Assay Detail
Binding
CHEMBL829504
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In vitro inhibitory concentration was measured against dipeptidylpeptidase IV
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.89 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL539077 | — | — | 1 | 7.75 |
| CHEMBL537400 | — | — | 1 | 7.57 |
| CHEMBL557187 | — | — | 1 | 7.17 |
| CHEMBL558585 | — | — | 1 | 7.15 |
| CHEMBL559011 | — | — | 1 | 6.99 |
| CHEMBL558196 | — | — | 1 | 6.89 |
| CHEMBL175872 | — | — | 1 | 6.86 |
| CHEMBL537844 | — | — | 1 | 6.64 |
| CHEMBL537625 | — | — | 1 | 6.34 |
| CHEMBL366549 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL539077 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL537400 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL557187 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL558585 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL559011 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL558196 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL175872 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL537844 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL537625 | — | IC50 | = | 455.0 | nM | 6.34 |
| CHEMBL366549 | — | IC50 | = | 3100.0 | nM | 5.51 |