Assay Detail
Binding
CHEMBL4688539
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-Histamine from human histamine 3 receptor transfected in HEK293T cells incubated for 16 hrs by liquid scintillation counter analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel potent (dihydro)benzofuranyl piperazines as human histamine receptor ligands - Functional characterization and modeling studies on H and H receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.13 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL90 | HISTAMINE | 4.0 | 1 | 8.60 |
| CHEMBL4749654 | — | — | 1 | 8.40 |
| CHEMBL4747180 | — | — | 1 | 8.20 |
| CHEMBL4756432 | — | — | 1 | 7.80 |
| CHEMBL4798369 | — | — | 1 | 7.40 |
| CHEMBL4747747 | — | — | 1 | 6.40 |
| CHEMBL4752345 | — | — | 1 | 6.20 |
| CHEMBL4758983 | — | — | 1 | 6.10 |
| CHEMBL4792753 | — | — | 1 | 6.10 |
| CHEMBL4764535 | — | — | 1 | 6.10 |
| CHEMBL4568949 | — | — | 1 | - |
| CHEMBL4746519 | — | — | 1 | - |
| CHEMBL4778595 | — | — | 1 | - |
| CHEMBL4745175 | — | — | 1 | - |
| CHEMBL4753344 | — | — | 1 | - |
| CHEMBL4762254 | — | — | 1 | - |
| CHEMBL4750456 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL90 | HISTAMINE | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL4749654 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL4747180 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL4756432 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL4798369 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL4747747 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL4752345 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL4758983 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL4792753 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL4764535 | — | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL4568949 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4746519 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4778595 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4745175 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4753344 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4762254 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4750456 | — | Ki | > | 10000.0 | nM | - |