Assay Detail
Binding
CHEMBL2149800
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of DPP4 in human plasma using GLY-Pro-MCA as substrate after 60 mins by fluorescence assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 25 | 8.82 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2147704 | — | — | 1 | 9.70 |
| CHEMBL2147703 | — | — | 1 | 9.59 |
| CHEMBL2147712 | — | — | 1 | 9.52 |
| CHEMBL2147709 | — | — | 1 | 9.49 |
| CHEMBL2147777 | TENELIGLIPTIN | 4.0 | 1 | 9.43 |
| CHEMBL2058971 | — | — | 1 | 9.43 |
| CHEMBL2147773 | — | — | 1 | 9.21 |
| CHEMBL2147771 | — | — | 1 | 9.20 |
| CHEMBL2147713 | — | — | 1 | 9.07 |
| CHEMBL2147707 | — | — | 1 | 9.03 |
| CHEMBL2058969 | — | — | 1 | 9.02 |
| CHEMBL391466 | — | — | 1 | 8.80 |
| CHEMBL241253 | — | — | 1 | 8.80 |
| CHEMBL2058968 | — | — | 1 | 8.66 |
| CHEMBL2147711 | — | — | 1 | 8.54 |
| CHEMBL2147714 | — | — | 1 | 8.47 |
| CHEMBL2147705 | — | — | 1 | 8.40 |
| CHEMBL2147706 | — | — | 1 | 8.37 |
| CHEMBL2147702 | — | — | 1 | 8.35 |
| CHEMBL2147772 | — | — | 1 | 8.30 |
| CHEMBL2147710 | — | — | 1 | 8.25 |
| CHEMBL2147775 | — | — | 1 | 8.20 |
| CHEMBL2147715 | — | — | 1 | 7.92 |
| CHEMBL2147774 | — | — | 1 | 7.82 |
| CHEMBL2147776 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2147704 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL2147703 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL2147712 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL2147709 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL2147777 | TENELIGLIPTIN | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL2058971 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL2147773 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL2147771 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL2147713 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL2147707 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL2058969 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL391466 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL241253 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2058968 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL2147711 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL2147714 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL2147705 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2147706 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL2147702 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL2147772 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2147710 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL2147775 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL2147715 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2147774 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2147776 | — | IC50 | > | 1000.0 | nM | - |