Assay Detail
Binding
CHEMBL839953
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In vitro inhibition constant against human Dipeptidyl peptidase IV
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 8.08 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | 4.0 | 1 | 9.22 |
| CHEMBL3350935 | — | — | 1 | 9.05 |
| CHEMBL3350934 | — | — | 1 | 8.85 |
| CHEMBL3350937 | — | — | 1 | 8.74 |
| CHEMBL3350936 | — | — | 1 | 8.68 |
| CHEMBL3350924 | — | — | 1 | 8.26 |
| CHEMBL3350920 | — | — | 1 | 8.15 |
| CHEMBL3350933 | — | — | 1 | 8.13 |
| CHEMBL3350926 | — | — | 1 | 8.10 |
| CHEMBL3350927 | — | — | 1 | 8.00 |
| CHEMBL3350928 | — | — | 1 | 8.00 |
| CHEMBL3350923 | — | — | 1 | 7.92 |
| CHEMBL3350925 | — | — | 1 | 7.68 |
| CHEMBL3350922 | — | — | 1 | 7.60 |
| CHEMBL3350921 | — | — | 1 | 7.51 |
| CHEMBL3350931 | — | — | 1 | 7.38 |
| CHEMBL3350930 | — | — | 1 | 7.24 |
| CHEMBL3350929 | — | — | 1 | 6.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL385517 | SAXAGLIPTIN ANHYDROUS | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3350935 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3350934 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3350937 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL3350936 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3350924 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL3350920 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL3350933 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL3350926 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL3350927 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3350928 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3350923 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3350925 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL3350922 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL3350921 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL3350931 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL3350930 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL3350929 | — | Ki | = | 143.0 | nM | 6.84 |