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Compound Detail

CHEMBL3605440

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Cc1cc(C)c(CNC(=O)c2ccc(Oc3ccccc3)cc2)c(=O)[nH]1

Basic Information

ChEMBL ID CHEMBL3605440
Phase Preclinical
Structure Type MOL
InChI Key WEXSIZXYLPOYGS-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

348.4
MW (Da)
3.71
ALogP
3
HBA
2
HBD
71.2
PSA (Ų)
0.74
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H20N2O3
MW 348.40
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -1.12

Activity Summary

IC50 2 meas. best 6.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone-lysine N-methyltransferase EZH2
CHEMBL2189110
IC50 6.37 6.37 430.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26189078 10.1016/j.bmcl.2015.06.056 Histone-lysine N-methyltransferase EZH2 1
35531606 10.1021/acs.jmedchem.2c00047 Histone-lysine N-methyltransferase EZH2 1

Data from ChEMBL 36 via Core Engine