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Compound Detail

CHEMBL537638

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Cl.Oc1ccc2c(Oc3ccc(OCCN4CCCCC4)cc3)c(-c3ccc(F)cc3)ccc2c1

Basic Information

ChEMBL ID CHEMBL537638
Phase Preclinical
Structure Type MOL
InChI Key VNJAOSPLSJJGTL-UHFFFAOYSA-N
Parent Compound CHEMBL244205
Active Moiety CHEMBL244205
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

457.6
MW (Da)
7.01
ALogP
4
HBA
1
HBD
41.9
PSA (Ų)
0.32
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 C29H29ClFNO3
MW 494.01
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.51

Activity Summary

IC50 2 meas. best 9.47
Ki 2 meas. best 9.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Estrogen receptor
CHEMBL2724
Ki 9.6 9.6 0.2 1
Estrogen receptor beta
CHEMBL3021
Ki 9.52 9.52 0.3 1
Estrogen receptor
CHEMBL2093866
IC50 9.47 8.985 0.3 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16250633 10.1021/jm050723z Estrogen receptor 4
16250633 10.1021/jm050723z Estrogen receptor beta 1

Data from ChEMBL 36 via Core Engine