Assay Detail
Binding
CHEMBL693558
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Inhibition of [3H]- N-alpha-methylhistamine from histamine H3 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.48 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | — | 1 | 9.74 |
| CHEMBL15075 | VERONGAMINE | — | 1 | 9.30 |
| CHEMBL280076 | — | — | 1 | 9.10 |
| CHEMBL274977 | — | — | 1 | 9.02 |
| CHEMBL14722 | — | — | 1 | 9.00 |
| CHEMBL15000 | — | — | 1 | 8.54 |
| CHEMBL14811 | — | — | 1 | 8.46 |
| CHEMBL14497 | — | — | 1 | 8.43 |
| CHEMBL276798 | GR-175737 | — | 1 | 8.15 |
| CHEMBL276804 | — | — | 1 | 7.57 |
| CHEMBL14812 | GT-2016 | — | 1 | 7.40 |
| CHEMBL14721 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL15075 | VERONGAMINE | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL280076 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL274977 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL14722 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL15000 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL14811 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL14497 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL276798 | GR-175737 | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL276804 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL14812 | GT-2016 | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL14721 | — | Ki | = | 79.0 | nM | 7.10 |