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Compound Detail

CHEMBL2315489

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CC(C)(C)c1ccc(CC(=O)N2CCC3(CC2)CCN(CNC(=O)c2cccnc2)c2ccccc2O3)cc1

Basic Information

ChEMBL ID CHEMBL2315489
Phase Preclinical
Structure Type MOL
InChI Key NJHIXFGZOJNQNH-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

526.7
MW (Da)
4.96
ALogP
5
HBA
1
HBD
74.8
PSA (Ų)
0.51
QED
1
Ro5 Violations
5
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 3
Heavy Atoms 39
NP-Likeness -1.08

Activity Summary

IC50 1 meas. best 5.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acyl-CoA desaturase 1
CHEMBL5424
IC50 5.82 5.82 1500.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 341.0 ng/g.hr Rattus norvegicus
Cmax 169.0 ng/g Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acyl-CoA desaturase 1 IC50 = 1500.0 nM 5.82 Inhibition of rat SCD1 by rat microsomal assay 23265904

Literature References

PubMed DOI Target Context # Activities
23265904 10.1016/j.bmcl.2012.11.075 Rattus norvegicus 2
23265904 10.1016/j.bmcl.2012.11.075 Nucleic Acid 1
23265904 10.1016/j.bmcl.2012.11.075 Liver 1
23265904 10.1016/j.bmcl.2012.11.075 Plasma 1
23265904 10.1016/j.bmcl.2012.11.075 Acyl-CoA desaturase 1 1

Data from ChEMBL 36 via Core Engine