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Compound Detail

CHEMBL403418

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Cc1cc(NCc2cccc(-c3c(Cc4ccccc4)cnc4c(C(F)(F)F)cccc34)c2)c(C)cc1CC(=O)O

Basic Information

ChEMBL ID CHEMBL403418
Phase Preclinical
Structure Type MOL
InChI Key LFYZXWABUGTSOT-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

554.6
MW (Da)
8.37
ALogP
3
HBA
2
HBD
62.2
PSA (Ų)
0.20
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 C34H29F3N2O2
MW 554.61
Aromatic Rings 5
Heavy Atoms 41
NP-Likeness -0.70

Activity Summary

IC50 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxysterols receptor LXR-beta
CHEMBL4093
IC50 8.7 8.7 2.0 1
Oxysterols receptor LXR-alpha
CHEMBL2808
IC50 7.68 7.68 21.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Oxysterols receptor LXR-beta IC50 = 2.0 nM 8.7 Binding affinity at human LXRbeta 18023179
Oxysterols receptor LXR-alpha IC50 = 21.0 nM 7.68 Binding affinity at human LXRalpha 18023179

Literature References

PubMed DOI Target Context # Activities
18023179 10.1016/j.bmcl.2007.11.013 Oxysterols receptor LXR-beta 1
18023179 10.1016/j.bmcl.2007.11.013 Oxysterols receptor LXR-alpha 1
18023179 10.1016/j.bmcl.2007.11.013 Liver X receptor (LXR alpha AND LXR beta) 1

Data from ChEMBL 36 via Core Engine