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Compound Detail

CHEMBL4753261

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COc1ccc(-c2nc(C(N)=O)cs2)c2c1oc1ccccc12

Basic Information

ChEMBL ID CHEMBL4753261
Phase Preclinical
Structure Type MOL
InChI Key OAGLCSHEZLIPME-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

324.4
MW (Da)
3.82
ALogP
5
HBA
1
HBD
78.3
PSA (Ų)
0.62
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H12N2O3S
MW 324.36
Aromatic Rings 4
Heavy Atoms 23
NP-Likeness -0.43

Activity Summary

IC50 1 meas. best 6.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.41 6.41 385.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 385.7 nM 6.41 Inhibition of PDE-4 in human PBMC assessed as LPS-induced TNFalpha production in... 27713015

Literature References

PubMed DOI Target Context # Activities
27713015 10.1016/j.bmc.2016.09.011 3',5'-cyclic-AMP phosphodiesterase 4B 3
27713015 10.1016/j.bmc.2016.09.011 Unchecked 3

Data from ChEMBL 36 via Core Engine