Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetHistone-lysine N-methyltransferase EZH2
LigandBDBM378912
Substrate/Competitorn/a
Meas. Tech.EZH2 enzymatic activity
IC50 1.000±n/a nM
Citation Marx, MALee, MRGalemmo, RABobinski, TP EZH2 inhibitors US Patent US10266542 Publication Date 4/23/2019
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM378912
n/a
NameBDBM378912
Synonyms:5,8-dichloro-7-[methoxy(oxetan-3-yl)methyl]-2-[(7-methyl-5-oxo-1,6-dihydropyrrolo[2,3-c]pyridin-4-yl)methyl]-3,4-dihydroisoquinolin-1-one | US10266542, Example 17
TypeSmall organic molecule
Emp. Form.C24H25Cl2N3O4
Mol. Mass.490.379
SMILESCOC(C1COC1)c1cc(Cl)c2CCN(Cc3c4ccn(C)c4c(C)[nH]c3=O)C(=O)c2c1Cl
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: