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Compound Detail

CHEMBL3414617

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O=C(O)c1ccc2c(c1)nc(NC(=O)c1ccccc1)n2CCCc1ccccc1

Basic Information

ChEMBL ID CHEMBL3414617
Phase Preclinical
Structure Type MOL
InChI Key WPXMEOBILYVKBC-UHFFFAOYSA-N
2
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

399.4
MW (Da)
4.62
ALogP
4
HBA
2
HBD
84.2
PSA (Ų)
0.47
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H21N3O3
MW 399.45
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.12

Activity Summary

IC50 5 meas. best 5.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone-lysine N-methyltransferase EHMT2
CHEMBL6032
IC50 5.82 5.355 1500.0 4
Histone-lysine N-methyltransferase EHMT1
CHEMBL6031
IC50 5.8 5.8 1600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25406853 10.1021/jm501234a Histone-lysine N-methyltransferase EHMT2 1
31276898 10.1016/j.ejmech.2019.06.072 Histone-lysine N-methyltransferase EHMT2 1
30753076 10.1021/acs.jmedchem.8b02008 Histone-lysine N-methyltransferase EHMT2 1
30753076 10.1021/acs.jmedchem.8b02008 Histone-lysine N-methyltransferase EHMT1 1
37974951 10.1021/acsmedchemlett.3c00344 Histone-lysine N-methyltransferase EHMT2 1

Data from ChEMBL 36 via Core Engine