Assay Detail
Binding
CHEMBL750288
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Inhibition of [3H]-substance P binding to human NK1 receptor expressed in chinese hamster ovary cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Tetrazole NK1 receptor antagonists: The identification of an exceptionally potent orally active antiemetic compound
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 9.95 | 10.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL557983 | VOFOPITANT DIHYDROCHLORIDE | -1.0 | 1 | 10.60 |
| CHEMBL542044 | — | — | 1 | 10.40 |
| CHEMBL555572 | — | — | 1 | 10.40 |
| CHEMBL545594 | — | — | 1 | 10.40 |
| CHEMBL536103 | — | — | 1 | 10.30 |
| CHEMBL545360 | — | — | 1 | 10.30 |
| CHEMBL544891 | — | — | 1 | 10.20 |
| CHEMBL558990 | — | — | 1 | 10.10 |
| CHEMBL556981 | — | — | 1 | 9.60 |
| CHEMBL556562 | — | — | 1 | 9.40 |
| CHEMBL544660 | — | — | 1 | 9.00 |
| CHEMBL544892 | — | — | 1 | 8.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL557983 | VOFOPITANT DIHYDROCHLORIDE | Ki | = | 0.02512 | nM | 10.60 |
| CHEMBL542044 | — | Ki | = | 0.03981 | nM | 10.40 |
| CHEMBL555572 | — | Ki | = | 0.03981 | nM | 10.40 |
| CHEMBL545594 | — | Ki | = | 0.03981 | nM | 10.40 |
| CHEMBL536103 | — | Ki | = | 0.05012 | nM | 10.30 |
| CHEMBL545360 | — | Ki | = | 0.05012 | nM | 10.30 |
| CHEMBL544891 | — | Ki | = | 0.0631 | nM | 10.20 |
| CHEMBL558990 | — | Ki | = | 0.07943 | nM | 10.10 |
| CHEMBL556981 | — | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL556562 | — | Ki | = | 0.3981 | nM | 9.40 |
| CHEMBL544660 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL544892 | — | Ki | = | 1.995 | nM | 8.70 |