Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL414357

EXENATIDE
💊 Approved Drug
Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
💊 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

Known Names

AC 2993 AC-002993 AC-2993 AC-2993A AC-2993LAR AC002993 AC2993 AC2993A Bydureon Bydureon bcise Bydureon pen Byetta +9 more
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

Routes of Administration

Parenteral

Flags

Black Box Warning
USAN Stem -tide
USAN Year 2003

Extended Properties

Molecular Formula C184H282N50O60S
MW 4186.64

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
Country: United States

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

Target Type Rel. Value Units pChEMBL Assay PubMed
Glucagon-like peptide 1 receptor EC50 = 0.016 nM 10.8 Agonist activity at human GLP-1R expressed in HEK293 cells assessed as stimulati... 33449689
Glucagon-like peptide 1 receptor Ki = 0.053 nM 10.28 Displacement of [3H]PF-06883365 from FAP-tagged human GLP-1R expressed in CHO ce... 35647711
Glucagon-like peptide 1 receptor EC50 = 0.061 nM 10.21 Agonist activity at human GLP-1R expressed in CHO-K1 cells assessed as cAMP accu... 35647711
Glucagon-like peptide 1 receptor Ki = 0.092 nM 10.04 Displacement of [125I]GLP-1 from FAP-tagged human GLP-1R expressed in CHO cells ... 35647711
Glucagon-like peptide 1 receptor EC50 = 0.1 nM 10.0 Agonist activity at human GLP-1 receptor expressed in CHO cells assessed as incr... 20576431
Glucagon-like peptide 1 receptor EC50 = 0.11 nM 9.96 Agonist activity at GLP-1R (unknown origin) expressed in candidate selection CHO... 35647711
Glucagon-like peptide 1 receptor IC50 = 0.14 nM 9.85 Displacement of [125I]exendin-4 from GLP1 receptor in rat RINm5F cells after 2 h... 19827752
Glucagon-like peptide 1 receptor IC50 = 0.3981 nM 9.4 Binding affinity to human GLP-1R expressed in CHO cells coexpressing beta-arrest... 35984914
Glucagon-like peptide 1 receptor EC50 = 0.6 nM 9.22 Agonist activity at FAP-tagged human GLP-1R expressed in HEK293 cells assessed a... 35647711
Glucagon-like peptide 1 receptor IC50 = 0.66 nM 9.18 Displacement of [125I]GLP1 from human GLP1R expressed in CHOK1 cells 18412318
Glucagon-like peptide 1 receptor IC50 = 5.98 nM 8.22 Displacement of GLP-1-red from human GLP-1R expressed in CHO-K1 cells by fluores... 33449689
Glucagon-like peptide 1 receptor EC50 = 9.0 nM 8.05 Agonist activity at human GLP-1R expressed in PathHunter CHO-K1 GLP1R beta-arres... 35647711
Glucagon-like peptide 1 receptor EC50 = 14.0 nM 7.85 Agonist activity at human GLP-1R expressed in PathHunter CHO-K1 GLP1R beta-arres... 35647711
Glucagon-like peptide 1 receptor EC50 = 25.12 nM 7.6 Agonist activity at human GLP-1R assessed as increase in ERK1/2 phosphorylation ... 35984914
Glucagon-like peptide 1 receptor EC50 = 50.12 nM 7.3 Agonist activity at human GLP-1R expressed in CHO cells coexpressing beta-arrest... 35984914
Glucagon-like peptide 1 receptor EC50 = 794.33 nM 6.1 Agonist activity at human GLP-1R expressed in CHO cells coexpressing beta-arrest... 35984914

Literature References

PubMed DOI Target Context # Activities
35647711 10.1021/acs.jmedchem.1c01856 Glucagon-like peptide 1 receptor 12
31471103 10.1016/j.bmc.2019.115070 Mus musculus 9
35984914 10.1021/acs.jmedchem.2c00653 Glucagon-like peptide 1 receptor 9
24308627 10.1021/jm4017448 Rattus norvegicus 9
19827752 10.1021/jm901153x Mus musculus 7
19827752 10.1021/jm901153x Rattus norvegicus 7
24384551 10.1016/j.ejmech.2013.11.043 Mus musculus 6
23743288 10.1016/j.bmcl.2013.05.022 Homo sapiens 5
30878191 10.1016/j.bmc.2019.03.014 Mus musculus 5
29673717 10.1016/j.bmc.2018.04.022 Mus musculus 4
19702274 10.1021/jm900752a Mus musculus 4
24308627 10.1021/jm4017448 Mus musculus 4
17339113 10.1016/j.bmc.2007.02.029 Unchecked 3
33449689 10.1021/acs.jmedchem.0c01783 ADMET 3
30878191 10.1016/j.bmc.2019.03.014 INS1 3
33449689 10.1021/acs.jmedchem.0c01783 Unchecked 3
29673717 10.1016/j.bmc.2018.04.022 Rattus norvegicus 3
39254428 10.1021/acs.jmedchem.4c01553 Amyloid-beta precursor protein 3
29673717 10.1016/j.bmc.2018.04.022 INS1 2
18412318 10.1021/jm701522b Glucagon-like peptide 1 receptor 2

Data from ChEMBL 36 via Core Engine