Assay Detail
Functional
CHEMBL1028279
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Agonist activity at human histamine H4 receptor expressed in HEK293 cells coexpressing Gqi5 protein assessed as calcium flux by FLIPR assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 6.41 | 7.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL494667 | — | — | 1 | 7.79 |
| CHEMBL507063 | — | — | 1 | 7.57 |
| CHEMBL493478 | — | — | 1 | 7.47 |
| CHEMBL501882 | — | — | 1 | 7.36 |
| CHEMBL492677 | — | — | 1 | 7.19 |
| CHEMBL495280 | — | — | 1 | 6.75 |
| CHEMBL492489 | — | — | 1 | 5.92 |
| CHEMBL493262 | — | — | 1 | 5.63 |
| CHEMBL448085 | — | — | 1 | 5.60 |
| CHEMBL493664 | — | — | 1 | 5.41 |
| CHEMBL495265 | — | — | 1 | 5.31 |
| CHEMBL449157 | — | — | 1 | 4.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL494667 | — | EC50 | = | 16.22 | nM | 7.79 |
| CHEMBL507063 | — | EC50 | = | 26.92 | nM | 7.57 |
| CHEMBL493478 | — | EC50 | = | 33.88 | nM | 7.47 |
| CHEMBL501882 | — | EC50 | = | 43.65 | nM | 7.36 |
| CHEMBL492677 | — | EC50 | = | 64.57 | nM | 7.19 |
| CHEMBL495280 | — | EC50 | = | 177.83 | nM | 6.75 |
| CHEMBL492489 | — | EC50 | = | 1202.26 | nM | 5.92 |
| CHEMBL493262 | — | EC50 | = | 2344.23 | nM | 5.63 |
| CHEMBL448085 | — | EC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL493664 | — | EC50 | = | 3890.45 | nM | 5.41 |
| CHEMBL495265 | — | EC50 | = | 4897.79 | nM | 5.31 |
| CHEMBL449157 | — | EC50 | = | 11481.54 | nM | 4.94 |