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Compound Detail

CHEMBL1402

4-HYDROXYTORMIFENE
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CN(C)CCOc1ccc(/C(=C(/CCCl)c2ccccc2)c2ccc(O)cc2)cc1

Basic Information

ChEMBL ID CHEMBL1402
Name 4-HYDROXYTORMIFENE
Phase Preclinical
Structure Type MOL
InChI Key OIUCUUXSMIJSEB-QPLCGJKRSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

422.0
MW (Da)
5.92
ALogP
3
HBA
1
HBD
32.7
PSA (Ų)
0.34
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 C26H28ClNO2
MW 421.97
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.25

Activity Summary

IC50 2 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Estrogen receptor
CHEMBL206
IC50 8.4 8.4 4.0 1
Estrogen-related receptor gamma
CHEMBL4245
IC50 7.89 7.89 13.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22434874 10.1124/dmd.111.044040 ADMET 9
22434874 10.1124/dmd.111.044040 Liver cytosol 4
22434874 10.1124/dmd.111.044040 Sulfotransferase 1E1 2
22434874 10.1124/dmd.111.044040 Sulfotransferase 1A1 2
16307879 10.1016/j.bmcl.2005.11.030 Estrogen-related receptor gamma 1
16307879 10.1016/j.bmcl.2005.11.030 Estrogen receptor 1
16307879 10.1016/j.bmcl.2005.11.030 Unchecked 1
22434874 10.1124/dmd.111.044040 No relevant target 1

Data from ChEMBL 36 via Core Engine