Compound Detail
CHEMBL1715
PIOGLITAZONE HYDROCHLORIDE 💊 Approved Drug
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💊 Approved Drug
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
20
Publications
24
Known Names
8
Indications
1
Mechanisms
Molecular Properties
356.4
MW (Da)
3.16
ALogP
5
HBA
1
HBD
68.3
PSA (Ų)
0.83
QED
0
Ro5 Violations
7
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1999 |
| Availability | Prescription |
| Chirality | Racemic |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Peroxisome proliferator-activated receptor gamma agonist | AGONIST | Peroxisome proliferator-activated receptor gamma | ✓ | ✓ |
Indications
Diabetes Mellitus, Type 2 Carcinoma, Non-Small-Cell Lung Depressive Disorder, Major Leukoplakia, Oral Renal Insufficiency, Chronic Amyotrophic Lateral Sclerosis Non-alcoholic Fatty Liver Disease Pancreatic Neoplasms
Drug Warnings
Black Box Warning
cardiotoxicity
Activity Summary
EC50 2 meas. best 6.31
IC50 1 meas. best 4.63
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| RXR alpha/PPAR gamma CHEMBL2111394 | EC50 | 6.31 | 6.31 | 490.0 | 1 |
| Peroxisome proliferator-activated receptor gamma CHEMBL235 | EC50 | 5.12 | 5.12 | 7600.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 4.63 | 4.63 | 23250.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| RXR alpha/PPAR gamma | EC50 | = | 490.0 | nM | 6.31 | Transcriptional activation in COS cells expressing PPAR gamma and RXR alpha; val... | 11906293 |
| Peroxisome proliferator-activated receptor gamma | EC50 | = | 7600.0 | nM | 5.12 | Peroxisome proliferator activated receptor gamma agonistic activity in HepG2 cel... | 10714503 |
| Unchecked | IC50 | = | 23250.0 | nM | 4.63 | PUBCHEM_BIOASSAY: High Throughput Screening Assay used to Identify Novel Compoun... | - |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 22836190 | 10.1016/j.bmc.2012.06.049 | Mus musculus | 3 |
| - | 10.1007/s00044-010-9359-5 | Rattus norvegicus | 3 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 1635060 | 10.1021/jm00092a012 | Mus musculus | 2 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| 23571415 | 10.1124/mol.112.084152 | Solute carrier organic anion transporter family member 1B1 | 1 |
| 34555615 | 10.1016/j.ejmech.2021.113847 | Transthyretin | 1 |
| - | 10.6019/CHEMBL4513141 | Pseudomonas aeruginosa | 1 |
| - | 10.6019/CHEMBL4513141 | Klebsiella pneumoniae | 1 |
| - | 10.6019/CHEMBL4513141 | Escherichia coli | 1 |
| - | 10.6019/CHEMBL4513141 | Cryptococcus neoformans | 1 |
| - | 10.6019/CHEMBL4513141 | Candida albicans | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| 11906293 | 10.1021/jm010490l | Unchecked | 1 |
| 23571415 | 10.1124/mol.112.084152 | Solute carrier organic anion transporter family member 1B3 | 1 |
| 10714503 | 10.1016/s0960-894x(00)00003-2 | Mus musculus | 1 |
| 10714503 | 10.1016/s0960-894x(00)00003-2 | Peroxisome proliferator-activated receptor gamma | 1 |
| 11906293 | 10.1021/jm010490l | RXR alpha/PPAR gamma | 1 |
| 11906293 | 10.1021/jm010490l | Rattus norvegicus | 1 |
Data from ChEMBL 36 via Core Engine