Assay Detail
Binding
CHEMBL1037637
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Displacement of [3H]substance P from human recombinant NK1 receptor expressed in HEK293 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 6.85 | 7.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL567198 | — | — | 1 | 7.15 |
| CHEMBL567849 | — | — | 1 | 6.82 |
| CHEMBL565894 | — | — | 1 | 6.74 |
| CHEMBL346178 | OSANETANT | 2.0 | 1 | 6.68 |
| CHEMBL10188 | TALNETANT | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL567198 | — | Ki | = | 70.9 | nM | 7.15 |
| CHEMBL567849 | — | Ki | = | 151.8 | nM | 6.82 |
| CHEMBL565894 | — | Ki | = | 181.6 | nM | 6.74 |
| CHEMBL346178 | OSANETANT | Ki | = | 209.6 | nM | 6.68 |
| CHEMBL10188 | TALNETANT | Ki | > | 10000.0 | nM | - |