Assay Detail
Binding
CHEMBL4383937
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Displacement of [3H]N-alpha-methylhistamine from full length recombinant human H3R expressed in HEK293 cell membranes after 90 mins by beta scintillation counting method
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization and preclinical evaluation of novel histamine H<sub>3</sub>receptor ligands: Acetyl and propionyl phenoxyalkyl piperazine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 6.20 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4449790 | — | — | 1 | 8.28 |
| CHEMBL4547780 | — | — | 1 | 7.99 |
| CHEMBL4593213 | — | — | 1 | 7.81 |
| CHEMBL4462632 | — | — | 1 | 6.94 |
| CHEMBL4532780 | — | — | 1 | 6.72 |
| CHEMBL4581913 | — | — | 1 | 6.50 |
| CHEMBL4448015 | — | — | 1 | 6.42 |
| CHEMBL4453714 | — | — | 1 | 6.30 |
| CHEMBL4473431 | — | — | 1 | 6.04 |
| CHEMBL4467220 | — | — | 1 | 5.91 |
| CHEMBL4526298 | — | — | 1 | 5.86 |
| CHEMBL4467342 | — | — | 1 | 5.86 |
| CHEMBL4465046 | — | — | 1 | 5.84 |
| CHEMBL4566960 | — | — | 1 | 5.79 |
| CHEMBL4445569 | — | — | 1 | 5.76 |
| CHEMBL4519189 | — | — | 1 | 5.63 |
| CHEMBL4578432 | — | — | 1 | 5.61 |
| CHEMBL4453108 | — | — | 1 | 5.47 |
| CHEMBL4471691 | — | — | 1 | 5.44 |
| CHEMBL4452580 | — | — | 1 | 5.43 |
| CHEMBL4451316 | — | — | 1 | 5.39 |
| CHEMBL4542051 | — | — | 1 | 5.31 |
| CHEMBL4545685 | — | — | 1 | - |
| CHEMBL4551195 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4449790 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL4547780 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL4593213 | — | Ki | = | 15.4 | nM | 7.81 |
| CHEMBL4462632 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL4532780 | — | Ki | = | 192.0 | nM | 6.72 |
| CHEMBL4581913 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL4448015 | — | Ki | = | 377.0 | nM | 6.42 |
| CHEMBL4453714 | — | Ki | = | 499.0 | nM | 6.30 |
| CHEMBL4473431 | — | Ki | = | 908.0 | nM | 6.04 |
| CHEMBL4467220 | — | Ki | = | 1230.0 | nM | 5.91 |
| CHEMBL4526298 | — | Ki | = | 1392.0 | nM | 5.86 |
| CHEMBL4467342 | — | Ki | = | 1392.0 | nM | 5.86 |
| CHEMBL4465046 | — | Ki | = | 1444.0 | nM | 5.84 |
| CHEMBL4566960 | — | Ki | = | 1634.0 | nM | 5.79 |
| CHEMBL4445569 | — | Ki | = | 1720.0 | nM | 5.76 |
| CHEMBL4519189 | — | Ki | = | 2316.0 | nM | 5.63 |
| CHEMBL4578432 | — | Ki | = | 2453.0 | nM | 5.61 |
| CHEMBL4453108 | — | Ki | = | 3390.0 | nM | 5.47 |
| CHEMBL4471691 | — | Ki | = | 3627.0 | nM | 5.44 |
| CHEMBL4452580 | — | Ki | = | 3697.0 | nM | 5.43 |
| CHEMBL4451316 | — | Ki | = | 4040.0 | nM | 5.39 |
| CHEMBL4542051 | — | Ki | = | 4889.0 | nM | 5.31 |
| CHEMBL4545685 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4551195 | — | Ki | > | 10000.0 | nM | - |