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Compound Detail

CHEMBL381489

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CC(C)(C)C(=O)Oc1ccc2c(c1)O[C@@H](c1ccc(OCCN3CCCCC3)cc1)C1=C2COc2cc(OC(=O)C(C)(C)C)ccc21

Basic Information

ChEMBL ID CHEMBL381489
Phase Preclinical
Structure Type MOL
InChI Key HFEFFYLNWHUHTO-DHUJRADRSA-N
1
Targets
2
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

639.8
MW (Da)
7.89
ALogP
8
HBA
0
HBD
83.5
PSA (Ų)
0.19
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H45NO7
MW 639.79
Aromatic Rings 3
Heavy Atoms 47
NP-Likeness -0.10

Activity Summary

IC50 2 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Estrogen receptor
CHEMBL2093866
IC50 7.0 6.585 99.0 2

Pharmacokinetic Data

Parameter Value Units Species
F 9.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Estrogen receptor IC50 = 99.0 nM 7.0 Inhibition of estrogen receptor in Ishikawa cells 16722623
Estrogen receptor IC50 = 670.0 nM 6.17 Inhibition of estrogen receptor in MCF7 cells 16722623

Literature References

PubMed DOI Target Context # Activities
16722623 10.1021/jm060353u Rattus norvegicus 9
16722623 10.1021/jm060353u Estrogen receptor 5
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
16722623 10.1021/jm060353u Estrogen receptor beta 1

Data from ChEMBL 36 via Core Engine