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Compound Detail

CHEMBL487

DROLOXIFENE
🧪 Phase III
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🧪 Phase III
CC/C(=C(/c1ccc(OCCN(C)C)cc1)c1cccc(O)c1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL487
Name DROLOXIFENE
Phase Phase III
Structure Type MOL
InChI Key ZQZFYGIXNQKOAV-OCEACIFDSA-N

Known Names

3-hydroxytamoxifen Droloxifene Droloxifeno E-droloxifene Fk-435 K-060 K-21060E K060 K060E
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
12
Publications
9
Known Names
1
Mechanisms

Molecular Properties

387.5
MW (Da)
5.70
ALogP
3
HBA
1
HBD
32.7
PSA (Ų)
0.50
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral
USAN Stem -ifene
USAN Year 1994

Extended Properties

Molecular Formula C26H29NO2
MW 387.52
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.23

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Estrogen receptor modulator MODULATOR Estrogen receptor

Activity Summary

IC50 1 meas. best 5.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
SARS-CoV-2
CHEMBL4303835
IC50 5.18 5.18 6600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
SARS-CoV-2 IC50 = 6600.0 nM 5.18 Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in ... -

Literature References

PubMed DOI Target Context # Activities
15646539 10.1016/s0399-8320(04)95062-2 Unchecked 11
15646539 10.1016/s0399-8320(04)95062-2 NON-PROTEIN TARGET 8
4045924 10.1021/jm00148a020 MCF7 4
7131484 10.1021/jm00351a010 Estrogen receptor 3
20014752 10.1021/tx900326k Hepatotoxicity 3
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
7914405 10.1016/0006-2952(94)90099-x ATP-dependent translocase ABCB1 1
- 10.1101/2020.03.20.999730 SARS-CoV-2 1
- 10.1101/2020.03.20.999730 Vero 1
- 10.1101/2020.03.20.999730 ADMET 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1

Data from ChEMBL 36 via Core Engine