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Compound Detail

CHEMBL3425539

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CCCCOc1cncc(-c2nnc3c(C)nc4ccncc4n23)c1

Basic Information

ChEMBL ID CHEMBL3425539
Phase Preclinical
Structure Type MOL
InChI Key IDPOAJGPSIINOF-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

334.4
MW (Da)
3.22
ALogP
7
HBA
0
HBD
78.1
PSA (Ų)
0.52
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 C18H18N6O
MW 334.38
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -1.41

Activity Summary

IC50 4 meas. best 7.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cGMP-dependent 3',5'-cyclic phosphodiesterase
CHEMBL2652
IC50 7.27 7.27 54.0 2
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
CHEMBL6140
IC50 5.42 5.42 3800.0 2

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.3 - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25815146 10.1021/ml500463t Brain 2
25815146 10.1021/ml500463t Liver microsome 2
25815146 10.1021/ml500463t Rattus norvegicus 1
25815146 10.1021/ml500463t Nucleic Acid 1
25815146 10.1021/ml500463t cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A 1
25815146 10.1021/ml500463t cGMP-dependent 3',5'-cyclic phosphodiesterase 1

Data from ChEMBL 36 via Core Engine