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Compound Detail

CHEMBL1099077

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C[C@@H]1/C=C\C(=O)[C@@H](O)[C@@H](O)C/C=C/c2c(c(O)cc3c2ncn3C)C(=O)O[C@H]1C

Basic Information

ChEMBL ID CHEMBL1099077
Phase Preclinical
Structure Type MOL
InChI Key MUNVTEPUQYCYQU-NJZSEKELSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

400.4
MW (Da)
1.72
ALogP
8
HBA
3
HBD
121.9
PSA (Ų)
0.58
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 C21H24N2O6
MW 400.43
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness 1.73

Activity Summary

IC50 1 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
THP-1
CHEMBL614245
IC50 7.64 7.64 23.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 49.0 % Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
THP-1 IC50 = 23.0 nM 7.64 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 4
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