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Compound Detail

CHEMBL1684833

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CCCCNC(=O)C1CCN(C(=O)CCC(=O)N(CC(C)(C)C)c2ccc(Cl)cc2C(O)c2ccccc2Cl)CC1

Basic Information

ChEMBL ID CHEMBL1684833
Phase Preclinical
Structure Type MOL
InChI Key TVRGAQKACWPKOD-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

604.6
MW (Da)
6.39
ALogP
4
HBA
2
HBD
90.0
PSA (Ų)
0.29
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H43Cl2N3O4
MW 604.62
Aromatic Rings 2
Heavy Atoms 41
NP-Likeness -1.36

Activity Summary

IC50 2 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Squalene synthase
CHEMBL3338
IC50 8.8 8.8 1.6 1
Rattus norvegicus
CHEMBL376
IC50 5.7 5.7 2000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Squalene synthase IC50 = 1.6 nM 8.8 Inhibition of squalene synthase 21353782
Rattus norvegicus IC50 = 2000.0 nM 5.7 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
21353782 10.1016/j.bmc.2011.01.065 Unchecked 1

Data from ChEMBL 36 via Core Engine