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Compound Detail

CHEMBL595045

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Cc1cnc2c(C(F)(F)F)cccc2c1-c1cccc(Oc2ccccc2S(C)(=O)=O)c1

Basic Information

ChEMBL ID CHEMBL595045
Phase Preclinical
Structure Type MOL
InChI Key ZTQHPDHGMFCHSE-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

457.5
MW (Da)
6.42
ALogP
4
HBA
0
HBD
56.3
PSA (Ų)
0.35
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H18F3NO3S
MW 457.47
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -0.97

Activity Summary

IC50 1 meas. best 6.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxysterols receptor LXR-alpha
CHEMBL2808
IC50 6.25 6.25 560.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.1333 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Oxysterols receptor LXR-alpha IC50 = 560.0 nM 6.25 Displacement of [3H]T0901317 from human recombinant LXRalpha-LBD 19932617

Literature References

PubMed DOI Target Context # Activities
19932617 10.1016/j.bmcl.2009.10.132 Liver microsomes 1
19932617 10.1016/j.bmcl.2009.10.132 J774.A1 1
19932617 10.1016/j.bmcl.2009.10.132 Liver X receptor 1
19932617 10.1016/j.bmcl.2009.10.132 Oxysterols receptor LXR-beta 1
19932617 10.1016/j.bmcl.2009.10.132 Oxysterols receptor LXR-alpha 1

Data from ChEMBL 36 via Core Engine