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Compound Detail

CHEMBL1094742

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Cc1cnc2c(C(F)(F)F)cccc2c1-c1cccc(-c2ccc(S(C)(=O)=O)cc2)c1

Basic Information

ChEMBL ID CHEMBL1094742
Phase Preclinical
Structure Type MOL
InChI Key AWHRFIKOWGDBRL-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

441.5
MW (Da)
6.30
ALogP
3
HBA
0
HBD
47.0
PSA (Ų)
0.37
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H18F3NO2S
MW 441.47
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -0.97

Activity Summary

IC50 1 meas. best 6.45

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxysterols receptor LXR-beta
CHEMBL4093
IC50 6.45 6.45 355.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.5 hr Rattus norvegicus
T1/2 0.5 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Oxysterols receptor LXR-beta IC50 = 355.0 nM 6.45 Displacement of [3H]T0901317 from LXRbeta ligand binding domain 20382019

Literature References

PubMed DOI Target Context # Activities
20382019 10.1016/j.bmcl.2010.03.031 Oxysterols receptor LXR-beta 2
20382019 10.1016/j.bmcl.2010.03.031 Liver microsomes 2
20382019 10.1016/j.bmcl.2010.03.031 Oxysterols receptor LXR-alpha 1

Data from ChEMBL 36 via Core Engine