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Compound Detail

CHEMBL2070634

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COc1ccc2nnc3c(C)nc(-c4ccccc4C)n3c2n1

Basic Information

ChEMBL ID CHEMBL2070634
Phase Preclinical
Structure Type MOL
InChI Key XLZOIIVTFPXQAK-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

305.3
MW (Da)
2.96
ALogP
6
HBA
0
HBD
65.2
PSA (Ų)
0.57
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H15N5O
MW 305.34
Aromatic Rings 4
Heavy Atoms 23
NP-Likeness -1.26

Activity Summary

IC50 4 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-dependent 3',5'-cyclic phosphodiesterase
CHEMBL2652
IC50 7.8 7.8 15.8 1
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
CHEMBL4409
IC50 7.32 7.32 47.6 1
Phosphodiesterase 6
CHEMBL2097163
IC50 5.8 5.8 1570.0 1
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL2304402
IC50 5.47 5.47 3410.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22902656 10.1016/j.bmcl.2012.07.076 cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A 1
22902656 10.1016/j.bmcl.2012.07.076 cGMP-dependent 3',5'-cyclic phosphodiesterase 1
22902656 10.1016/j.bmcl.2012.07.076 Phosphodiesterase 3 1
22902656 10.1016/j.bmcl.2012.07.076 Phosphodiesterase 4 1
22902656 10.1016/j.bmcl.2012.07.076 cGMP-specific 3',5'-cyclic phosphodiesterase 1
22902656 10.1016/j.bmcl.2012.07.076 Phosphodiesterase 6 1

Data from ChEMBL 36 via Core Engine