Assay Detail
Binding
CHEMBL751790
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Inhibition of [125I]NKA binding to neurokinin NK2 receptor from rat duodenum membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Pharmacological profile and chemical synthesis of SR 48968, a non-peptide antagonist of the neurokinin A (NK2) receptor
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.80 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL368995 | — | — | 1 | 9.52 |
| CHEMBL173203 | — | — | 1 | 9.52 |
| CHEMBL308148 | SAREDUTANT | 3.0 | 1 | 9.30 |
| CHEMBL173841 | — | — | 1 | 9.05 |
| CHEMBL176588 | — | — | 1 | 9.00 |
| CHEMBL71397 | — | — | 1 | 9.00 |
| CHEMBL173008 | — | — | 1 | 8.85 |
| CHEMBL176853 | — | — | 1 | 8.82 |
| CHEMBL367542 | — | — | 1 | 7.64 |
| CHEMBL368372 | — | — | 1 | 7.30 |
| CHEMBL69335 | — | — | 1 | - |
| CHEMBL366382 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL368995 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL173203 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL308148 | SAREDUTANT | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL173841 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL176588 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL71397 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL173008 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL176853 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL367542 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL368372 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL69335 | — | Ki | > | 100.0 | nM | - |
| CHEMBL366382 | — | Ki | > | 100.0 | nM | - |