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Compound Detail

CHEMBL4438589

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CN1CCN(c2ccc(/C(=C(/CCCO)c3ccccc3)c3ccc(O)cc3)cc2)CC1.Cl.Cl

Basic Information

ChEMBL ID CHEMBL4438589
Phase Preclinical
Structure Type MOL
InChI Key ZTABGVCSNBOTNS-JZYARHMISA-N
Parent Compound CHEMBL4595968
Active Moiety CHEMBL4595968
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

428.6
MW (Da)
4.88
ALogP
4
HBA
2
HBD
46.9
PSA (Ų)
0.53
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H34Cl2N2O2
MW 501.50
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.24

Activity Summary

IC50 3 meas. best 7.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Estrogen-related receptor gamma
CHEMBL4245
IC50 7.22 7.22 60.0 1
Estrogen receptor
CHEMBL206
IC50 5.77 5.77 1700.0 1
Steroid hormone receptor ERR2
CHEMBL3751
IC50 5.7 5.7 1980.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30657313 10.1021/acs.jmedchem.8b01296 Estrogen-related receptor gamma 2
30657313 10.1021/acs.jmedchem.8b01296 Steroid hormone receptor ERR1 1
30657313 10.1021/acs.jmedchem.8b01296 Steroid hormone receptor ERR2 1
30657313 10.1021/acs.jmedchem.8b01296 Estrogen receptor 1

Data from ChEMBL 36 via Core Engine