Assay Detail
Binding
CHEMBL842693
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Tested for binding affinity against H197A mutant NK1 receptor using [125]SP radioligand in COS cells.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | COS |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.67 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL235363 | SUBSTANCE P | 1.0 | 1 | 9.05 |
| CHEMBL2112245 | — | — | 1 | 6.05 |
| CHEMBL2112246 | — | — | 1 | 6.02 |
| CHEMBL2369630 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL235363 | SUBSTANCE P | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL2112245 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2112246 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL2369630 | — | IC50 | = | 2700.0 | nM | 5.57 |