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Compound Detail

CHEMBL1933481

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CCCC[C@H](C)[C@@H]1CC(=O)N[C@@H](C(c2ccccc2)c2ccccc2)C(=O)N[C@H](Cn2cc(CNC(=O)CCCCNC(=O)CCCC[C@@H]3SC[C@@H]4NC(=O)N[C@@H]43)nn2)C(=O)N[C@H](C2CCCCC2)C(=O)O1

Basic Information

ChEMBL ID CHEMBL1933481
Phase Preclinical
Structure Type MOL
InChI Key QFDXNRLQXUHQMI-ACRGOTNFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

1011.3
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C53H74N10O8S
MW 1011.30

Activity Summary

IC50 1 meas. best 6.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sterol O-acyltransferase 1
CHEMBL2782
IC50 6.1 6.1 800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sterol O-acyltransferase 1 IC50 = 800.0 nM 6.1 Inhibition of ACAT1- mediated cholesteryl ester synthesis in macrophages 22079027

Literature References

PubMed DOI Target Context # Activities
22079027 10.1016/j.bmcl.2011.10.045 Sterol O-acyltransferase 1 2
22079027 10.1016/j.bmcl.2011.10.045 ADMET 1

Data from ChEMBL 36 via Core Engine