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

CHEMBL1561

MIGLITOL
💊 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
OCCN1C[C@H](O)[C@@H](O)[C@H](O)[C@H]1CO

Basic Information

ChEMBL ID CHEMBL1561
Name MIGLITOL
Phase Approved
Structure Type MOL
InChI Key IBAQFPQHRJAVAV-ULAWRXDQSA-N
Therapeutic ✓ Yes

Known Names

BAY M 1099 BAY-M-1099 Diastabol Glyset Miglitol NSC-758702
13
Targets
69
Activities
3
Assay Types
8
PK Parameters
20
Publications
6
Known Names
3
Indications
2
Mechanisms

Molecular Properties

207.2
MW (Da)
-3.26
ALogP
6
HBA
5
HBD
104.4
PSA (Ų)
0.33
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 1996
Availability Prescription
Chirality Single Enantiomer

Routes of Administration

Oral

Flags

Natural Product
USAN Year 1990

Extended Properties

Molecular Formula C8H17NO5
MW 207.23
Aromatic Rings 0
Heavy Atoms 14
NP-Likeness 1.65

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Maltase-glucoamylase inhibitor INHIBITOR Maltase-glucoamylase
Lysosomal alpha-glucosidase inhibitor INHIBITOR Lysosomal alpha-glucosidase

Indications

Diabetes Mellitus Diabetes Mellitus, Type 2 Diabetes Mellitus, Type 1

ATC Classification

A10BF02
miglitol
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: DRUGS USED IN DIABETES

Activity Summary

IC50 50 meas. best 7.3
Ki 17 meas. best 7.55
Kd 2 meas. best 4.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 7.55 6.2315 28.0 13
Unchecked
CHEMBL612545
IC50 7.3 6.3163 50.0 8
Sucrase-isomaltase, intestinal
CHEMBL3114
IC50 6.96 5.582 110.0 10
Lysosomal alpha-glucosidase
CHEMBL2608
IC50 6.46 6.0533 350.0 3
Glycogen debranching enzyme
CHEMBL5273
IC50 6.41 6.41 390.0 1
Acidic alpha-glucosidase
CHEMBL3513
Ki 6.34 6.34 460.0 1
Sucrase-isomaltase, intestinal
CHEMBL2748
IC50 6.3 6.3 500.0 1
Acidic alpha-glucosidase
CHEMBL3513
IC50 6.23 5.975 590.0 4
Maltase-glucoamylase
CHEMBL2074
Ki 6.0 6.0 1000.0 1
Maltase-glucoamylase
CHEMBL2074
IC50 5.43 5.36 3700.0 3
Unchecked
CHEMBL612545
Kd 4.68 4.68 20640.0 1
Alpha-glucosidase
CHEMBL5291954
IC50 4.46 4.46 34500.0 1
Lactase/phlorizin hydrolase
CHEMBL1075131
IC50 4.3 4.3 50000.0 1
Alpha-glucosidase
CHEMBL3435
IC50 4.24 4.24 57140.0 1
Alpha-mannosidase
CHEMBL3392945
IC50 4.12 4.12 75880.0 1
Lysosomal acid glucosylceramidase
CHEMBL2179
IC50 4.08 4.08 84000.0 1
Beta-galactosidase
CHEMBL3482
Ki 4.0 4.0 100000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 1.7 mL.min-1.kg-1 Homo sapiens
CL 1.7 mL.min-1.kg-1 Homo sapiens
CL - mL.min-1.kg-1 Homo sapiens
CL 1.7 mL.min-1.kg-1 Homo sapiens
Fu 1.0 - Homo sapiens
Fu 1.0 - Homo sapiens
MRT 2.7 hr Homo sapiens
T1/2 2.3 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Ki = 28.0 nM 7.55 Inhibition of rice alpha-glucosidase pre-incubated for 1 hr followed by p-nitrop... 28751199
Unchecked IC50 = 50.0 nM 7.3 Inhibition of rice alpha-glucosidase pre-incubated for 1 hr followed by p-nitrop... 28751199
Unchecked Ki = 60.0 nM 7.22 Inhibition of rice alpha-glucosidase using 10 mM p-nitrophenyl-alpha-D-glucopyra... 26375725
Unchecked IC50 = 100.0 nM 7.0 Inhibition of rice alpha-glucosidase using 10 mM p-nitrophenyl-alpha-D-glucopyra... 26375725
Unchecked IC50 = 99.0 nM 7.0 Inhibition of rice alpha-glucosidase assessed as reduction in production of D-gl... 27956035
Sucrase-isomaltase, intestinal IC50 = 110.0 nM 6.96 Inhibition of rat intestinal brush border membrane sucrase 18595718
Unchecked Ki = 130.0 nM 6.89 Inhibition of mouse his-tagged ctSI expressed in Sf9 cells assessed as amount of... 21669536
Unchecked Ki = 148.0 nM 6.83 Inhibition of human ntSI expressed in Drosophila S2 cells assessed as amount of ... 21669536
Unchecked Ki = 180.0 nM 6.75 Inhibition of rice alpha-glucosidase by Lineweaver-Burk plot analysis 35931006
Unchecked Ki = 180.0 nM 6.75 Inhibition of rice Alpha-glucosidase incubated for 10 mins by Lineweaver-Burk pl... 38504504
Unchecked Ki = 211.0 nM 6.68 Inhibition of mouse his-tagged ctMGAM-N2 expressed in Sf9 cells assessed as amou... 21669536
Unchecked Ki = 230.0 nM 6.64 Inhibition of mouse his-tagged ctMGAM-N20 expressed in Sf9 cells assessed as amo... 21669536
Lysosomal alpha-glucosidase IC50 = 350.0 nM 6.46 Inhibition of human lysosomal alpha-glucosidase 18595718
Unchecked IC50 = 390.0 nM 6.41 Inhibition of alpha-glucosidase (unknown origin) 36680985
Glycogen debranching enzyme IC50 = 390.0 nM 6.41 Inhibition of rabbit muscle amylo-1,6-glucosidase 18595718
Sucrase-isomaltase, intestinal IC50 = 430.0 nM 6.37 Inhibition of rat small intestinal sucrase using sucrose as substrate incubated ... 27325449
Acidic alpha-glucosidase Ki = 460.0 nM 6.34 Competitive inhibition of rat intestinal maltase by Lineweaver-Burk plot analysi... 23106358
Sucrase-isomaltase, intestinal IC50 = 500.0 nM 6.3 Inhibition of sucrase by HPLC 20000679
Acidic alpha-glucosidase IC50 = 590.0 nM 6.23 Inhibition of Wistar rat small intestine maltase after 30 mins 21185187
Unchecked IC50 = 590.0 nM 6.23 Inhibition of rat small intestinal brush border membrane maltase assessed as red... 27956035

Literature References

Data from ChEMBL 36 via Core Engine