Assay Detail
Binding
CHEMBL2210307
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Partial noncompetitive inhibition of human F264Y6.51 mutant expressed in HEK293 cells assessed as decrease in SP1-induced [3H]IP accumulation after 20 mins
3
Total Activities
3
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 | 3 | 7.57 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2203707 | — | — | 1 | 7.77 |
| CHEMBL2203703 | — | — | 1 | 7.54 |
| CHEMBL2203705 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2203707 | — | Kd | = | 16.98 | nM | 7.77 |
| CHEMBL2203703 | — | Kd | = | 28.84 | nM | 7.54 |
| CHEMBL2203705 | — | Kd | = | 39.81 | nM | 7.40 |