Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL4074192

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
O=C(O)/C=C/c1ccc(Oc2c(-c3ccc(F)cc3)sc3cc(O)ccc23)cc1

Basic Information

ChEMBL ID CHEMBL4074192
Phase Preclinical
Structure Type MOL
InChI Key PABHIXCWEYDYLO-KGVSQERTSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
3
Publications
0
Known Names

Molecular Properties

406.4
MW (Da)
6.30
ALogP
4
HBA
2
HBD
66.8
PSA (Ų)
0.38
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H15FO4S
MW 406.43
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -0.25

Activity Summary

IC50 1 meas. best 5.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Estrogen receptor
CHEMBL206
IC50 5.74 5.74 1823.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 24.0 mL.min-1.kg-1 Rattus norvegicus
CL 22.0 mL.min-1.kg-1 Mus musculus
Cmax 847.0 nM Rattus norvegicus
Cmax 505.0 nM Mus musculus
F 33.0 % Rattus norvegicus
F 19.0 % Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Estrogen receptor IC50 = 1823.0 nM 5.74 Induction of selective estrogen receptor alpha degradation in human MCF7 cells h... 29562737

Literature References

PubMed DOI Target Context # Activities
29562737 10.1021/acs.jmedchem.7b01682 Rattus norvegicus 3
29562737 10.1021/acs.jmedchem.7b01682 Mus musculus 3
29562737 10.1021/acs.jmedchem.7b01682 Estrogen receptor 2

Data from ChEMBL 36 via Core Engine