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Compound Detail

CHEMBL537863

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CCCCn1c(=O)c(NC(=O)Nc2c(C(C)C)cc(CN(CC)CC)cc2C(C)C)c(-c2cccc(OC)c2)c2cccnc21.Cl

Basic Information

ChEMBL ID CHEMBL537863
Phase Preclinical
Structure Type MOL
InChI Key HTDWRSKVZLJUDL-UHFFFAOYSA-N
Parent Compound CHEMBL1188980
Active Moiety CHEMBL1188980
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

611.8
MW (Da)
8.60
ALogP
6
HBA
2
HBD
88.5
PSA (Ų)
0.16
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H50ClN5O3
MW 648.29
Aromatic Rings 4
Heavy Atoms 45
NP-Likeness -0.95

Activity Summary

IC50 1 meas. best 6.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sterol O-acyltransferase 1
CHEMBL285
IC50 6.17 6.17 680.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sterol O-acyltransferase 1 IC50 = 680.0 nM 6.17 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

Data from ChEMBL 36 via Core Engine