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Compound Detail

CHEMBL5396467

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O=C(O)C1(c2cccc(-c3ccc(OCc4c(-c5c(Cl)cccc5Cl)noc4C4CC4)cc3)c2)CC1

Basic Information

ChEMBL ID CHEMBL5396467
Phase Preclinical
Structure Type MOL
InChI Key GFQRXOXNBQDNBC-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

520.4
MW (Da)
7.89
ALogP
4
HBA
1
HBD
72.6
PSA (Ų)
0.26
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H23Cl2NO4
MW 520.41
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.49

Activity Summary

IC50 3 meas. best 5.57
EC50 2 meas. best 6.84

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bile acid receptor
CHEMBL2047
EC50 6.84 6.575 143.0 2
Fatty acid-binding protein, liver
CHEMBL5421
IC50 5.57 5.57 2700.0 1
Fatty acid-binding protein, adipocyte
CHEMBL2083
IC50 5.21 5.205 6200.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
37079895 10.1021/acs.jmedchem.2c01918 Mus musculus 28
37079895 10.1021/acs.jmedchem.2c01918 ADMET 24
37079895 10.1021/acs.jmedchem.2c01918 Bile acid receptor 11
37079895 10.1021/acs.jmedchem.2c01918 Unchecked 11
37079895 10.1021/acs.jmedchem.2c01918 Peroxisome proliferator-activated receptor alpha 2
37079895 10.1021/acs.jmedchem.2c01918 Fatty acid-binding protein, liver 2
37079895 10.1021/acs.jmedchem.2c01918 Peroxisome proliferator-activated receptor gamma 2
37079895 10.1021/acs.jmedchem.2c01918 Vitamin D3 receptor 1
37079895 10.1021/acs.jmedchem.2c01918 G-protein coupled bile acid receptor 1 1
39067439 10.1016/j.ejmech.2024.116705 Fatty acid-binding protein, adipocyte 1
37079895 10.1021/acs.jmedchem.2c01918 Glucocorticoid receptor 1
37079895 10.1021/acs.jmedchem.2c01918 Mineralocorticoid receptor 1
37079895 10.1021/acs.jmedchem.2c01918 Androgen receptor 1
37079895 10.1021/acs.jmedchem.2c01918 Progesterone receptor 1
37079895 10.1021/acs.jmedchem.2c01918 Estrogen receptor beta 1
37079895 10.1021/acs.jmedchem.2c01918 Estrogen receptor 1
37079895 10.1021/acs.jmedchem.2c01918 Oxysterols receptor LXR-alpha 1
37079895 10.1021/acs.jmedchem.2c01918 Retinoic acid receptor alpha 1
37079895 10.1021/acs.jmedchem.2c01918 Retinoic acid receptor gamma 1
37079895 10.1021/acs.jmedchem.2c01918 Thyroid hormone receptor beta 1

Data from ChEMBL 36 via Core Engine