.54,;,.77,;-1.33,1.54,;-1.33,3.08,;-2.67,3.85,;,3.85,;,5.39,;1.33,6.16,;1.33,7.7,;,8.47,;2.67,8.47,;4,7.7,;5.33,8.47,;4,6.16,;2.67,5.39,;2.67,3.85,;-2.67,.77,;-4,1.54,)|

Structure