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Compound Detail

CHEMBL1213959

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COc1cc2c(NC3CCN(C)CC3)nc(N3CCCN(C)CC3)nc2cc1OCCCC(C)C

Basic Information

ChEMBL ID CHEMBL1213959
Phase Preclinical
Structure Type MOL
InChI Key BHTMDPGDPXZJBX-UHFFFAOYSA-N
2
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

484.7
MW (Da)
4.10
ALogP
8
HBA
1
HBD
66.0
PSA (Ų)
0.53
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H44N6O2
MW 484.69
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.88

Activity Summary

IC50 5 meas. best 6.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 6.82 6.82 150.0 1
Histone-lysine N-methyltransferase EHMT2
CHEMBL6032
IC50 5.47 5.375 3400.0 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