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Compound Detail

CHEMBL445098

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CNc1ncnc2c1ncn2Cc1ccccc1F.CS(=O)(=O)O

Basic Information

ChEMBL ID CHEMBL445098
Phase Preclinical
Structure Type MOL
InChI Key OAOJUQDGTDJXBZ-UHFFFAOYSA-N
Parent Compound CHEMBL7359
Active Moiety CHEMBL7359
5
Targets
8
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

257.3
MW (Da)
2.06
ALogP
5
HBA
1
HBD
55.6
PSA (Ų)
0.78
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 C14H16FN5O3S
MW 353.38
Aromatic Rings 3
Heavy Atoms 19
NP-Likeness -1.65

Activity Summary

Ki 5 meas. best 5.7
IC50 3 meas. best 5.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphodiesterase 4
CHEMBL2093863
Ki 5.7 5.7 2000.0 1
Phosphodiesterase 4
CHEMBL2093863
IC50 5.52 5.52 3000.0 1
Phosphodiesterase 1
CHEMBL2095150
Ki 5.43 5.43 3700.0 1
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL1827
Ki 5.19 5.19 6500.0 1
GABA-A receptor; anion channel
CHEMBL1907607
IC50 4.89 4.89 13000.0 1
Phosphodiesterase 3
CHEMBL2094125
Ki 4.46 4.46 35000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9191951 10.1021/jm960827x Phosphodiesterase 3 2
9191951 10.1021/jm960827x Phosphodiesterase 4 2
9191951 10.1021/jm960827x Phosphodiesterase 1 1
9191951 10.1021/jm960827x cGMP-dependent 3',5'-cyclic phosphodiesterase 1
9191951 10.1021/jm960827x cGMP-specific 3',5'-cyclic phosphodiesterase 1
9191951 10.1021/jm960827x GABA-A receptor; anion channel 1
9191951 10.1021/jm960827x Adenosine receptor A1 1
9191951 10.1021/jm960827x Adenosine A2 receptor 1

Data from ChEMBL 36 via Core Engine