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Compound Detail

CHEMBL373102

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CCN1C(=O)c2c(nc(Br)n2Cc2ccc(O)cc2)N2C[C@@H](Cc3ccccc3)N=C12

Basic Information

ChEMBL ID CHEMBL373102
Phase Preclinical
Structure Type MOL
InChI Key HVDQYPSFEUUGDN-QGZVFWFLSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

480.4
MW (Da)
3.66
ALogP
6
HBA
1
HBD
74.0
PSA (Ų)
0.61
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H22BrN5O2
MW 480.37
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.40

Activity Summary

IC50 5 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL1827
IC50 8.6 8.6 2.5 1
Phosphodiesterase 6
CHEMBL2097163
IC50 6.75 6.75 180.0 1
Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A
CHEMBL2717
IC50 6.27 6.27 540.0 1
Phosphodiesterase 4
CHEMBL2093863
IC50 5.85 5.85 1400.0 1
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
CHEMBL4409
IC50 5.66 5.66 2200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15837326 10.1016/j.bmcl.2005.02.083 cGMP-specific 3',5'-cyclic phosphodiesterase 1
15837326 10.1016/j.bmcl.2005.02.083 Unchecked 1
15837326 10.1016/j.bmcl.2005.02.083 High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A 1
15837326 10.1016/j.bmcl.2005.02.083 cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A 1
15837326 10.1016/j.bmcl.2005.02.083 Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A 1
15837326 10.1016/j.bmcl.2005.02.083 Phosphodiesterase, PDE1/PDE5 1
15837326 10.1016/j.bmcl.2005.02.083 Phosphodiesterases; PDE5 & PDE6 1
15837326 10.1016/j.bmcl.2005.02.083 Phosphodiesterase 1 1
15837326 10.1016/j.bmcl.2005.02.083 cGMP-dependent 3',5'-cyclic phosphodiesterase 1
15837326 10.1016/j.bmcl.2005.02.083 Phosphodiesterase 3 1
15837326 10.1016/j.bmcl.2005.02.083 Phosphodiesterase 4 1
15837326 10.1016/j.bmcl.2005.02.083 Phosphodiesterase 6 1
15837326 10.1016/j.bmcl.2005.02.083 Phosphodiesterase 7 1

Data from ChEMBL 36 via Core Engine