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Compound Detail

CHEMBL329023

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COc1ccc(C(=O)Nc2c(Cl)cncc2Cl)c2nc(C3CCCC3)n(C)c12

Basic Information

ChEMBL ID CHEMBL329023
Phase Preclinical
Structure Type MOL
InChI Key FZGLZPNZCVMSQV-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

419.3
MW (Da)
5.19
ALogP
5
HBA
1
HBD
69.0
PSA (Ų)
0.63
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H20Cl2N4O2
MW 419.31
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.94

Activity Summary

IC50 1 meas. best 5.36
Ki 1 meas. best 5.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphodiesterase 4
CHEMBL2093863
IC50 5.36 5.36 4400.0 1
Unchecked
CHEMBL612545
Ki 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Phosphodiesterase 4 IC50 = 4400.0 nM 5.36 Inhibition of PDE4 from guinea pig macrophages 9873613
Unchecked Ki = 10000.0 nM 5.0 Inhibition of Rolipram binding to PDE4 9873613

Literature References

PubMed DOI Target Context # Activities
9873613 10.1016/s0960-894x(98)00497-1 Phosphodiesterase 4 1
9873613 10.1016/s0960-894x(98)00497-1 Unchecked 1

Data from ChEMBL 36 via Core Engine