Compound Detail
CHEMBL4084119
LIRAGLUTIDE 💊 Approved Drug
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💊 Approved Drug
CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)O)C(C)C)[C@@H](C)CC)C(=O)O
Basic Information
| ChEMBL ID | CHEMBL4084119 |
| Name | LIRAGLUTIDE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | YSDQQAXHVYUZIW-QCIJIYAXSA-N |
| Therapeutic | ✓ Yes |
2
Targets
16
Activities
4
Assay Types
19
PK Parameters
20
Publications
13
Known Names
20
Indications
1
Mechanisms
Molecular Properties
3751.3
MW (Da)
Drug Information
| Molecule Type | Protein |
| First Approval | 2009 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Glucagon-like peptide 1 receptor agonist | AGONIST | Glucagon-like peptide 1 receptor | ✓ | ✓ |
Indications
Diabetes Mellitus Diabetes Mellitus, Type 2 Diabetes Mellitus, Type 2 Obesity Overweight Bipolar Disorder Delirium Depressive Disorder, Major Diabetes Mellitus, Type 1 Diabetic Nephropathies Feeding and Eating Disorders Glucose Intolerance Hyperglycemia Metabolic Syndrome Nutrition Disorders Polycystic Ovary Syndrome Prediabetic State Weight Loss Alzheimer Disease Heart Failure
ATC Classification
A10BJ02
liraglutide
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: DRUGS USED IN DIABETES
Drug Warnings
Black Box Warning
carcinogenicity
Activity Summary
EC50 10 meas. best 10.2
IC50 3 meas. best 9.96
Ki 2 meas. best 8.36
Kd 1 meas. best 5.2
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Glucagon-like peptide 1 receptor CHEMBL1784 | EC50 | 10.2 | 8.8113 | 0.1 | 8 |
| Glucagon-like peptide 1 receptor CHEMBL1784 | IC50 | 9.96 | 9.14 | 0.1 | 2 |
| Glucagon-like peptide 1 receptor CHEMBL1784 | Ki | 8.36 | 8.28 | 4.4 | 2 |
| MUS81-ECE1 CHEMBL5465380 | IC50 | 5.93 | 5.93 | 1170.0 | 1 |
| Glucagon-like peptide 1 receptor CHEMBL1784 | Kd | 5.2 | 5.2 | 6270.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 18073.59 | ng.hr.mL-1 | Rattus norvegicus |
| CL | 0.06333 | mL.min-1.kg-1 | Sus scrofa |
| Cmax | 240.43 | nM | Rattus norvegicus |
| F | 66.0 | % | Sus scrofa |
| Ka | 1.82 | 10^3(1/Ms) | Homo sapiens |
| MRT | 18.34 | hr | Rattus norvegicus |
| MRT | 23.0 | hr | Sus scrofa |
| T1/2 | 264.0 | hr | Homo sapiens |
| T1/2 | 12.54 | hr | Rattus norvegicus |
| T1/2 | 17.1 | hr | Rattus norvegicus |
| T1/2 | 12.4 | hr | Sus scrofa |
| T1/2 | 13.93 | hr | Rattus norvegicus |
| T1/2 | 20.0 | hr | Sus scrofa |
| T1/2 | 25.0 | hr | Sus scrofa |
| T1/2 | 19.0 | hr | Sus scrofa |
| T1/2 | 21.0 | hr | Sus scrofa |
| Tmax | 1.51 | hr | Rattus norvegicus |
| Tmax | 7.0 | hr | Sus scrofa |
| Vd | 0.0674 | L.kg-1 | Sus scrofa |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine