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Target
Histone-lysine N-methyltransferase EZH2
Ligand
BDBM359808
Substrate
n/a
Meas. Tech.
Biological Assay
IC50
750±n/a nM
Citation
Seitz, SP; Markwalder, JA; Purandare, AV Inhibitors of lysine methyl transferase US Patent US9822103 Publication Date 11/21/2017
More Info.:
Target
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:
MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEWKQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNFMVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQYNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEELKEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFHATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPNNSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKMKPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPAPAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQNFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVSCKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDKYMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGEELFFDYRYSQADALKYVGIEREMEIP
Inhibitor
Name:
BDBM359808
Synonyms:
US9822103, Example 68 | rac-(3aS,8bS)—N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3a-methyl-5-(4-(piperazin-1-yl)phenyl)-2,3,3a,8b-tetrahydro-1H-cyclopenta[b]benzofuran-7-carboxamide
Type:
Small organic molecule
Emp. Form.:
C31H36N4O3
Mol. Mass.:
512.6425
SMILES:
Cc1cc(C)c(CNC(=O)c2cc3[C@@H]4CCC[C@]4(C)Oc3c(c2)-c2ccc(cc2)N2CCNCC2)c(=O)[nH]1 |r|