Assay Detail
Binding
CHEMBL1909157
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DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
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 | 5.71 | 7.38 |
| Ki | 871 | 5.72 | 7.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL902 | FAMOTIDINE | 4.0 | 2 | 7.39 |
| CHEMBL404849 | SULOCTIDIL | 4.0 | 2 | 7.05 |
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 2 | 6.71 |
| CHEMBL1626 | CLEMASTINE | 4.0 | 2 | 6.44 |
| CHEMBL21731 | MAPROTILINE | 4.0 | 2 | 6.41 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 2 | 6.14 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 2 | 6.03 |
| CHEMBL19215 | METERGOLINE | 2.0 | 2 | 6.02 |
| CHEMBL6437 | MIANSERIN | 4.0 | 2 | 6.00 |
| CHEMBL157138 | LISURIDE | 3.0 | 2 | 5.99 |
| CHEMBL1172 | DESLORATADINE | 4.0 | 2 | 5.97 |
| CHEMBL64894 | GENTIAN VIOLET | 4.0 | 2 | 5.95 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 2 | 5.94 |
| CHEMBL643 | PROMETHAZINE | 4.0 | 2 | 5.94 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 2 | 5.93 |
| CHEMBL726 | FLUPHENAZINE | 4.0 | 2 | 5.92 |
| CHEMBL85 | RISPERIDONE | 4.0 | 2 | 5.84 |
| CHEMBL1282 | IMIQUIMOD | 4.0 | 2 | 5.83 |
| CHEMBL808 | ECONAZOLE | 4.0 | 2 | 5.80 |
| CHEMBL1123 | DICYCLOMINE | 4.0 | 2 | 5.80 |
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 2 | 5.78 |
| CHEMBL1628227 | DOXEPIN | 4.0 | 2 | 5.74 |
| CHEMBL941 | IMATINIB | 4.0 | 2 | 5.71 |
| CHEMBL415 | CLOMIPRAMINE | 4.0 | 2 | 5.70 |
| CHEMBL445 | NORTRIPTYLINE | 4.0 | 2 | 5.64 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 2 | 5.59 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 2 | 5.59 |
| CHEMBL564 | PROMAZINE | 4.0 | 2 | 5.55 |
| CHEMBL305660 | EBASTINE | 4.0 | 2 | 5.54 |
| CHEMBL841 | LOPERAMIDE | 4.0 | 2 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL902 | FAMOTIDINE | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL902 | FAMOTIDINE | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL404849 | SULOCTIDIL | Ki | = | 88.5 | nM | 7.05 |
| CHEMBL404849 | SULOCTIDIL | IC50 | = | 108.1 | nM | 6.97 |
| CHEMBL516 | CYPROHEPTADINE | Ki | = | 195.0 | nM | 6.71 |
| CHEMBL516 | CYPROHEPTADINE | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL1626 | CLEMASTINE | Ki | = | 364.0 | nM | 6.44 |
| CHEMBL1626 | CLEMASTINE | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL21731 | MAPROTILINE | Ki | = | 393.0 | nM | 6.41 |
| CHEMBL21731 | MAPROTILINE | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 718.0 | nM | 6.14 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL479 | THIORIDAZINE | Ki | = | 934.0 | nM | 6.03 |
| CHEMBL479 | THIORIDAZINE | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL19215 | METERGOLINE | Ki | = | 959.0 | nM | 6.02 |
| CHEMBL19215 | METERGOLINE | IC50 | = | 975.0 | nM | 6.01 |
| CHEMBL6437 | MIANSERIN | IC50 | = | 1008.0 | nM | 6.00 |
| CHEMBL6437 | MIANSERIN | Ki | = | 992.0 | nM | 6.00 |
| CHEMBL157138 | LISURIDE | Ki | = | 1022.0 | nM | 5.99 |
| CHEMBL157138 | LISURIDE | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL1172 | DESLORATADINE | Ki | = | 1080.0 | nM | 5.97 |
| CHEMBL1172 | DESLORATADINE | IC50 | = | 1099.0 | nM | 5.96 |
| CHEMBL64894 | GENTIAN VIOLET | Ki | = | 1136.0 | nM | 5.95 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 1147.0 | nM | 5.94 |
| CHEMBL643 | PROMETHAZINE | Ki | = | 1146.0 | nM | 5.94 |
| CHEMBL64894 | GENTIAN VIOLET | IC50 | = | 1155.0 | nM | 5.94 |
| CHEMBL643 | PROMETHAZINE | IC50 | = | 1165.0 | nM | 5.93 |
| CHEMBL1201203 | BENZTROPINE | Ki | = | 1185.0 | nM | 5.93 |
| CHEMBL54 | HALOPERIDOL | IC50 | = | 1166.0 | nM | 5.93 |
| CHEMBL1201203 | BENZTROPINE | IC50 | = | 1206.0 | nM | 5.92 |
| CHEMBL726 | FLUPHENAZINE | Ki | = | 1205.0 | nM | 5.92 |
| CHEMBL726 | FLUPHENAZINE | IC50 | = | 1226.0 | nM | 5.91 |
| CHEMBL85 | RISPERIDONE | Ki | = | 1458.0 | nM | 5.84 |
| CHEMBL85 | RISPERIDONE | IC50 | = | 1483.0 | nM | 5.83 |
| CHEMBL1282 | IMIQUIMOD | Ki | = | 1481.0 | nM | 5.83 |
| CHEMBL1282 | IMIQUIMOD | IC50 | = | 1506.0 | nM | 5.82 |
| CHEMBL808 | ECONAZOLE | Ki | = | 1565.0 | nM | 5.80 |
| CHEMBL1123 | DICYCLOMINE | Ki | = | 1598.0 | nM | 5.80 |
| CHEMBL808 | ECONAZOLE | IC50 | = | 1592.0 | nM | 5.80 |
| CHEMBL1123 | DICYCLOMINE | IC50 | = | 1625.0 | nM | 5.79 |
| CHEMBL296419 | ASTEMIZOLE | Ki | = | 1654.0 | nM | 5.78 |
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 1682.0 | nM | 5.77 |
| CHEMBL1628227 | DOXEPIN | Ki | = | 1836.0 | nM | 5.74 |
| CHEMBL1628227 | DOXEPIN | IC50 | = | 1867.0 | nM | 5.73 |
| CHEMBL941 | IMATINIB | IC50 | = | 1963.0 | nM | 5.71 |
| CHEMBL941 | IMATINIB | Ki | = | 1930.0 | nM | 5.71 |
| CHEMBL415 | CLOMIPRAMINE | Ki | = | 2015.0 | nM | 5.70 |
| CHEMBL415 | CLOMIPRAMINE | IC50 | = | 2049.0 | nM | 5.69 |
| CHEMBL445 | NORTRIPTYLINE | Ki | = | 2295.0 | nM | 5.64 |
| CHEMBL445 | NORTRIPTYLINE | IC50 | = | 2334.0 | nM | 5.63 |