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Compound Detail

CHEMBL2070669

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COc1cc(OC(F)F)cc2c1nnc1c(C)nc(-c3ccncc3C)n12

Basic Information

ChEMBL ID CHEMBL2070669
Phase Preclinical
Structure Type MOL
InChI Key QBLWGJRSTWQUGT-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

371.4
MW (Da)
3.57
ALogP
7
HBA
0
HBD
74.4
PSA (Ų)
0.55
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 C18H15F2N5O2
MW 371.35
Aromatic Rings 4
Heavy Atoms 27
NP-Likeness -1.23

Activity Summary

IC50 4 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
CHEMBL4409
IC50 8.15 8.15 7.0 1
Phosphodiesterase 6
CHEMBL2097163
IC50 6.04 6.04 909.0 1
cGMP-dependent 3',5'-cyclic phosphodiesterase
CHEMBL2652
IC50 6.03 6.03 944.0 1
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL2304402
IC50 5.4 5.4 4020.0 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