Assay Detail
Binding
CHEMBL2215534
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Competitive inhibition at wild type human NK3 expressed in HEK293 cells assessed as decrease in [MePhe7]NKB-induced [3H]IP accumulation after 20 mins
6
Total Activities
6
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 | 6 | 7.43 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10188 | TALNETANT | 2.0 | 1 | 8.24 |
| CHEMBL2203704 | — | — | 1 | 7.79 |
| CHEMBL346178 | OSANETANT | 2.0 | 1 | 7.73 |
| CHEMBL2203709 | — | — | 1 | 7.01 |
| CHEMBL2203706 | — | — | 1 | 6.92 |
| CHEMBL2203708 | — | — | 1 | 6.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10188 | TALNETANT | Kd | = | 5.754 | nM | 8.24 |
| CHEMBL2203704 | — | Kd | = | 16.22 | nM | 7.79 |
| CHEMBL346178 | OSANETANT | Kd | = | 18.62 | nM | 7.73 |
| CHEMBL2203709 | — | Kd | = | 97.72 | nM | 7.01 |
| CHEMBL2203706 | — | Kd | = | 120.23 | nM | 6.92 |
| CHEMBL2203708 | — | Kd | = | 123.03 | nM | 6.91 |