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Compound Detail

CHEMBL4166822

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COc1cc2c(NC3CCN(C)CC3)cc(C(F)(F)F)nc2cc1OCCCN1CCCC1

Basic Information

ChEMBL ID CHEMBL4166822
Phase Preclinical
Structure Type MOL
InChI Key UXDIXDDGEATWIR-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

466.6
MW (Da)
4.63
ALogP
6
HBA
1
HBD
49.9
PSA (Ų)
0.57
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H33F3N4O2
MW 466.55
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.17

Activity Summary

IC50 1 meas. best 6.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone-lysine N-methyltransferase EHMT2
CHEMBL6032
IC50 6.2 6.2 637.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29953809 10.1021/acs.jmedchem.7b01926 Histone-lysine N-methyltransferase EHMT2 1
29953809 10.1021/acs.jmedchem.7b01926 DNA (cytosine-5)-methyltransferase 1 1
29953809 10.1021/acs.jmedchem.7b01926 Unchecked 1

Data from ChEMBL 36 via Core Engine