Assay Detail
Functional
CHEMBL692770
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In vitro antagonistic activity tested against Histamine H3 receptor on synaptosomes from rat cerebral cortex
22
Total Activities
22
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 | 22 | 7.59 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.40 |
| CHEMBL19010 | IODOPROXYFAN | — | 1 | 8.30 |
| CHEMBL281187 | — | — | 1 | 8.20 |
| CHEMBL16874 | — | — | 1 | 8.00 |
| CHEMBL19172 | — | — | 1 | 7.90 |
| CHEMBL16496 | — | — | 1 | 7.90 |
| CHEMBL277227 | — | — | 1 | 7.90 |
| CHEMBL20064 | — | — | 1 | 7.80 |
| CHEMBL440788 | — | — | 1 | 7.80 |
| CHEMBL21230 | — | — | 1 | 7.70 |
| CHEMBL20295 | — | — | 1 | 7.70 |
| CHEMBL282688 | — | — | 1 | 7.60 |
| CHEMBL20328 | — | — | 1 | 7.60 |
| CHEMBL20211 | — | — | 1 | 7.50 |
| CHEMBL20686 | — | — | 1 | 7.50 |
| CHEMBL20191 | — | — | 1 | 7.40 |
| CHEMBL20338 | — | — | 1 | 7.40 |
| CHEMBL423473 | — | — | 1 | 7.30 |
| CHEMBL12608 | IMPROMIDINE | 2.0 | 1 | 7.20 |
| CHEMBL20357 | — | — | 1 | 6.80 |
| CHEMBL20147 | — | — | 1 | 6.60 |
| CHEMBL555594 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL19010 | IODOPROXYFAN | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL281187 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL16874 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL19172 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL16496 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL277227 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL20064 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL440788 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL21230 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL20295 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL282688 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL20328 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL20211 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL20686 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL20191 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL20338 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL423473 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL12608 | IMPROMIDINE | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL20357 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL20147 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL555594 | — | Ki | = | 398.11 | nM | 6.40 |