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Compound Detail

CHEMBL5201654

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CCOC(=O)c1nc(-c2cccc(N(CC34CCC(c5nc(C6CC6)no5)(CC3)CC4)C(=O)C3CCCCC3)c2)cs1

Basic Information

ChEMBL ID CHEMBL5201654
Phase Preclinical
Structure Type MOL
InChI Key HESOEIFBFGIYEQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

588.8
MW (Da)
7.45
ALogP
8
HBA
0
HBD
98.4
PSA (Ų)
0.24
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H40N4O4S
MW 588.77
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -1.18

Activity Summary

EC50 1 meas. best 6.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bile acid receptor
CHEMBL2047
EC50 6.04 6.04 919.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bile acid receptor EC50 = 919.0 nM 6.04 Agonist activity at Gal4-fused human FXR in HEK293 cells incubated for 15 min by... 35704802

Literature References

PubMed DOI Target Context # Activities
35704802 10.1021/acs.jmedchem.2c00165 Bile acid receptor 2

Data from ChEMBL 36 via Core Engine