Ki Summary

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Target

Histone-lysine N-methyltransferase EZH2 [Y641F]

Ligand

BDBM310800

Substrate/Competitor

n/a

Meas. Tech.

Wild-Type PRC2 Enzyme Assay

IC50

1.000±n/a nM

Citation

Campbell, JE Substituted benzene compounds US Patent US10150764 Publication Date 12/11/2018

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

BDBM310800

n/a

Name

BDBM310800

Synonyms:

US10150764, Compound 86

Type

Small organic molecule

Emp. Form.

C24H36ClN5O3

Mol. Mass.

478.027

SMILES

CCN([C@H]1CC[C@@H](CC1)N(C)C)c1cc(Cl)cc(C(=O)NCc2c(OC)n(C)[nH]c2=O)c1C |r,wU:6.9,wD:3.2,(-2.82,.13,;-2.82,1.67,;-1.48,2.44,;-1.48,3.98,;-.15,4.75,;-.15,6.29,;-1.48,7.06,;-2.82,6.29,;-2.82,4.75,;-1.48,8.6,;-.15,9.37,;-2.82,9.37,;-.15,1.67,;1.18,2.44,;2.52,1.67,;3.85,2.44,;2.52,.13,;1.18,-.64,;1.18,-2.18,;2.52,-2.95,;-.15,-2.95,;-.15,-4.49,;-1.48,-5.26,;-1.48,-6.8,;-.39,-7.89,;-.79,-9.37,;-2.95,-7.27,;-3.72,-8.61,;-3.85,-6.03,;-2.95,-4.78,;-3.72,-3.45,;-.15,.13,;-1.48,-.64,)|

Structure