Assay Detail
Binding
CHEMBL956579
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]prazosin from human adrenergic alpha1A receptor expressed in LMtk- cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LMtk- |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.42 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL488251 | — | — | 1 | 5.96 |
| CHEMBL519067 | — | — | 1 | 5.89 |
| CHEMBL487230 | — | — | 1 | 5.75 |
| CHEMBL488248 | — | — | 1 | 5.66 |
| CHEMBL487060 | — | — | 1 | 5.62 |
| CHEMBL487064 | — | — | 1 | 5.54 |
| CHEMBL453653 | — | — | 1 | 5.38 |
| CHEMBL454642 | — | — | 1 | 5.35 |
| CHEMBL453654 | — | — | 1 | 5.23 |
| CHEMBL455681 | — | — | 1 | 5.21 |
| CHEMBL488249 | — | — | 1 | 5.20 |
| CHEMBL487063 | — | — | 1 | 5.19 |
| CHEMBL453893 | — | — | 1 | 5.19 |
| CHEMBL487059 | — | — | 1 | 5.14 |
| CHEMBL508712 | — | — | 1 | 5.00 |
| CHEMBL454879 | — | — | 1 | - |
| CHEMBL453892 | — | — | 1 | - |
| CHEMBL453894 | — | — | 1 | - |
| CHEMBL507360 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL488251 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL519067 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL487230 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL488248 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL487060 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL487064 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL453653 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL454642 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL453654 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL455681 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL488249 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL487063 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL453893 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL487059 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL508712 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL454879 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL453892 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL453894 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL507360 | — | IC50 | > | 10000.0 | nM | - |