Compound Detail
CHEMBL429910
DAPAGLIFLOZIN 💊 Approved Drug
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💊 Approved Drug
CCOc1ccc(Cc2cc([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)ccc2Cl)cc1
Basic Information
| ChEMBL ID | CHEMBL429910 |
| Name | DAPAGLIFLOZIN |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | JVHXJTBJCFBINQ-ADAARDCZSA-N |
| Therapeutic | ✓ Yes |
4
Targets
70
Activities
2
Assay Types
30
PK Parameters
20
Publications
11
Known Names
20
Indications
1
Mechanisms
Molecular Properties
408.9
MW (Da)
1.84
ALogP
6
HBA
4
HBD
99.4
PSA (Ų)
0.58
QED
0
Ro5 Violations
6
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2012 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Sodium/glucose cotransporter 2 inhibitor | INHIBITOR | Sodium/glucose cotransporter 2 | ✓ | ✓ |
Indications
Diabetes Mellitus Diabetes Mellitus, Type 2 Heart Failure Renal Insufficiency, Chronic Acute Kidney Injury Atrial Fibrillation Coronary Disease Diabetes Mellitus, Type 1 Diabetic Retinopathy Fatty Liver Glomerulonephritis, IGA Insulin Resistance Kidney Failure, Chronic Non-alcoholic Fatty Liver Disease Polycystic Ovary Syndrome Renal Insufficiency Severe Acute Respiratory Syndrome ST Elevation Myocardial Infarction Albuminuria Amyloidosis, Familial
ATC Classification
A10BK01
dapagliflozin
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: DRUGS USED IN DIABETES
Activity Summary
IC50 57 meas. best 9.31
EC50 13 meas. best 8.96
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Sodium/glucose cotransporter 2 CHEMBL3884 | IC50 | 9.31 | 8.7997 | 0.5 | 36 |
| Sodium/glucose cotransporter 2 CHEMBL3884 | EC50 | 8.96 | 8.7867 | 1.1 | 6 |
| Sodium/glucose cotransporter 2 CHEMBL4316 | EC50 | 8.52 | 8.52 | 3.0 | 2 |
| Sodium/glucose cotransporter 1 CHEMBL4979 | IC50 | 6.43 | 5.9375 | 370.0 | 20 |
| Sodium/myo-inositol cotransporter 2 CHEMBL1744524 | IC50 | 6.42 | 6.42 | 380.0 | 1 |
| Sodium/glucose cotransporter 1 CHEMBL4979 | EC50 | 6.37 | 6.076 | 428.5 | 5 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 11658.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 3011.2 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 13313.3 | ng.hr.mL-1 | Rattus norvegicus |
| CL | 4.8 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 6.0 | ml/min | Homo sapiens |
| CL | 10.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 1.5 | mL.min-1.kg-1 | Canis lupus familiaris |
| CL | 0.08 | mL.min-1.kg-1 | Rattus norvegicus |
| Cmax | 1467.42 | nM | Rattus norvegicus |
| Cmax | 26169.05 | nM | Canis lupus familiaris |
| Cmax | 6114.26 | nM | Rattus norvegicus |
| Cmax | 6114.26 | nM | Rattus norvegicus |
| Cmax | 3920.47 | nM | Rattus norvegicus |
| Cmax | 3186.75 | nM | Rattus norvegicus |
| Cmax | 6114.26 | nM | Rattus norvegicus |
| F | 84.0 | % | Rattus norvegicus |
| F | 100.0 | % | Rattus norvegicus |
| F | 83.0 | % | Canis lupus familiaris |
| F | 88.42 | % | Rattus norvegicus |
| F | 88.0 | % | Rattus norvegicus |
| F | 88.4 | % | Rattus norvegicus |
| Fu | 0.04 | - | Homo sapiens |
| Fu | 0.03 | - | Rattus norvegicus |
| Fu | 0.085 | - | Homo sapiens |
| T1/2 | 4.6 | hr | Rattus norvegicus |
| T1/2 | 7.4 | hr | Canis lupus familiaris |
| T1/2 | 3.0 | hr | Macaca mulatta |
| T1/2 | 15.0 | hr | Homo sapiens |
| T1/2 | 4.4 | hr | Rattus norvegicus |
| T1/2 | 7.4 | hr | Canis lupus familiaris |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine