Assay Detail
Functional
CHEMBL664533
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against Dipeptidylpeptidase IV mediated cleavage of Ala-Pro-7-amido-4-tri-fluoromethylcoumarin in a fluorogenic assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.36 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34062 | — | — | 1 | 10.00 |
| CHEMBL36666 | — | — | 1 | 9.70 |
| CHEMBL34842 | — | — | 1 | 9.70 |
| CHEMBL35116 | — | — | 1 | 9.05 |
| CHEMBL37960 | — | — | 1 | 8.52 |
| CHEMBL36020 | — | — | 1 | 8.00 |
| CHEMBL37536 | — | — | 1 | 7.33 |
| CHEMBL37687 | — | — | 1 | 7.28 |
| CHEMBL34972 | — | — | 1 | 7.05 |
| CHEMBL37289 | — | — | 1 | 7.00 |
| CHEMBL37654 | — | — | 1 | 6.89 |
| CHEMBL34764 | — | — | 1 | 6.75 |
| CHEMBL37655 | — | — | 1 | 6.62 |
| CHEMBL37748 | — | — | 1 | 6.47 |
| CHEMBL34779 | — | — | 1 | 6.46 |
| CHEMBL38165 | — | — | 1 | 6.00 |
| CHEMBL35000 | — | — | 1 | 5.96 |
| CHEMBL34603 | — | — | 1 | 5.85 |
| CHEMBL37229 | — | — | 1 | 5.82 |
| CHEMBL35016 | — | — | 1 | 5.82 |
| CHEMBL37645 | — | — | 1 | 5.76 |
| CHEMBL36333 | — | — | 1 | 5.60 |
| CHEMBL37980 | — | — | 1 | 5.00 |
| CHEMBL287847 | — | — | 1 | 4.85 |
| CHEMBL288171 | — | — | 1 | 4.85 |
| CHEMBL286301 | — | — | 1 | 4.75 |
| CHEMBL287534 | — | — | 1 | 4.70 |
| CHEMBL416787 | — | — | 1 | 4.51 |
| CHEMBL35451 | — | — | 1 | 4.40 |
| CHEMBL289562 | — | — | 1 | 4.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34062 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL36666 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL34842 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL35116 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL37960 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL36020 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL37536 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL37687 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL34972 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL37289 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL37654 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL34764 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL37655 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL37748 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL34779 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL38165 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL35000 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL34603 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL37229 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL35016 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL37645 | — | IC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL36333 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL37980 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL287847 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL288171 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL286301 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL287534 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL416787 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL35451 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL289562 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL36282 | — | IC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL290620 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL289399 | — | IC50 | = | 170000.0 | nM | - |