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Compound Detail

CHEMBL557117

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CN([C@@H]1CCc2c(CC(=O)O)c3ncccc3n2C1)S(=O)(=O)c1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL557117
Phase Preclinical
Structure Type MOL
InChI Key NROVVWMGTIZNGL-CQSZACIVSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

417.5
MW (Da)
2.44
ALogP
5
HBA
1
HBD
92.5
PSA (Ų)
0.69
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H20FN3O4S
MW 417.46
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.37

Activity Summary

IC50 4 meas. best 4.6
Ki 1 meas. best 5.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prostaglandin D2 receptor 2
CHEMBL5071
Ki 5.14 5.14 7189.0 1
Prostaglandin D2 receptor 2
CHEMBL5071
IC50 4.6 4.445 24900.0 2
Prostaglandin D2 receptor
CHEMBL4427
IC50 4.38 4.38 41700.0 1
Blood
CHEMBL613416
IC50 4.38 4.38 41600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19608418 10.1016/j.bmcl.2009.06.085 Prostaglandin D2 receptor 2 2
19608418 10.1016/j.bmcl.2009.06.085 Cytochrome P450 3A4 2
19608418 10.1016/j.bmcl.2009.06.085 Blood 1
19608418 10.1016/j.bmcl.2009.06.085 Prostaglandin D2 receptor 1
19608418 10.1016/j.bmcl.2009.06.085 Thromboxane A2 receptor 1
19608418 10.1016/j.bmcl.2009.06.085 Prostacyclin receptor 1
19608418 10.1016/j.bmcl.2009.06.085 Cytochrome P450 2C9 1
19608418 10.1016/j.bmcl.2009.06.085 Cytochrome P450 2D6 1
21185722 10.1016/j.bmcl.2010.11.084 Prostaglandin D2 receptor 2 1
21185722 10.1016/j.bmcl.2010.11.084 Prostaglandin D2 receptor 1
21185722 10.1016/j.bmcl.2010.11.084 Thromboxane A2 receptor 1

Data from ChEMBL 36 via Core Engine