Assay Detail
Binding
CHEMBL2444440
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Inhibition of DPP8 (unknown origin)
34
Total Activities
27
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
Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 8.48 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2441846 | — | — | 1 | 9.10 |
| CHEMBL2441955 | — | — | 1 | 9.00 |
| CHEMBL2441844 | — | — | 2 | 9.00 |
| CHEMBL2441954 | — | — | 1 | 8.85 |
| CHEMBL2441839 | — | — | 1 | 8.85 |
| CHEMBL2441837 | — | — | 2 | 8.77 |
| CHEMBL2441845 | — | — | 1 | 8.74 |
| CHEMBL2441953 | — | — | 1 | 8.70 |
| CHEMBL2441829 | — | — | 1 | 8.55 |
| CHEMBL2441841 | — | — | 1 | 8.42 |
| CHEMBL2441830 | — | — | 3 | 8.42 |
| CHEMBL2441848 | — | — | 1 | 8.42 |
| CHEMBL2441838 | — | — | 1 | 8.41 |
| CHEMBL2441847 | — | — | 1 | 8.41 |
| CHEMBL2441951 | — | — | 1 | 8.37 |
| CHEMBL2441952 | — | — | 2 | 8.31 |
| CHEMBL2441833 | — | — | 1 | 8.28 |
| CHEMBL2441828 | — | — | 1 | 8.28 |
| CHEMBL2441836 | — | — | 3 | 8.27 |
| CHEMBL2441831 | — | — | 1 | 8.26 |
| CHEMBL2441835 | — | — | 1 | 8.22 |
| CHEMBL2441832 | — | — | 1 | 8.19 |
| CHEMBL2441834 | — | — | 1 | 8.05 |
| CHEMBL2441950 | — | — | 1 | 7.89 |
| CHEMBL2441843 | — | — | 1 | - |
| CHEMBL2441842 | — | — | 1 | - |
| CHEMBL2441840 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2441846 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL2441955 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2441844 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2441954 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL2441839 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL2441837 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL2441845 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL2441953 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2441844 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL2441829 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL2441848 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL2441841 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL2441830 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL2441847 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL2441838 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL2441830 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL2441951 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL2441952 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL2441828 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL2441833 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL2441836 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL2441831 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL2441835 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2441832 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL2441836 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL2441834 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL2441950 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2441836 | — | Ki | > | 30.0 | nM | - |
| CHEMBL2441837 | — | Ki | > | 30.0 | nM | - |
| CHEMBL2441830 | — | Ki | > | 30.0 | nM | - |
| CHEMBL2441840 | — | Ki | > | 30.0 | nM | - |
| CHEMBL2441842 | — | Ki | > | 30.0 | nM | - |
| CHEMBL2441843 | — | Ki | > | 30.0 | nM | - |
| CHEMBL2441952 | — | Ki | > | 30.0 | nM | - |