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Compound Detail

CHEMBL5194045

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CC(CN1CCCC2CCCNC21)OCC(=O)N1NC2c3ccc(O)cc3OCC2c2ccc(O)cc21

Basic Information

ChEMBL ID CHEMBL5194045
Phase Preclinical
Structure Type MOL
InChI Key MPHRADSGLDMDNB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

508.6
MW (Da)
2.99
ALogP
8
HBA
4
HBD
106.5
PSA (Ų)
0.49
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H36N4O5
MW 508.62
Aromatic Rings 2
Heavy Atoms 37
NP-Likeness 0.52

Activity Summary

IC50 2 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Estrogen receptor beta
CHEMBL242
IC50 7.5 7.5 31.9 1
Estrogen receptor
CHEMBL206
IC50 6.77 6.77 168.4 1

Pharmacokinetic Data

Parameter Value Units Species
Ka 37.84 nM Homo sapiens
Ka 17.9 nM Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Estrogen receptor beta IC50 = 31.87 nM 7.5 Antagonist activity at ERbeta (unknown origin) 34710747
Estrogen receptor IC50 = 168.41 nM 6.77 Antagonist activity at ERalpha (unknown origin) 34710747

Literature References

PubMed DOI Target Context # Activities
34710747 10.1016/j.ejmech.2021.113869 Estrogen receptor 3
34710747 10.1016/j.ejmech.2021.113869 Estrogen receptor beta 3

Data from ChEMBL 36 via Core Engine