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Compound Detail

CHEMBL602059

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CC(C)OC(=O)C1=CN(C(=O)c2cccc(OCCCN3CCCC3)c2)CC(C)(C)c2c1[nH]c1ccccc21

Basic Information

ChEMBL ID CHEMBL602059
Phase Preclinical
Structure Type MOL
InChI Key TZTZOKQTFAKCOX-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

529.7
MW (Da)
5.76
ALogP
5
HBA
1
HBD
74.9
PSA (Ų)
0.30
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H39N3O4
MW 529.68
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -0.59

Activity Summary

EC50 1 meas. best 5.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bile acid receptor
CHEMBL2047
EC50 5.79 5.79 1603.0 1

Pharmacokinetic Data

Parameter Value Units Species
t1/2 - - Homo sapiens
t1/2 - - Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bile acid receptor EC50 = 1603.0 nM 5.79 Agonist activity at human FXR-LBD expressed in HEL293 cells by Gal4-luciferase a... 20095622

Literature References

PubMed DOI Target Context # Activities
20095622 10.1021/jm901650u Bile acid receptor 2
20095622 10.1021/jm901650u Liver microsomes 1
20095622 10.1021/jm901650u ADMET 1
20095622 10.1021/jm901650u No relevant target 1

Data from ChEMBL 36 via Core Engine