Assay Detail
Binding
CHEMBL3090540
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Inhibition of recombinant human PrCP using Mca-Ala-Pro-Lys(Dnp)-OH as substrate measured for 30 mins by fluorescence assay
24
Total Activities
22
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 and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.09 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3086040 | — | — | 1 | 10.10 |
| CHEMBL3086037 | — | — | 1 | 9.74 |
| CHEMBL3085780 | — | — | 1 | 9.22 |
| CHEMBL3086036 | — | — | 1 | 9.18 |
| CHEMBL3086041 | — | — | 1 | 9.02 |
| CHEMBL3086029 | — | — | 1 | 8.92 |
| CHEMBL3086038 | — | — | 1 | 8.66 |
| CHEMBL3086048 | — | — | 1 | 8.60 |
| CHEMBL3086045 | — | — | 2 | 8.60 |
| CHEMBL3086035 | — | — | 1 | 8.59 |
| CHEMBL3086039 | — | — | 1 | 8.57 |
| CHEMBL3086034 | — | — | 1 | 8.52 |
| CHEMBL3086042 | — | — | 1 | 8.34 |
| CHEMBL3086032 | — | — | 1 | 7.92 |
| CHEMBL3086028 | — | — | 1 | 7.78 |
| CHEMBL3086030 | — | — | 1 | 7.77 |
| CHEMBL3086047 | — | — | 1 | 7.54 |
| CHEMBL3086043 | — | — | 1 | 7.44 |
| CHEMBL3086046 | — | — | 2 | 7.37 |
| CHEMBL3086044 | — | — | 1 | 6.70 |
| CHEMBL3086031 | — | — | 1 | 6.36 |
| CHEMBL3086033 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3086040 | — | IC50 | = | 0.079 | nM | 10.10 |
| CHEMBL3086037 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL3085780 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3086036 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL3086041 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL3086029 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3086038 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3086048 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3086045 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3086035 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3086039 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3086034 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3086042 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3086032 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3086028 | — | IC50 | = | 16.7 | nM | 7.78 |
| CHEMBL3086030 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3086047 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3086043 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3086046 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3086045 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL3086044 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL3086031 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL3086033 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3086046 | — | IC50 | = | 642.0 | nM | 6.19 |