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Compound Detail

CHEMBL204376

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CN(C)CCOc1ccc(/C(=C(/CCO)c2ccccc2)c2ccc(O)cc2)cc1

Basic Information

ChEMBL ID CHEMBL204376
Phase Preclinical
Structure Type MOL
InChI Key MZLLOCKOYWOFPI-QPLCGJKRSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

403.5
MW (Da)
4.67
ALogP
4
HBA
2
HBD
52.9
PSA (Ų)
0.51
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29NO3
MW 403.52
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.09

Activity Summary

IC50 2 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Estrogen receptor
CHEMBL206
IC50 6.6 6.6 250.0 1
Estrogen-related receptor gamma
CHEMBL4245
IC50 6.6 6.6 250.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Estrogen-related receptor gamma IC50 = 250.0 nM 6.6 Displacement of [3H]4-OHT from ERRgamma 16307879
Estrogen receptor IC50 = 250.0 nM 6.6 Displacement of [3H]estradiol from ERalpha 16307879

Literature References

PubMed DOI Target Context # Activities
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

Data from ChEMBL 36 via Core Engine