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Compound Detail

CHEMBL181369

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C[C@@H]1c2c(ccc(O)c2F)O[C@@H](c2ccc(OCCN3CCCC3)cc2)[C@H]1c1ccc(O)cc1

Basic Information

ChEMBL ID CHEMBL181369
Phase Preclinical
Structure Type MOL
InChI Key SZXSUSMBHOMKSB-IRTCRQIFSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

463.6
MW (Da)
5.73
ALogP
5
HBA
2
HBD
62.2
PSA (Ų)
0.49
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H30FNO4
MW 463.55
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness 0.09

Activity Summary

IC50 2 meas. best 9.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Estrogen receptor
CHEMBL206
IC50 9.05 9.05 0.9 1
Estrogen receptor beta
CHEMBL242
IC50 7.96 7.96 11.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Estrogen receptor IC50 = 0.9 nM 9.05 Inhibition of estrogen receptor alpha 15745820
Estrogen receptor beta IC50 = 11.0 nM 7.96 Inhibition of estrogen receptor beta 15745820

Literature References

PubMed DOI Target Context # Activities
15745820 10.1016/j.bmcl.2005.01.046 Estrogen receptor 5
15745820 10.1016/j.bmcl.2005.01.046 Estrogen receptor beta 1

Data from ChEMBL 36 via Core Engine