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Compound Detail

CHEMBL5275490

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c1ccc(-c2nc([C@H]3OC[C@@H](CCCCN4CCSCC4)CO3)[nH]c2-c2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL5275490
Phase Preclinical
Structure Type MOL
InChI Key UHHFXYUTIIVKOG-ZSQTZEJBSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

463.6
MW (Da)
5.62
ALogP
5
HBA
1
HBD
50.4
PSA (Ų)
0.44
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H33N3O2S
MW 463.65
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.62

Activity Summary

IC50 1 meas. best 7.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sterol O-acyltransferase 1
CHEMBL2782
IC50 7.16 7.16 70.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sterol O-acyltransferase 1 IC50 = 70.0 nM 7.16 Inhibition of ACAT in human THP-1 34213340

Literature References

PubMed DOI Target Context # Activities
34213340 10.1021/acs.jmedchem.1c00790 Sterol O-acyltransferase 1 1
34213340 10.1021/acs.jmedchem.1c00790 ADMET 1

Data from ChEMBL 36 via Core Engine