Assay Detail
Binding
CHEMBL1037641
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Displacement of [3H]osanetant from guinea pig recombinant NK3 receptor A1142.58T expressed in HEK293 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Identification of a critical residue in the transmembrane domain 2 of tachykinin neurokinin 3 receptor affecting the dissociation kinetics and antagonism mode of osanetant (SR 142801) and piperidine-based structures.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 8.55 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL346178 | OSANETANT | 2.0 | 1 | 9.10 |
| CHEMBL565894 | — | — | 1 | 8.74 |
| CHEMBL567849 | — | — | 1 | 8.57 |
| CHEMBL10188 | TALNETANT | 2.0 | 1 | 8.42 |
| CHEMBL567198 | — | — | 1 | 7.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL346178 | OSANETANT | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL565894 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL567849 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL10188 | TALNETANT | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL567198 | — | Ki | = | 11.9 | nM | 7.92 |