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Compound Detail

CHEMBL322358

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CCCn1cnc2c1c1nnnn1c(=O)n2CCC

Basic Information

ChEMBL ID CHEMBL322358
Phase Preclinical
Structure Type MOL
InChI Key MKHXPKWGXFTWQV-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

261.3
MW (Da)
0.46
ALogP
8
HBA
0
HBD
82.9
PSA (Ų)
0.68
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 C11H15N7O
MW 261.29
Aromatic Rings 3
Heavy Atoms 19
NP-Likeness -1.99

Activity Summary

EC50 1 meas. best 4.29
IC50 1 meas. best 4.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphodiesterase 4
CHEMBL2093863
IC50 4.75 4.75 18000.0 1
Cavia porcellus
CHEMBL369
EC50 4.29 4.29 51000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Phosphodiesterase 4 IC50 = 18000.0 nM 4.75 Inhibitory activity against Phosphodiesterase 4 from heart. 9379444
Cavia porcellus EC50 = 51000.0 nM 4.29 Tested in vitro for tracheal relaxation 9379444

Literature References

PubMed DOI Target Context # Activities
9379444 10.1021/jm970089s Cavia porcellus 2
9379444 10.1021/jm970089s Phosphodiesterase 1 1
9379444 10.1021/jm970089s Phosphodiesterase 3 1
9379444 10.1021/jm970089s Phosphodiesterase 4 1

Data from ChEMBL 36 via Core Engine