Assay Detail
Functional
CHEMBL817417
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In vitro agonistic activity against tachykinin receptor 1 of guinea pig ileum longitudinal smooth muscle.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 19 | 6.63 | 8.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL235363 | SUBSTANCE P | 1.0 | 1 | 8.25 |
| CHEMBL407511 | — | — | 1 | 7.87 |
| CHEMBL217406 | NEUROKININ A | — | 1 | 7.86 |
| CHEMBL262049 | — | — | 1 | 7.42 |
| CHEMBL134091 | — | — | 1 | 7.36 |
| CHEMBL134481 | — | — | 1 | 7.35 |
| CHEMBL335054 | — | — | 1 | 7.21 |
| CHEMBL437797 | NEUROKININ B | — | 1 | 7.17 |
| CHEMBL135186 | — | — | 1 | 7.07 |
| CHEMBL335248 | — | — | 1 | 7.07 |
| CHEMBL133362 | — | — | 1 | 6.51 |
| CHEMBL134012 | — | — | 1 | 6.26 |
| CHEMBL262048 | — | — | 1 | 6.08 |
| CHEMBL267712 | — | — | 1 | 5.99 |
| CHEMBL131923 | — | — | 1 | 5.95 |
| CHEMBL339391 | — | — | 1 | 5.43 |
| CHEMBL131872 | — | — | 1 | 5.37 |
| CHEMBL337037 | — | — | 1 | 5.28 |
| CHEMBL337465 | — | — | 1 | 4.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL235363 | SUBSTANCE P | EC50 | = | 5.6 | nM | 8.25 |
| CHEMBL407511 | — | EC50 | = | 13.4 | nM | 7.87 |
| CHEMBL217406 | NEUROKININ A | EC50 | = | 13.7 | nM | 7.86 |
| CHEMBL262049 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL134091 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL134481 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL335054 | — | EC50 | = | 61.0 | nM | 7.21 |
| CHEMBL437797 | NEUROKININ B | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL135186 | — | EC50 | = | 86.0 | nM | 7.07 |
| CHEMBL335248 | — | EC50 | = | 86.0 | nM | 7.07 |
| CHEMBL133362 | — | EC50 | = | 307.0 | nM | 6.51 |
| CHEMBL134012 | — | EC50 | = | 545.0 | nM | 6.26 |
| CHEMBL262048 | — | EC50 | = | 830.0 | nM | 6.08 |
| CHEMBL267712 | — | EC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL131923 | — | EC50 | = | 1125.0 | nM | 5.95 |
| CHEMBL339391 | — | EC50 | = | 3732.0 | nM | 5.43 |
| CHEMBL131872 | — | EC50 | = | 4237.0 | nM | 5.37 |
| CHEMBL337037 | — | EC50 | = | 5225.0 | nM | 5.28 |
| CHEMBL337465 | — | EC50 | = | 37700.0 | nM | 4.42 |