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Compound Detail

CHEMBL234749

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CC(C)(C)c1onc(-c2c(Cl)cccc2Cl)c1COc1ccc(C(=O)Nc2cccc(C(=O)O)c2)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL234749
Phase Preclinical
Structure Type MOL
InChI Key ZQFCMJUELRQQFZ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

573.9
MW (Da)
8.13
ALogP
5
HBA
2
HBD
101.7
PSA (Ų)
0.23
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H23Cl3N2O5
MW 573.86
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.25

Activity Summary

EC50 1 meas. best 5.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bile acid receptor
CHEMBL2047
EC50 5.89 5.89 1300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bile acid receptor EC50 = 1300.0 nM 5.89 Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity 17292610

Literature References

PubMed DOI Target Context # Activities
17292610 10.1016/j.bmc.2007.01.046 Bile acid receptor 2

Data from ChEMBL 36 via Core Engine