Assay Detail
Binding
CHEMBL2215533
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive inhibition at human NK3 Y315F6.51 mutant expressed in HEK293 cells assessed as decrease in [MePhe7]NKB-induced [3H]IP accumulation after 20 mins
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 | Autocuration |
Publication
Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK₁/NK₃ antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 5 | 7.98 | 8.63 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10188 | TALNETANT | 2.0 | 1 | 8.63 |
| CHEMBL2203708 | — | — | 1 | 8.61 |
| CHEMBL2203706 | — | — | 1 | 7.68 |
| CHEMBL346178 | OSANETANT | 2.0 | 1 | 7.53 |
| CHEMBL2203709 | — | — | 1 | 7.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10188 | TALNETANT | Kd | = | 2.344 | nM | 8.63 |
| CHEMBL2203708 | — | Kd | = | 2.455 | nM | 8.61 |
| CHEMBL2203706 | — | Kd | = | 20.89 | nM | 7.68 |
| CHEMBL346178 | OSANETANT | Kd | = | 29.51 | nM | 7.53 |
| CHEMBL2203709 | — | Kd | = | 37.15 | nM | 7.43 |