Assay Detail
Binding
CHEMBL1218971
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Inhibition of human DPP8
34
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 8.85 | 10.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1215374 | — | — | 1 | 10.07 |
| CHEMBL1215376 | — | — | 1 | 9.57 |
| CHEMBL1215167 | — | — | 1 | 9.40 |
| CHEMBL1215087 | — | — | 1 | 9.38 |
| CHEMBL1215448 | — | — | 1 | 9.24 |
| CHEMBL1215375 | — | — | 1 | 9.22 |
| CHEMBL1215302 | — | — | 1 | 9.19 |
| CHEMBL1215089 | — | — | 1 | 9.15 |
| CHEMBL1215236 | — | — | 1 | 9.02 |
| CHEMBL1215164 | — | — | 1 | 8.96 |
| CHEMBL1215299 | — | — | 1 | 8.96 |
| CHEMBL1215301 | — | — | 1 | 8.92 |
| CHEMBL1215017 | — | — | 1 | 8.89 |
| CHEMBL1215233 | — | — | 1 | 8.89 |
| CHEMBL1215300 | — | — | 1 | 8.85 |
| CHEMBL1214877 | — | — | 1 | 8.77 |
| CHEMBL1215166 | — | — | 1 | 8.77 |
| CHEMBL1214876 | — | — | 3 | 8.72 |
| CHEMBL1215018 | — | — | 1 | 8.70 |
| CHEMBL1215088 | — | — | 1 | 8.66 |
| CHEMBL1215373 | — | — | 1 | 8.66 |
| CHEMBL1214944 | — | — | 1 | 8.66 |
| CHEMBL1214942 | — | — | 1 | 8.66 |
| CHEMBL1215090 | — | — | 1 | 8.64 |
| CHEMBL1214943 | — | — | 1 | 8.62 |
| CHEMBL1215235 | — | — | 1 | 8.60 |
| CHEMBL1215016 | — | — | 1 | 8.55 |
| CHEMBL1215163 | — | — | 1 | 8.54 |
| CHEMBL1215165 | — | — | 1 | 8.39 |
| CHEMBL1215234 | — | — | 1 | 8.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1215374 | — | Ki | = | 0.086 | nM | 10.07 |
| CHEMBL1215376 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL1215167 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL1215087 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL1215448 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL1215375 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1215302 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL1215089 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL1215236 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL1215164 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1215299 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1215301 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL1215017 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL1215233 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL1215300 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL1214877 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL1215166 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL1214876 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL1215018 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1214942 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL1215373 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL1214944 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL1215088 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL1215090 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL1214943 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL1215235 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL1215016 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL1215163 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL1214876 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL1215165 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL1215234 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL1215015 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1214945 | — | Ki | > | 10.0 | nM | - |
| CHEMBL1214876 | — | Ki | > | 30.0 | nM | - |