Assay Detail
Functional
CHEMBL986305
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Antagonist activity at mouse histamine H4 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced intracellular calcium elevation by FLIPR assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| 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 | 10 | 7.83 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129198 | JNJ-7777120 | — | 1 | 8.62 |
| CHEMBL521996 | — | — | 1 | 8.36 |
| CHEMBL523225 | — | — | 1 | 8.32 |
| CHEMBL502347 | — | — | 1 | 8.24 |
| CHEMBL522673 | — | — | 1 | 8.04 |
| CHEMBL503605 | — | — | 1 | 7.75 |
| CHEMBL509540 | — | — | 1 | 7.74 |
| CHEMBL492231 | — | — | 1 | 7.34 |
| CHEMBL494890 | — | — | 1 | 6.99 |
| CHEMBL494678 | — | — | 1 | 6.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129198 | JNJ-7777120 | EC50 | = | 2.399 | nM | 8.62 |
| CHEMBL521996 | — | EC50 | = | 4.365 | nM | 8.36 |
| CHEMBL523225 | — | EC50 | = | 4.786 | nM | 8.32 |
| CHEMBL502347 | — | EC50 | = | 5.754 | nM | 8.24 |
| CHEMBL522673 | — | EC50 | = | 9.12 | nM | 8.04 |
| CHEMBL503605 | — | EC50 | = | 17.78 | nM | 7.75 |
| CHEMBL509540 | — | EC50 | = | 18.2 | nM | 7.74 |
| CHEMBL492231 | — | EC50 | = | 45.71 | nM | 7.34 |
| CHEMBL494890 | — | EC50 | = | 102.33 | nM | 6.99 |
| CHEMBL494678 | — | EC50 | = | 123.03 | nM | 6.91 |