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Compound Detail

CHEMBL54079

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CCCc1nn(C)c2c(=O)[nH]c(-c3ccccc3OCC)nc12

Basic Information

ChEMBL ID CHEMBL54079
Phase Preclinical
Structure Type MOL
InChI Key MXQUEDUMKWBYHI-UHFFFAOYSA-N
3
Targets
9
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

312.4
MW (Da)
2.67
ALogP
5
HBA
1
HBD
72.8
PSA (Ų)
0.79
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 C17H20N4O2
MW 312.37
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.08

Activity Summary

IC50 9 meas. best 7.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL1827
IC50 7.57 7.5214 26.9 7
Phosphodiesterase 1
CHEMBL2095150
IC50 6.1 6.1 790.0 1
Phosphodiesterase 1
CHEMBL2111322
IC50 6.1 6.1 790.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/0960-894X(96)00323-X cGMP-specific 3',5'-cyclic phosphodiesterase 2
18656371 10.1016/j.bmc.2008.07.022 cGMP-specific 3',5'-cyclic phosphodiesterase 2
- 10.1016/0960-894X(96)00323-X Phosphodiesterase 1 1
- 10.1016/0960-894X(96)00323-X Phosphodiesterase 3 1
- 10.1016/0960-894X(96)00323-X No relevant target 1
11958981 10.1016/s0960-894x(02)00030-6 Phosphodiesterase 1 1
11958981 10.1016/s0960-894x(02)00030-6 cGMP-specific 3',5'-cyclic phosphodiesterase 1
11958981 10.1016/s0960-894x(02)00030-6 Phosphodiesterase 3 1
11958981 10.1016/s0960-894x(02)00030-6 Phosphodiesterase 4 1
15993055 10.1016/j.bmcl.2005.05.090 Phosphodiesterase 1 1
15993055 10.1016/j.bmcl.2005.05.090 cGMP-specific 3',5'-cyclic phosphodiesterase 1
22370268 10.1016/j.bmcl.2012.01.119 Class 1 phosphodiesterase PDEB1 1
33314936 10.1021/acs.jmedchem.0c01093 cGMP-specific 3',5'-cyclic phosphodiesterase 1

Data from ChEMBL 36 via Core Engine