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Compound Detail

CHEMBL3926292

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CC(C)(O)c1cn(-c2ccc(-c3cc(F)c(CO)c(S(C)(=O)=O)c3)cc2F)c(C(C)(C)c2ccccc2Cl)n1

Basic Information

ChEMBL ID CHEMBL3926292
Phase Preclinical
Structure Type MOL
InChI Key GUQJFTLEMOZJBL-UHFFFAOYSA-N
4
Targets
6
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

575.1
MW (Da)
5.92
ALogP
6
HBA
2
HBD
92.4
PSA (Ų)
0.29
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 C29H29ClF2N2O4S
MW 575.08
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.91

Activity Summary

EC50 4 meas. best 8.7
Ki 2 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxysterols receptor LXR-beta
CHEMBL4093
EC50 8.7 7.78 2.0 3
Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha
CHEMBL3430879
Ki 8.05 8.05 9.0 1
Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta
CHEMBL3430878
Ki 7.75 7.75 18.0 1
Oxysterols receptor LXR-alpha
CHEMBL2808
EC50 7.24 7.24 57.0 1

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 Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta 1
27994765 10.1021/acsmedchemlett.6b00234 Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha 1

Data from ChEMBL 36 via Core Engine