Assay Detail
Binding
CHEMBL3078211
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at histamine H3 receptor in Cavia porcellus (guinea pig) ileum assessed as inhibition of electrically-induced contraction
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1-Phenoxyalkyl-4-[(N,N-disubstitutedamino)alkyl]piperazine derivatives as non-imidazole histamine H3-antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 27 | 6.96 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.66 |
| CHEMBL2283086 | — | — | 1 | 7.27 |
| CHEMBL2283093 | — | — | 1 | 7.18 |
| CHEMBL2283081 | — | — | 1 | 7.16 |
| CHEMBL2283084 | — | — | 1 | 7.13 |
| CHEMBL2283078 | — | — | 1 | 7.12 |
| CHEMBL2283087 | — | — | 1 | 7.05 |
| CHEMBL2283097 | — | — | 1 | 7.04 |
| CHEMBL2283082 | — | — | 1 | 7.04 |
| CHEMBL2283077 | — | — | 1 | 7.03 |
| CHEMBL2283090 | — | — | 1 | 7.01 |
| CHEMBL2283080 | — | — | 1 | 7.00 |
| CHEMBL2283095 | — | — | 1 | 6.99 |
| CHEMBL2283092 | — | — | 1 | 6.99 |
| CHEMBL2283079 | — | — | 1 | 6.98 |
| CHEMBL2283083 | — | — | 1 | 6.95 |
| CHEMBL2283088 | — | — | 1 | 6.85 |
| CHEMBL2283096 | — | — | 1 | 6.84 |
| CHEMBL2283099 | — | — | 1 | 6.80 |
| CHEMBL2283102 | — | — | 1 | 6.75 |
| CHEMBL2283098 | — | — | 1 | 6.72 |
| CHEMBL2283089 | — | — | 1 | 6.67 |
| CHEMBL2283091 | — | — | 1 | 6.67 |
| CHEMBL2283100 | — | — | 1 | 6.62 |
| CHEMBL2283085 | — | — | 1 | 6.60 |
| CHEMBL2283094 | — | — | 1 | 6.42 |
| CHEMBL2283101 | — | — | 1 | 6.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260374 | THIOPERAMIDE | Kd | = | 2.188 | nM | 8.66 |
| CHEMBL2283086 | — | Kd | = | 53.7 | nM | 7.27 |
| CHEMBL2283093 | — | Kd | = | 66.07 | nM | 7.18 |
| CHEMBL2283081 | — | Kd | = | 69.18 | nM | 7.16 |
| CHEMBL2283084 | — | Kd | = | 74.13 | nM | 7.13 |
| CHEMBL2283078 | — | Kd | = | 75.86 | nM | 7.12 |
| CHEMBL2283087 | — | Kd | = | 89.13 | nM | 7.05 |
| CHEMBL2283097 | — | Kd | = | 91.2 | nM | 7.04 |
| CHEMBL2283082 | — | Kd | = | 91.2 | nM | 7.04 |
| CHEMBL2283077 | — | Kd | = | 93.33 | nM | 7.03 |
| CHEMBL2283090 | — | Kd | = | 97.72 | nM | 7.01 |
| CHEMBL2283080 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL2283095 | — | Kd | = | 102.33 | nM | 6.99 |
| CHEMBL2283092 | — | Kd | = | 102.33 | nM | 6.99 |
| CHEMBL2283079 | — | Kd | = | 104.71 | nM | 6.98 |
| CHEMBL2283083 | — | Kd | = | 112.2 | nM | 6.95 |
| CHEMBL2283088 | — | Kd | = | 141.25 | nM | 6.85 |
| CHEMBL2283096 | — | Kd | = | 144.54 | nM | 6.84 |
| CHEMBL2283099 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL2283102 | — | Kd | = | 177.83 | nM | 6.75 |
| CHEMBL2283098 | — | Kd | = | 190.55 | nM | 6.72 |
| CHEMBL2283089 | — | Kd | = | 213.8 | nM | 6.67 |
| CHEMBL2283091 | — | Kd | = | 213.8 | nM | 6.67 |
| CHEMBL2283100 | — | Kd | = | 239.88 | nM | 6.62 |
| CHEMBL2283085 | — | Kd | = | 251.19 | nM | 6.60 |
| CHEMBL2283094 | — | Kd | = | 380.19 | nM | 6.42 |
| CHEMBL2283101 | — | Kd | = | 512.86 | nM | 6.29 |