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Compound Detail

CHEMBL593225

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COc1ccc(CNc2ncnc3c(CCO)c(OC)c(NS(=O)(=O)N(C)C)cc23)cc1Cl

Basic Information

ChEMBL ID CHEMBL593225
Phase Preclinical
Structure Type MOL
InChI Key GCBJQSZJMUMFEM-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

496.0
MW (Da)
2.67
ALogP
8
HBA
3
HBD
125.9
PSA (Ų)
0.39
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H26ClN5O5S
MW 495.99
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.94

Activity Summary

IC50 2 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL3478
IC50 7.92 7.92 12.0 1
Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha
CHEMBL3741
IC50 5.1 5.1 7950.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19906530 10.1016/j.bmcl.2009.10.071 cGMP-specific 3',5'-cyclic phosphodiesterase 1
19906530 10.1016/j.bmcl.2009.10.071 Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha 1
19906530 10.1016/j.bmcl.2009.10.071 Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A 1
19906530 10.1016/j.bmcl.2009.10.071 Liver microsomes 1

Data from ChEMBL 36 via Core Engine