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Compound Detail

CHEMBL604271

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CCC(=O)N(C)c1cc2c(NCc3ccc(OC)c(Cl)c3)ncnc2c(CCO)c1OC

Basic Information

ChEMBL ID CHEMBL604271
Phase Preclinical
Structure Type MOL
InChI Key JVYRZEUKHPHYCW-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

458.9
MW (Da)
3.82
ALogP
7
HBA
2
HBD
96.8
PSA (Ų)
0.50
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H27ClN4O4
MW 458.95
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.86

Activity Summary

IC50 3 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL3478
IC50 9.0 9.0 1.0 1
Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha
CHEMBL3741
IC50 6.5 6.5 320.0 1
Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A
CHEMBL2717
IC50 5.28 5.28 5200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19906530 10.1016/j.bmcl.2009.10.071 Liver microsomes 2
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 ADMET 1
19906530 10.1016/j.bmcl.2009.10.071 Caco-2 1
19906530 10.1016/j.bmcl.2009.10.071 Oryctolagus cuniculus 1

Data from ChEMBL 36 via Core Engine