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Compound Detail

CHEMBL210613

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CCCc1c(OCCCn2cnc3cc(CC(=O)O)ccc32)ccc2c(C(F)(F)F)noc12

Basic Information

ChEMBL ID CHEMBL210613
Phase Preclinical
Structure Type MOL
InChI Key GMKDRYOJWQXLTE-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

461.4
MW (Da)
5.25
ALogP
6
HBA
1
HBD
90.4
PSA (Ų)
0.34
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H22F3N3O4
MW 461.44
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -0.91

Activity Summary

IC50 3 meas. best 6.75
EC50 1 meas. best 5.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxysterols receptor LXR-alpha
CHEMBL2808
IC50 6.75 6.75 180.0 1
Oxysterols receptor LXR-beta
CHEMBL4093
IC50 6.39 6.39 410.0 1
Peroxisome proliferator-activated receptor delta
CHEMBL3979
IC50 5.75 5.75 1800.0 1
Oxysterols receptor LXR-beta
CHEMBL4093
EC50 5.07 5.07 8600.0 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