Compound Detail
CHEMBL404271
ACARBOSE 💊 Approved Drug
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💊 Approved Drug
C[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O[C@H]3[C@H](O)[C@@H](O)C(O)O[C@@H]3CO)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1N[C@H]1C=C(CO)[C@@H](O)[C@H](O)[C@H]1O
Basic Information
| ChEMBL ID | CHEMBL404271 |
| Name | ACARBOSE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | XUFXOAAUWZOOIT-UGEKTDRHSA-N |
| Therapeutic | ✓ Yes |
14
Targets
386
Activities
2
Assay Types
7
PK Parameters
20
Publications
8
Known Names
15
Indications
2
Mechanisms
Molecular Properties
645.6
MW (Da)
-8.56
ALogP
19
HBA
14
HBD
321.2
PSA (Ų)
0.10
QED
3
Ro5 Violations
9
Rot. Bonds
Drug Information
| Molecule Type | Oligosaccharide |
| First Approval | 1995 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Pancreatic alpha-amylase inhibitor | INHIBITOR | Pancreatic alpha-amylase | ✓ | ✓ |
| Maltase-glucoamylase inhibitor | INHIBITOR | Maltase-glucoamylase | ✓ | ✓ |
Indications
Diabetes Mellitus Diabetes Mellitus, Type 2 Atherosclerosis Coronary Disease Diabetes, Gestational Hypercholesterolemia Hypertension Metabolic Diseases Metabolic Syndrome Aging Kidney Neoplasms Non-alcoholic Fatty Liver Disease Hypotension, Orthostatic Nesidioblastosis Obesity
ATC Classification
A10BF01
acarbose
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: DRUGS USED IN DIABETES
Activity Summary
IC50 366 meas. best 7.48
Ki 20 meas. best 8.05
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Unchecked CHEMBL612545 | Ki | 8.05 | 5.65 | 9.0 | 9 |
| Unchecked CHEMBL612545 | IC50 | 7.48 | 5.0252 | 33.0 | 87 |
| Alpha amylase CHEMBL6066863 | IC50 | 6.92 | 5.5393 | 120.0 | 15 |
| Acidic alpha-glucosidase CHEMBL3513 | IC50 | 6.8 | 5.7359 | 160.0 | 17 |
| Alpha-glucosidase CHEMBL4412 | Ki | 6.47 | 6.47 | 340.0 | 1 |
| Sucrase-isomaltase, intestinal CHEMBL3114 | IC50 | 6.4 | 5.5647 | 400.0 | 17 |
| Maltase-glucoamylase CHEMBL2074 | IC50 | 6.38 | 4.7438 | 421.0 | 8 |
| Alpha-amylase 1A CHEMBL2478 | IC50 | 6.37 | 6.2233 | 430.0 | 3 |
| Alpha glucosidase CHEMBL3833502 | Ki | 6.36 | 6.36 | 440.0 | 1 |
| Alpha-glucosidase CHEMBL5291954 | IC50 | 5.97 | 4.8259 | 1060.3 | 22 |
| Pancreatic alpha-amylase CHEMBL5730 | IC50 | 5.87 | 5.0657 | 1353.0 | 7 |
| Alpha glucosidase CHEMBL3833502 | IC50 | 5.7 | 4.9375 | 2000.0 | 4 |
| Acidic alpha-glucosidase CHEMBL3513 | Ki | 5.46 | 5.46 | 3500.0 | 1 |
| Lysosomal alpha-glucosidase CHEMBL2608 | IC50 | 5.3 | 4.84 | 5000.0 | 2 |
| Alpha-amylase CHEMBL3308960 | IC50 | 5.29 | 4.8775 | 5080.0 | 4 |
| SARS-CoV-2 CHEMBL4303835 | IC50 | 4.66 | 4.66 | 21980.0 | 1 |
| Oligo-1,6-glucosidase IMA1 CHEMBL5848 | IC50 | 4.42 | 4.42 | 38250.0 | 1 |
| Alpha-amylase CHEMBL3308960 | Ki | 4.21 | 4.21 | 62400.0 | 1 |
| Alpha amylase CHEMBL6066863 | Ki | 4.21 | 4.21 | 62000.0 | 1 |
| Alpha-glucosidase CHEMBL5291954 | Ki | 4.04 | 4.04 | 90700.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 3343000.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 2232000.0 | ng.hr.mL-1 | Mus musculus |
| CL | 2.2 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.1 | mL.min-1.kg-1 | Homo sapiens |
| CL | 2.2 | mL.min-1.kg-1 | Homo sapiens |
| MRT | 2.4 | hr | Homo sapiens |
| T1/2 | 2.7 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine