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Compound Detail

CHEMBL318502

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O=c1c2c(ncn2Cc2ccccc2)c2cccnc2n1-c1ccccc1

Basic Information

ChEMBL ID CHEMBL318502
Phase Preclinical
Structure Type MOL
InChI Key HNQGGXAGBKEMKM-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

352.4
MW (Da)
3.78
ALogP
5
HBA
0
HBD
52.7
PSA (Ų)
0.50
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H16N4O
MW 352.40
Aromatic Rings 5
Heavy Atoms 27
NP-Likeness -1.15

Activity Summary

IC50 1 meas. best 9.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
3',5'-cyclic-AMP phosphodiesterase 4A
CHEMBL254
IC50 9.22 9.22 0.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
3',5'-cyclic-AMP phosphodiesterase 4A IC50 = 0.6 nM 9.22 Inhibition of recombinant human PDE4A expressed in Sf9 cells 11052785

Literature References

PubMed DOI Target Context # Activities
1495017 10.1021/jm00093a020 Rattus norvegicus 6
11052785 10.1021/jm000065c Phosphodiesterase 4 2
1495017 10.1021/jm00093a020 Mus musculus 1
11052785 10.1021/jm000065c 3',5'-cyclic-AMP phosphodiesterase 4A 1

Data from ChEMBL 36 via Core Engine