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Compound Detail

CHEMBL4577891

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CCC/C(=C\c1cc(OCc2ccc3nc(C(F)(F)F)cc(OC)c3c2)ccc1OCC1CCN(C)CC1)C(=O)O

Basic Information

ChEMBL ID CHEMBL4577891
Phase Preclinical
Structure Type MOL
InChI Key QQBUOAQHLBBDFR-PXLXIMEGSA-N
1
Targets
1
Activities
1
Assay Types
7
PK Parameters
11
Publications
0
Known Names

Molecular Properties

572.6
MW (Da)
6.83
ALogP
6
HBA
1
HBD
81.1
PSA (Ų)
0.25
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H35F3N2O5
MW 572.62
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness -0.48

Activity Summary

IC50 1 meas. best 5.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Peroxisome proliferator-activated receptor gamma
CHEMBL235
IC50 5.6 5.6 2500.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 101.02 ng.hr.mL-1 Mus musculus
AUC 649.96 ng.hr.mL-1 Mus musculus
Cmax 60.0 nM Mus musculus
Cmax 380.0 nM Mus musculus
T1/2 1.0 hr Rattus norvegicus
Tmax 1.0 hr Mus musculus
Tmax 2.0 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31548084 10.1016/j.bmc.2019.115082 ADMET 10
31548084 10.1016/j.bmc.2019.115082 Peroxisome proliferator-activated receptor alpha 2
31548084 10.1016/j.bmc.2019.115082 Peroxisome proliferator-activated receptor delta 2
31548084 10.1016/j.bmc.2019.115082 Oxysterols receptor LXR-beta 2
31548084 10.1016/j.bmc.2019.115082 Retinoic acid receptor RXR-alpha 2
31548084 10.1016/j.bmc.2019.115082 Retinoic acid receptor alpha 2
31548084 10.1016/j.bmc.2019.115082 Bile acid receptor 2
31548084 10.1016/j.bmc.2019.115082 Vitamin D3 receptor 2
31548084 10.1016/j.bmc.2019.115082 Nuclear receptor subfamily 1 group I member 3 2
31548084 10.1016/j.bmc.2019.115082 Peroxisome proliferator-activated receptor gamma 1
31548084 10.1016/j.bmc.2019.115082 No relevant target 1

Data from ChEMBL 36 via Core Engine