Compound Detail
CHEMBL832
SULFINPYRAZONE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL832 |
| Name | SULFINPYRAZONE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | MBGGBVCUIVRRBF-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
4
Targets
12
Activities
2
Assay Types
10
PK Parameters
20
Publications
5
Known Names
1
Indications
1
Mechanisms
Molecular Properties
404.5
MW (Da)
3.80
ALogP
3
HBA
0
HBD
63.7
PSA (Ų)
0.46
QED
0
Ro5 Violations
6
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1959 |
| Availability | Discontinued |
| Chirality | Racemic |
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
ATC Classification
M04AB02
sulfinpyrazone
Level 1: MUSCULO-SKELETAL SYSTEM
Level 2: ANTIGOUT PREPARATIONS
Activity Summary
IC50 9 meas. best 5.0
Ki 3 meas. best 9.3
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Nicotinate phosphoribosyltransferase CHEMBL4523354 | Ki | 9.3 | 9.3 | 0.5 | 1 |
| fMet-Leu-Phe receptor CHEMBL3359 | IC50 | 5.0 | 5.0 | 10000.0 | 1 |
| Bile salt export pump CHEMBL6020 | IC50 | 4.96 | 4.96 | 11000.0 | 1 |
| fMet-Leu-Phe receptor CHEMBL3359 | Ki | 4.84 | 4.84 | 14400.0 | 1 |
| Solute carrier family 22 member 12 CHEMBL6120 | IC50 | 4.0 | 4.0 | 100000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 0.34 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.1 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.34 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.34 | mL.min-1.kg-1 | Homo sapiens |
| Cmax | 44250.0 | nM | Homo sapiens |
| F | 80.0 | % | Homo sapiens |
| Fu | 0.017 | - | Homo sapiens |
| Fu | 0.017 | - | Homo sapiens |
| MRT | 5.9 | hr | Homo sapiens |
| T1/2 | 6.2 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Nicotinate phosphoribosyltransferase | Ki | = | 0.5 | nM | 9.3 | Inhibition of NAPRT (unknown origin) | - |
| fMet-Leu-Phe receptor | IC50 | = | 10000.0 | nM | 5.0 | Antagonist activity at FPR1 | 21486695 |
| Bile salt export pump | IC50 | = | 11000.0 | nM | 4.96 | Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell ... | 24799086 |
| fMet-Leu-Phe receptor | Ki | = | 14400.0 | nM | 4.84 | PubChem BioAssay. Dose Response Assay for Formylpeptide Receptor (FPR) Ligands a... | - |
| Solute carrier family 22 member 12 | IC50 | = | 100000.0 | nM | 4.0 | Inhibition of human URAT1-mediated urate uptake in HEK293 cells | 17325024 |
Literature References
Data from ChEMBL 36 via Core Engine