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Compound Detail

CHEMBL291034

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CCCCCCCOc1c(-c2cccc3sc(/C(C)=C/C(=O)O)cc23)cc(C(C)(C)C)cc1C(C)(C)C

Basic Information

ChEMBL ID CHEMBL291034
Phase Preclinical
Structure Type MOL
InChI Key WRGWXGCPDRRZSK-RELWKKBWSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

520.8
MW (Da)
10.00
ALogP
3
HBA
1
HBD
46.5
PSA (Ų)
0.21
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H44O3S
MW 520.78
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.20

Activity Summary

Ki 3 meas. best 8.3
IC50 1 meas. best 7.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinoic acid receptor RXR-alpha
CHEMBL2061
Ki 8.3 8.3 5.0 1
Retinoic acid receptor RXR-beta
CHEMBL1870
Ki 7.92 7.92 12.0 1
Retinoic acid receptor RXR-gamma
CHEMBL2004
Ki 7.55 7.55 28.0 1
Retinoic acid receptor RXR-alpha
CHEMBL2061
IC50 7.08 7.08 83.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15006411 10.1016/j.bmcl.2003.12.089 Retinoic acid receptor RXR-alpha 5
15006411 10.1016/j.bmcl.2003.12.089 Retinoic acid receptor RXR-beta 2
15006411 10.1016/j.bmcl.2003.12.089 Retinoic acid receptor RXR-gamma 2
15006411 10.1016/j.bmcl.2003.12.089 Retinoic acid receptor alpha 1

Data from ChEMBL 36 via Core Engine