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Compound Detail

CHEMBL329556

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COc1ccc(C(=O)Nc2c(Cl)cncc2Cl)c2[nH]c(C(C)C)nc12

Basic Information

ChEMBL ID CHEMBL329556
Phase Preclinical
Structure Type MOL
InChI Key ZDUSDAZRVNATDN-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

379.2
MW (Da)
4.65
ALogP
4
HBA
2
HBD
79.9
PSA (Ų)
0.69
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H16Cl2N4O2
MW 379.25
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.06

Activity Summary

IC50 1 meas. best 7.57
Ki 1 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 7.62 7.62 24.0 1
Phosphodiesterase 4
CHEMBL2093863
IC50 7.57 7.57 27.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 16.0 % Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Ki = 24.0 nM 7.62 Inhibition of Rolipram binding to PDE4 9873613
Phosphodiesterase 4 IC50 = 27.0 nM 7.57 Inhibition of PDE4 from guinea pig macrophages 9873613

Literature References

PubMed DOI Target Context # Activities
9873613 10.1016/s0960-894x(98)00497-1 Mus musculus 2
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