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Compound Detail

CHEMBL478726

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Cc1oc(-c2ccccc2)nc1CC#Cc1ccc(CC(C(=O)O)c2cccnc2)cc1

Basic Information

ChEMBL ID CHEMBL478726
Phase Preclinical
Structure Type MOL
InChI Key JANZNJGVOWUOBK-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

422.5
MW (Da)
5.05
ALogP
4
HBA
1
HBD
76.2
PSA (Ų)
0.44
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H22N2O3
MW 422.48
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -0.79

Activity Summary

EC50 2 meas. best 5.35
IC50 1 meas. best 4.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Peroxisome proliferator-activated receptor gamma
CHEMBL235
EC50 5.35 5.35 4500.0 1
Peroxisome proliferator-activated receptor alpha
CHEMBL239
EC50 4.8 4.8 16000.0 1
Peroxisome proliferator-activated receptor gamma
CHEMBL235
IC50 4.58 4.58 26000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18394907 10.1016/j.bmc.2008.03.043 Peroxisome proliferator-activated receptor gamma 3
18394907 10.1016/j.bmc.2008.03.043 Peroxisome proliferator-activated receptor alpha 3
18394907 10.1016/j.bmc.2008.03.043 Unchecked 1

Data from ChEMBL 36 via Core Engine