Assay Detail
Functional
CHEMBL1015363
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Agonist activity at histamine H2 receptor in guinea pig atrium assessed as increase in heart rate
10
Total Activities
10
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
N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 6.57 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL483406 | — | — | 1 | 7.80 |
| CHEMBL514641 | — | — | 1 | 7.11 |
| CHEMBL471724 | — | — | 1 | 6.96 |
| CHEMBL474447 | — | — | 1 | 6.74 |
| CHEMBL465170 | — | — | 1 | 6.73 |
| CHEMBL475621 | — | — | 1 | 6.52 |
| CHEMBL475620 | — | — | 1 | 6.31 |
| CHEMBL443896 | — | — | 1 | 6.09 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 6.00 |
| CHEMBL474617 | — | — | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL483406 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL514641 | — | EC50 | = | 77.62 | nM | 7.11 |
| CHEMBL471724 | — | EC50 | = | 109.65 | nM | 6.96 |
| CHEMBL474447 | — | EC50 | = | 181.97 | nM | 6.74 |
| CHEMBL465170 | — | EC50 | = | 186.21 | nM | 6.73 |
| CHEMBL475621 | — | EC50 | = | 302.0 | nM | 6.52 |
| CHEMBL475620 | — | EC50 | = | 489.78 | nM | 6.31 |
| CHEMBL443896 | — | EC50 | = | 812.83 | nM | 6.09 |
| CHEMBL90 | HISTAMINE | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL474617 | — | EC50 | = | 3548.13 | nM | 5.45 |