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Compound Detail

CHEMBL104246

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Cc1oc(-c2ccccc2)nc1CCOc1ccc(C[C@@H](C(=O)O)N2CCOCC2)cc1

Basic Information

ChEMBL ID CHEMBL104246
Phase Preclinical
Structure Type MOL
InChI Key VUGWDUAFDNEHMZ-QHCPKHFHSA-N
2
Targets
5
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

436.5
MW (Da)
3.60
ALogP
6
HBA
1
HBD
85.0
PSA (Ų)
0.55
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H28N2O5
MW 436.51
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.17

Activity Summary

EC50 4 meas. best 7.62
Ki 1 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Peroxisome proliferator-activated receptor gamma
CHEMBL235
EC50 7.62 7.62 24.0 2
Peroxisome proliferator-activated receptor gamma
CHEMBL235
Ki 6.8 6.8 158.0 1
Peroxisome proliferator-activated receptor alpha
CHEMBL239
EC50 5.16 5.16 6900.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11720854 10.1016/s0960-894x(01)00649-7 Peroxisome proliferator-activated receptor gamma 2
11720854 10.1016/s0960-894x(01)00649-7 Peroxisome proliferator-activated receptor alpha 1
- 10.1007/s00044-011-9818-7 Peroxisome proliferator-activated receptor gamma 1
- 10.1007/s00044-011-9818-7 Peroxisome proliferator-activated receptor alpha 1

Data from ChEMBL 36 via Core Engine