Assay Detail
Binding
CHEMBL3887953
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DPP-IV Activity InhibitoryAssay: Gly-Pro-7-amido-4-methylcoumarin can be hydrolyzed by dipeptidyl peptidase IV (DPP-IV) at room temperature, to generate 7-amido-4-methyl coumarin, which can emit fluorescence with wavelength of 460 nm at excitation wavelength of 355 nm. The variation of the product amount can be determined by the variation of fluorescence intensity, so as to reflect the activity level of the enzyme. The dipeptidyl peptidase IV (DPP-IV), DPP-IV buffer and test samples were used to construct the reaction system of 200 uL, while the blank control (without enzyme and samples) and negative control (without samples) having the same volume were set up. The reaction system and the controls were reacted at room temperature for 10 min, and then dipeptidyl peptidase IV substrate was added thereto respectively, then reacted at room temperature for 30 min. The fluorescence intensity F (excitation wavelength of 355 nm, emission wavelength of 460 nm) was determined.
6
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Xanthine derivative
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 9.82 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4113723 | — | — | 2 | 10.30 |
| CHEMBL4111229 | — | — | 2 | 10.00 |
| CHEMBL4109453 | — | — | 1 | 9.70 |
| CHEMBL237500 | LINAGLIPTIN | 4.0 | 1 | 9.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4113723 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL4113723 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL4111229 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4111229 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL4109453 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL237500 | LINAGLIPTIN | IC50 | = | 1.0 | nM | 9.00 |