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Compound Detail

CHEMBL1097280

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Cc1nc2c3c(c(O)cc2n1C)C(=O)O[C@@H](C)[C@H](C)/C=C\C(=O)[C@@H](O)[C@@H](O)C/C=C/3

Basic Information

ChEMBL ID CHEMBL1097280
Phase Preclinical
Structure Type MOL
InChI Key PMLCSVJQDJQDQA-XTMHZFSDSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

414.5
MW (Da)
2.03
ALogP
8
HBA
3
HBD
121.9
PSA (Ų)
0.56
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H26N2O6
MW 414.46
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness 1.52

Activity Summary

IC50 1 meas. best 6.97

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
THP-1
CHEMBL614245
IC50 6.97 6.97 108.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
THP-1 IC50 = 108.0 nM 6.97 Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-indu... 20399648

Literature References

PubMed DOI Target Context # Activities
20399648 10.1016/j.bmcl.2010.03.087 Mus musculus 3
20399648 10.1016/j.bmcl.2010.03.087 THP-1 1
20399648 10.1016/j.bmcl.2010.03.087 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine