Assay Detail
Functional
CHEMBL1104101
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Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay
16
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 5.54 | 6.42 |
| pKb | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1078746 | — | — | 1 | 6.42 |
| CHEMBL1078359 | — | — | 2 | 6.36 |
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 5.92 |
| CHEMBL1078358 | — | — | 1 | 5.70 |
| CHEMBL275443 | 4-METHYLHISTAMINE | — | 1 | 5.54 |
| CHEMBL1080772 | — | — | 1 | 5.41 |
| CHEMBL1078529 | — | — | 1 | 5.14 |
| CHEMBL1078212 | — | — | 1 | 5.05 |
| CHEMBL1077596 | — | — | 1 | 4.92 |
| CHEMBL1078747 | — | — | 1 | 4.92 |
| CHEMBL1078210 | — | — | 1 | 4.85 |
| CHEMBL1081318 | — | — | 1 | - |
| CHEMBL1078357 | — | — | 1 | - |
| CHEMBL1081319 | — | — | 1 | - |
| CHEMBL1078105 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1078746 | — | EC50 | = | 380.19 | nM | 6.42 |
| CHEMBL1078359 | — | EC50 | = | 436.52 | nM | 6.36 |
| CHEMBL1078359 | — | EC50 | = | 645.65 | nM | 6.19 |
| CHEMBL90 | HISTAMINE | EC50 | = | 1202.26 | nM | 5.92 |
| CHEMBL1078358 | — | EC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL275443 | 4-METHYLHISTAMINE | EC50 | = | 2884.03 | nM | 5.54 |
| CHEMBL1080772 | — | EC50 | = | 3890.45 | nM | 5.41 |
| CHEMBL1078529 | — | EC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL1078212 | — | EC50 | = | 8912.51 | nM | 5.05 |
| CHEMBL1077596 | — | EC50 | = | 12022.64 | nM | 4.92 |
| CHEMBL1078747 | — | EC50 | = | 12022.64 | nM | 4.92 |
| CHEMBL1078210 | — | EC50 | = | 14125.38 | nM | 4.85 |
| CHEMBL1081318 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1078357 | — | pKb | = | 5.8 | — | - |
| CHEMBL1081319 | — | pKb | < | 5.0 | — | - |
| CHEMBL1078105 | — | pKb | < | 5.0 | — | - |