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Compound Detail

CHEMBL3397323

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Nc1ncnc2c1ncn2[C@@H]1O[C@H](CSCC[C@H](N)C(=O)NCc2cnn(Cc3ccccc3)c2)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL3397323
Phase Preclinical
Structure Type MOL
InChI Key RNCWYNOSSMWXMM-PJBGZOMASA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

553.6
MW (Da)
0.04
ALogP
13
HBA
5
HBD
192.2
PSA (Ų)
0.16
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H31N9O4S
MW 553.65
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.41

Activity Summary

IC50 1 meas. best 4.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone-lysine N-methyltransferase EZH2
CHEMBL2189110
IC50 4.62 4.62 24000.0 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