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Compound Detail

CHEMBL5188827

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CCCc1cc(C)[nH]c(=O)c1CNC(=O)c1cc(-c2ccc(N3CCOCC3)nc2)c2ccn(C(C)C)c2c1C

Basic Information

ChEMBL ID CHEMBL5188827
Phase Preclinical
Structure Type MOL
InChI Key LJZMJJJDAJFPJX-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

541.7
MW (Da)
5.31
ALogP
6
HBA
2
HBD
92.2
PSA (Ų)
0.32
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H39N5O3
MW 541.70
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -1.27

Activity Summary

IC50 1 meas. best 11.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone-lysine N-methyltransferase EZH2
CHEMBL2189110
IC50 11.0 11.0 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone-lysine N-methyltransferase EZH2 IC50 = 0.01 nM 11.0 Inhibition of EZH2 (unknown origin) 35531606

Literature References

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

Data from ChEMBL 36 via Core Engine