Assay Detail
Functional
CHEMBL953166
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at histamine H2 receptor in guinea pig spontaneously beating right atrium assessed as positive chronotropic activity
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Cardiac atrium |
| 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 |
|---|---|---|---|
| EC50 | 34 | 6.95 | 8.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL293802 | ARPROMIDINE | 2.0 | 1 | 8.01 |
| CHEMBL483406 | — | — | 1 | 7.80 |
| CHEMBL12608 | IMPROMIDINE | 2.0 | 1 | 7.70 |
| CHEMBL471413 | — | — | 1 | 7.55 |
| CHEMBL513056 | — | — | 1 | 7.51 |
| CHEMBL472273 | — | — | 1 | 7.47 |
| CHEMBL501589 | — | — | 1 | 7.42 |
| CHEMBL502339 | — | — | 1 | 7.42 |
| CHEMBL472441 | — | — | 1 | 7.42 |
| CHEMBL472039 | — | — | 1 | 7.41 |
| CHEMBL486153 | — | — | 1 | 7.32 |
| CHEMBL513755 | — | — | 1 | 7.30 |
| CHEMBL472272 | — | — | 1 | 7.29 |
| CHEMBL512716 | — | — | 1 | 7.27 |
| CHEMBL469749 | — | — | 1 | 7.26 |
| CHEMBL486962 | — | — | 1 | 7.25 |
| CHEMBL486974 | — | — | 1 | 7.21 |
| CHEMBL486965 | — | — | 1 | 7.17 |
| CHEMBL470563 | — | — | 1 | 7.01 |
| CHEMBL485958 | — | — | 1 | 7.00 |
| CHEMBL486964 | — | — | 1 | 6.86 |
| CHEMBL470790 | — | — | 1 | 6.78 |
| CHEMBL499092 | — | — | 1 | 6.74 |
| CHEMBL513883 | — | — | 1 | 6.69 |
| CHEMBL472054 | — | — | 1 | 6.51 |
| CHEMBL486746 | — | — | 1 | 6.43 |
| CHEMBL513039 | — | — | 1 | 6.40 |
| CHEMBL486963 | — | — | 1 | 6.33 |
| CHEMBL499301 | — | — | 1 | 6.19 |
| CHEMBL472271 | — | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL293802 | ARPROMIDINE | EC50 | = | 9.772 | nM | 8.01 |
| CHEMBL483406 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL12608 | IMPROMIDINE | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL471413 | — | EC50 | = | 28.18 | nM | 7.55 |
| CHEMBL513056 | — | EC50 | = | 30.9 | nM | 7.51 |
| CHEMBL472273 | — | EC50 | = | 33.88 | nM | 7.47 |
| CHEMBL501589 | — | EC50 | = | 38.02 | nM | 7.42 |
| CHEMBL502339 | — | EC50 | = | 38.02 | nM | 7.42 |
| CHEMBL472441 | — | EC50 | = | 38.02 | nM | 7.42 |
| CHEMBL472039 | — | EC50 | = | 38.9 | nM | 7.41 |
| CHEMBL486153 | — | EC50 | = | 47.86 | nM | 7.32 |
| CHEMBL513755 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL472272 | — | EC50 | = | 51.29 | nM | 7.29 |
| CHEMBL512716 | — | EC50 | = | 53.7 | nM | 7.27 |
| CHEMBL469749 | — | EC50 | = | 54.95 | nM | 7.26 |
| CHEMBL486962 | — | EC50 | = | 56.23 | nM | 7.25 |
| CHEMBL486974 | — | EC50 | = | 61.66 | nM | 7.21 |
| CHEMBL486965 | — | EC50 | = | 67.61 | nM | 7.17 |
| CHEMBL470563 | — | EC50 | = | 97.72 | nM | 7.01 |
| CHEMBL485958 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL486964 | — | EC50 | = | 138.04 | nM | 6.86 |
| CHEMBL470790 | — | EC50 | = | 165.96 | nM | 6.78 |
| CHEMBL499092 | — | EC50 | = | 181.97 | nM | 6.74 |
| CHEMBL513883 | — | EC50 | = | 204.17 | nM | 6.69 |
| CHEMBL472054 | — | EC50 | = | 309.03 | nM | 6.51 |
| CHEMBL486746 | — | EC50 | = | 371.54 | nM | 6.43 |
| CHEMBL513039 | — | EC50 | = | 398.11 | nM | 6.40 |
| CHEMBL486963 | — | EC50 | = | 467.74 | nM | 6.33 |
| CHEMBL499301 | — | EC50 | = | 645.65 | nM | 6.19 |
| CHEMBL472271 | — | EC50 | = | 776.25 | nM | 6.11 |
| CHEMBL90 | HISTAMINE | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL469748 | — | EC50 | = | 1047.13 | nM | 5.98 |
| CHEMBL111988 | — | EC50 | = | 1174.9 | nM | 5.93 |
| CHEMBL470564 | — | EC50 | = | 3630.78 | nM | 5.44 |