Assay Detail
Binding
CHEMBL694992
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Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cardiac atrium |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Conformational requirements for histamine H2-receptor inhibitors: a structure-activity study of phenylene analogues related to cimetidine and tiotidine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 5.97 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL269646 | TIOTIDINE | 2.0 | 1 | 7.50 |
| CHEMBL33850 | — | — | 1 | 6.70 |
| CHEMBL284743 | — | — | 1 | 6.50 |
| CHEMBL441965 | — | — | 1 | 6.50 |
| CHEMBL284556 | — | — | 1 | 6.40 |
| CHEMBL30 | CIMETIDINE | 4.0 | 1 | 6.30 |
| CHEMBL284379 | — | — | 1 | 6.10 |
| CHEMBL33996 | — | — | 1 | 4.80 |
| CHEMBL33108 | — | — | 1 | 4.50 |
| CHEMBL32409 | — | — | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL269646 | TIOTIDINE | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL33850 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL284743 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL441965 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL284556 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL30 | CIMETIDINE | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL284379 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL33996 | — | Ki | = | 15848.93 | nM | 4.80 |
| CHEMBL33108 | — | Ki | = | 31622.78 | nM | 4.50 |
| CHEMBL32409 | — | Ki | = | 39810.72 | nM | 4.40 |