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Compound Detail

CHEMBL492976

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COc1ccc(-c2nc3cnc(NCc4ccc(Cl)c(Cl)c4)nc3n(CCNS(C)(=O)=O)c2=O)cc1

Basic Information

ChEMBL ID CHEMBL492976
Phase Preclinical
Structure Type MOL
InChI Key JSOGDVANKKEGRE-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

549.4
MW (Da)
3.33
ALogP
9
HBA
2
HBD
128.1
PSA (Ų)
0.33
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H22Cl2N6O4S
MW 549.44
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.43

Activity Summary

IC50 2 meas. best 5.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Stearoyl-CoA desaturase
CHEMBL5555
IC50 5.78 5.78 1670.0 1
Unchecked
CHEMBL612545
IC50 5.55 5.55 2800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Stearoyl-CoA desaturase IC50 = 1670.0 nM 5.78 Inhibition of Delta-9-desaturase in human HepG2 cells 19249203
Unchecked IC50 = 2800.0 nM 5.55 Inhibition of rat microsomal Delta-9-desaturase 19249203

Literature References

PubMed DOI Target Context # Activities
19249203 10.1016/j.bmcl.2009.02.019 Unchecked 1
19249203 10.1016/j.bmcl.2009.02.019 Stearoyl-CoA desaturase 1

Data from ChEMBL 36 via Core Engine