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Compound Detail

CHEMBL5268158

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COc1cc(CCc2ccccc2)c(C(=O)O)c(O)c1C/C=C(\C)CC=C(C)C

Basic Information

ChEMBL ID CHEMBL5268158
Phase Preclinical
Structure Type MOL
InChI Key WNQYHTVUADEJHB-LDADJPATSA-N
3
Targets
6
Activities
2
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

394.5
MW (Da)
5.73
ALogP
3
HBA
2
HBD
66.8
PSA (Ų)
0.53
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H30O4
MW 394.51
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness 1.65

Activity Summary

EC50 3 meas. best 7.14
Ki 3 meas. best 7.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Peroxisome proliferator-activated receptor gamma
CHEMBL235
Ki 7.72 7.72 19.0 1
Peroxisome proliferator-activated receptor gamma
CHEMBL235
EC50 7.14 7.14 73.0 1
Peroxisome proliferator-activated receptor delta
CHEMBL3979
EC50 6.13 6.13 740.0 1
Peroxisome proliferator-activated receptor alpha
CHEMBL239
EC50 6.04 6.04 906.0 1
Peroxisome proliferator-activated receptor delta
CHEMBL3979
Ki 5.75 5.75 1800.0 1
Peroxisome proliferator-activated receptor alpha
CHEMBL239
Ki 5.58 5.58 2600.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 77057.62 nM Mus musculus
T1/2 2.0 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33992930 10.1016/j.ejmech.2021.113535 Peroxisome proliferator-activated receptor gamma 3
33992930 10.1016/j.ejmech.2021.113535 Peroxisome proliferator-activated receptor alpha 3
33992930 10.1016/j.ejmech.2021.113535 Peroxisome proliferator-activated receptor delta 3
33992930 10.1016/j.ejmech.2021.113535 ADMET 2

Data from ChEMBL 36 via Core Engine