Compound Detail
CHEMBL2105720
LESINURAD 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL2105720 |
| Name | LESINURAD |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | FGQFOYHRJSUHMR-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
8
Targets
41
Activities
1
Assay Types
30
PK Parameters
20
Publications
6
Known Names
2
Indications
1
Mechanisms
Molecular Properties
404.3
MW (Da)
4.24
ALogP
5
HBA
1
HBD
68.0
PSA (Ų)
0.64
QED
0
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2015 |
| Availability | Discontinued |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Solute carrier family 22 member 12 inhibitor | INHIBITOR | Solute carrier family 22 member 12 | ✓ | ✓ |
Indications
Gout Hyperuricemia
ATC Classification
M04AB05
lesinurad
Level 1: MUSCULO-SKELETAL SYSTEM
Level 2: ANTIGOUT PREPARATIONS
Drug Warnings
Black Box Warning
General Warning
Activity Summary
IC50 41 meas. best 5.69
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Solute carrier family 22 member 11 CHEMBL2073677 | IC50 | 5.69 | 5.42 | 2030.0 | 3 |
| Solute carrier family 22 member 12 CHEMBL6120 | IC50 | 5.45 | 4.995 | 3530.0 | 24 |
| Cytochrome P450 2C19 CHEMBL3622 | IC50 | 4.97 | 4.7167 | 10600.0 | 3 |
| Unchecked CHEMBL612545 | IC50 | 4.94 | 4.94 | 11500.0 | 1 |
| Cytochrome P450 1A2 CHEMBL3356 | IC50 | 4.76 | 4.61 | 17300.0 | 3 |
| Cytochrome P450 2C9 CHEMBL3397 | IC50 | 4.51 | 4.305 | 31200.0 | 2 |
| Cytochrome P450 3A4 CHEMBL340 | IC50 | 4.51 | 4.3767 | 31000.0 | 3 |
| Cytochrome P450 2D6 CHEMBL289 | IC50 | 4.49 | 4.265 | 32600.0 | 2 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 5821.78 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 6064.35 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 18961.2 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 13220.28 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 3840.76 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 3598.18 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 16939.75 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 14392.72 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 5862.2 | ng.hr.mL-1 | Macaca fascicularis |
| AUC | 4042.9 | ng.hr.mL-1 | Macaca fascicularis |
| AUC | 40186.43 | ng.hr.mL-1 | Macaca fascicularis |
| AUC | 11400.98 | ng.hr.mL-1 | Macaca fascicularis |
| AUC | 10794.54 | ng.hr.mL-1 | Macaca fascicularis |
| AUC | 7762.37 | ng.hr.mL-1 | Macaca fascicularis |
| AUC | 33919.93 | ng.hr.mL-1 | Macaca fascicularis |
| AUC | 15080.02 | ng.hr.mL-1 | Macaca fascicularis |
| AUC | 144648.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 143855.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 7118.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 7079.0 | ng.hr.mL-1 | Mus musculus |
| CL | 5.8 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 5.5 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 9.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 9.4 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 5.9 | mL.min-1.kg-1 | Macaca fascicularis |
| CL | 8.8 | mL.min-1.kg-1 | Macaca fascicularis |
| CL | 3.3 | mL.min-1.kg-1 | Macaca fascicularis |
| CL | 4.7 | mL.min-1.kg-1 | Macaca fascicularis |
| Cmax | 65472.8 | nM | Mus musculus |
| Cmax | 3702.79 | nM | Mus musculus |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine