Assay Detail
Binding
CHEMBL814484
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Binding affinity to Tachykinin receptor 1 stably expressed in chinese hamster ovary (CHO) cells
19
Total Activities
19
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
Discovery of an orally bioavailable NK1 receptor antagonist, (2S,3S)-(2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with potent antiemetic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 9.72 | 10.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL149557 | — | — | 1 | 10.50 |
| CHEMBL146885 | — | — | 1 | 10.30 |
| CHEMBL356062 | — | — | 1 | 10.30 |
| CHEMBL344536 | — | — | 1 | 10.30 |
| CHEMBL356786 | — | — | 1 | 10.20 |
| CHEMBL359188 | — | — | 1 | 10.20 |
| CHEMBL434884 | — | — | 1 | 10.10 |
| CHEMBL424301 | — | — | 1 | 9.90 |
| CHEMBL358575 | — | — | 1 | 9.80 |
| CHEMBL359255 | — | — | 1 | 9.80 |
| CHEMBL147776 | — | — | 1 | 9.80 |
| CHEMBL357029 | — | — | 1 | 9.70 |
| CHEMBL441225 | CP-99994 | — | 1 | 9.60 |
| CHEMBL343404 | — | — | 1 | 9.30 |
| CHEMBL342966 | — | — | 1 | 9.30 |
| CHEMBL144793 | — | — | 1 | 9.10 |
| CHEMBL147619 | — | — | 1 | 9.10 |
| CHEMBL146210 | — | — | 1 | 8.70 |
| CHEMBL343219 | — | — | 1 | 8.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL149557 | — | Ki | = | 0.03162 | nM | 10.50 |
| CHEMBL146885 | — | Ki | = | 0.05012 | nM | 10.30 |
| CHEMBL356062 | — | Ki | = | 0.05012 | nM | 10.30 |
| CHEMBL344536 | — | Ki | = | 0.05012 | nM | 10.30 |
| CHEMBL356786 | — | Ki | = | 0.0631 | nM | 10.20 |
| CHEMBL359188 | — | Ki | = | 0.0631 | nM | 10.20 |
| CHEMBL434884 | — | Ki | = | 0.07943 | nM | 10.10 |
| CHEMBL424301 | — | Ki | = | 0.1259 | nM | 9.90 |
| CHEMBL358575 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL359255 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL147776 | — | Ki | = | 0.1585 | nM | 9.80 |
| CHEMBL357029 | — | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL441225 | CP-99994 | Ki | = | 0.2512 | nM | 9.60 |
| CHEMBL343404 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL342966 | — | Ki | = | 0.5012 | nM | 9.30 |
| CHEMBL144793 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL147619 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL146210 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL343219 | — | Ki | = | 2.512 | nM | 8.60 |