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Compound Detail

CHEMBL452578

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CC(C)(Nc1ccc(C(Cc2cc[n+]([O-])cc2)c2ccc(OC(F)F)c(OC(F)F)c2)cc1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL452578
Phase Preclinical
Structure Type MOL
InChI Key PEPATKYVXSEWGQ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

540.6
MW (Da)
7.24
ALogP
4
HBA
1
HBD
57.4
PSA (Ų)
0.12
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H28F4N2O3
MW 540.56
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.88

Activity Summary

IC50 2 meas. best 9.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Blood
CHEMBL613416
IC50 9.92 9.92 0.1 1
3',5'-cyclic-AMP phosphodiesterase 4A
CHEMBL254
IC50 9.1 9.1 0.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Blood IC50 = 0.12 nM 9.92 Inhibition of TNFalpha release in human whole blood 18686943
3',5'-cyclic-AMP phosphodiesterase 4A IC50 = 0.8 nM 9.1 Inhibition of GST-tagged PDE4A 18686943

Literature References

PubMed DOI Target Context # Activities
18686943 10.1021/jm800582j 3',5'-cyclic-AMP phosphodiesterase 4A 1
18686943 10.1021/jm800582j Blood 1

Data from ChEMBL 36 via Core Engine