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Compound Detail

CHEMBL539597

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CCCCn1c(=O)c(NC(=O)Nc2c(C(C)C)cc(N)cc2C(C)C)c(-c2cccc(OCCCO)c2)c2cccnc21.Cl

Basic Information

ChEMBL ID CHEMBL539597
Phase Preclinical
Structure Type MOL
InChI Key FAFVVBJEQCPDIA-UHFFFAOYSA-N
Parent Compound CHEMBL573970
Active Moiety CHEMBL573970
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

585.8
MW (Da)
7.10
ALogP
7
HBA
4
HBD
131.5
PSA (Ų)
0.10
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H44ClN5O4
MW 622.21
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -0.67

Activity Summary

IC50 1 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sterol O-acyltransferase 1
CHEMBL285
IC50 7.68 7.68 21.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 39.8 ng.hr.mL-1 Oryctolagus cuniculus
Cmax 36363.64 nM Mus musculus
Cmax 27.32 nM Oryctolagus cuniculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sterol O-acyltransferase 1 IC50 = 21.0 nM 7.68 Inhibitory activity against ACAT in rat macrophages 16242323

Literature References

PubMed DOI Target Context # Activities
16242323 10.1016/j.bmcl.2005.09.056 No relevant target 3
16242323 10.1016/j.bmcl.2005.09.056 Oryctolagus cuniculus 3
16242323 10.1016/j.bmcl.2005.09.056 Sterol O-acyltransferase 1 1
16242323 10.1016/j.bmcl.2005.09.056 Mus musculus 1

Data from ChEMBL 36 via Core Engine