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Compound Detail

CHEMBL5570505

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Cc1cccc(CN(C(=O)C2CCCC2)c2ccc(CC(=O)NCc3ccc4c(c3)OCO4)cc2)c1

Basic Information

ChEMBL ID CHEMBL5570505
Phase Preclinical
Structure Type MOL
InChI Key XXQKGHXWZVWLPV-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

484.6
MW (Da)
5.31
ALogP
4
HBA
1
HBD
67.9
PSA (Ų)
0.47
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H32N2O4
MW 484.60
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.28

Activity Summary

IC50 1 meas. best 5.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bile acid receptor
CHEMBL2047
IC50 5.37 5.37 4270.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bile acid receptor IC50 = 4270.0 nM 5.37 Antagonist activity against human FXR transfected in HEK293T cells co-transfecte... 38043493

Literature References

PubMed DOI Target Context # Activities
38043493 10.1016/j.ejmech.2023.115992 Mus musculus 40
38043493 10.1016/j.ejmech.2023.115992 Unchecked 8
38043493 10.1016/j.ejmech.2023.115992 HepG2 3
38043493 10.1016/j.ejmech.2023.115992 Bile acid receptor 2
38043493 10.1016/j.ejmech.2023.115992 L02 1
38043493 10.1016/j.ejmech.2023.115992 Peroxisome proliferator-activated receptor alpha 1
38043493 10.1016/j.ejmech.2023.115992 Peroxisome proliferator-activated receptor delta 1
38043493 10.1016/j.ejmech.2023.115992 Peroxisome proliferator-activated receptor gamma 1
38043493 10.1016/j.ejmech.2023.115992 ADMET 1

Data from ChEMBL 36 via Core Engine