Assay Detail
Binding
CHEMBL807971
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of binding of [125I]-substance P to tachykinin receptor 1
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 9.68 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1471 | APREPITANT | 4.0 | 1 | 10.05 |
| CHEMBL553778 | — | — | 1 | 9.72 |
| CHEMBL135263 | — | — | 1 | 9.72 |
| CHEMBL2112743 | — | — | 1 | 9.68 |
| CHEMBL2112741 | — | — | 1 | 9.60 |
| CHEMBL133140 | — | — | 1 | 9.54 |
| CHEMBL2112742 | — | — | 1 | 9.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1471 | APREPITANT | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL553778 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL135263 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL2112743 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL2112741 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL133140 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL2112742 | — | IC50 | = | 0.35 | nM | 9.46 |