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Compound Detail

CHEMBL205308

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CS(=O)(=O)c1ccc(-n2nc(C(F)(F)F)cc2-c2ccc(-c3ccco3)c(C(N)=O)c2)nc1

Basic Information

ChEMBL ID CHEMBL205308
Phase Preclinical
Structure Type MOL
InChI Key RTYBDSFNSYNBEF-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

476.4
MW (Da)
3.72
ALogP
7
HBA
1
HBD
121.1
PSA (Ų)
0.47
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 C21H15F3N4O4S
MW 476.44
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.70

Activity Summary

IC50 2 meas. best 6.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclooxygenase-2
CHEMBL4033
IC50 6.39 6.39 410.0 1
Prostaglandin G/H synthase 1
CHEMBL4133
IC50 5.7 5.7 2000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclooxygenase-2 IC50 = 410.0 nM 6.39 Inhibition of COX2 in canine whole blood 16464588
Prostaglandin G/H synthase 1 IC50 = 2000.0 nM 5.7 Inhibition of COX1 in canine whole blood 16464588

Literature References

PubMed DOI Target Context # Activities
16464588 10.1016/j.bmcl.2006.01.059 Cyclooxygenase-2 1
16464588 10.1016/j.bmcl.2006.01.059 Prostaglandin G/H synthase 1 1
16464588 10.1016/j.bmcl.2006.01.059 Unchecked 1

Data from ChEMBL 36 via Core Engine