Assay Detail
Functional
CHEMBL986303
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Antagonist activity at rat histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
18
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 15 | 7.71 | 8.59 |
| pKb | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129198 | JNJ-7777120 | — | 1 | 8.59 |
| CHEMBL523225 | — | — | 1 | 8.22 |
| CHEMBL521996 | — | — | 1 | 8.18 |
| CHEMBL522673 | — | — | 1 | 8.03 |
| CHEMBL502347 | — | — | 1 | 8.00 |
| CHEMBL509540 | — | — | 1 | 7.83 |
| CHEMBL494093 | — | — | 1 | 7.81 |
| CHEMBL446269 | — | — | 1 | 7.72 |
| CHEMBL521995 | — | — | 1 | 7.70 |
| CHEMBL493281 | — | — | 1 | 7.62 |
| CHEMBL503605 | — | — | 1 | 7.51 |
| CHEMBL492884 | — | — | 1 | 7.40 |
| CHEMBL492231 | — | — | 1 | 7.26 |
| CHEMBL494678 | — | — | 1 | 7.23 |
| CHEMBL494890 | — | — | 1 | 6.61 |
| CHEMBL494683 | — | — | 1 | - |
| CHEMBL522989 | — | — | 1 | - |
| CHEMBL492232 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129198 | JNJ-7777120 | EC50 | = | 2.57 | nM | 8.59 |
| CHEMBL523225 | — | EC50 | = | 6.026 | nM | 8.22 |
| CHEMBL521996 | — | EC50 | = | 6.607 | nM | 8.18 |
| CHEMBL522673 | — | EC50 | = | 9.333 | nM | 8.03 |
| CHEMBL502347 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL509540 | — | EC50 | = | 14.79 | nM | 7.83 |
| CHEMBL494093 | — | EC50 | = | 15.49 | nM | 7.81 |
| CHEMBL446269 | — | EC50 | = | 19.05 | nM | 7.72 |
| CHEMBL521995 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL493281 | — | EC50 | = | 23.99 | nM | 7.62 |
| CHEMBL503605 | — | EC50 | = | 30.9 | nM | 7.51 |
| CHEMBL492884 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL492231 | — | EC50 | = | 54.95 | nM | 7.26 |
| CHEMBL494678 | — | EC50 | = | 58.88 | nM | 7.23 |
| CHEMBL494890 | — | EC50 | = | 245.47 | nM | 6.61 |
| CHEMBL494683 | — | pKb | = | 7.25 | — | - |
| CHEMBL522989 | — | pKb | = | 7.5 | — | - |
| CHEMBL492232 | — | pKb | = | 7.66 | — | - |