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Compound Detail

CHEMBL3113737

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O=C(OC(Cc1c(Cl)cncc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1)c1ccc(OC(F)F)c(OCC2CC2)c1

Basic Information

ChEMBL ID CHEMBL3113737
Phase Preclinical
Structure Type MOL
InChI Key QWJORUKKCABZPO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

644.5
MW (Da)
8.31
ALogP
7
HBA
0
HBD
76.1
PSA (Ų)
0.12
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H27Cl2F4NO6
MW 644.45
Aromatic Rings 3
Heavy Atoms 43
NP-Likeness -0.59

Activity Summary

IC50 1 meas. best 8.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphodiesterase 4
CHEMBL2093863
IC50 8.46 8.46 3.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Phosphodiesterase 4 IC50 = 3.45 nM 8.46 Inhibition of PDE4 isolated from human U937 cells assessed as reduction in cAMP ... 24400806

Literature References

PubMed DOI Target Context # Activities
24400806 10.1021/jm401549m cGMP-dependent 3',5'-cyclic phosphodiesterase 1
24400806 10.1021/jm401549m Phosphodiesterase 3 1
24400806 10.1021/jm401549m cGMP-specific 3',5'-cyclic phosphodiesterase 1
24400806 10.1021/jm401549m Phosphodiesterase 4 1

Data from ChEMBL 36 via Core Engine