Assay Detail
Binding
CHEMBL1103488
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]histamine dihydrochloride from human histamine H4 receptor after 2.5 hrs by scintillation proximity assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.60 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1091874 | — | — | 1 | 9.00 |
| CHEMBL1091875 | — | — | 1 | 7.89 |
| CHEMBL1093180 | — | — | 1 | 7.72 |
| CHEMBL1088859 | — | — | 1 | 7.52 |
| CHEMBL1090190 | — | — | 1 | 7.48 |
| CHEMBL1091558 | — | — | 1 | 7.43 |
| CHEMBL1092542 | — | — | 1 | 7.08 |
| CHEMBL1091729 | — | — | 1 | 7.07 |
| CHEMBL1091569 | — | — | 1 | 7.06 |
| CHEMBL1093439 | — | — | 1 | 7.05 |
| CHEMBL1088889 | — | — | 1 | 7.02 |
| CHEMBL1092332 | — | — | 1 | 6.96 |
| CHEMBL1090532 | — | — | 1 | 6.90 |
| CHEMBL1092064 | — | — | 1 | 6.77 |
| CHEMBL1092933 | — | — | 1 | 6.77 |
| CHEMBL1090655 | — | — | 1 | 6.63 |
| CHEMBL1090531 | — | — | 1 | 6.54 |
| CHEMBL1093138 | — | — | 1 | 6.51 |
| CHEMBL1092934 | — | — | 1 | 6.36 |
| CHEMBL1093438 | — | — | 1 | 6.00 |
| CHEMBL1090520 | — | — | 1 | 5.85 |
| CHEMBL1090519 | — | — | 1 | 5.85 |
| CHEMBL1091559 | — | — | 1 | 5.80 |
| CHEMBL1092330 | — | — | 1 | 5.72 |
| CHEMBL1092880 | — | — | 1 | 5.21 |
| CHEMBL1092331 | — | — | 1 | 5.00 |
| CHEMBL1092543 | — | — | 1 | 4.85 |
| CHEMBL1088888 | — | — | 1 | 4.68 |
| CHEMBL1092881 | — | — | 1 | - |
| CHEMBL1089167 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1091874 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1091875 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1093180 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1088859 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1090190 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1091558 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1092542 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL1091729 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL1091569 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL1093439 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1088889 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL1092332 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL1090532 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL1092064 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL1092933 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL1090655 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL1090531 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL1093138 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1092934 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1093438 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1090520 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1090519 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1091559 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1092330 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL1092880 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL1092331 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1092543 | — | IC50 | = | 14200.0 | nM | 4.85 |
| CHEMBL1088888 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL1092881 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1089167 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1076867 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1089166 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1091568 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1093139 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1091567 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1091389 | — | IC50 | > | 10000.0 | nM | - |