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Compound Detail

CHEMBL3944154

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CC(C)(O)c1cn(-c2ccc(-c3cc(F)c(CO)c(S(C)(=O)=O)c3)cc2)c(C(C)(C)c2ccccc2Cl)n1

Basic Information

ChEMBL ID CHEMBL3944154
Phase Preclinical
Structure Type MOL
InChI Key WUVSLEJBHNUDBB-UHFFFAOYSA-N
4
Targets
6
Activities
2
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

557.1
MW (Da)
5.78
ALogP
6
HBA
2
HBD
92.4
PSA (Ų)
0.30
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H30ClFN2O4S
MW 557.09
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -0.96

Activity Summary

EC50 4 meas. best 8.1
Ki 2 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxysterols receptor LXR-beta
CHEMBL4093
EC50 8.1 7.4933 8.0 3
Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta
CHEMBL3430878
Ki 8.0 8.0 10.0 1
Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha
CHEMBL3430879
Ki 7.28 7.28 53.0 1
Oxysterols receptor LXR-alpha
CHEMBL2808
EC50 7.12 7.12 76.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 8.4 mL.min-1.kg-1 Macaca fascicularis
T1/2 5.6 hr Macaca fascicularis

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27994765 10.1021/acsmedchemlett.6b00234 Oxysterols receptor LXR-beta 6
27994765 10.1021/acsmedchemlett.6b00234 Oxysterols receptor LXR-alpha 2
27994765 10.1021/acsmedchemlett.6b00234 ADMET 2
27994765 10.1021/acsmedchemlett.6b00234 Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha 1
27994765 10.1021/acsmedchemlett.6b00234 Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta 1
27994765 10.1021/acsmedchemlett.6b00234 Alpha-1-acid glycoprotein 1 1
27994765 10.1021/acsmedchemlett.6b00234 Albumin 1

Data from ChEMBL 36 via Core Engine