Assay Detail
Functional
CHEMBL956577
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Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| 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 | 9.30 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL508712 | — | — | 1 | 10.00 |
| CHEMBL453893 | — | — | 1 | 9.74 |
| CHEMBL488249 | — | — | 1 | 9.66 |
| CHEMBL454642 | — | — | 1 | 9.60 |
| CHEMBL507360 | — | — | 1 | 9.51 |
| CHEMBL453654 | — | — | 1 | 9.51 |
| CHEMBL487059 | — | — | 1 | 9.51 |
| CHEMBL454879 | — | — | 1 | 9.47 |
| CHEMBL487230 | — | — | 1 | 9.33 |
| CHEMBL453892 | — | — | 1 | 9.32 |
| CHEMBL453653 | — | — | 1 | 9.27 |
| CHEMBL488248 | — | — | 1 | 9.17 |
| CHEMBL453894 | — | — | 1 | 9.15 |
| CHEMBL455681 | — | — | 1 | 9.13 |
| CHEMBL488251 | — | — | 1 | 9.06 |
| CHEMBL519067 | — | — | 1 | 9.06 |
| CHEMBL487064 | — | — | 1 | 8.92 |
| CHEMBL487060 | — | — | 1 | 8.80 |
| CHEMBL487063 | — | — | 1 | 8.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL508712 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL453893 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL488249 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL454642 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL507360 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL453654 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL487059 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL454879 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL487230 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL453892 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL453653 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL488248 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL453894 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL455681 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL488251 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL519067 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL487064 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL487060 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL487063 | — | IC50 | = | 3.1 | nM | 8.51 |