Assay Detail
Binding
CHEMBL691842
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Binding affinity towards Histamine H3 receptor on synaptosomes from rat cerebral cortex
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 21 | 7.93 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19010 | IODOPROXYFAN | — | 1 | 9.00 |
| CHEMBL19172 | — | — | 1 | 8.90 |
| CHEMBL281187 | — | — | 1 | 8.90 |
| CHEMBL440788 | — | — | 1 | 8.60 |
| CHEMBL21230 | — | — | 1 | 8.50 |
| CHEMBL20328 | — | — | 1 | 8.40 |
| CHEMBL20211 | — | — | 1 | 8.30 |
| CHEMBL20064 | — | — | 1 | 8.10 |
| CHEMBL16874 | — | — | 1 | 8.10 |
| CHEMBL20686 | — | — | 1 | 8.10 |
| CHEMBL20295 | — | — | 1 | 8.10 |
| CHEMBL277227 | — | — | 1 | 7.90 |
| CHEMBL16496 | — | — | 1 | 7.90 |
| CHEMBL20191 | — | — | 1 | 7.70 |
| CHEMBL282688 | — | — | 1 | 7.60 |
| CHEMBL20338 | — | — | 1 | 7.50 |
| CHEMBL20357 | — | — | 1 | 7.50 |
| CHEMBL12608 | IMPROMIDINE | 2.0 | 1 | 7.40 |
| CHEMBL423473 | — | — | 1 | 7.10 |
| CHEMBL20147 | — | — | 1 | 6.70 |
| CHEMBL555594 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19010 | IODOPROXYFAN | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL19172 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL281187 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL440788 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL21230 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL20328 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL20211 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL20064 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL16874 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL20686 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL20295 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL277227 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL16496 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL20191 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL282688 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL20338 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL20357 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL12608 | IMPROMIDINE | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL423473 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL20147 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL555594 | — | Ki | = | 630.96 | nM | 6.20 |