Assay Detail
Binding
CHEMBL986308
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Displacement of [3H]histamine from rat histamine H4 receptor expressed in HEK293 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.07 | 8.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL523225 | — | — | 1 | 8.84 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 8.57 |
| CHEMBL522673 | — | — | 1 | 8.44 |
| CHEMBL502347 | — | — | 1 | 8.42 |
| CHEMBL503605 | — | — | 1 | 8.40 |
| CHEMBL492231 | — | — | 1 | 8.35 |
| CHEMBL521995 | — | — | 1 | 8.32 |
| CHEMBL521996 | — | — | 1 | 8.29 |
| CHEMBL494093 | — | — | 1 | 8.27 |
| CHEMBL509540 | — | — | 1 | 8.12 |
| CHEMBL493281 | — | — | 1 | 8.04 |
| CHEMBL492884 | — | — | 1 | 7.85 |
| CHEMBL494678 | — | — | 1 | 6.56 |
| CHEMBL494890 | — | — | 1 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL523225 | — | Ki | = | 1.445 | nM | 8.84 |
| CHEMBL129198 | JNJ-7777120 | Ki | = | 2.692 | nM | 8.57 |
| CHEMBL522673 | — | Ki | = | 3.631 | nM | 8.44 |
| CHEMBL502347 | — | Ki | = | 3.802 | nM | 8.42 |
| CHEMBL503605 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL492231 | — | Ki | = | 4.467 | nM | 8.35 |
| CHEMBL521995 | — | Ki | = | 4.786 | nM | 8.32 |
| CHEMBL521996 | — | Ki | = | 5.129 | nM | 8.29 |
| CHEMBL494093 | — | Ki | = | 5.37 | nM | 8.27 |
| CHEMBL509540 | — | Ki | = | 7.586 | nM | 8.12 |
| CHEMBL493281 | — | Ki | = | 9.12 | nM | 8.04 |
| CHEMBL492884 | — | Ki | = | 14.13 | nM | 7.85 |
| CHEMBL494678 | — | Ki | = | 275.42 | nM | 6.56 |
| CHEMBL494890 | — | Ki | = | 338.84 | nM | 6.47 |