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Compound Detail

CHEMBL426115

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COc1cc(O)cc2ncn(-c3ccc(O)cc3)c(=O)c12

Basic Information

ChEMBL ID CHEMBL426115
Phase Preclinical
Structure Type MOL
InChI Key VHZMSDGAAMARIU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

284.3
MW (Da)
1.81
ALogP
6
HBA
2
HBD
84.6
PSA (Ų)
0.75
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H12N2O4
MW 284.27
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -0.02

Activity Summary

EC50 1 meas. best 5.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Estrogen receptor beta
CHEMBL242
EC50 5.07 5.07 8506.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Estrogen receptor beta EC50 = 8506.0 nM 5.07 Inhibition of ER beta-mediated transactivation of ERE in HeLa cell luciferase as... 16610787

Literature References

PubMed DOI Target Context # Activities
16610787 10.1021/jm0509389 Estrogen receptor beta 2
16610787 10.1021/jm0509389 Estrogen receptor 2

Data from ChEMBL 36 via Core Engine