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Compound Detail

CHEMBL274652

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O=C(O)c1cccc(/C=C/c2ccc(OCc3c(-c4c(Cl)cccc4Cl)noc3-c3ccccc3)cc2Cl)c1

Basic Information

ChEMBL ID CHEMBL274652
Phase Preclinical
Structure Type MOL
InChI Key CNZACFCLDVRZJS-OUKQBFOZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

576.9
MW (Da)
9.42
ALogP
4
HBA
1
HBD
72.6
PSA (Ų)
0.19
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H20Cl3NO4
MW 576.86
Aromatic Rings 5
Heavy Atoms 39
NP-Likeness -0.59

Activity Summary

IC50 1 meas. best 4.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bile acid receptor
CHEMBL2047
IC50 4.8 4.8 15800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bile acid receptor IC50 = 15800.0 nM 4.8 Inhibition of FXR in HEK293 cells in presence of CDCA by GAL4 transactivation ac... 17292610

Literature References

PubMed DOI Target Context # Activities
17292610 10.1016/j.bmc.2007.01.046 Bile acid receptor 2

Data from ChEMBL 36 via Core Engine