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Compound Detail

CHEMBL4638644

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C[C@@H](Nc1nc2c(cnn2C2CCCC2)c(=O)[nH]1)C(=O)Nc1ccc2[nH]ncc2c1

Basic Information

ChEMBL ID CHEMBL4638644
Phase Preclinical
Structure Type MOL
InChI Key CXUUMUHNWGRMLN-LLVKDONJSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

406.4
MW (Da)
2.55
ALogP
7
HBA
4
HBD
133.4
PSA (Ų)
0.40
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H22N8O2
MW 406.45
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.92

Activity Summary

IC50 1 meas. best 8.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A
CHEMBL3535
IC50 8.74 8.74 1.8 1

Pharmacokinetic Data

Parameter Value Units Species
CL 0.0484 mL.min-1.kg-1 Rattus norvegicus
CL 10040.0 mL.min-1.g-1 Rattus norvegicus
T1/2 0.7233 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A IC50 = 1.8 nM 8.74 Inhibition of PDE9A (unknown origin) 32527553

Literature References

PubMed DOI Target Context # Activities
32527553 10.1016/j.bmcl.2020.127254 High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A 4
32527553 10.1016/j.bmcl.2020.127254 ADMET 4
32527553 10.1016/j.bmcl.2020.127254 No relevant target 1

Data from ChEMBL 36 via Core Engine