Ki Summary

Reaction Details

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Target

Histone-lysine N-methyltransferase EZH2

Ligand

BDBM190210

Substrate/Competitor

n/a

Meas. Tech.

Inhibition Assay

IC50

9.4±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

Name:

Histone-lysine N-methyltransferase EZH2

Synonyms:

ENX-1 | EZH2 | EZH2_HUMAN | Enhancer of zeste homolog 2 (EZH2) | Histone-lysine N-methyltransferase EZH2 | KMT6 | Lysine N-methyltransferase 6

Type:

Protein

Mol. Mass.:

85367.84

Organism:

Homo sapiens (Human)

Description:

Q15910

Residue:

746

Sequence:

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

BDBM190210

n/a

Name

BDBM190210

Synonyms:

EPZ008989 | US9175331, 46

Type

Small organic molecule

Emp. Form.

C27H37ClF2N4O2

Mol. Mass.

523.058

SMILES

CCN([C@H]1CC[C@@H](CC1)N(C)CC(F)F)c1cc(Cl)cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C |r,wU:3.2,wD:6.9,(-4.67,1.93,;-4.67,.38,;-3.33,-.38,;-3.33,-1.93,;-2,-2.69,;-2,-4.23,;-3.33,-5,;-4.67,-4.23,;-4.67,-2.69,;-3.33,-6.54,;-2,-7.31,;-4.67,-7.31,;-4.67,-8.85,;-6,-9.63,;-3.33,-9.63,;-2,.38,;-.67,-.38,;.67,.38,;2,-.38,;.67,1.93,;-.67,2.69,;-.67,4.23,;-2,5,;.67,5,;.67,6.54,;2,7.31,;2,8.85,;.67,9.63,;3.33,9.63,;4.67,8.85,;6,9.63,;4.67,7.31,;3.33,6.54,;3.33,5,;-2,1.93,;-3.33,2.69,)|

Structure