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Compound Detail

CHEMBL59408

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COc1ccc(/C=C2\C(=O)Nc3ccc([N+](=O)[O-])cc32)cc1OC1CC2CCC1C2

Basic Information

ChEMBL ID CHEMBL59408
Phase Preclinical
Structure Type MOL
InChI Key WBZLODXOELQXEH-NVMNQCDNSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

406.4
MW (Da)
4.66
ALogP
5
HBA
1
HBD
90.7
PSA (Ų)
0.44
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H22N2O5
MW 406.44
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.25

Activity Summary

IC50 2 meas. best 5.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphodiesterase 4
CHEMBL2093863
IC50 5.92 5.92 1200.0 1
Phosphodiesterase 4
CHEMBL2111373
IC50 4.21 4.21 62000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Phosphodiesterase 4 IC50 = 1200.0 nM 5.92 Inhibition of Phosphodiesterase 4 -
Phosphodiesterase 4 IC50 = 62000.0 nM 4.21 Inhibition of [3H]rolipram binding to Phosphodiesterase 4 (PDE IV) -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(95)00333-O Phosphodiesterase 4 2
- 10.1016/0960-894X(95)00333-O Phosphodiesterase 3 1

Data from ChEMBL 36 via Core Engine