Assay Detail
Functional
CHEMBL1002435
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at histamine H3 receptor in guinea pig jejunum assessed as electrically evoked contractions
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Jejunum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Non-imidazole histamine H3 ligands, part IV: SAR of 1-[2-thiazol-5-yl-(2-aminoethyl)]-4-n-propylpiperazine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 18 | 7.40 | 9.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 9.06 |
| CHEMBL473093 | — | — | 1 | 8.27 |
| CHEMBL475323 | — | — | 1 | 7.78 |
| CHEMBL472690 | — | — | 1 | 7.76 |
| CHEMBL514976 | — | — | 1 | 7.53 |
| CHEMBL515121 | — | — | 1 | 7.36 |
| CHEMBL474716 | — | — | 1 | 7.26 |
| CHEMBL471715 | — | — | 1 | 7.25 |
| CHEMBL473296 | — | — | 1 | 7.25 |
| CHEMBL361775 | — | — | 1 | 7.21 |
| CHEMBL474715 | — | — | 1 | 7.20 |
| CHEMBL467899 | — | — | 1 | 7.19 |
| CHEMBL510187 | — | — | 1 | 7.16 |
| CHEMBL447370 | — | — | 1 | 7.10 |
| CHEMBL514924 | — | — | 1 | 7.05 |
| CHEMBL503019 | — | — | 1 | 7.02 |
| CHEMBL474109 | — | — | 1 | 6.93 |
| CHEMBL474314 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260374 | THIOPERAMIDE | Kd | = | 0.871 | nM | 9.06 |
| CHEMBL473093 | — | Kd | = | 5.37 | nM | 8.27 |
| CHEMBL475323 | — | Kd | = | 16.6 | nM | 7.78 |
| CHEMBL472690 | — | Kd | = | 17.38 | nM | 7.76 |
| CHEMBL514976 | — | Kd | = | 29.51 | nM | 7.53 |
| CHEMBL515121 | — | Kd | = | 43.65 | nM | 7.36 |
| CHEMBL474716 | — | Kd | = | 54.95 | nM | 7.26 |
| CHEMBL471715 | — | Kd | = | 56.23 | nM | 7.25 |
| CHEMBL473296 | — | Kd | = | 56.23 | nM | 7.25 |
| CHEMBL361775 | — | Kd | = | 61.66 | nM | 7.21 |
| CHEMBL474715 | — | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL467899 | — | Kd | = | 64.57 | nM | 7.19 |
| CHEMBL510187 | — | Kd | = | 69.18 | nM | 7.16 |
| CHEMBL447370 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL514924 | — | Kd | = | 89.13 | nM | 7.05 |
| CHEMBL503019 | — | Kd | = | 95.5 | nM | 7.02 |
| CHEMBL474109 | — | Kd | = | 117.49 | nM | 6.93 |
| CHEMBL474314 | — | Kd | = | 125.89 | nM | 6.90 |