Assay Detail
Binding
CHEMBL616409
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Inhibition activity against 5-hydroxytryptamine 1A receptor in rat hippocampus membranes using radio binding assays
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Hippocampus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
New selective and potent 5-HT(1B/1D) antagonists: chemistry and pharmacological evaluation of N-piperazinylphenyl biphenylcarboxamides and biphenylsulfonamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.31 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL147503 | — | — | 1 | 7.64 |
| CHEMBL147071 | — | — | 1 | 7.24 |
| CHEMBL15928 | GR-127935 | — | 1 | 6.37 |
| CHEMBL151894 | — | — | 1 | 6.16 |
| CHEMBL151420 | — | — | 1 | 5.30 |
| CHEMBL443762 | — | — | 1 | 5.16 |
| CHEMBL359447 | — | — | 1 | - |
| CHEMBL151695 | — | — | 1 | - |
| CHEMBL281350 | SB-224289 | — | 1 | - |
| CHEMBL146735 | — | — | 1 | - |
| CHEMBL422504 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL147503 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL147071 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL15928 | GR-127935 | IC50 | = | 425.0 | nM | 6.37 |
| CHEMBL151894 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL151420 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL443762 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL359447 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL151695 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL281350 | SB-224289 | IC50 | > | 1000.0 | nM | - |
| CHEMBL146735 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL422504 | — | IC50 | > | 1000.0 | nM | - |