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Compound Detail

CHEMBL3814478

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CC(C)[C@@H]1CN(c2ccc(F)c(S(C)(=O)=O)c2)CCN1c1ncc(C(C)(C)O)c(C(F)(F)F)n1

Basic Information

ChEMBL ID CHEMBL3814478
Phase Preclinical
Structure Type MOL
InChI Key HXOUVMGQDQYWNM-KRWDZBQOSA-N
2
Targets
9
Activities
2
Assay Types
3
PK Parameters
5
Publications
0
Known Names

Molecular Properties

504.6
MW (Da)
3.62
ALogP
7
HBA
1
HBD
86.6
PSA (Ų)
0.62
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H28F4N4O3S
MW 504.55
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -1.20

Activity Summary

Ki 6 meas. best 8.1
EC50 3 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxysterols receptor LXR-beta
CHEMBL4093
Ki 8.1 8.0167 8.0 3
Oxysterols receptor LXR-beta
CHEMBL4093
EC50 7.1 7.1 80.0 1
Oxysterols receptor LXR-alpha
CHEMBL2808
Ki 6.8 6.6367 157.0 3
Oxysterols receptor LXR-alpha
CHEMBL2808
EC50 6.67 6.395 213.0 2

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.9333 hr Homo sapiens
T1/2 0.85 hr Rattus norvegicus
T1/2 1.2 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26990539 10.1021/acs.jmedchem.5b02029 Oxysterols receptor LXR-alpha 3
26990539 10.1021/acs.jmedchem.5b02029 Oxysterols receptor LXR-beta 3
26990539 10.1021/acs.jmedchem.5b02029 Liver microsome 2
26990539 10.1021/acs.jmedchem.5b02029 Unchecked 1
26990539 10.1021/acs.jmedchem.5b02029 ADMET 1

Data from ChEMBL 36 via Core Engine