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Compound Detail

CHEMBL3945820

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CC(c1c(Cl)cccc1Cl)c1nc(C(C)(C)O)cn1-c1ccc(-c2cc(F)c(CO)c(S(C)(=O)=O)c2)cc1F

Basic Information

ChEMBL ID CHEMBL3945820
Phase Preclinical
Structure Type MOL
InChI Key OSCBEESEHIRILI-UHFFFAOYSA-N
4
Targets
6
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

595.5
MW (Da)
6.40
ALogP
6
HBA
2
HBD
92.4
PSA (Ų)
0.26
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 C28H26Cl2F2N2O4S
MW 595.50
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.82

Activity Summary

EC50 4 meas. best 8.7
Ki 2 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Oxysterols receptor LXR-beta
CHEMBL4093
EC50 8.7 7.98 2.0 3
Oxysterols receptor LXR-alpha
CHEMBL2808
EC50 7.92 7.92 12.0 1
Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta
CHEMBL3430878
Ki 7.89 7.89 13.0 1
Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha
CHEMBL3430879
Ki 7.77 7.77 17.0 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