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Compound Detail

CHEMBL251883

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CC(C)(c1cc(-c2cccc(-c3ccc[n+]([O-])c3)c2)c2ncccc2c1)S(C)(=O)=O

Basic Information

ChEMBL ID CHEMBL251883
Phase Preclinical
Structure Type MOL
InChI Key TVDKLCZIHMRFLG-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

418.5
MW (Da)
4.48
ALogP
4
HBA
0
HBD
74.0
PSA (Ų)
0.36
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 C24H22N2O3S
MW 418.52
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -0.62

Activity Summary

IC50 3 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.52 7.52 30.0 1
Blood
CHEMBL613416
IC50 6.24 6.24 580.0 1
Cytochrome P450 2C9
CHEMBL3397
IC50 4.44 4.44 36000.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 76.0 % Rattus norvegicus
T1/2 1.2 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 30.0 nM 7.52 Inhibition of PDE4 expressed in SF9 cells 18207397
Blood IC50 = 580.0 nM 6.24 Inhibition of LPS-stimulated TNFalpha release in human whole blood 18207397
Cytochrome P450 2C9 IC50 = 36000.0 nM 4.44 Inhibition of CYP2C9 18207397

Literature References

PubMed DOI Target Context # Activities
18207397 10.1016/j.bmcl.2008.01.004 Rattus norvegicus 2
18207397 10.1016/j.bmcl.2008.01.004 Unchecked 1
18207397 10.1016/j.bmcl.2008.01.004 Blood 1
18207397 10.1016/j.bmcl.2008.01.004 Cytochrome P450 2C9 1

Data from ChEMBL 36 via Core Engine