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Compound Detail

CHEMBL207382

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CCCc1c(OCCCN2C(=O)Cc3cc(C(=O)O)ccc32)ccc2c(C(F)(F)F)noc12

Basic Information

ChEMBL ID CHEMBL207382
Phase Preclinical
Structure Type MOL
InChI Key JBHHUSIDAMWIJB-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

462.4
MW (Da)
4.86
ALogP
5
HBA
1
HBD
92.9
PSA (Ų)
0.48
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H21F3N2O5
MW 462.42
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.70

Activity Summary

EC50 2 meas. best 5.52
IC50 2 meas. best 7.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxysterols receptor LXR-alpha
CHEMBL2808
IC50 7.01 7.01 97.0 1
Oxysterols receptor LXR-beta
CHEMBL4093
IC50 6.16 6.16 700.0 1
Oxysterols receptor LXR-alpha
CHEMBL2808
EC50 5.52 5.52 3000.0 1
Oxysterols receptor LXR-beta
CHEMBL4093
EC50 5.36 5.36 4400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16529931 10.1016/j.bmcl.2006.02.050 Oxysterols receptor LXR-alpha 2
16529931 10.1016/j.bmcl.2006.02.050 Oxysterols receptor LXR-beta 2
16529931 10.1016/j.bmcl.2006.02.050 Peroxisome proliferator-activated receptor alpha 1
16529931 10.1016/j.bmcl.2006.02.050 Peroxisome proliferator-activated receptor delta 1
16529931 10.1016/j.bmcl.2006.02.050 Peroxisome proliferator-activated receptor gamma 1

Data from ChEMBL 36 via Core Engine