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Compound Detail

CHEMBL592054

IMIGLITAZAR
🧪 Phase III
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🧪 Phase III
Cc1oc(-c2ccccc2)nc1COc1ccc(CO/N=C(\CCC(=O)O)c2ccccc2)cc1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL592054
Name IMIGLITAZAR
Phase Phase III
Structure Type MOL
InChI Key ULVDFHLHKNJICZ-QCWLDUFUSA-N

Known Names

Imiglitazar Tak-559
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
2
Known Names
1
Indications
2
Mechanisms

Molecular Properties

470.5
MW (Da)
6.01
ALogP
6
HBA
1
HBD
94.2
PSA (Ų)
0.21
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral

Flags

Natural Product
USAN Stem -glitazar

Extended Properties

Molecular Formula C28H26N2O5
MW 470.53
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.93

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Peroxisome proliferator-activated receptor alpha agonist AGONIST Peroxisome proliferator-activated receptor alpha ✓ ✓
Peroxisome proliferator-activated receptor gamma agonist AGONIST Peroxisome proliferator-activated receptor gamma ✓ ✓

Indications

Diabetes Mellitus

Activity Summary

EC50 4 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Peroxisome proliferator-activated receptor gamma
CHEMBL235
 EC50 8.4 8.4 4.0 2
Peroxisome proliferator-activated receptor alpha
CHEMBL239
 EC50 8.3 8.2 5.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Peroxisome proliferator-activated receptor gamma EC50 = 4.0 nM 8.4 Agonist activity at human PPARgamma transactivation expressed in human HePG2 cel... 18976908
Peroxisome proliferator-activated receptor gamma EC50 = 4.0 nM 8.4 Agonist activity at human full length PPARgamma expressed in human HepG2 cells c... 20022492
Peroxisome proliferator-activated receptor alpha EC50 = 5.0 nM 8.3 Agonist activity at human full length PPARalpha expressed in human HepG2 cells c... 20022492
Peroxisome proliferator-activated receptor alpha EC50 = 8.0 nM 8.1 Agonist activity at human PPARalpha transactivation expressed in human HePG2 cel... 18976908

Literature References

PubMed DOI Target Context # Activities
20022492 10.1016/j.bmcl.2009.12.022 Peroxisome proliferator-activated receptor gamma 2
20022492 10.1016/j.bmcl.2009.12.022 Peroxisome proliferator-activated receptor alpha 2
18976908 10.1016/j.bmcl.2008.10.062 Peroxisome proliferator-activated receptor delta 1
18976908 10.1016/j.bmcl.2008.10.062 Peroxisome proliferator-activated receptor alpha 1
18976908 10.1016/j.bmcl.2008.10.062 Peroxisome proliferator-activated receptor gamma 1
18976908 10.1016/j.bmcl.2008.10.062 Unchecked 1
20022492 10.1016/j.bmcl.2009.12.022 Mus musculus 1
20022492 10.1016/j.bmcl.2009.12.022 Peroxisome proliferator-activated receptor delta 1

Data from ChEMBL 36 via Core Engine