Assay Detail
Binding
CHEMBL749394
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Inhibition of cloned human NK1 (Neurokinin 1) receptor, stably expressed in chinese hamster ovary (CHO) cells was determined
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
L-tryptophan urea amides as NK1/NK2 dual antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.29 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL72234 | — | — | 1 | 9.24 |
| CHEMBL306400 | — | — | 1 | 9.00 |
| CHEMBL22870 | L-732138 | — | 1 | 8.80 |
| CHEMBL74237 | — | — | 1 | 8.00 |
| CHEMBL306065 | — | — | 1 | 7.85 |
| CHEMBL73097 | — | — | 1 | 7.64 |
| CHEMBL73618 | — | — | 1 | 7.25 |
| CHEMBL305509 | — | — | 1 | 7.17 |
| CHEMBL73839 | — | — | 1 | 7.11 |
| CHEMBL23851 | — | — | 1 | 6.99 |
| CHEMBL2114103 | — | — | 1 | 6.79 |
| CHEMBL303868 | — | — | 1 | 6.64 |
| CHEMBL73896 | — | — | 1 | 6.62 |
| CHEMBL74176 | — | — | 1 | 6.48 |
| CHEMBL305609 | — | — | 1 | 6.32 |
| CHEMBL308148 | SAREDUTANT | 3.0 | 1 | 6.10 |
| CHEMBL70461 | — | — | 1 | 5.96 |
| CHEMBL305608 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL72234 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL306400 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL22870 | L-732138 | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL74237 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL306065 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL73097 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL73618 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL305509 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL73839 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL23851 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL2114103 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL303868 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL73896 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL74176 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL305609 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL308148 | SAREDUTANT | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL70461 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL305608 | — | IC50 | > | 1100.0 | nM | - |