Compound Detail
CHEMBL1017
TELMISARTAN 💊 Approved Drug
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💊 Approved Drug
CCCc1nc2c(C)cc(-c3nc4ccccc4n3C)cc2n1Cc1ccc(-c2ccccc2C(=O)O)cc1
Basic Information
| ChEMBL ID | CHEMBL1017 |
| Name | TELMISARTAN |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | RMMXLENWKUUMAY-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
22
Targets
60
Activities
4
Assay Types
30
PK Parameters
20
Publications
23
Known Names
20
Indications
1
Mechanisms
Molecular Properties
514.6
MW (Da)
7.26
ALogP
5
HBA
1
HBD
72.9
PSA (Ų)
0.24
QED
2
Ro5 Violations
7
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1998 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Type-1 angiotensin II receptor antagonist | ANTAGONIST | Type-1 angiotensin II receptor | ✓ | ✓ |
Indications
Cardiovascular Diseases Diabetes Mellitus Hypertension Myocardial Infarction Stroke Albuminuria Diabetes Mellitus, Type 2 Diabetic Nephropathies Essential Hypertension Heart Diseases Kidney Diseases Kidney Failure, Chronic Lipid Metabolism Disorders Polycystic Kidney Diseases Severe Acute Respiratory Syndrome Severe Acute Respiratory Syndrome Alzheimer Disease HIV Infections HIV Infections Neuralgia
ATC Classification
C09CA07
telmisartan
Level 1: CARDIOVASCULAR SYSTEM
Level 2: AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
Drug Warnings
Black Box Warning
teratogenicity
Black Box Warning
cardiotoxicity
Activity Summary
IC50 33 meas. best 9.48
EC50 16 meas. best 6.16
Ki 10 meas. best 9.64
Kd 1 meas.
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Type-1 angiotensin II receptor A CHEMBL329 | Ki | 9.64 | 9.64 | 0.2 | 2 |
| Type-2 angiotensin II receptor CHEMBL4607 | IC50 | 9.48 | 9.48 | 0.3 | 1 |
| Type-1 angiotensin II receptor CHEMBL227 | IC50 | 9.31 | 8.663 | 0.5 | 10 |
| Unchecked CHEMBL612545 | Ki | 8.56 | 8.495 | 2.8 | 2 |
| Type-1 angiotensin II receptor B CHEMBL263 | IC50 | 8.52 | 8.52 | 3.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 8.42 | 5.8067 | 3.8 | 3 |
| Plasmodium berghei CHEMBL612653 | IC50 | 7.6 | 7.6 | 25.0 | 1 |
| Plasmodium CHEMBL4888483 | IC50 | 7.6 | 7.6 | 25.0 | 1 |
| Liver CHEMBL613642 | IC50 | 7.15 | 7.15 | 70.5 | 1 |
| Cytochrome P450 2J2 CHEMBL3491 | Ki | 7.0 | 6.86 | 100.0 | 2 |
| Cytochrome P450 2J2 CHEMBL3491 | IC50 | 6.38 | 6.3067 | 420.0 | 3 |
| Peroxisome proliferator-activated receptor gamma CHEMBL235 | EC50 | 6.16 | 5.5708 | 700.0 | 13 |
| Solute carrier organic anion transporter family member 1B3 CHEMBL1743121 | Ki | 6.02 | 6.02 | 960.0 | 1 |
| Solute carrier organic anion transporter family member 1B1 CHEMBL1697668 | Ki | 5.99 | 5.99 | 1030.0 | 1 |
| Peroxisome proliferator-activated receptor gamma CHEMBL235 | Ki | 5.97 | 5.97 | 1080.0 | 1 |
| Solute carrier organic anion transporter family member 1B3 CHEMBL1743121 | IC50 | 5.9 | 5.9 | 1258.9 | 1 |
| Plasmodium falciparum CHEMBL364 | IC50 | 5.79 | 5.79 | 1612.0 | 1 |
| Solute carrier organic anion transporter family member 1B1 CHEMBL1697668 | IC50 | 5.73 | 5.73 | 1862.1 | 1 |
| Glycine receptor subunit alpha-1 CHEMBL5845 | EC50 | 5.5 | 5.5 | 3200.0 | 1 |
| Peroxisome proliferator-activated receptor gamma CHEMBL2459 | EC50 | 5.39 | 5.39 | 4060.0 | 1 |
| Unchecked CHEMBL612545 | EC50 | 5.33 | 5.33 | 4700.0 | 1 |
| Cytochrome P450 2C9 CHEMBL3397 | IC50 | 5.32 | 5.32 | 4780.0 | 1 |
| Angiotensin-converting enzyme CHEMBL1808 | Ki | 5.22 | 5.22 | 6000.0 | 1 |
| Peroxisome proliferator-activated receptor gamma CHEMBL235 | IC50 | 4.91 | 4.91 | 12200.0 | 1 |
| Bile salt export pump CHEMBL6020 | IC50 | 4.79 | 4.79 | 16200.0 | 3 |
| Broad substrate specificity ATP-binding cassette transporter ABCG2 CHEMBL5393 | IC50 | 4.77 | 4.77 | 16900.0 | 1 |
| Multidrug and toxin extrusion protein 1 CHEMBL1743126 | IC50 | 4.75 | 4.75 | 17900.0 | 1 |
| ATP-binding cassette sub-family C member 4 CHEMBL1743128 | IC50 | 4.44 | 4.44 | 36000.0 | 1 |
| ATP-binding cassette sub-family C member 3 CHEMBL5918 | IC50 | 4.22 | 4.22 | 60000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 3010.9 | ng.hr.mL-1 | Homo sapiens |
| AUC | 3682.7 | ng.hr.mL-1 | Homo sapiens |
| AUC | 3231.4 | ng.hr.mL-1 | Homo sapiens |
| AUC | 3133.4 | ng.hr.mL-1 | Homo sapiens |
| AUC | 3399.7 | ng.hr.mL-1 | Homo sapiens |
| AUC | 2469.9 | ng.hr.mL-1 | Homo sapiens |
| AUC | 3677.2 | ng.hr.mL-1 | Homo sapiens |
| AUC | 1835.17 | ng.hr.mL-1 | Homo sapiens |
| CL | 8.4 | mL.min-1.kg-1 | Homo sapiens |
| CL | 8.3 | mL.min-1.kg-1 | Homo sapiens |
| CL | 8.4 | mL.min-1.kg-1 | Homo sapiens |
| CL | 8.4 | mL.min-1.kg-1 | Homo sapiens |
| CL | 3.98 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 3.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 245.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 163.33 | mL.min-1.kg-1 | Homo sapiens |
| CL | 283.33 | mL.min-1.kg-1 | Homo sapiens |
| CL | 231.67 | mL.min-1.kg-1 | Homo sapiens |
| CL | 243.33 | mL.min-1.kg-1 | Homo sapiens |
| CL | - | mL.min-1.kg-1 | Homo sapiens |
| CL | 8.4 | mL.min-1.kg-1 | Homo sapiens |
| CL | 20.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 21.7 | mL.min-1.g-1 | Homo sapiens |
| CL | - | - | Homo sapiens |
| CL | 17.8 | mL.min-1.kg-1 | Homo sapiens |
| CL | 8.4 | mL.min-1.kg-1 | Homo sapiens |
| CL | 9.93 | mL.min-1.kg-1 | Homo sapiens |
| CL | 9.93 | mL.min-1.kg-1 | Homo sapiens |
| CL | 298.33 | mL.min-1.kg-1 | Homo sapiens |
| CL | 195.0 | mL.min-1.kg-1 | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine