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Compound Detail

CHEMBL5420532

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O=C(O)Cc1ccc(-c2ccc(OCc3c(-c4c(Cl)cccc4Cl)noc3C3CC3)cc2)cc1

Basic Information

ChEMBL ID CHEMBL5420532
Phase Preclinical
Structure Type MOL
InChI Key AJXYOQYFSSSTMZ-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

494.4
MW (Da)
7.40
ALogP
4
HBA
1
HBD
72.6
PSA (Ų)
0.28
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H21Cl2NO4
MW 494.37
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.57

Activity Summary

IC50 3 meas. best 5.54
EC50 2 meas. best 6.87

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bile acid receptor
CHEMBL2047
EC50 6.87 6.445 135.0 2
Fatty acid-binding protein, liver
CHEMBL5421
IC50 5.54 5.54 2900.0 1
Fatty acid-binding protein, adipocyte
CHEMBL2083
IC50 5.25 5.25 5600.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
37079895 10.1021/acs.jmedchem.2c01918 Mus musculus 15
37079895 10.1021/acs.jmedchem.2c01918 Bile acid receptor 11
37079895 10.1021/acs.jmedchem.2c01918 ADMET 10
37079895 10.1021/acs.jmedchem.2c01918 Unchecked 9
37079895 10.1021/acs.jmedchem.2c01918 Fatty acid-binding protein, liver 2
37079895 10.1021/acs.jmedchem.2c01918 Peroxisome proliferator-activated receptor alpha 2
37079895 10.1021/acs.jmedchem.2c01918 Peroxisome proliferator-activated receptor gamma 2
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 Vitamin D3 receptor 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
37079895 10.1021/acs.jmedchem.2c01918 Oxysterols receptor LXR-beta 1

Data from ChEMBL 36 via Core Engine