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Compound Detail

CHEMBL454397

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

Basic Information

ChEMBL ID CHEMBL454397
Phase Preclinical
Structure Type MOL
InChI Key ZUCFGSAENWHFPO-UHFFFAOYSA-N
Parent Compound CHEMBL573970
Active Moiety CHEMBL573970
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
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 C34H46ClN5O5
MW 640.22
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -0.67

Activity Summary

IC50 1 meas. best 7.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sterol O-acyltransferase 1
CHEMBL2782
IC50 7.51 7.51 31.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sterol O-acyltransferase 1 IC50 = 31.0 nM 7.51 Inhibition of ACAT in human HepG2 cells 19167888

Literature References

PubMed DOI Target Context # Activities
20356098 10.1021/jm901909p Hamster 2
19167888 10.1016/j.bmcl.2009.01.020 Sterol O-acyltransferase 1 1
19167888 10.1016/j.bmcl.2009.01.020 HepG2 1
20356098 10.1021/jm901909p Sterol O-acyltransferase 1 1
20356098 10.1021/jm901909p HepG2 1

Data from ChEMBL 36 via Core Engine