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Compound Detail

CHEMBL4281889

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COc1cc([N+](=O)[O-])ccc1NC(=O)CNc1ccccc1N1CCCC1=O

Basic Information

ChEMBL ID CHEMBL4281889
Phase Preclinical
Structure Type MOL
InChI Key RYEOXOFCHTYTFM-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

384.4
MW (Da)
2.78
ALogP
6
HBA
2
HBD
113.8
PSA (Ų)
0.56
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H20N4O5
MW 384.39
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.96

Activity Summary

EC50 1 meas. best 5.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bile acid receptor
CHEMBL2047
EC50 5.36 5.36 4330.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bile acid receptor EC50 = 4330.0 nM 5.36 Transactivation of full-length FXR (unknown origin) expressed in HEK293 cells af... 30393515

Literature References

PubMed DOI Target Context # Activities
30393515 10.1039/C8MD00272J Bile acid receptor 2
30393515 10.1039/C8MD00272J HEK293 2

Data from ChEMBL 36 via Core Engine