Assay Detail
Binding
CHEMBL1909181
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DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 5.56 | 8.08 |
| Ki | 871 | 5.96 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL118865 | SPIRADOLINE | 2.0 | 2 | 8.48 |
| CHEMBL19019 | NALTREXONE | 4.0 | 2 | 8.14 |
| CHEMBL80 | NALOXONE | 4.0 | 2 | 7.52 |
| CHEMBL1618305 | NALOXONAZINE | — | 2 | 7.47 |
| CHEMBL895 | NALBUPHINE | 4.0 | 2 | 7.36 |
| CHEMBL1289 | HALOPROGIN | 4.0 | 2 | 6.34 |
| CHEMBL508112 | BENZOTHIAZYL DISULFIDE | — | 2 | 6.30 |
| CHEMBL64894 | GENTIAN VIOLET | 4.0 | 2 | 6.21 |
| CHEMBL81 | RALOXIFENE | 4.0 | 2 | 6.19 |
| CHEMBL942 | BISACODYL | 4.0 | 2 | 6.01 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 2 | 6.00 |
| CHEMBL841 | LOPERAMIDE | 4.0 | 2 | 5.90 |
| CHEMBL411 | DIETHYLSTILBESTROL | 4.0 | 2 | 5.74 |
| CHEMBL964 | DISULFIRAM | 4.0 | 2 | 5.61 |
| CHEMBL104 | CLOTRIMAZOLE | 4.0 | 2 | 5.60 |
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 2 | 5.58 |
| CHEMBL91 | MICONAZOLE | 4.0 | 2 | 5.58 |
| CHEMBL114 | SAQUINAVIR | 4.0 | 2 | 5.56 |
| CHEMBL219916 | DOMPERIDONE | 3.0 | 2 | 5.55 |
| CHEMBL808 | ECONAZOLE | 4.0 | 2 | 5.46 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 2 | 5.35 |
| CHEMBL163 | RITONAVIR | 4.0 | 2 | 5.26 |
| CHEMBL1479 | DANAZOL | 4.0 | 2 | 5.21 |
| CHEMBL83 | TAMOXIFEN | 4.0 | 2 | 5.20 |
| CHEMBL633 | AMIODARONE | 4.0 | 2 | 5.18 |
| CHEMBL1276308 | MIFEPRISTONE | 4.0 | 2 | 5.09 |
| CHEMBL726 | FLUPHENAZINE | 4.0 | 2 | 5.00 |
| CHEMBL691 | ETHINYL ESTRADIOL | 4.0 | 2 | 4.99 |
| CHEMBL584 | NELFINAVIR | 4.0 | 2 | 4.84 |
| CHEMBL515914 | AZARIBINE | 4.0 | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL118865 | SPIRADOLINE | Ki | = | 3.32 | nM | 8.48 |
| CHEMBL19019 | NALTREXONE | Ki | = | 7.175 | nM | 8.14 |
| CHEMBL118865 | SPIRADOLINE | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL19019 | NALTREXONE | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL80 | NALOXONE | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL1618305 | NALOXONAZINE | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL895 | NALBUPHINE | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL80 | NALOXONE | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL1618305 | NALOXONAZINE | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL895 | NALBUPHINE | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL1289 | HALOPROGIN | Ki | = | 459.0 | nM | 6.34 |
| CHEMBL508112 | BENZOTHIAZYL DISULFIDE | Ki | = | 497.0 | nM | 6.30 |
| CHEMBL64894 | GENTIAN VIOLET | Ki | = | 616.0 | nM | 6.21 |
| CHEMBL81 | RALOXIFENE | Ki | = | 641.0 | nM | 6.19 |
| CHEMBL942 | BISACODYL | Ki | = | 975.0 | nM | 6.01 |
| CHEMBL479 | THIORIDAZINE | Ki | = | 996.0 | nM | 6.00 |
| CHEMBL1289 | HALOPROGIN | IC50 | = | 1147.0 | nM | 5.94 |
| CHEMBL508112 | BENZOTHIAZYL DISULFIDE | IC50 | = | 1243.0 | nM | 5.91 |
| CHEMBL841 | LOPERAMIDE | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL64894 | GENTIAN VIOLET | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 1602.0 | nM | 5.79 |
| CHEMBL411 | DIETHYLSTILBESTROL | Ki | = | 1825.0 | nM | 5.74 |
| CHEMBL942 | BISACODYL | IC50 | = | 2437.0 | nM | 5.61 |
| CHEMBL964 | DISULFIRAM | Ki | = | 2441.0 | nM | 5.61 |
| CHEMBL479 | THIORIDAZINE | IC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL104 | CLOTRIMAZOLE | Ki | = | 2521.0 | nM | 5.60 |
| CHEMBL91 | MICONAZOLE | Ki | = | 2637.0 | nM | 5.58 |
| CHEMBL296419 | ASTEMIZOLE | Ki | = | 2646.0 | nM | 5.58 |
| CHEMBL114 | SAQUINAVIR | Ki | = | 2780.0 | nM | 5.56 |
| CHEMBL219916 | DOMPERIDONE | Ki | = | 2798.0 | nM | 5.55 |
| CHEMBL841 | LOPERAMIDE | IC50 | = | 3125.0 | nM | 5.50 |
| CHEMBL808 | ECONAZOLE | Ki | = | 3446.0 | nM | 5.46 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 4433.0 | nM | 5.35 |
| CHEMBL411 | DIETHYLSTILBESTROL | IC50 | = | 4563.0 | nM | 5.34 |
| CHEMBL163 | RITONAVIR | Ki | = | 5462.0 | nM | 5.26 |
| CHEMBL964 | DISULFIRAM | IC50 | = | 6103.0 | nM | 5.21 |
| CHEMBL1479 | DANAZOL | Ki | = | 6207.0 | nM | 5.21 |
| CHEMBL104 | CLOTRIMAZOLE | IC50 | = | 6303.0 | nM | 5.20 |
| CHEMBL83 | TAMOXIFEN | Ki | = | 6252.0 | nM | 5.20 |
| CHEMBL91 | MICONAZOLE | IC50 | = | 6594.0 | nM | 5.18 |
| CHEMBL633 | AMIODARONE | Ki | = | 6672.0 | nM | 5.18 |
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 6616.0 | nM | 5.18 |
| CHEMBL114 | SAQUINAVIR | IC50 | = | 6951.0 | nM | 5.16 |
| CHEMBL219916 | DOMPERIDONE | IC50 | = | 6994.0 | nM | 5.16 |
| CHEMBL1276308 | MIFEPRISTONE | Ki | = | 8038.0 | nM | 5.09 |
| CHEMBL808 | ECONAZOLE | IC50 | = | 8616.0 | nM | 5.07 |
| CHEMBL726 | FLUPHENAZINE | Ki | = | 9891.0 | nM | 5.00 |
| CHEMBL691 | ETHINYL ESTRADIOL | Ki | = | 10358.0 | nM | 4.99 |
| CHEMBL71 | CHLORPROMAZINE | IC50 | = | 11082.0 | nM | 4.96 |
| CHEMBL163 | RITONAVIR | IC50 | = | 13655.0 | nM | 4.87 |