Assay Detail
Binding
CHEMBL809493
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In vitro inhibition of binding of [125I]Bolton-Hunter SP to Tachykinin receptor 1 in human IM-9 cell line
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | IM-9 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Expedited discovery of second generation NK-1 antagonists: identification of a nonbasic aryloxy substituent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.53 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42407 | LANEPITANT | 2.0 | 1 | 9.64 |
| CHEMBL43044 | — | — | 1 | 9.37 |
| CHEMBL47070 | — | — | 1 | 9.32 |
| CHEMBL296013 | — | — | 1 | 9.19 |
| CHEMBL42259 | — | — | 1 | 9.09 |
| CHEMBL42191 | — | — | 1 | 9.01 |
| CHEMBL42295 | — | — | 1 | 8.49 |
| CHEMBL289600 | — | — | 1 | 8.48 |
| CHEMBL42597 | — | — | 1 | 8.46 |
| CHEMBL296216 | — | — | 1 | 8.22 |
| CHEMBL45316 | — | — | 1 | 8.08 |
| CHEMBL539937 | — | — | 1 | 8.01 |
| CHEMBL434012 | — | — | 1 | 7.99 |
| CHEMBL43970 | — | — | 1 | 7.97 |
| CHEMBL42845 | — | — | 1 | 7.62 |
| CHEMBL295107 | — | — | 1 | 7.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42407 | LANEPITANT | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL43044 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL47070 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL296013 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL42259 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL42191 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL42295 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL289600 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL42597 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL296216 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL45316 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL539937 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL434012 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL43970 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL42845 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL295107 | — | IC50 | = | 34.0 | nM | 7.47 |