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Compound Detail

CHEMBL25244

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CC(C)=C(c1ccc(C(=O)O)cc1)c1cc2c(cc1C)C(C)(C)CCC2(C)C

Basic Information

ChEMBL ID CHEMBL25244
Phase Preclinical
Structure Type MOL
InChI Key QDSXVZMDVWIEJZ-UHFFFAOYSA-N
3
Targets
6
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

376.5
MW (Da)
6.88
ALogP
1
HBA
1
HBD
37.3
PSA (Ų)
0.63
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H32O2
MW 376.54
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness 0.33

Activity Summary

EC50 3 meas. best 6.89
Kd 3 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinoic acid receptor RXR-alpha
CHEMBL2061
Kd 7.3 7.3 50.0 1
Retinoic acid receptor RXR-beta
CHEMBL4047
EC50 6.89 6.89 130.0 1
Retinoic acid receptor RXR-gamma
CHEMBL4402
Kd 6.82 6.82 150.0 1
Retinoic acid receptor RXR-beta
CHEMBL4047
Kd 6.8 6.8 160.0 1
Retinoic acid receptor RXR-gamma
CHEMBL4402
EC50 6.62 6.62 240.0 1
Retinoic acid receptor RXR-alpha
CHEMBL2061
EC50 6.52 6.52 300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7636877 10.1021/jm00016a018 Retinoic acid receptor RXR-alpha 2
7636877 10.1021/jm00016a018 Retinoic acid receptor RXR-beta 2
7636877 10.1021/jm00016a018 Retinoic acid receptor RXR-gamma 2
10890152 10.1016/s0960-894x(00)00243-2 Retinoic acid receptor alpha 2
10890152 10.1016/s0960-894x(00)00243-2 Retinoic acid receptor beta 2
10890152 10.1016/s0960-894x(00)00243-2 Retinoic acid receptor gamma 2
10890152 10.1016/s0960-894x(00)00243-2 Retinoic acid receptor RXR-alpha 2
10890152 10.1016/s0960-894x(00)00243-2 MDA-MB-231 2

Data from ChEMBL 36 via Core Engine