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Compound Detail

CHEMBL207594

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C[S+]([O-])c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1

Basic Information

ChEMBL ID CHEMBL207594
Phase Preclinical
Structure Type MOL
InChI Key RAECDKKKKNJXTF-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
5
Publications
0
Known Names

Molecular Properties

298.4
MW (Da)
2.89
ALogP
3
HBA
0
HBD
49.4
PSA (Ų)
0.65
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H14O3S
MW 298.36
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness 0.58

Activity Summary

IC50 1 meas. best 5.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prostaglandin G/H synthase 2
CHEMBL230
IC50 5.31 5.31 4930.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 318.0 ng.hr.mL-1 Rattus norvegicus
AUC 979.0 ng.hr.mL-1 Rattus norvegicus
Cmax 1119.45 nM Rattus norvegicus
Cmax 1568.57 nM Rattus norvegicus
Tmax 0.3 hr Rattus norvegicus
Tmax 0.4 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prostaglandin G/H synthase 2 IC50 = 4930.0 nM 5.31 Inhibition of COX2 in human whole blood 16616494

Literature References

PubMed DOI Target Context # Activities
16616494 10.1016/j.bmcl.2006.03.052 Rattus norvegicus 8
16616494 10.1016/j.bmcl.2006.03.052 No relevant target 2
16616494 10.1016/j.bmcl.2006.03.052 Liver microsomes 2
16616494 10.1016/j.bmcl.2006.03.052 Prostaglandin G/H synthase 2 1
16616494 10.1016/j.bmcl.2006.03.052 Cyclooxygenase 1

Data from ChEMBL 36 via Core Engine