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Compound Detail

CHEMBL1642568

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Cc1ccc2nc(CCc3nc(-c4ccccc4)cn3C)n3nc(C)cc3c2c1

Basic Information

ChEMBL ID CHEMBL1642568
Phase Preclinical
Structure Type MOL
InChI Key PXIUKGSKVQLIBW-UHFFFAOYSA-N
7
Targets
9
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

381.5
MW (Da)
4.69
ALogP
5
HBA
0
HBD
48.0
PSA (Ų)
0.45
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 C24H23N5
MW 381.48
Aromatic Rings 5
Heavy Atoms 29
NP-Likeness -1.34

Activity Summary

IC50 9 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
CHEMBL4409
IC50 7.8 7.8 16.0 1
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL1827
IC50 5.0 5.0 10000.0 1
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A
CHEMBL241
IC50 5.0 5.0 10000.0 1
3',5'-cyclic-AMP phosphodiesterase 4D
CHEMBL288
IC50 5.0 5.0 10000.0 1
Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B
CHEMBL4425
IC50 5.0 5.0 10000.0 1
3',5'-cyclic-AMP phosphodiesterase 7B
CHEMBL4716
IC50 5.0 5.0 10000.0 1
Unchecked
CHEMBL612545
IC50 5.0 5.0 10000.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21087867 10.1016/j.bmc.2010.10.038 Unchecked 3
21087867 10.1016/j.bmc.2010.10.038 cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A 1
21087867 10.1016/j.bmc.2010.10.038 Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B 1
21087867 10.1016/j.bmc.2010.10.038 cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A 1
21087867 10.1016/j.bmc.2010.10.038 3',5'-cyclic-AMP phosphodiesterase 4D 1
21087867 10.1016/j.bmc.2010.10.038 cGMP-specific 3',5'-cyclic phosphodiesterase 1
21087867 10.1016/j.bmc.2010.10.038 3',5'-cyclic-AMP phosphodiesterase 7B 1

Data from ChEMBL 36 via Core Engine