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Compound Detail

CHEMBL382183

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CCCCn1c(=O)c(NC(=O)Nc2c(C(C)C)cccc2C(C)C)c(-c2cccc(OC)c2)c2cccnc21

Basic Information

ChEMBL ID CHEMBL382183
Phase Preclinical
Structure Type MOL
InChI Key ORFMGXFFDRWECM-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

526.7
MW (Da)
7.76
ALogP
5
HBA
2
HBD
85.2
PSA (Ų)
0.23
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 C32H38N4O3
MW 526.68
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.84

Activity Summary

IC50 1 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sterol O-acyltransferase 1
CHEMBL285
IC50 7.96 7.96 11.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 0.01899 nM Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sterol O-acyltransferase 1 IC50 = 11.0 nM 7.96 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 Sterol O-acyltransferase 1 1
16242323 10.1016/j.bmcl.2005.09.056 Mus musculus 1

Data from ChEMBL 36 via Core Engine