Molecule Details
| InChIKey | PSIFNNKUMBGKDQ-UHFFFAOYSA-N |
|---|---|
| Compound Name | Losartan |
| Canonical SMILES | CCCCc1nc(Cl)c(CO)n1Cc1ccc(-c2ccccc2-c2nnn[nH]2)cc1 |
| Clinical Status | Data-mined Candidate |
| Targets (Human+Pathogen) | 5 |
| Pfam Stratification | Cross-Family |
| Avg pChEMBL | 7.29 |
| Source | ChEMBL;BindingDB |
2D Structure
Activity Profile
DrugBank Annotations
| DrugBank ID | DB00678 |
|---|---|
| Drug Name | Losartan |
| CAS Number | 114798-26-4 |
| Groups | approved investigational |
| ATC Codes | C09CA01 C09DA01 C09DB06 |
| Description | Losartan is an angiotensin II receptor blocker (ARB) used to treat hypertension.[L7423] Angiotensin-converting enzyme (ACE) inhibitors are used for a similar indication but are associated with a cough.[L7423] When patients with ACE inhibitor associated coughs are switched to ARBs like losartan, they... |
Categories: Agents Acting on the Renin-Angiotensin System Agents causing angioedema Agents causing hyperkalemia Angiotensin 2 Receptor Blocker Angiotensin II Type 1 Receptor Blockers Angiotensin II Type 2 Receptor Blockers Angiotensin II receptor antagonists Angiotensin II receptor blockers (ARBs) and calcium channel blockers Angiotensin II receptor blockers (ARBs) and diuretics Angiotensin II receptor blockers (ARBs), plain Angiotensin Receptor Antagonists Antiarrhythmic agents Antihypertensive Agents Antihypertensive Agents Indicated for Hypertension BSEP/ABCB11 Substrates Benzene Derivatives Biphenyl Compounds Cardiovascular Agents Cytochrome P-450 CYP2C19 Inhibitors Cytochrome P-450 CYP2C19 inhibitors (strength unknown) Cytochrome P-450 CYP2C8 Inhibitors Cytochrome P-450 CYP2C8 Inhibitors (strength unknown) Cytochrome P-450 CYP2C9 Substrates Cytochrome P-450 CYP3A Inhibitors Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Inhibitors Cytochrome P-450 CYP3A4 Inhibitors (strength unknown) Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Drugs causing inadvertant photosensitivity Hypotensive Agents Imidazoles OAT1/SLC22A6 inhibitors P-glycoprotein inhibitors P-glycoprotein substrates Photosensitizing Agents Tetrazoles UGT1A1 Substrates UGT1A3 substrates UGT2B17 substrates UGT2B7 substrates
Cross-references: BindingDB: 82258 ChEBI: 6541 CHEMBL191 ChemSpider: 3824 Drugs Product Database (DPD): 144 Guide to Pharmacology: 590 IUPHAR: 590 C07072 D08146 PDB: LSN PharmGKB: PA450268 PubChem:3961 PubChem:46506538 RxCUI: 52175 Therapeutic Targets Database: DAP000523 Wikipedia: Losartan ZINC: ZINC000003873160
Target Activities (5)
| Target | Gene | Organism | Category | Pfam | pChEMBL | Type | Source |
|---|---|---|---|---|---|---|---|
| P50052 | AGTR2 | Homo sapiens | Human | PF00001 | 8.1 | IC50 | ChEMBL;BindingDB |
| P30556 | AGTR1 | Homo sapiens | Human | PF00001 | 7.9 | IC50 | ChEMBL;BindingDB |
| P12821 | ACE | Homo sapiens | Human | PF01401 | 7.7 | IC50 | ChEMBL;BindingDB |
| Q9Y6L6 | SLCO1B1 | Homo sapiens | Human | PF07648 PF03137 | 6.7 | IC50 | ChEMBL;BindingDB |
| Q9NPD5 | SLCO1B3 | Homo sapiens | Human | PF07648 PF03137 | 6.0 | Ki | ChEMBL;BindingDB |
DrugBank Target Actions (19)
| Target | Gene | Target Name | Action | Type |
|---|---|---|---|---|
| P02768 | ALB | Albumin | substrate | carriers |
| P08684 | CYP3A4 | Cytochrome P450 3A4 | inhibitor | enzymes |
| P10632 | CYP2C8 | Cytochrome P450 2C8 | inhibitor | enzymes |
| P33261 | CYP2C19 | Cytochrome P450 2C19 | inhibitor | enzymes |
| O75795 | O75795 | UDP-glucuronosyltransferase 2B17 | substrate | enzymes |
| P08684 | CYP3A4 | Cytochrome P450 3A4 | substrate | enzymes |
| P11712 | CYP2C9 | Cytochrome P450 2C9 | substrate | enzymes |
| P16662 | UGT2B7 | UDP-glucuronosyltransferase 2B7 | substrate | enzymes |
| P22309 | UGT1A1 | UDP-glucuronosyltransferase 1A1 | substrate | enzymes |
| P35503 | P35503 | UDP-glucuronosyltransferase 1A3 | substrate | enzymes |
| Q9HAW8 | Q9HAW8 | UDP-glucuronosyltransferase 1A10 | substrate | enzymes |
| P30556 | AGTR1 | Type-1 angiotensin II receptor | antagonist | targets |
| P19235 | P19235 | Erythropoietin receptor | stimulator | targets |
| P08183 | ABCB1 | ATP-dependent translocase ABCB1 | inhibitor | transporters |
| Q4U2R8 | SLC22A6 | Solute carrier family 22 member 6 | inhibitor | transporters |
| Q96S37 | SLC22A12 | Solute carrier family 22 member 12 | inhibitor | transporters |
| Q9NRM0 | Q9NRM0 | Solute carrier family 2, facilitated glucose transporter member 9 | inhibitor | transporters |
| O95342 | ABCB11 | Bile salt export pump | substrate | transporters |
| P08183 | ABCB1 | ATP-dependent translocase ABCB1 | substrate | transporters |