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Compound Detail

CHEMBL1685014

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COc1ccccc1C(O)c1cc(Cl)ccc1N(CC(C)(C)C)C(=O)CCC(=O)N1CCC(C(=O)O)CC1

Basic Information

ChEMBL ID CHEMBL1685014
Phase Preclinical
Structure Type MOL
InChI Key OJERQCMUTJNFNE-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

545.1
MW (Da)
4.91
ALogP
5
HBA
2
HBD
107.4
PSA (Ų)
0.46
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H37ClN2O6
MW 545.08
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -1.02

Activity Summary

IC50 2 meas. best 8.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Squalene synthase
CHEMBL3338
IC50 8.77 8.77 1.7 1
Rattus norvegicus
CHEMBL376
IC50 6.22 6.22 600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Squalene synthase IC50 = 1.7 nM 8.77 Inhibition of squalene synthase 21353782
Rattus norvegicus IC50 = 600.0 nM 6.22 Inhibition of cholesterol synthesis in rat hepatic cells 21353782

Literature References

PubMed DOI Target Context # Activities
21353782 10.1016/j.bmc.2011.01.065 Squalene synthase 1
21353782 10.1016/j.bmc.2011.01.065 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine