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Compound Detail

CHEMBL4081283

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CCCCN(C)C(=O)/C=C/c1ccc(C(=C2C3CC4CC(C3)CC2C4)c2ccc(O)cc2)cc1

Basic Information

ChEMBL ID CHEMBL4081283
Phase Preclinical
Structure Type MOL
InChI Key GYWHDQKFLIMDEI-MMBXMCLJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

455.6
MW (Da)
6.92
ALogP
2
HBA
1
HBD
40.5
PSA (Ų)
0.46
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H37NO2
MW 455.64
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.09

Activity Summary

Ki 1 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Estrogen receptor
CHEMBL206
Ki 9.15 9.15 0.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Estrogen receptor Ki = 0.71 nM 9.15 Displacement of [3H]estradiol from full-length human ERalpha receptor by scintil... 28657320

Literature References

PubMed DOI Target Context # Activities
28657320 10.1021/acs.jmedchem.7b00585 Estrogen receptor 3
28657320 10.1021/acs.jmedchem.7b00585 MDA-MB-231 1
28657320 10.1021/acs.jmedchem.7b00585 MCF7 1

Data from ChEMBL 36 via Core Engine