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Compound Detail

CHEMBL3960606

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CC(C)(O)c1cn(-c2ccc(-c3ccc(CO)c(S(C)(=O)=O)c3)cc2)c(Cc2ccccc2Cl)n1

Basic Information

ChEMBL ID CHEMBL3960606
Phase Preclinical
Structure Type MOL
InChI Key VVVMBZVHNIYCQS-UHFFFAOYSA-N
4
Targets
6
Activities
2
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

511.0
MW (Da)
4.91
ALogP
6
HBA
2
HBD
92.4
PSA (Ų)
0.37
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H27ClN2O4S
MW 511.04
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.92

Activity Summary

EC50 4 meas. best 8.05
Ki 2 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta
CHEMBL3430878
Ki 8.3 8.3 5.0 1
Oxysterols receptor LXR-beta
CHEMBL4093
EC50 8.05 7.2633 9.0 3
Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha
CHEMBL3430879
Ki 7.51 7.51 31.0 1
Oxysterols receptor LXR-alpha
CHEMBL2808
EC50 7.0 7.0 100.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 61.0 mL.min-1.kg-1 Macaca fascicularis
T1/2 0.8 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

Data from ChEMBL 36 via Core Engine