Assay Detail
Binding
CHEMBL697537
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Binding affinity against H3 receptor in rat cerebral cortex membranes was evaluated using [3H]N-methyl-histamine as radioligand
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Novel 1, 2, 4-oxadiazoles as potent and selective histamine H3 receptor antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.48 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 9.80 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.70 |
| CHEMBL168960 | — | — | 1 | 8.50 |
| CHEMBL276798 | GR-175737 | — | 1 | 8.20 |
| CHEMBL169994 | — | — | 1 | 8.20 |
| CHEMBL169426 | — | — | 1 | 8.10 |
| CHEMBL169348 | — | — | 1 | 8.00 |
| CHEMBL423445 | — | — | 1 | 7.90 |
| CHEMBL353939 | — | — | 1 | 7.70 |
| CHEMBL168196 | — | — | 1 | 7.70 |
| CHEMBL166603 | — | — | 1 | 7.60 |
| CHEMBL354348 | — | — | 1 | 7.60 |
| CHEMBL45056 | — | — | 1 | 7.60 |
| CHEMBL424010 | — | — | 1 | 7.40 |
| CHEMBL168973 | — | — | 1 | 7.20 |
| CHEMBL354711 | — | — | 1 | 7.00 |
| CHEMBL166761 | — | — | 1 | 6.90 |
| CHEMBL169026 | — | — | 1 | 6.70 |
| CHEMBL166802 | — | — | 1 | 6.70 |
| CHEMBL353915 | — | — | 1 | 6.60 |
| CHEMBL352869 | — | — | 1 | 6.50 |
| CHEMBL165537 | — | — | 1 | 5.90 |
| CHEMBL168889 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL168960 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL276798 | GR-175737 | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL169994 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL169426 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL169348 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL423445 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL353939 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL168196 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL166603 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL354348 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL45056 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL424010 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL168973 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL354711 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL166761 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL169026 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL166802 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL353915 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL352869 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL165537 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL168889 | — | Ki | = | 2511.89 | nM | 5.60 |