Assay Detail
Binding
CHEMBL2156596
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Displacement of 3[H]ligand from recombinant human CB1 receptor
44
Total Activities
42
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
JD-5006 and JD-5037: peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 7.74 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2153670 | — | — | 1 | 9.30 |
| CHEMBL2153672 | — | — | 1 | 8.70 |
| CHEMBL2153669 | — | — | 1 | 8.70 |
| CHEMBL2153763 | — | — | 1 | 8.40 |
| CHEMBL2153772 | — | — | 1 | 8.15 |
| CHEMBL2153674 | — | — | 1 | 8.15 |
| CHEMBL2153767 | — | — | 1 | 8.10 |
| CHEMBL2153673 | — | — | 1 | 8.08 |
| CHEMBL2153666 | — | — | 1 | 8.07 |
| CHEMBL2153765 | — | — | 1 | 8.00 |
| CHEMBL2153757 | — | — | 1 | 7.89 |
| CHEMBL2153662 | — | — | 3 | 7.75 |
| CHEMBL2153665 | — | — | 1 | 7.70 |
| CHEMBL158784 | RAC-IBIPINABANT | — | 1 | 7.66 |
| CHEMBL2153764 | — | — | 1 | 7.60 |
| CHEMBL2153664 | — | — | 1 | 7.58 |
| CHEMBL2153766 | — | — | 1 | 7.57 |
| CHEMBL2153663 | — | — | 1 | 7.50 |
| CHEMBL2153758 | — | — | 1 | 7.18 |
| CHEMBL2153761 | — | — | 1 | 7.16 |
| CHEMBL2153759 | — | — | 1 | 7.00 |
| CHEMBL2153771 | — | — | 1 | 7.00 |
| CHEMBL158138 | — | — | 1 | 7.00 |
| CHEMBL2153648 | — | — | 1 | 7.00 |
| CHEMBL2153655 | — | — | 1 | 6.52 |
| CHEMBL2153654 | — | — | 1 | - |
| CHEMBL2153649 | — | — | 1 | - |
| CHEMBL2153770 | — | — | 1 | - |
| CHEMBL2153769 | — | — | 1 | - |
| CHEMBL2153768 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2153670 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL2153672 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2153669 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2153763 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2153772 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2153674 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2153767 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2153673 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL2153666 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL2153765 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2153757 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2153662 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2153665 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL158784 | RAC-IBIPINABANT | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2153764 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2153664 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2153766 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2153662 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2153663 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2153758 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2153761 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2153759 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2153648 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2153771 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL158138 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2153655 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2153662 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2153661 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2153659 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2153667 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL2153651 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2153650 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2153671 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2153649 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2153657 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2153675 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL2153760 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL2153762 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL2153652 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2153654 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2153653 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL2153768 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL2153769 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL2153770 | — | IC50 | > | 100.0 | nM | - |