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Compound Detail

CHEMBL43238

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C/C(=C\C(=O)O)c1cc2c(-c3cc(C(C)(C)C)cc(C(C)(C)C)c3OCCC(F)F)cccc2s1

Basic Information

ChEMBL ID CHEMBL43238
Phase Preclinical
Structure Type MOL
InChI Key JLAHIRHKOIBLKL-GHRIWEEISA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

500.6
MW (Da)
8.69
ALogP
3
HBA
1
HBD
46.5
PSA (Ų)
0.33
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 C29H34F2O3S
MW 500.65
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.39

Activity Summary

Ki 3 meas. best 8.15
IC50 1 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinoic acid receptor RXR-alpha
CHEMBL2061
Ki 8.15 8.15 7.0 1
Retinoic acid receptor RXR-beta
CHEMBL1870
Ki 7.92 7.92 12.0 1
Retinoic acid receptor RXR-alpha
CHEMBL2061
IC50 7.8 7.8 16.0 1
Retinoic acid receptor RXR-gamma
CHEMBL2004
Ki 7.43 7.43 37.0 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