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Compound Detail

CHEMBL1684826

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

Basic Information

ChEMBL ID CHEMBL1684826
Phase Preclinical
Structure Type MOL
InChI Key AJHBBNODEDFSIB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

577.5
MW (Da)
6.04
ALogP
5
HBA
1
HBD
87.2
PSA (Ų)
0.37
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H38Cl2N2O5
MW 577.55
Aromatic Rings 2
Heavy Atoms 39
NP-Likeness -1.18

Activity Summary

IC50 2 meas. best 9.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Squalene synthase
CHEMBL3338
IC50 9.07 9.07 0.8 1
Rattus norvegicus
CHEMBL376
IC50 5.77 5.77 1700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Squalene synthase IC50 = 0.85 nM 9.07 Inhibition of squalene synthase 21353782
Rattus norvegicus IC50 = 1700.0 nM 5.77 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