Assay Detail
Functional
CHEMBL953171
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 22 | 5.70 | 7.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL293802 | ARPROMIDINE | 2.0 | 1 | 7.65 |
| CHEMBL486963 | — | — | 1 | 6.25 |
| CHEMBL499092 | — | — | 1 | 6.24 |
| CHEMBL486746 | — | — | 1 | 6.13 |
| CHEMBL471413 | — | — | 1 | 6.13 |
| CHEMBL483406 | — | — | 1 | 5.87 |
| CHEMBL486962 | — | — | 1 | 5.74 |
| CHEMBL470790 | — | — | 1 | 5.67 |
| CHEMBL486965 | — | — | 1 | 5.66 |
| CHEMBL486964 | — | — | 1 | 5.63 |
| CHEMBL485958 | — | — | 1 | 5.61 |
| CHEMBL12608 | IMPROMIDINE | 2.0 | 1 | 5.47 |
| CHEMBL472273 | — | — | 1 | 5.43 |
| CHEMBL513056 | — | — | 1 | 5.37 |
| CHEMBL513755 | — | — | 1 | 5.33 |
| CHEMBL472441 | — | — | 1 | 5.33 |
| CHEMBL486153 | — | — | 1 | 5.29 |
| CHEMBL486974 | — | — | 1 | 5.21 |
| CHEMBL499301 | — | — | 1 | 5.01 |
| CHEMBL472272 | — | — | 1 | 4.95 |
| CHEMBL111988 | — | — | 1 | - |
| CHEMBL470564 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL293802 | ARPROMIDINE | Kd | = | 22.39 | nM | 7.65 |
| CHEMBL486963 | — | Kd | = | 562.34 | nM | 6.25 |
| CHEMBL499092 | — | Kd | = | 575.44 | nM | 6.24 |
| CHEMBL486746 | — | Kd | = | 741.31 | nM | 6.13 |
| CHEMBL471413 | — | Kd | = | 741.31 | nM | 6.13 |
| CHEMBL483406 | — | Kd | = | 1348.96 | nM | 5.87 |
| CHEMBL486962 | — | Kd | = | 1819.7 | nM | 5.74 |
| CHEMBL470790 | — | Kd | = | 2137.96 | nM | 5.67 |
| CHEMBL486965 | — | Kd | = | 2187.76 | nM | 5.66 |
| CHEMBL486964 | — | Kd | = | 2344.23 | nM | 5.63 |
| CHEMBL485958 | — | Kd | = | 2454.71 | nM | 5.61 |
| CHEMBL12608 | IMPROMIDINE | Kd | = | 3388.44 | nM | 5.47 |
| CHEMBL472273 | — | Kd | = | 3715.35 | nM | 5.43 |
| CHEMBL513056 | — | Kd | = | 4265.8 | nM | 5.37 |
| CHEMBL513755 | — | Kd | = | 4677.35 | nM | 5.33 |
| CHEMBL472441 | — | Kd | = | 4677.35 | nM | 5.33 |
| CHEMBL486153 | — | Kd | = | 5128.61 | nM | 5.29 |
| CHEMBL486974 | — | Kd | = | 6165.95 | nM | 5.21 |
| CHEMBL499301 | — | Kd | = | 9772.37 | nM | 5.01 |
| CHEMBL472272 | — | Kd | = | 11220.18 | nM | 4.95 |
| CHEMBL111988 | — | Kd | < | 10000.0 | nM | - |
| CHEMBL470564 | — | Kd | > | 10000.0 | nM | - |