Assay Detail
Functional
CHEMBL698413
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antagonistic activity tested against Histamine H3 receptor on synaptosomes from rat cerebral cortex
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
[125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.62 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19010 | IODOPROXYFAN | — | 1 | 8.30 |
| CHEMBL281187 | — | — | 1 | 8.15 |
| CHEMBL16874 | — | — | 1 | 7.96 |
| CHEMBL16496 | — | — | 1 | 7.92 |
| CHEMBL19172 | — | — | 1 | 7.85 |
| CHEMBL277227 | — | — | 1 | 7.85 |
| CHEMBL20064 | — | — | 1 | 7.80 |
| CHEMBL440788 | — | — | 1 | 7.77 |
| CHEMBL20295 | — | — | 1 | 7.70 |
| CHEMBL21230 | — | — | 1 | 7.66 |
| CHEMBL282688 | — | — | 1 | 7.60 |
| CHEMBL20328 | — | — | 1 | 7.60 |
| CHEMBL20211 | — | — | 1 | 7.52 |
| CHEMBL20686 | — | — | 1 | 7.46 |
| CHEMBL20191 | — | — | 1 | 7.41 |
| CHEMBL20338 | — | — | 1 | 7.39 |
| CHEMBL423473 | — | — | 1 | 7.33 |
| CHEMBL20357 | — | — | 1 | 6.84 |
| CHEMBL20147 | — | — | 1 | 6.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19010 | IODOPROXYFAN | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL281187 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL16874 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL16496 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL19172 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL277227 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL20064 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL440788 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL20295 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL21230 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL282688 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL20328 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL20211 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL20686 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL20191 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL20338 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL423473 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL20357 | — | Ki | = | 146.0 | nM | 6.84 |
| CHEMBL20147 | — | Ki | = | 232.0 | nM | 6.63 |