Assay Detail
Binding
CHEMBL817414
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Effective concentration to activate Tachykinin receptor 1 in guinea pig ileum(GPI)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and biological activity of NK-1 selective, N-backbone cyclic analogs of the C-terminal hexapeptide of substance P.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 6.99 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL422779 | — | — | 1 | 8.52 |
| CHEMBL321228 | — | — | 1 | 8.30 |
| CHEMBL264395 | — | — | 1 | 7.96 |
| CHEMBL431243 | — | — | 1 | 7.22 |
| CHEMBL323028 | — | — | 1 | 6.80 |
| CHEMBL110177 | — | — | 1 | 6.75 |
| CHEMBL106184 | — | — | 1 | 6.52 |
| CHEMBL265115 | — | — | 1 | 6.40 |
| CHEMBL106124 | SENKTIDE | — | 1 | 4.46 |
| CHEMBL319473 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL422779 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL321228 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL264395 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL431243 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL323028 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL110177 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL106184 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL265115 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL106124 | SENKTIDE | EC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL319473 | — | EC50 | > | 10000.0 | nM | - |