Compound Detail
CHEMBL1093423
LUSEOGLIFLOZIN 🧪 Phase II
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🧪 Phase II
CCOc1ccc(Cc2cc([C@@H]3S[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)c(OC)cc2C)cc1
Basic Information
| ChEMBL ID | CHEMBL1093423 |
| Name | LUSEOGLIFLOZIN |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | WHSOLWOTCHFFBK-ZQGJOIPISA-N |
2
Targets
8
Activities
2
Assay Types
12
PK Parameters
20
Publications
6
Known Names
1
Indications
Molecular Properties
434.6
MW (Da)
2.22
ALogP
7
HBA
4
HBD
99.4
PSA (Ų)
0.53
QED
0
Ro5 Violations
7
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Indications
Diabetes Mellitus
ATC Classification
A10BK07
luseogliflozin
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: DRUGS USED IN DIABETES
Activity Summary
IC50 6 meas. best 8.65
EC50 2 meas. best 8.64
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Sodium/glucose cotransporter 2 CHEMBL3884 | IC50 | 8.65 | 8.6475 | 2.3 | 4 |
| Sodium/glucose cotransporter 2 CHEMBL3884 | EC50 | 8.64 | 8.64 | 2.3 | 1 |
| Sodium/glucose cotransporter 1 CHEMBL4979 | EC50 | 5.4 | 5.4 | 4000.0 | 1 |
| Sodium/glucose cotransporter 1 CHEMBL4979 | IC50 | 5.4 | 5.4 | 3990.0 | 2 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 36.3 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 3.19 | mL.min-1.kg-1 | Canis lupus familiaris |
| Cmax | 2103.33 | nM | Canis lupus familiaris |
| Cmax | 82.15 | nM | Rattus norvegicus |
| F | 35.3 | % | Rattus norvegicus |
| F | 92.7 | % | Canis lupus familiaris |
| Fu | 0.038 | - | Homo sapiens |
| T1/2 | 2.93 | hr | Rattus norvegicus |
| T1/2 | 4.07 | hr | Canis lupus familiaris |
| T1/2 | 7.0 | hr | Homo sapiens |
| Tmax | 0.67 | hr | Canis lupus familiaris |
| Tmax | 0.5 | hr | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Sodium/glucose cotransporter 2 | IC50 | = | 2.26 | nM | 8.65 | Inhibition of human SGLT2 expressed in CHOK1 cells assessed as inhibition of glu... | 20302302 |
| Sodium/glucose cotransporter 2 | IC50 | = | 2.26 | nM | 8.65 | Inhibition of human SGLT2 | 31630053 |
| Sodium/glucose cotransporter 2 | IC50 | = | 2.26 | nM | 8.65 | Inhibition OF SGLT2 (unknown origin) | 31630053 |
| Sodium/glucose cotransporter 2 | EC50 | = | 2.3 | nM | 8.64 | Inhibition of SGLT2 (unknown origin) | 31930920 |
| Sodium/glucose cotransporter 2 | IC50 | = | 2.3 | nM | 8.64 | Inhibition of SGLT2 (unknown origin) | 29954682 |
| Sodium/glucose cotransporter 1 | EC50 | = | 4000.0 | nM | 5.4 | Inhibition of SGLT1 (unknown origin) | 31930920 |
| Sodium/glucose cotransporter 1 | IC50 | = | 3990.0 | nM | 5.4 | Inhibition of human SGLT1 expressed in CHOK1 cells assessed as inhibition of glu... | 20302302 |
| Sodium/glucose cotransporter 1 | IC50 | = | 3990.0 | nM | 5.4 | Inhibition of human SGLT1 | 31630053 |
Literature References
Data from ChEMBL 36 via Core Engine