Compound Detail
CHEMBL414357
EXENATIDE 💊 Approved Drug
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💊 Approved Drug
CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)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)CNC(=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](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O
Basic Information
| ChEMBL ID | CHEMBL414357 |
| Name | EXENATIDE |
| Phase | Approved |
| Structure Type | BOTH |
| InChI Key | HTQBXNHDCUEHJF-XWLPCZSASA-N |
| Therapeutic | ✓ Yes |
2
Targets
24
Activities
3
Assay Types
19
PK Parameters
20
Publications
21
Known Names
20
Indications
1
Mechanisms
Molecular Properties
4186.6
MW (Da)
Drug Information
| Molecule Type | Protein |
| First Approval | 2005 |
| 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 Coronary Disease Diabetes Mellitus, Type 1 Myocardial Infarction Myocardial Infarction Obesity Parkinson Disease Weight Loss Alcoholism Cerebral Small Vessel Diseases Hyperglycemia Ischemic Stroke Multiple System Atrophy Non-alcoholic Fatty Liver Disease Obesity, Morbid Polycystic Ovary Syndrome Prediabetic State Stroke Cocaine-Related Disorders
ATC Classification
A10BJ01
exenatide
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: DRUGS USED IN DIABETES
Drug Warnings
Black Box Warning
carcinogenicity
Activity Summary
EC50 18 meas. best 10.8
IC50 4 meas. best 9.85
Ki 2 meas. best 10.28
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Glucagon-like peptide 1 receptor CHEMBL1784 | EC50 | 10.8 | 8.709 | 0.0 | 10 |
| Glucagon-like peptide 1 receptor CHEMBL1784 | Ki | 10.28 | 10.16 | 0.1 | 2 |
| Glucagon-like peptide 1 receptor CHEMBL5862 | IC50 | 9.85 | 9.85 | 0.1 | 1 |
| Glucagon-like peptide 1 receptor CHEMBL1784 | IC50 | 9.4 | 8.9333 | 0.4 | 3 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 291.88 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 3153.07 | ng.hr.mL-1 | Rattus norvegicus |
| CL | 24.7 | mL.min-1.g-1 | Rattus norvegicus |
| Cmax | 5.0 | nM | Mus musculus |
| Cmax | 36.35 | nM | Rattus norvegicus |
| Cmax | 184.28 | nM | Rattus norvegicus |
| MRT | 1.24 | hr | Rattus norvegicus |
| MRT | 4.17 | hr | Rattus norvegicus |
| T1/2 | 0.55 | hr | Rattus norvegicus |
| T1/2 | 120.0 | hr | Homo sapiens |
| T1/2 | 2.82 | hr | Rattus norvegicus |
| T1/2 | 6.2 | hr | Rattus norvegicus |
| T1/2 | 2.4 | hr | Homo sapiens |
| T1/2 | 3.6 | hr | Rattus norvegicus |
| T1/2 | 4.34 | hr | Rattus norvegicus |
| T1/2 | 3.683 | hr | Rattus norvegicus |
| T1/2 | 2.4 | hr | Homo sapiens |
| Tmax | 0.63 | hr | Rattus norvegicus |
| Tmax | 0.8 | hr | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine