Assay Detail
Binding
CHEMBL1909182
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DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-K1 |
| 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 | 5.68 | 8.84 |
| Ki | 871 | 6.07 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL841 | LOPERAMIDE | 4.0 | 2 | 9.23 |
| CHEMBL19019 | NALTREXONE | 4.0 | 2 | 8.78 |
| CHEMBL1618305 | NALOXONAZINE | — | 2 | 8.53 |
| CHEMBL80 | NALOXONE | 4.0 | 2 | 8.09 |
| CHEMBL895 | NALBUPHINE | 4.0 | 2 | 8.00 |
| CHEMBL118865 | SPIRADOLINE | 2.0 | 2 | 7.02 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | — | 2 | 6.46 |
| CHEMBL81 | RALOXIFENE | 4.0 | 2 | 6.32 |
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 2 | 6.22 |
| CHEMBL104 | CLOTRIMAZOLE | 4.0 | 2 | 6.14 |
| CHEMBL64894 | GENTIAN VIOLET | 4.0 | 2 | 6.06 |
| CHEMBL139835 | CYPROTERONE ACETATE | 3.0 | 2 | 6.05 |
| CHEMBL43064 | CINNARIZINE | 2.0 | 2 | 6.04 |
| CHEMBL1403281 | ERGOCRYPTINE | — | 2 | 6.01 |
| CHEMBL1276308 | MIFEPRISTONE | 4.0 | 2 | 6.00 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 2 | 6.00 |
| CHEMBL508112 | BENZOTHIAZYL DISULFIDE | — | 2 | 5.90 |
| CHEMBL964 | DISULFIRAM | 4.0 | 2 | 5.85 |
| CHEMBL219916 | DOMPERIDONE | 3.0 | 2 | 5.77 |
| CHEMBL772 | RESERPINE | 4.0 | 2 | 5.77 |
| CHEMBL30008 | FLUNARIZINE | 2.0 | 2 | 5.67 |
| CHEMBL290106 | BITHIONOL | 4.0 | 2 | 5.65 |
| CHEMBL808 | ECONAZOLE | 4.0 | 2 | 5.64 |
| CHEMBL411 | DIETHYLSTILBESTROL | 4.0 | 2 | 5.63 |
| CHEMBL91 | MICONAZOLE | 4.0 | 2 | 5.61 |
| CHEMBL114 | SAQUINAVIR | 4.0 | 2 | 5.41 |
| CHEMBL141343 | — | — | 2 | 5.36 |
| CHEMBL1479 | DANAZOL | 4.0 | 2 | 5.24 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 2 | 5.23 |
| CHEMBL584 | NELFINAVIR | 4.0 | 2 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL841 | LOPERAMIDE | Ki | = | 0.586 | nM | 9.23 |
| CHEMBL841 | LOPERAMIDE | IC50 | = | 1.445 | nM | 8.84 |
| CHEMBL19019 | NALTREXONE | Ki | = | 1.657 | nM | 8.78 |
| CHEMBL1618305 | NALOXONAZINE | Ki | = | 2.921 | nM | 8.53 |
| CHEMBL19019 | NALTREXONE | IC50 | = | 4.083 | nM | 8.39 |
| CHEMBL1618305 | NALOXONAZINE | IC50 | = | 7.196 | nM | 8.14 |
| CHEMBL80 | NALOXONE | Ki | = | 8.063 | nM | 8.09 |
| CHEMBL895 | NALBUPHINE | Ki | = | 9.925 | nM | 8.00 |
| CHEMBL80 | NALOXONE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL895 | NALBUPHINE | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL118865 | SPIRADOLINE | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL118865 | SPIRADOLINE | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | Ki | = | 345.0 | nM | 6.46 |
| CHEMBL81 | RALOXIFENE | Ki | = | 477.0 | nM | 6.32 |
| CHEMBL296419 | ASTEMIZOLE | Ki | = | 606.0 | nM | 6.22 |
| CHEMBL104 | CLOTRIMAZOLE | Ki | = | 731.0 | nM | 6.14 |
| CHEMBL1255837 | DIHYDROERGOCRISTINE MESYLATE | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL64894 | GENTIAN VIOLET | Ki | = | 871.0 | nM | 6.06 |
| CHEMBL139835 | CYPROTERONE ACETATE | Ki | = | 886.0 | nM | 6.05 |
| CHEMBL43064 | CINNARIZINE | Ki | = | 922.0 | nM | 6.04 |
| CHEMBL1403281 | ERGOCRYPTINE | Ki | = | 985.0 | nM | 6.01 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 992.0 | nM | 6.00 |
| CHEMBL1276308 | MIFEPRISTONE | Ki | = | 997.0 | nM | 6.00 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 1176.0 | nM | 5.93 |
| CHEMBL508112 | BENZOTHIAZYL DISULFIDE | Ki | = | 1264.0 | nM | 5.90 |
| CHEMBL964 | DISULFIRAM | Ki | = | 1425.0 | nM | 5.85 |
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 1492.0 | nM | 5.83 |
| CHEMBL772 | RESERPINE | Ki | = | 1686.0 | nM | 5.77 |
| CHEMBL219916 | DOMPERIDONE | Ki | = | 1712.0 | nM | 5.77 |
| CHEMBL104 | CLOTRIMAZOLE | IC50 | = | 1802.0 | nM | 5.74 |
| CHEMBL30008 | FLUNARIZINE | Ki | = | 2125.0 | nM | 5.67 |
| CHEMBL64894 | GENTIAN VIOLET | IC50 | = | 2145.0 | nM | 5.67 |
| CHEMBL139835 | CYPROTERONE ACETATE | IC50 | = | 2183.0 | nM | 5.66 |
| CHEMBL290106 | BITHIONOL | Ki | = | 2236.0 | nM | 5.65 |
| CHEMBL808 | ECONAZOLE | Ki | = | 2311.0 | nM | 5.64 |
| CHEMBL43064 | CINNARIZINE | IC50 | = | 2272.0 | nM | 5.64 |
| CHEMBL411 | DIETHYLSTILBESTROL | Ki | = | 2345.0 | nM | 5.63 |
| CHEMBL1403281 | ERGOCRYPTINE | IC50 | = | 2427.0 | nM | 5.62 |
| CHEMBL1276308 | MIFEPRISTONE | IC50 | = | 2457.0 | nM | 5.61 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 2443.0 | nM | 5.61 |
| CHEMBL91 | MICONAZOLE | Ki | = | 2460.0 | nM | 5.61 |
| CHEMBL508112 | BENZOTHIAZYL DISULFIDE | IC50 | = | 3113.0 | nM | 5.51 |
| CHEMBL964 | DISULFIRAM | IC50 | = | 3511.0 | nM | 5.46 |
| CHEMBL114 | SAQUINAVIR | Ki | = | 3907.0 | nM | 5.41 |
| CHEMBL772 | RESERPINE | IC50 | = | 4152.0 | nM | 5.38 |
| CHEMBL219916 | DOMPERIDONE | IC50 | = | 4218.0 | nM | 5.38 |
| CHEMBL141343 | — | Ki | = | 4363.0 | nM | 5.36 |
| CHEMBL30008 | FLUNARIZINE | IC50 | = | 5236.0 | nM | 5.28 |
| CHEMBL290106 | BITHIONOL | IC50 | = | 5507.0 | nM | 5.26 |
| CHEMBL808 | ECONAZOLE | IC50 | = | 5693.0 | nM | 5.25 |