Assay Detail
Functional
CHEMBL4815481
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
30
Total Activities
30
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H<sub>2</sub>R and D<sub>3</sub>R.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 6.41 | 7.34 |
| pEC50 | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4856059 | — | — | 1 | 7.34 |
| CHEMBL4875600 | — | — | 1 | 7.19 |
| CHEMBL4853668 | — | — | 1 | 7.07 |
| CHEMBL4856005 | — | — | 1 | 7.00 |
| CHEMBL4853107 | — | — | 1 | 6.88 |
| CHEMBL4856572 | — | — | 1 | 6.80 |
| CHEMBL4864067 | — | — | 1 | 6.78 |
| CHEMBL4874758 | — | — | 1 | 6.77 |
| CHEMBL4860528 | — | — | 1 | 6.75 |
| CHEMBL4846638 | — | — | 1 | 6.65 |
| CHEMBL4846380 | — | — | 1 | 6.63 |
| CHEMBL4848815 | — | — | 1 | 6.57 |
| CHEMBL4871482 | — | — | 1 | 6.55 |
| CHEMBL4857560 | — | — | 1 | 6.52 |
| CHEMBL4876025 | — | — | 1 | 6.48 |
| CHEMBL4865765 | — | — | 1 | 6.45 |
| CHEMBL4853772 | — | — | 1 | 6.43 |
| CHEMBL4876743 | — | — | 1 | 6.41 |
| CHEMBL4846201 | — | — | 1 | 5.60 |
| CHEMBL4858567 | — | — | 1 | 5.47 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 5.42 |
| CHEMBL4878215 | — | — | 1 | 5.36 |
| CHEMBL249420 | DEXPRAMIPEXOLE | 3.0 | 1 | 4.40 |
| CHEMBL4865670 | — | — | 1 | - |
| CHEMBL4872375 | — | — | 1 | - |
| CHEMBL4874969 | — | — | 1 | - |
| CHEMBL4863393 | — | — | 1 | - |
| CHEMBL4872277 | — | — | 1 | - |
| CHEMBL4871221 | — | — | 1 | - |
| CHEMBL4876799 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4856059 | — | EC50 | = | 45.71 | nM | 7.34 |
| CHEMBL4875600 | — | EC50 | = | 64.57 | nM | 7.19 |
| CHEMBL4853668 | — | EC50 | = | 85.11 | nM | 7.07 |
| CHEMBL4856005 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4853107 | — | EC50 | = | 131.83 | nM | 6.88 |
| CHEMBL4856572 | — | EC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4864067 | — | EC50 | = | 165.96 | nM | 6.78 |
| CHEMBL4874758 | — | EC50 | = | 169.82 | nM | 6.77 |
| CHEMBL4860528 | — | EC50 | = | 177.83 | nM | 6.75 |
| CHEMBL4846638 | — | EC50 | = | 223.87 | nM | 6.65 |
| CHEMBL4846380 | — | EC50 | = | 234.42 | nM | 6.63 |
| CHEMBL4848815 | — | EC50 | = | 269.15 | nM | 6.57 |
| CHEMBL4871482 | — | EC50 | = | 281.84 | nM | 6.55 |
| CHEMBL4857560 | — | EC50 | = | 302.0 | nM | 6.52 |
| CHEMBL4876025 | — | EC50 | = | 331.13 | nM | 6.48 |
| CHEMBL4865765 | — | EC50 | = | 354.81 | nM | 6.45 |
| CHEMBL4853772 | — | EC50 | = | 371.54 | nM | 6.43 |
| CHEMBL4876743 | — | EC50 | = | 389.05 | nM | 6.41 |
| CHEMBL4846201 | — | EC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4858567 | — | EC50 | = | 3388.44 | nM | 5.47 |
| CHEMBL90 | HISTAMINE | EC50 | = | 3801.89 | nM | 5.42 |
| CHEMBL4878215 | — | EC50 | = | 4365.16 | nM | 5.36 |
| CHEMBL249420 | DEXPRAMIPEXOLE | EC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL4865670 | — | pEC50 | - | — | - | |
| CHEMBL4872375 | — | pEC50 | - | — | - | |
| CHEMBL4874969 | — | pEC50 | - | — | - | |
| CHEMBL4863393 | — | pEC50 | - | — | - | |
| CHEMBL4872277 | — | pEC50 | - | — | - | |
| CHEMBL4871221 | — | pEC50 | - | — | - | |
| CHEMBL4876799 | — | pEC50 | - | — | - |