Assay Detail
Binding
CHEMBL2021179
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Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]AMG accumulation after 2 hrs by scintillation counting
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Ipragliflozin (ASP1941): a novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.01 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2018097 | — | — | 1 | 8.43 |
| CHEMBL2018096 | IPRAGLIFLOZIN | 4.0 | 1 | 8.13 |
| CHEMBL2018090 | — | — | 1 | 8.01 |
| CHEMBL2017954 | — | — | 1 | 8.00 |
| CHEMBL2018091 | — | — | 1 | 7.89 |
| CHEMBL2018095 | — | — | 1 | 7.85 |
| CHEMBL2018084 | — | — | 1 | 7.52 |
| CHEMBL2018092 | — | — | 1 | 7.33 |
| CHEMBL2017956 | — | — | 1 | 7.16 |
| CHEMBL2018094 | — | — | 1 | 7.12 |
| CHEMBL2018093 | — | — | 1 | 7.04 |
| CHEMBL2017955 | — | — | 1 | 7.00 |
| CHEMBL2018080 | — | — | 1 | 6.21 |
| CHEMBL2018087 | — | — | 1 | 6.19 |
| CHEMBL2018085 | — | — | 1 | 6.17 |
| CHEMBL2018088 | — | — | 1 | 5.64 |
| CHEMBL2018081 | — | — | 1 | 5.31 |
| CHEMBL2018086 | — | — | 1 | 5.20 |
| CHEMBL2018089 | — | — | 1 | - |
| CHEMBL2018083 | — | — | 1 | - |
| CHEMBL2018082 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2018097 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL2018096 | IPRAGLIFLOZIN | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL2018090 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL2017954 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2018091 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2018095 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2018084 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2018092 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2017956 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2018094 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL2018093 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL2017955 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2018080 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL2018087 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL2018085 | — | IC50 | = | 675.0 | nM | 6.17 |
| CHEMBL2018088 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL2018081 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL2018086 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL2018089 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2018083 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2018082 | — | IC50 | > | 100000.0 | nM | - |