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Compound Detail

CHEMBL2070631

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COc1ccc2nnc3c(C)nc(-c4ccc(F)cc4Cl)n3c2n1

Basic Information

ChEMBL ID CHEMBL2070631
Phase Preclinical
Structure Type MOL
InChI Key CIKOPVDFPXGTDP-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

343.8
MW (Da)
3.45
ALogP
6
HBA
0
HBD
65.2
PSA (Ų)
0.56
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 C16H11ClFN5O
MW 343.75
Aromatic Rings 4
Heavy Atoms 24
NP-Likeness -1.75

Activity Summary

IC50 3 meas. best 7.93

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-dependent 3',5'-cyclic phosphodiesterase
CHEMBL2652
IC50 7.93 7.93 11.8 1
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
CHEMBL4409
IC50 7.88 7.88 13.1 1
Phosphodiesterase 6
CHEMBL2097163
IC50 6.33 6.33 462.0 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