Assay Detail
Binding
CHEMBL616544
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Binding affinity for human 5-hydroxytryptamine 1D receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.34 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL15928 | GR-127935 | — | 1 | 8.60 |
| CHEMBL282229 | — | — | 1 | 8.30 |
| CHEMBL277467 | — | — | 1 | 7.90 |
| CHEMBL20791 | — | — | 1 | 7.70 |
| CHEMBL21724 | — | — | 1 | 7.60 |
| CHEMBL20963 | — | — | 1 | 7.50 |
| CHEMBL282693 | — | — | 1 | 7.40 |
| CHEMBL20771 | — | — | 1 | 7.40 |
| CHEMBL21790 | — | — | 1 | 7.00 |
| CHEMBL21369 | — | — | 1 | 6.70 |
| CHEMBL281350 | SB-224289 | — | 1 | 6.30 |
| CHEMBL15933 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL15928 | GR-127935 | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL282229 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL277467 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL20791 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL21724 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL20963 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL282693 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL20771 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL21790 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL21369 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL281350 | SB-224289 | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL15933 | — | Ki | = | 1995.26 | nM | 5.70 |