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Compound Detail

CHEMBL1685028

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COc1cccc(C(O)c2cc(Cl)ccc2N(CC(C)(C)C)C(=O)CCC(=O)N2CCCC(C(=O)O)C2)c1OC

Basic Information

ChEMBL ID CHEMBL1685028
Phase Preclinical
Structure Type MOL
InChI Key CZHJOZMJUZDQIB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

575.1
MW (Da)
4.92
ALogP
6
HBA
2
HBD
116.6
PSA (Ų)
0.41
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H39ClN2O7
MW 575.10
Aromatic Rings 2
Heavy Atoms 40
NP-Likeness -0.96

Activity Summary

IC50 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Squalene synthase
CHEMBL3338
IC50 8.7 8.7 2.0 1
Rattus norvegicus
CHEMBL376
IC50 5.82 5.82 1500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Squalene synthase IC50 = 2.0 nM 8.7 Inhibition of squalene synthase 21353782
Rattus norvegicus IC50 = 1500.0 nM 5.82 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 No relevant target 1
21353782 10.1016/j.bmc.2011.01.065 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine