Assay Detail
Binding
CHEMBL1034549
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in human SK-N-MC cells by liquid scintillation counting
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-N-MC |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.99 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19439 | IMETIT | — | 1 | 8.80 |
| CHEMBL281576 | — | — | 1 | 8.60 |
| CHEMBL1743881 | — | — | 1 | 8.60 |
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 8.50 |
| CHEMBL1202321 | — | — | 1 | 8.50 |
| CHEMBL1202328 | — | — | 1 | 8.30 |
| CHEMBL1202332 | — | — | 1 | 8.20 |
| CHEMBL1202329 | — | — | 1 | 8.20 |
| CHEMBL1202318 | — | — | 1 | 8.10 |
| CHEMBL1202326 | — | — | 1 | 8.10 |
| CHEMBL1202319 | — | — | 1 | 8.10 |
| CHEMBL561250 | — | — | 1 | 8.10 |
| CHEMBL1237146 | IODOPHENPROPIT HYDROBROMIDE | — | 1 | 8.10 |
| CHEMBL1202324 | — | — | 1 | 8.10 |
| CHEMBL1202322 | — | — | 1 | 8.00 |
| CHEMBL1202331 | — | — | 1 | 8.00 |
| CHEMBL1202320 | — | — | 1 | 7.90 |
| CHEMBL1202330 | — | — | 1 | 7.70 |
| CHEMBL1202325 | — | — | 1 | 7.70 |
| CHEMBL551047 | — | — | 1 | 7.70 |
| CHEMBL1202323 | — | — | 1 | 7.50 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 7.30 |
| CHEMBL552694 | — | — | 1 | 7.10 |
| CHEMBL561651 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19439 | IMETIT | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL281576 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL1743881 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL1202321 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL1202328 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL1202332 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL1202329 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL1202318 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1202326 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1202319 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL561250 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1237146 | IODOPHENPROPIT HYDROBROMIDE | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1202324 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1202322 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1202331 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1202320 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1202330 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL1202325 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL551047 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL1202323 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL552694 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL561651 | — | Ki | = | 316.23 | nM | 6.50 |