Assay Detail
Binding
CHEMBL1767555
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Displacement of [3H]PK11195 from TSPO receptor in rat kidney membranes
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
N-(4-cyanotetrahydro-2H-pyran-4-yl) and N-(1-cyanocyclohexyl) derivatives of 1,5-diarylpyrazole-3-carboxamides showing high affinity for 18 kDa translocator protein and/or cannabinoid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 6.52 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL481537 | PK-11195 | — | 1 | 9.00 |
| CHEMBL1765683 | — | — | 1 | 7.54 |
| CHEMBL1765685 | — | — | 1 | 7.21 |
| CHEMBL1765676 | — | — | 1 | 7.12 |
| CHEMBL1765678 | — | — | 1 | 6.94 |
| CHEMBL1765682 | — | — | 1 | 6.88 |
| CHEMBL1765819 | — | — | 1 | 6.81 |
| CHEMBL1765684 | — | — | 1 | 6.55 |
| CHEMBL1765673 | — | — | 1 | 6.41 |
| CHEMBL1765679 | — | — | 1 | 6.38 |
| CHEMBL1765674 | — | — | 1 | 6.36 |
| CHEMBL1765820 | — | — | 1 | 6.31 |
| CHEMBL1765675 | — | — | 1 | 6.24 |
| CHEMBL1765821 | — | — | 1 | 6.16 |
| CHEMBL1765680 | — | — | 1 | 6.12 |
| CHEMBL1765096 | — | — | 1 | 6.06 |
| CHEMBL1765818 | — | — | 1 | 5.72 |
| CHEMBL1765681 | — | — | 1 | 5.55 |
| CHEMBL1765672 | — | — | 1 | 5.51 |
| CHEMBL1765677 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL481537 | PK-11195 | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1765683 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL1765685 | — | Ki | = | 61.8 | nM | 7.21 |
| CHEMBL1765676 | — | Ki | = | 75.2 | nM | 7.12 |
| CHEMBL1765678 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL1765682 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL1765819 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL1765684 | — | Ki | = | 279.0 | nM | 6.55 |
| CHEMBL1765673 | — | Ki | = | 394.0 | nM | 6.41 |
| CHEMBL1765679 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL1765674 | — | Ki | = | 436.0 | nM | 6.36 |
| CHEMBL1765820 | — | Ki | = | 492.0 | nM | 6.31 |
| CHEMBL1765675 | — | Ki | = | 576.0 | nM | 6.24 |
| CHEMBL1765821 | — | Ki | = | 693.0 | nM | 6.16 |
| CHEMBL1765680 | — | Ki | = | 762.0 | nM | 6.12 |
| CHEMBL1765096 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL1765818 | — | Ki | = | 1920.0 | nM | 5.72 |
| CHEMBL1765681 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL1765672 | — | Ki | = | 3110.0 | nM | 5.51 |
| CHEMBL1765677 | — | Ki | = | 3690.0 | nM | 5.43 |