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Compound Detail

CHEMBL421748

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CCCCOc1c(-c2cn(C)c3ccc(/C(C)=C/C(=O)O)cc23)cc(C(C)C)cc1C(C)C

Basic Information

ChEMBL ID CHEMBL421748
Phase Preclinical
Structure Type MOL
InChI Key VVRKVTWLLQOKMZ-DEDYPNTBSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

447.6
MW (Da)
7.76
ALogP
3
HBA
1
HBD
51.5
PSA (Ų)
0.27
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H37NO3
MW 447.62
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness 0.21

Activity Summary

EC50 1 meas. best 5.81
Ki 1 meas. best 6.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinoic acid receptor RXR-alpha
CHEMBL2061
Ki 6.13 6.13 740.0 1
Retinoic acid receptor RXR-alpha
CHEMBL2061
EC50 5.81 5.81 1533.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15125928 10.1016/j.bmcl.2004.03.073 Retinoic acid receptor RXR-alpha 5
15125928 10.1016/j.bmcl.2004.03.073 Peroxisome proliferator-activated receptor gamma 2
15125928 10.1016/j.bmcl.2004.03.073 Retinoic acid receptor gamma 1
15125928 10.1016/j.bmcl.2004.03.073 Unchecked 1

Data from ChEMBL 36 via Core Engine