Assay Detail
Binding
CHEMBL1177482
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H] (R)-alpha-methylhistamine from human recombinant histamine H3 receptor expressed in CHO cells after 1 hr by liquid scintillation counting
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.27 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18661 | IMMEPIP | — | 1 | 9.52 |
| CHEMBL1098230 | — | — | 1 | 9.37 |
| CHEMBL1172774 | — | — | 1 | 9.00 |
| CHEMBL1172579 | — | — | 1 | 9.00 |
| CHEMBL1170855 | — | — | 1 | 8.85 |
| CHEMBL1169687 | — | — | 1 | 8.80 |
| CHEMBL1172754 | — | — | 1 | 8.74 |
| CHEMBL1172775 | — | — | 1 | 8.27 |
| CHEMBL1173809 | — | — | 1 | 7.92 |
| CHEMBL1172712 | — | — | 1 | 7.85 |
| CHEMBL1172776 | — | — | 1 | 7.85 |
| CHEMBL1173390 | — | — | 1 | 7.80 |
| CHEMBL1172753 | — | — | 1 | 7.70 |
| CHEMBL1171443 | — | — | 1 | 7.52 |
| CHEMBL1173391 | — | — | 1 | 7.21 |
| CHEMBL1173033 | — | — | 1 | 6.90 |
| CHEMBL1173032 | — | — | 1 | - |
| CHEMBL1173808 | — | — | 1 | - |
| CHEMBL1173807 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18661 | IMMEPIP | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL1098230 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL1172774 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1172579 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1170855 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL1169687 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL1172754 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL1172775 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL1173809 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1172712 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1172776 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1173390 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL1172753 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1171443 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL1173391 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL1173033 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL1173032 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1173808 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1173807 | — | Ki | > | 1000.0 | nM | - |