Assay Detail
Functional
CHEMBL2166522
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Agonist activity at guinea pig H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay
25
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The bivalent ligand approach leads to highly potent and selective acylguanidine-type histamine H₂ receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 25 | 8.14 | 9.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2165632 | — | — | 2 | 9.41 |
| CHEMBL2165628 | — | — | 2 | 9.29 |
| CHEMBL2165630 | — | — | 2 | 9.20 |
| CHEMBL2165642 | — | — | 1 | 8.94 |
| CHEMBL2165636 | — | — | 1 | 8.87 |
| CHEMBL2165647 | — | — | 1 | 8.59 |
| CHEMBL2165633 | — | — | 1 | 8.57 |
| CHEMBL2165631 | — | — | 1 | 8.56 |
| CHEMBL2165641 | — | — | 1 | 8.49 |
| CHEMBL2165645 | — | — | 1 | 8.46 |
| CHEMBL2165637 | — | — | 1 | 8.30 |
| CHEMBL2165629 | — | — | 1 | 7.99 |
| CHEMBL2165640 | — | — | 1 | 7.96 |
| CHEMBL2165646 | — | — | 1 | 7.80 |
| CHEMBL2165643 | — | — | 1 | 7.70 |
| CHEMBL2165644 | — | — | 1 | 7.46 |
| CHEMBL2165634 | — | — | 1 | 7.46 |
| CHEMBL2165638 | — | — | 1 | 7.23 |
| CHEMBL293762 | AMTHAMINE | — | 1 | 6.72 |
| CHEMBL2165639 | — | — | 1 | 6.69 |
| CHEMBL2165635 | — | — | 1 | 6.48 |
| CHEMBL1533310 | HISTAMINE DIHYDROCHLORIDE | 4.0 | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2165632 | — | EC50 | = | 0.39 | nM | 9.41 |
| CHEMBL2165628 | — | EC50 | = | 0.51 | nM | 9.29 |
| CHEMBL2165628 | — | EC50 | = | 0.5129 | nM | 9.29 |
| CHEMBL2165630 | — | EC50 | = | 0.631 | nM | 9.20 |
| CHEMBL2165630 | — | EC50 | = | 0.63 | nM | 9.20 |
| CHEMBL2165632 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2165642 | — | EC50 | = | 1.148 | nM | 8.94 |
| CHEMBL2165636 | — | EC50 | = | 1.349 | nM | 8.87 |
| CHEMBL2165647 | — | EC50 | = | 2.57 | nM | 8.59 |
| CHEMBL2165633 | — | EC50 | = | 2.692 | nM | 8.57 |
| CHEMBL2165631 | — | EC50 | = | 2.754 | nM | 8.56 |
| CHEMBL2165641 | — | EC50 | = | 3.236 | nM | 8.49 |
| CHEMBL2165645 | — | EC50 | = | 3.467 | nM | 8.46 |
| CHEMBL2165637 | — | EC50 | = | 5.012 | nM | 8.30 |
| CHEMBL2165629 | — | EC50 | = | 10.23 | nM | 7.99 |
| CHEMBL2165640 | — | EC50 | = | 10.96 | nM | 7.96 |
| CHEMBL2165646 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL2165643 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL2165634 | — | EC50 | = | 34.67 | nM | 7.46 |
| CHEMBL2165644 | — | EC50 | = | 34.67 | nM | 7.46 |
| CHEMBL2165638 | — | EC50 | = | 58.88 | nM | 7.23 |
| CHEMBL293762 | AMTHAMINE | EC50 | = | 190.55 | nM | 6.72 |
| CHEMBL2165639 | — | EC50 | = | 204.17 | nM | 6.69 |
| CHEMBL2165635 | — | EC50 | = | 331.13 | nM | 6.48 |
| CHEMBL1533310 | HISTAMINE DIHYDROCHLORIDE | EC50 | = | 1202.26 | nM | 5.92 |