Assay Detail
Binding
CHEMBL2149801
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Inhibition of DPP4 in rat plasma using GLY-Pro-MCA as substrate after 60 mins by fluorescence assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 8.83 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2147704 | — | — | 1 | 9.74 |
| CHEMBL2147703 | — | — | 1 | 9.72 |
| CHEMBL2147777 | TENELIGLIPTIN | 4.0 | 1 | 9.54 |
| CHEMBL2147709 | — | — | 1 | 9.51 |
| CHEMBL2147712 | — | — | 1 | 9.31 |
| CHEMBL2147713 | — | — | 1 | 9.28 |
| CHEMBL2147707 | — | — | 1 | 9.16 |
| CHEMBL2147771 | — | — | 1 | 9.14 |
| CHEMBL2147773 | — | — | 1 | 9.11 |
| CHEMBL2058969 | — | — | 1 | 9.00 |
| CHEMBL2147711 | — | — | 1 | 8.64 |
| CHEMBL2147710 | — | — | 1 | 8.60 |
| CHEMBL2147705 | — | — | 1 | 8.54 |
| CHEMBL2147714 | — | — | 1 | 8.54 |
| CHEMBL2058968 | — | — | 1 | 8.52 |
| CHEMBL2147706 | — | — | 1 | 8.51 |
| CHEMBL2147772 | — | — | 1 | 8.33 |
| CHEMBL2147702 | — | — | 1 | 8.27 |
| CHEMBL2147775 | — | — | 1 | 8.24 |
| CHEMBL2147715 | — | — | 1 | 7.89 |
| CHEMBL2147774 | — | — | 1 | 7.85 |
| CHEMBL2147776 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2147704 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL2147703 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL2147777 | TENELIGLIPTIN | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL2147709 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL2147712 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL2147713 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL2147707 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL2147771 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL2147773 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL2058969 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2147711 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2147710 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2147705 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL2147714 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL2058968 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2147706 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL2147772 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL2147702 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL2147775 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL2147715 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2147774 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2147776 | — | IC50 | > | 1000.0 | nM | - |