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Compound Detail

CHEMBL210990

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CCCc1c(OCCCN(C)c2ncc(CC(=O)O)cn2)ccc2c(C(F)(F)F)noc12

Basic Information

ChEMBL ID CHEMBL210990
Phase Preclinical
Structure Type MOL
InChI Key HNBMEVGNLQVKHO-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

452.4
MW (Da)
4.12
ALogP
7
HBA
1
HBD
101.6
PSA (Ų)
0.46
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23F3N4O4
MW 452.43
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.64

Activity Summary

EC50 2 meas. best 6.33
IC50 2 meas. best 7.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxysterols receptor LXR-alpha
CHEMBL2808
IC50 7.58 7.58 26.0 1
Oxysterols receptor LXR-beta
CHEMBL4093
IC50 7.26 7.26 55.0 1
Oxysterols receptor LXR-beta
CHEMBL4093
EC50 6.33 6.33 470.0 1
Oxysterols receptor LXR-alpha
CHEMBL2808
EC50 6.21 6.21 620.0 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