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Compound Detail

CHEMBL418848

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COc1cc2c3c(c1)C(c1ccccc1)=N[C@@H](NC(=O)c1ccncc1)C(=O)N3CC2

Basic Information

ChEMBL ID CHEMBL418848
Phase Preclinical
Structure Type MOL
InChI Key TYXDVWFULHZGTB-QFIPXVFZSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

412.4
MW (Da)
2.59
ALogP
5
HBA
1
HBD
83.9
PSA (Ų)
0.71
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 C24H20N4O3
MW 412.45
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.40

Activity Summary

IC50 6 meas. best 5.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphodiesterase 4
CHEMBL2093863
IC50 5.36 5.36 4400.0 2
Phosphodiesterase 1
CHEMBL2095150
IC50 4.8 4.8 16000.0 1
Phosphodiesterase, PDE1/PDE5
CHEMBL2097161
IC50 4.79 4.79 16100.0 1
Phosphodiesterase 3
CHEMBL2094125
IC50 4.39 4.39 40800.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11123995 10.1021/jm000315p Phosphodiesterase 4 1
11123995 10.1021/jm000315p Phosphodiesterase 3 1
11123995 10.1021/jm000315p Phosphodiesterase, PDE1/PDE5 1
15149695 10.1016/j.bmcl.2004.03.067 Phosphodiesterase 4 1
15149695 10.1016/j.bmcl.2004.03.067 Phosphodiesterase 1 1
15149695 10.1016/j.bmcl.2004.03.067 Phosphodiesterase 3 1
15149695 10.1016/j.bmcl.2004.03.067 cGMP-specific 3',5'-cyclic phosphodiesterase 1

Data from ChEMBL 36 via Core Engine