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Compound Detail

CHEMBL1213766

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COc1cc2c(NC3CCN(C)CC3)nc(N3CCCN(C)CC3)nc2cc1OCCN(C)C

Basic Information

ChEMBL ID CHEMBL1213766
Phase Preclinical
Structure Type MOL
InChI Key PTRSMGYKEMPQRR-UHFFFAOYSA-N
1
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

471.6
MW (Da)
2.23
ALogP
9
HBA
1
HBD
69.2
PSA (Ų)
0.62
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 C25H41N7O2
MW 471.65
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -1.21

Activity Summary

IC50 4 meas. best 6.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone-lysine N-methyltransferase EHMT2
CHEMBL6032
IC50 6.96 6.94 110.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20614940 10.1021/jm100478y Histone-lysine N-methyltransferase EHMT2 2
29308121 10.1039/C7MD00052A Histone-lysine N-methyltransferase EHMT2 2
29308121 10.1039/C7MD00052A Plasmodium falciparum 1
29308121 10.1039/C7MD00052A HepG2 1
29308121 10.1039/C7MD00052A Unchecked 1

Data from ChEMBL 36 via Core Engine