Compound Detail
CHEMBL817
TOLAZAMIDE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL817 |
| Name | TOLAZAMIDE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | OUDSBRTVNLOZBN-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
20
Publications
5
Known Names
2
Indications
1
Mechanisms
Molecular Properties
311.4
MW (Da)
1.77
ALogP
4
HBA
2
HBD
78.5
PSA (Ų)
0.89
QED
0
Ro5 Violations
3
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1966 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Sulfonylurea receptor 1, Kir6.2 blocker | BLOCKER | Sulfonylurea receptor 1, Kir6.2 | ✓ | ✓ |
Indications
Diabetes Mellitus Diabetes Mellitus, Type 2
ATC Classification
A10BB05
tolazamide
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: DRUGS USED IN DIABETES
Activity Summary
IC50 3 meas. best 5.29
Ki 1 meas.
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Polyunsaturated fatty acid lipoxygenase ALOX15 CHEMBL4358 | IC50 | 5.29 | 5.29 | 5106.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 5.16 | 5.16 | 6976.9 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Polyunsaturated fatty acid lipoxygenase ALOX15 | IC50 | = | 5106.0 | nM | 5.29 | DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) | - |
| Unchecked | IC50 | = | 6976.89 | nM | 5.16 | PubChem BioAssay. insulin secretion from INS-1E cells in the presence of 5 mM gl... | - |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.6019/CHEMBL3885881 | Rattus norvegicus | 270 |
| - | 10.5281/zenodo.13943903 | ADMET | 89 |
| 31158845 | 10.1038/s41586-019-1291-3 | ADMET | 62 |
| 22194678 | 10.1371/journal.pcbi.1002310 | Hepatotoxicity | 14 |
| 15646539 | 10.1016/s0399-8320(04)95062-2 | Unchecked | 11 |
| 15646539 | 10.1016/s0399-8320(04)95062-2 | NON-PROTEIN TARGET | 8 |
| 7310831 | 10.1021/jm00144a031 | Rattus norvegicus | 8 |
| 7069714 | 10.1021/jm00346a006 | Rattus norvegicus | 7 |
| 7310831 | 10.1021/jm00144a031 | Cavia porcellus | 4 |
| 7069714 | 10.1021/jm00346a006 | Cavia porcellus | 4 |
| - | 10.6019/CHEMBL3301361 | No relevant target | 3 |
| 20014752 | 10.1021/tx900326k | Hepatotoxicity | 3 |
| 15801837 | 10.1021/jm049227l | Albumin | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 7310831 | 10.1021/jm00144a031 | Mus musculus | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Gamma-aminobutyric acid receptor subunit alpha-1 | 2 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| 7069714 | 10.1021/jm00346a006 | Mus musculus | 2 |
| 21601448 | 10.1016/j.bmcl.2011.04.133 | No relevant target | 2 |
| 7069714 | 10.1021/jm00346a006 | Monkey | 2 |
Data from ChEMBL 36 via Core Engine