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Compound Detail

CHEMBL52284

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CNc1nc(-c2ccccc2)nc2c1ncn2Cc1ccccc1F.CS(=O)(=O)O

Basic Information

ChEMBL ID CHEMBL52284
Phase Preclinical
Structure Type MOL
InChI Key FWQIEFSDCHJUON-UHFFFAOYSA-N
Parent Compound CHEMBL1178979
Active Moiety CHEMBL1178979
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

333.4
MW (Da)
3.72
ALogP
5
HBA
1
HBD
55.6
PSA (Ų)
0.62
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 C20H20FN5O3S
MW 429.48
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -1.62

Activity Summary

IC50 1 meas. best 6.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphodiesterase 4
CHEMBL2093863
IC50 6.3 6.3 500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Phosphodiesterase 4 IC50 = 500.0 nM 6.3 Inhibition of phosphodiesterase 4 at 1 uM cAMP 9191951

Literature References

PubMed DOI Target Context # Activities
9191951 10.1021/jm960827x Phosphodiesterase 3 1
9191951 10.1021/jm960827x Phosphodiesterase 4 1

Data from ChEMBL 36 via Core Engine