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Compound Detail

CHEMBL486903

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Cc1cc(C)c(NS(=O)(=O)c2cc(S(=O)(=O)Nc3c(C)cc(C)cc3C)c3cc(O)ccc3c2)c(C)c1

Basic Information

ChEMBL ID CHEMBL486903
Phase Preclinical
Structure Type MOL
InChI Key KTJZLVJCEOSQTP-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

538.7
MW (Da)
6.00
ALogP
5
HBA
3
HBD
112.6
PSA (Ų)
0.28
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H30N2O5S2
MW 538.69
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.64

Activity Summary

IC50 2 meas. best 5.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prostaglandin E synthase
CHEMBL5658
IC50 5.96 5.96 1100.0 1
Unchecked
CHEMBL612545
IC50 5.96 5.96 1100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 1100.0 nM 5.96 Inhibition of mPGES1 18459759
Prostaglandin E synthase IC50 = 1100.0 nM 5.96 Inhibition of mPGES1 20144869

Literature References

PubMed DOI Target Context # Activities
18459759 10.1021/jm800197b Unchecked 1
20144869 10.1016/j.bmcl.2010.01.060 Prostaglandin E synthase 1

Data from ChEMBL 36 via Core Engine