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Compound Detail

CHEMBL3397331

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COCc1cc(CNC(=O)[C@@H](N)CCSC[C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)n[nH]1

Basic Information

ChEMBL ID CHEMBL3397331
Phase Preclinical
Structure Type MOL
InChI Key ZIPKVYXPDYEQMJ-WUMBASEESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

507.6
MW (Da)
-1.34
ALogP
13
HBA
6
HBD
212.3
PSA (Ų)
0.17
QED
3
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H29N9O5S
MW 507.58
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.09

Activity Summary

IC50 1 meas. best 4.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone-lysine N-methyltransferase EZH2
CHEMBL2189110
IC50 4.4 4.4 40000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25746813 10.1016/j.bmcl.2015.02.017 Histone-lysine N-methyltransferase EZH2 2

Data from ChEMBL 36 via Core Engine