Assay Detail
Binding
CHEMBL812239
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Binding affinity towards Tachykinin receptor 1 binding in guinea pig cerebral cortex membranes was determined using [3H]SP as the radioligand
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
An SAR study for the non-peptide substance P receptor (NK1) antagonist, CP-96,345.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.55 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL235363 | SUBSTANCE P | 1.0 | 1 | 10.15 |
| CHEMBL346154 | — | — | 1 | 8.92 |
| CHEMBL217406 | NEUROKININ A | — | 1 | 8.46 |
| CHEMBL356912 | — | — | 1 | 8.07 |
| CHEMBL419500 | — | — | 1 | 8.00 |
| CHEMBL437797 | NEUROKININ B | — | 1 | 7.89 |
| CHEMBL345711 | — | — | 1 | 7.48 |
| CHEMBL152239 | — | — | 1 | 7.43 |
| CHEMBL357717 | — | — | 1 | 7.28 |
| CHEMBL449347 | — | — | 1 | 6.82 |
| CHEMBL153042 | — | — | 1 | 6.80 |
| CHEMBL346633 | — | — | 1 | 6.64 |
| CHEMBL346626 | — | — | 1 | 5.96 |
| CHEMBL152011 | — | — | 1 | 5.82 |
| CHEMBL358033 | — | — | 1 | - |
| CHEMBL152055 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL235363 | SUBSTANCE P | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL346154 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL217406 | NEUROKININ A | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL356912 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL419500 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL437797 | NEUROKININ B | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL345711 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL152239 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL357717 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL449347 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL153042 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL346633 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL346626 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL152011 | — | IC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL358033 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL152055 | — | IC50 | > | 10000.0 | nM | - |