Assay Detail
Binding
CHEMBL1048581
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]histamine from human histamine H4 receptor expressed in Sf9 cells co-expressing Galphai2 and Gbeta1gamma2
37
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 6.39 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL595180 | — | — | 2 | 7.94 |
| CHEMBL129198 | JNJ-7777120 | — | 1 | 7.85 |
| CHEMBL594721 | — | — | 2 | 7.77 |
| CHEMBL594731 | — | — | 2 | 7.63 |
| CHEMBL593103 | — | — | 2 | 7.37 |
| CHEMBL594022 | — | — | 1 | 7.15 |
| CHEMBL492677 | — | — | 1 | 7.01 |
| CHEMBL594490 | — | — | 1 | 6.84 |
| CHEMBL595215 | — | — | 1 | 6.82 |
| CHEMBL609161 | — | — | 1 | 6.69 |
| CHEMBL596551 | — | — | 1 | 6.62 |
| CHEMBL594491 | — | — | 1 | 6.61 |
| CHEMBL594949 | — | — | 1 | 6.55 |
| CHEMBL595639 | — | — | 1 | 6.54 |
| CHEMBL473662 | — | — | 1 | 6.54 |
| CHEMBL609289 | — | — | 1 | 6.47 |
| CHEMBL596562 | — | — | 1 | 6.38 |
| CHEMBL595880 | — | — | 1 | 6.27 |
| CHEMBL608717 | — | — | 1 | 6.27 |
| CHEMBL593551 | — | — | 1 | 6.14 |
| CHEMBL612131 | — | — | 1 | 5.92 |
| CHEMBL610626 | — | — | 1 | 5.66 |
| CHEMBL594973 | — | — | 1 | 5.60 |
| CHEMBL608864 | — | — | 1 | 5.47 |
| CHEMBL594729 | — | — | 1 | 5.46 |
| CHEMBL594730 | — | — | 1 | 5.18 |
| CHEMBL596348 | — | — | 1 | 5.09 |
| CHEMBL595413 | — | — | 1 | 4.86 |
| CHEMBL594468 | — | — | 1 | 4.84 |
| CHEMBL594694 | — | — | 1 | 4.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL595180 | — | Ki | = | 11.48 | nM | 7.94 |
| CHEMBL595180 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL129198 | JNJ-7777120 | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL594721 | — | Ki | = | 16.98 | nM | 7.77 |
| CHEMBL594721 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL594731 | — | Ki | = | 23.44 | nM | 7.63 |
| CHEMBL594731 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL593103 | — | Ki | = | 42.66 | nM | 7.37 |
| CHEMBL593103 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL594022 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL492677 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL594490 | — | Ki | = | 146.0 | nM | 6.84 |
| CHEMBL595215 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL609161 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL596551 | — | Ki | = | 237.0 | nM | 6.62 |
| CHEMBL594491 | — | Ki | = | 248.0 | nM | 6.61 |
| CHEMBL594949 | — | Ki | = | 282.0 | nM | 6.55 |
| CHEMBL595639 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL473662 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL609289 | — | Ki | = | 341.0 | nM | 6.47 |
| CHEMBL596562 | — | Ki | = | 417.0 | nM | 6.38 |
| CHEMBL608717 | — | Ki | = | 542.0 | nM | 6.27 |
| CHEMBL595880 | — | Ki | = | 538.0 | nM | 6.27 |
| CHEMBL593551 | — | Ki | = | 716.0 | nM | 6.14 |
| CHEMBL612131 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL610626 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL594973 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL608864 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL594729 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL594730 | — | Ki | = | 6600.0 | nM | 5.18 |
| CHEMBL596348 | — | Ki | = | 8100.0 | nM | 5.09 |
| CHEMBL595413 | — | Ki | = | 13700.0 | nM | 4.86 |
| CHEMBL594468 | — | Ki | = | 14300.0 | nM | 4.84 |
| CHEMBL594694 | — | Ki | = | 15600.0 | nM | 4.81 |
| CHEMBL594152 | — | Ki | = | 18400.0 | nM | 4.74 |
| CHEMBL593448 | — | Ki | = | 35000.0 | nM | 4.46 |
| CHEMBL594266 | — | Ki | = | 376600.0 | nM | - |