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Compound Detail

CHEMBL5208567

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CC(F)(F)c1nc(C23CCC(CN(C(=O)C45CC(F)(C4)C5)c4cccc(N5CCC(O)CC5)c4)(CC2)CC3)no1

Basic Information

ChEMBL ID CHEMBL5208567
Phase Preclinical
Structure Type MOL
InChI Key OXXHKIXKQSCOSO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

558.6
MW (Da)
5.66
ALogP
6
HBA
1
HBD
82.7
PSA (Ų)
0.47
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H37F3N4O3
MW 558.65
Aromatic Rings 2
Heavy Atoms 40
NP-Likeness -0.74

Activity Summary

EC50 1 meas. best 6.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bile acid receptor
CHEMBL2047
EC50 6.63 6.63 232.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bile acid receptor EC50 = 232.0 nM 6.63 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 ADMET 3
35704802 10.1021/acs.jmedchem.2c00165 Bile acid receptor 2
35704802 10.1021/acs.jmedchem.2c00165 Nuclear receptor subfamily 1 group I member 2 2
35704802 10.1021/acs.jmedchem.2c00165 Cytochrome P450 2C9 1
35704802 10.1021/acs.jmedchem.2c00165 Cytochrome P450 2C19 1

Data from ChEMBL 36 via Core Engine